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Solu-Medrol
Methylprednisolone Acetate
Solu-Medrol
Methylprednisolone Acetate
Indications
Wiskott-Aldrich syndrome
Indication detailsView
Methyl Prednisolone Acetate is indicated in the treatment of asthma, atopic dermatitis, contact dermatitis, bullous dermatitis herpetiformis, mycosis fungoides, pemphigus, severe erythema multiforme, primary or secondary adrenocortical insufficiency, hypercalcemia associated with cancer, nonsuppurative thyroiditis, ulcerative colitis, hematologic disorders, palliative management of leukemias and lymphomas, sympathetic ophthalmia, keratitis, allergic conjunctivitis, Juvenile rheumatoid arthritis, ankylosing spondylitis, symptomatic sarcoidosis, aspiration pneumonitis.
Therapeutic classView
Glucocorticoids
PharmacologyView
Methylprednisolone binds to and activates intracellular glucocorticoid receptors. Activated glucocorticoid receptors bind to promoter regions of DNA (which may activate or suppress transcription). Unbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors, modifying transcription and protein synthesis. By this mechanism, glucocorticoids can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
DosageView
1. Administration For Local Effect:
Rheumatoid and Osteoarthritis: The dose for intra-articular administration depends upon the size of the joint and varies with the severity of the condition in the individual patient. The doses in the following table are given as a general guide:
Dermatological Conditions: 20 to 60mg of the suspension is injected into the lesion. It may be necessary to distribute doses ranging from 20 to 40mg by repeated local injections in the case of large lesions. One to four injections are usually employed, the intervals between injections varying with the type of lesion being treated and the duration of improvement produced by the initial injection.
2. Administration For Systemic Effect: In patients with the adrenogenital syndrome, a single intramuscular injection of 40mg every two weeks may be adequate. For maintenance of patients with rheumatoid arthritis, the weekly intramuscular dose will vary from 40 to 120 mg. The usual dosage for patients with dermatologic lesions benefited by systemic corticoid therapy is 40 to 120 mg of methylprednisolone acetate administered intramuscularly at weekly intervals for one to four weeks. In acute severe dermatitis due to poison ivy, relief may result within 8 to 12 hours following intramuscular administration of a single dose of 80 to 120mg. In chronic contact dermatitis, repeated injections at 5 to 10 day intervals may be necessary. In seborrheic dermatitis, a weekly dose of 80mg may be adequate to control the condition. Following intramuscular administration of 80 to 120 mg to asthmatic patients, relief may result within 6 to 48 hours and persist for several days to two weeks. Similarly in patients with allergic rhinitis (hay fever), an intramuscular dose of 80 to 120mg may be followed by relief of coryzal symptoms within six hours persisting for several days to three weeks.
3. Multiple Sclerosis: In treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of methylprednisolone for a week followed by 64mg every other day for 1 month have been shown to be effective (4mg of methylprednisolone is equivalent to 5mg of prednisolone). Or, as directed by the registered physician.
Rheumatoid and Osteoarthritis: The dose for intra-articular administration depends upon the size of the joint and varies with the severity of the condition in the individual patient. The doses in the following table are given as a general guide:
- Large Size of joint (Knees, Ankles, Shoulders): 20 to 80 mg
- Medium Size of joint (Elbows, Wrists): 10 to 40 mg
- Small Size of joint (Metacarpophalangeal, Interphalangeal, Sternoclavicular, Acromioclavicular): 4 to 10 mg.
Dermatological Conditions: 20 to 60mg of the suspension is injected into the lesion. It may be necessary to distribute doses ranging from 20 to 40mg by repeated local injections in the case of large lesions. One to four injections are usually employed, the intervals between injections varying with the type of lesion being treated and the duration of improvement produced by the initial injection.
2. Administration For Systemic Effect: In patients with the adrenogenital syndrome, a single intramuscular injection of 40mg every two weeks may be adequate. For maintenance of patients with rheumatoid arthritis, the weekly intramuscular dose will vary from 40 to 120 mg. The usual dosage for patients with dermatologic lesions benefited by systemic corticoid therapy is 40 to 120 mg of methylprednisolone acetate administered intramuscularly at weekly intervals for one to four weeks. In acute severe dermatitis due to poison ivy, relief may result within 8 to 12 hours following intramuscular administration of a single dose of 80 to 120mg. In chronic contact dermatitis, repeated injections at 5 to 10 day intervals may be necessary. In seborrheic dermatitis, a weekly dose of 80mg may be adequate to control the condition. Following intramuscular administration of 80 to 120 mg to asthmatic patients, relief may result within 6 to 48 hours and persist for several days to two weeks. Similarly in patients with allergic rhinitis (hay fever), an intramuscular dose of 80 to 120mg may be followed by relief of coryzal symptoms within six hours persisting for several days to three weeks.
3. Multiple Sclerosis: In treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of methylprednisolone for a week followed by 64mg every other day for 1 month have been shown to be effective (4mg of methylprednisolone is equivalent to 5mg of prednisolone). Or, as directed by the registered physician.
Side effectsView
Congestive heart failure in susceptible patients, hypertension, sodium retention, muscle weakness, osteoporosis, peptic ulcer with possible subsequent and hemorrhage, abdominal distention, increased sweating, convulsion, vertigo, headache, menstrual irregularities, secondary adrenocortical and pituitary unresponsiveness, increased intraocular pressure, glaucoma, allergic or hypersensitivity reactions, urticaria, hyperpigmentation or hypopigmentation.
ContraindicationsView
Methylprednisolone acetate sterile aqueous suspension is contraindicated for intrathecal administration. It is also contraindicated in systemic fungal infections and patients with known hypersensitivity to the product and its constituents.
PrecautionsView
Corticosteroids should be used cautiously in patients with ocular herpes simplex, nonspecific ulcerative colitis, renal insufficiency, hypertension, osteoporosis and myasthenia gravis.
InteractionsView
Convulsions have been reported with concurrent use of methylprednisolone and cyclosporine. Drug that induce hepatic enzymes such as phenobarbital, phenytoin and rifampicin may increase the clearance of methylprednisolone. Drug such as troleandomycin and ketoconazole may inhibit the metabolism of methylprednisolone and decrease its clearance. Methylprednisolone may increase the clearance of chronic high dose aspirin. There are reports of enhanced as well as diminished effects of anticoagulant when given concurrently with corticosteroids.
Pregnancy & lactationView
Pregnancy Category C. Since adequate human reproduction studies have not been done with corticosteroids, the use of these drug in pregnancy, nursing mothers, or women of childbearing potential requires that the possible benefits of the drug be weighed against the potential hazards to the mother and embryo or fetus.
StorageView
Store between 20-25° C.
Solupred
Methylprednisolone
Solupred
Methylprednisolone
Indications
Rheumatic disorders
Indication detailsView
Endocrine Disorders: Primary or Secondary Adrenocortical Insufficiency, Congenital Adrenal Hyperplasia, Nonsuppurative Thyroiditis, Hypercalcemia associated with Cancer.
Rheumatic Disorders: Rheumatoid Arthritis. Juvenile Rheumatoid Arthritis, Ankylosing Spondylitis, Acute and Subacute Bursitis, Synovitis of Osteoarthritis, Acute nonspecific Tenosynovitis, Post-traumatic Osteoarthritis, Psoriatic Arthritis, Epicondylitis, Acute Gouty Arthritis.
Collagen Diseases: Systemic lupus Erythematosus, Systemic Dermatomyositis and Acute Rheumatic Carditis.
Dermatologic Diseases: Bullous Dermatitis Herpetiformis, Severe Erythema Multiforme (Stevens-Johnson syndrome), Severe Seborrheic Dermatitis, Exfoliative Dermatitis, Mycosis Fungoides, Pemphigus, Severe Psoriasis.
Allergy: Seasonal or Perennial Allergic Rhinitis, Drug hypersensitivity reactions, Serum Sickness, Contact Dermatitis, Bronchial Asthma and Atopic Dermatitis;
Ophthalmic Diseases: Allergic Corneal Ulcers, Herpes Zoster Ophthalmicus, Anterior segment inflammation, Sympathetic Ophthalmia, Keratitis, Optic Neuritis, Allergic Conjunctivitis, Chorioretinitis, iritis end iridocyclitis.
Respiratory Diseases: Symptomatic sarcoidosis, Loeffler's syndrome not manageable by other means, berylliosis, Aspiration Pneumonitis.
Hematological Disorders: Idiopathic Thrombocytopenic Purpura in adults, Secondary Thrombocytopenia in adults, Acquired (Autoimmune) Hemolytic Anemia, Erythroblastopenia, Congenital (Erythroid) Hypoplastic Anemia.
Neoplastic Diseases: For palliative management of Leukemias and Lymphomas in adults, Acute leukemia of childhood.
Edematous States: To induce a diuresis or remission of Proteinuria in the Nephrotic Syndrome, without Uremia, of the idiopathic type or that due to Lupus Erythematosus.
Gastrointestinal Disease: To tide the patient over a critical period of the disease in Ulcerative Colitis & Regional Enteritis.
CNS Disease: Acute Exacerbations of Multiple Sclerosis.
Rheumatic Disorders: Rheumatoid Arthritis. Juvenile Rheumatoid Arthritis, Ankylosing Spondylitis, Acute and Subacute Bursitis, Synovitis of Osteoarthritis, Acute nonspecific Tenosynovitis, Post-traumatic Osteoarthritis, Psoriatic Arthritis, Epicondylitis, Acute Gouty Arthritis.
Collagen Diseases: Systemic lupus Erythematosus, Systemic Dermatomyositis and Acute Rheumatic Carditis.
Dermatologic Diseases: Bullous Dermatitis Herpetiformis, Severe Erythema Multiforme (Stevens-Johnson syndrome), Severe Seborrheic Dermatitis, Exfoliative Dermatitis, Mycosis Fungoides, Pemphigus, Severe Psoriasis.
Allergy: Seasonal or Perennial Allergic Rhinitis, Drug hypersensitivity reactions, Serum Sickness, Contact Dermatitis, Bronchial Asthma and Atopic Dermatitis;
Ophthalmic Diseases: Allergic Corneal Ulcers, Herpes Zoster Ophthalmicus, Anterior segment inflammation, Sympathetic Ophthalmia, Keratitis, Optic Neuritis, Allergic Conjunctivitis, Chorioretinitis, iritis end iridocyclitis.
Respiratory Diseases: Symptomatic sarcoidosis, Loeffler's syndrome not manageable by other means, berylliosis, Aspiration Pneumonitis.
Hematological Disorders: Idiopathic Thrombocytopenic Purpura in adults, Secondary Thrombocytopenia in adults, Acquired (Autoimmune) Hemolytic Anemia, Erythroblastopenia, Congenital (Erythroid) Hypoplastic Anemia.
Neoplastic Diseases: For palliative management of Leukemias and Lymphomas in adults, Acute leukemia of childhood.
Edematous States: To induce a diuresis or remission of Proteinuria in the Nephrotic Syndrome, without Uremia, of the idiopathic type or that due to Lupus Erythematosus.
Gastrointestinal Disease: To tide the patient over a critical period of the disease in Ulcerative Colitis & Regional Enteritis.
CNS Disease: Acute Exacerbations of Multiple Sclerosis.
Therapeutic classView
Glucocorticoids
PharmacologyView
Pharmacodynamic properties: Methylprednisolone Is a potent anti-inflammatory agent with the capacity to profoundly inhibit the immune system. Glucocorticoids primarily bind to and activate intracellular glucocorticoid receptors that being activated bind to promoter regions of DMA (which may activate or suppress transcription) and activate transcription factors that result in inactivation of genes through deacetylation of histones. Methylprednisolone influences the kidney and fluid & electrolyte balance, lipid,
protein, and carbohydrate metabolism, skeletal muscle, the cardiovascular system, the immune system, the nervous system, and the endocrine system.
Pharmacokinetic properties: The absolute bioavailability of Methylprednisclone is generally high (82% to 89%) following oral administration and rapidly absorbed and the maximum plasma concentration is achieved around 1.5 to 2.3 hours across doses following oral administration in normal healthy adults. Methylprednisolone is widely distributed into the tissues and its volume of distribution is 41-61.5 liter. It crosses the Wood-brain barrier and the placental barrier and is secreted in breast milk. The plasma protein binding of Methylprednisolone in humans is approximately 77%. Methylprednisolone is metabolized in the liver to inactive metabolites. No dosing adjustments are necessary for renal failure. Methylprednisolone is haemodializable.
protein, and carbohydrate metabolism, skeletal muscle, the cardiovascular system, the immune system, the nervous system, and the endocrine system.
Pharmacokinetic properties: The absolute bioavailability of Methylprednisclone is generally high (82% to 89%) following oral administration and rapidly absorbed and the maximum plasma concentration is achieved around 1.5 to 2.3 hours across doses following oral administration in normal healthy adults. Methylprednisolone is widely distributed into the tissues and its volume of distribution is 41-61.5 liter. It crosses the Wood-brain barrier and the placental barrier and is secreted in breast milk. The plasma protein binding of Methylprednisolone in humans is approximately 77%. Methylprednisolone is metabolized in the liver to inactive metabolites. No dosing adjustments are necessary for renal failure. Methylprednisolone is haemodializable.
DosageView
The usual range is 2-48 mg daily in divided doses, depending on the specific disease being treated.
As anti-inflammatory or immunosuppressive initial dosage: As anti-inflammatory or immunosuppressive, the initial dosage of Methylprednisolone tablets may vary from 4-48 mg per day depending on the specific disease entity being treated, in situations of less severity lower doses will generally suffice while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory dirtied response, Methylprednisolone should be discontinued and the patient transferred to other appropriate therapy. It should be emphasized that dosage requirements are variable and must be Individualized on the basis of the disease under treatment and the response of the patient.
As anti-inflammatory or immunosuppressive maintenance dosage: After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.
Multiple Sclerosis: In the treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of Methylprednisolone for a week followed by 64 mg every other day for 1 month have been shown to be effective.
Methylprednisolone 4 mg tablet can be used to treat and to control severe allergy end dermatitis following the guideline listed below to minimize the steroid withdrawal syndromes:
The following should be kept in mind when considering alternate-day therapy:
As anti-inflammatory or immunosuppressive initial dosage: As anti-inflammatory or immunosuppressive, the initial dosage of Methylprednisolone tablets may vary from 4-48 mg per day depending on the specific disease entity being treated, in situations of less severity lower doses will generally suffice while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory dirtied response, Methylprednisolone should be discontinued and the patient transferred to other appropriate therapy. It should be emphasized that dosage requirements are variable and must be Individualized on the basis of the disease under treatment and the response of the patient.
As anti-inflammatory or immunosuppressive maintenance dosage: After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.
Multiple Sclerosis: In the treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of Methylprednisolone for a week followed by 64 mg every other day for 1 month have been shown to be effective.
Methylprednisolone 4 mg tablet can be used to treat and to control severe allergy end dermatitis following the guideline listed below to minimize the steroid withdrawal syndromes:
- Day 1: 2 tablets before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
- Day 2: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
- Day 3: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 1 tablet at bedtime
- Day 4: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet at bedtime
- Day 5: 1 tablet before breakfast + 1 tablet at bedtime
- Day 6: 1 tablet before breakfast
The following should be kept in mind when considering alternate-day therapy:
- Basic principles and indications for corticosteroid therapy should be applied.
- Alternate-day therapy is a therapeutic technique primarily designed for pefienis in whom long-term pharmacologic corticoid therapy is anticipated.
- In less severe disease processes in which corticoid therapy is indicated, it may be possible to initiate treatment with alternate-day therapy. More severe disease state usually will require daily divided high dose therapy for initiai control of the disease process. The initial suppressive dose level should be continued until a satisfactory clinical response is obtained, usually four to ten days in the case of many allergic and collagen diseases.
Side effectsView
Short courses of Methylprednisolone are usually well-tolerated with few, mild side effects. Long term, high doses of Methyiprednisoione may produce predictable and potentially serious side effects. Whenever possible, the lowest effective doses of Methylprednisolone should be used for the shortest length of time to minimize side effects. Alternate day dosing also can help reduce side effects. Side effects of Methylprednisolone and other corticosteroids range from mild annoyances to serious irreversible bodily damage. Side effects include fluid retention, weight gain, high blood pressure, potassium loss, headache, muscle weakness, hair growth on the face, glaucoma, cataracts, peptic ulceration, growth retardation in children, convulsions, and psychic disturbances including depression, euphoria, insomnia etc. Prolonged use of Methylprednisolone can depress the ability of the body's adrenal glands to produce corticosteroids. Abruptly stopping Methylprednisolone in these individuals can cause symptoms of corticosteroid insufficiency, with accompanying nausea, vomiting, and even shock. Therefore, withdrawal of Methylprednisolone usually is accomplished by gradually lowering the dose. Gradually tapering Methylprednisolone not only minimizes the symptoms of corticosteroid insufficiency, it also reduces the risk of an abrupt flare of the disease being treated.
ContraindicationsView
Systemic fungal infections arid known hypersensitivity to components.
PrecautionsView
Adrenocortical insufficiency may persist for months after discontinuation of therapy; therefore, in any situation of stress occurring during that period, hormone therapy should be reinstituted. Since mineralocorticoid secretion may be impaired, salt and/or a mineralocorticoid should be administered concurrently. There is an enhanced effect of corticosteroids on patients with hypothyroidism and in those with cirrhosis. Corticosteroids should be used cautiously in patients with ocular herpes simplex because of possible corneal perforation. Aspirin should be used cautiously in conjunction with corticosteroids in hypoprothrombinemia. The growth and development of infants and children on prolonged corticosteroid therapy should be carefully observed.
InteractionsView
Erythromycin, Clarithromycin, Phenobarbital, Phenytoin, Rifampin and Ketoconazole inhibit the metabolism of Methylprednisolone. Estrogens, including With control pills, can increase the effect of corticosteroids by 50%. Cyclosporin reduces the metabolism of Methylprednisolone. while Methylprednisolone reduces the metabolism of Cyclosporin. Methylprednisolone may increase or decrease the effect of blood thinners (e.g. Warfarin). For all these Interactions, the dose of Methylprednisolone may need to be lowered.
Pregnancy & lactationView
Pregnancy category C. Dregs should be given only if the potential benefit justifies the potential risk te the foetus. Mefhyiprednisofone has not been adequately evaluated in nursing mothers.
Overdose effectsView
Report of acute toxicity and/or death following an overdose of glucocorticoid ere rare. No specific antidote is available; treatment is supportive and symptomatic. Serum electrolytes should be monitored.
StorageView
Store in a cool and dry place, away from light. Keep out of reach of children.
Solupred
Methylprednisolone
Solupred
Methylprednisolone
Indications
Rheumatic disorders
Indication detailsView
Endocrine Disorders: Primary or Secondary Adrenocortical Insufficiency, Congenital Adrenal Hyperplasia, Nonsuppurative Thyroiditis, Hypercalcemia associated with Cancer.
Rheumatic Disorders: Rheumatoid Arthritis. Juvenile Rheumatoid Arthritis, Ankylosing Spondylitis, Acute and Subacute Bursitis, Synovitis of Osteoarthritis, Acute nonspecific Tenosynovitis, Post-traumatic Osteoarthritis, Psoriatic Arthritis, Epicondylitis, Acute Gouty Arthritis.
Collagen Diseases: Systemic lupus Erythematosus, Systemic Dermatomyositis and Acute Rheumatic Carditis.
Dermatologic Diseases: Bullous Dermatitis Herpetiformis, Severe Erythema Multiforme (Stevens-Johnson syndrome), Severe Seborrheic Dermatitis, Exfoliative Dermatitis, Mycosis Fungoides, Pemphigus, Severe Psoriasis.
Allergy: Seasonal or Perennial Allergic Rhinitis, Drug hypersensitivity reactions, Serum Sickness, Contact Dermatitis, Bronchial Asthma and Atopic Dermatitis;
Ophthalmic Diseases: Allergic Corneal Ulcers, Herpes Zoster Ophthalmicus, Anterior segment inflammation, Sympathetic Ophthalmia, Keratitis, Optic Neuritis, Allergic Conjunctivitis, Chorioretinitis, iritis end iridocyclitis.
Respiratory Diseases: Symptomatic sarcoidosis, Loeffler's syndrome not manageable by other means, berylliosis, Aspiration Pneumonitis.
Hematological Disorders: Idiopathic Thrombocytopenic Purpura in adults, Secondary Thrombocytopenia in adults, Acquired (Autoimmune) Hemolytic Anemia, Erythroblastopenia, Congenital (Erythroid) Hypoplastic Anemia.
Neoplastic Diseases: For palliative management of Leukemias and Lymphomas in adults, Acute leukemia of childhood.
Edematous States: To induce a diuresis or remission of Proteinuria in the Nephrotic Syndrome, without Uremia, of the idiopathic type or that due to Lupus Erythematosus.
Gastrointestinal Disease: To tide the patient over a critical period of the disease in Ulcerative Colitis & Regional Enteritis.
CNS Disease: Acute Exacerbations of Multiple Sclerosis.
Rheumatic Disorders: Rheumatoid Arthritis. Juvenile Rheumatoid Arthritis, Ankylosing Spondylitis, Acute and Subacute Bursitis, Synovitis of Osteoarthritis, Acute nonspecific Tenosynovitis, Post-traumatic Osteoarthritis, Psoriatic Arthritis, Epicondylitis, Acute Gouty Arthritis.
Collagen Diseases: Systemic lupus Erythematosus, Systemic Dermatomyositis and Acute Rheumatic Carditis.
Dermatologic Diseases: Bullous Dermatitis Herpetiformis, Severe Erythema Multiforme (Stevens-Johnson syndrome), Severe Seborrheic Dermatitis, Exfoliative Dermatitis, Mycosis Fungoides, Pemphigus, Severe Psoriasis.
Allergy: Seasonal or Perennial Allergic Rhinitis, Drug hypersensitivity reactions, Serum Sickness, Contact Dermatitis, Bronchial Asthma and Atopic Dermatitis;
Ophthalmic Diseases: Allergic Corneal Ulcers, Herpes Zoster Ophthalmicus, Anterior segment inflammation, Sympathetic Ophthalmia, Keratitis, Optic Neuritis, Allergic Conjunctivitis, Chorioretinitis, iritis end iridocyclitis.
Respiratory Diseases: Symptomatic sarcoidosis, Loeffler's syndrome not manageable by other means, berylliosis, Aspiration Pneumonitis.
Hematological Disorders: Idiopathic Thrombocytopenic Purpura in adults, Secondary Thrombocytopenia in adults, Acquired (Autoimmune) Hemolytic Anemia, Erythroblastopenia, Congenital (Erythroid) Hypoplastic Anemia.
Neoplastic Diseases: For palliative management of Leukemias and Lymphomas in adults, Acute leukemia of childhood.
Edematous States: To induce a diuresis or remission of Proteinuria in the Nephrotic Syndrome, without Uremia, of the idiopathic type or that due to Lupus Erythematosus.
Gastrointestinal Disease: To tide the patient over a critical period of the disease in Ulcerative Colitis & Regional Enteritis.
CNS Disease: Acute Exacerbations of Multiple Sclerosis.
Therapeutic classView
Glucocorticoids
PharmacologyView
Pharmacodynamic properties: Methylprednisolone Is a potent anti-inflammatory agent with the capacity to profoundly inhibit the immune system. Glucocorticoids primarily bind to and activate intracellular glucocorticoid receptors that being activated bind to promoter regions of DMA (which may activate or suppress transcription) and activate transcription factors that result in inactivation of genes through deacetylation of histones. Methylprednisolone influences the kidney and fluid & electrolyte balance, lipid,
protein, and carbohydrate metabolism, skeletal muscle, the cardiovascular system, the immune system, the nervous system, and the endocrine system.
Pharmacokinetic properties: The absolute bioavailability of Methylprednisclone is generally high (82% to 89%) following oral administration and rapidly absorbed and the maximum plasma concentration is achieved around 1.5 to 2.3 hours across doses following oral administration in normal healthy adults. Methylprednisolone is widely distributed into the tissues and its volume of distribution is 41-61.5 liter. It crosses the Wood-brain barrier and the placental barrier and is secreted in breast milk. The plasma protein binding of Methylprednisolone in humans is approximately 77%. Methylprednisolone is metabolized in the liver to inactive metabolites. No dosing adjustments are necessary for renal failure. Methylprednisolone is haemodializable.
protein, and carbohydrate metabolism, skeletal muscle, the cardiovascular system, the immune system, the nervous system, and the endocrine system.
Pharmacokinetic properties: The absolute bioavailability of Methylprednisclone is generally high (82% to 89%) following oral administration and rapidly absorbed and the maximum plasma concentration is achieved around 1.5 to 2.3 hours across doses following oral administration in normal healthy adults. Methylprednisolone is widely distributed into the tissues and its volume of distribution is 41-61.5 liter. It crosses the Wood-brain barrier and the placental barrier and is secreted in breast milk. The plasma protein binding of Methylprednisolone in humans is approximately 77%. Methylprednisolone is metabolized in the liver to inactive metabolites. No dosing adjustments are necessary for renal failure. Methylprednisolone is haemodializable.
DosageView
The usual range is 2-48 mg daily in divided doses, depending on the specific disease being treated.
As anti-inflammatory or immunosuppressive initial dosage: As anti-inflammatory or immunosuppressive, the initial dosage of Methylprednisolone tablets may vary from 4-48 mg per day depending on the specific disease entity being treated, in situations of less severity lower doses will generally suffice while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory dirtied response, Methylprednisolone should be discontinued and the patient transferred to other appropriate therapy. It should be emphasized that dosage requirements are variable and must be Individualized on the basis of the disease under treatment and the response of the patient.
As anti-inflammatory or immunosuppressive maintenance dosage: After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.
Multiple Sclerosis: In the treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of Methylprednisolone for a week followed by 64 mg every other day for 1 month have been shown to be effective.
Methylprednisolone 4 mg tablet can be used to treat and to control severe allergy end dermatitis following the guideline listed below to minimize the steroid withdrawal syndromes:
The following should be kept in mind when considering alternate-day therapy:
As anti-inflammatory or immunosuppressive initial dosage: As anti-inflammatory or immunosuppressive, the initial dosage of Methylprednisolone tablets may vary from 4-48 mg per day depending on the specific disease entity being treated, in situations of less severity lower doses will generally suffice while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory dirtied response, Methylprednisolone should be discontinued and the patient transferred to other appropriate therapy. It should be emphasized that dosage requirements are variable and must be Individualized on the basis of the disease under treatment and the response of the patient.
As anti-inflammatory or immunosuppressive maintenance dosage: After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.
Multiple Sclerosis: In the treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of Methylprednisolone for a week followed by 64 mg every other day for 1 month have been shown to be effective.
Methylprednisolone 4 mg tablet can be used to treat and to control severe allergy end dermatitis following the guideline listed below to minimize the steroid withdrawal syndromes:
- Day 1: 2 tablets before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
- Day 2: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
- Day 3: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 1 tablet at bedtime
- Day 4: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet at bedtime
- Day 5: 1 tablet before breakfast + 1 tablet at bedtime
- Day 6: 1 tablet before breakfast
The following should be kept in mind when considering alternate-day therapy:
- Basic principles and indications for corticosteroid therapy should be applied.
- Alternate-day therapy is a therapeutic technique primarily designed for pefienis in whom long-term pharmacologic corticoid therapy is anticipated.
- In less severe disease processes in which corticoid therapy is indicated, it may be possible to initiate treatment with alternate-day therapy. More severe disease state usually will require daily divided high dose therapy for initiai control of the disease process. The initial suppressive dose level should be continued until a satisfactory clinical response is obtained, usually four to ten days in the case of many allergic and collagen diseases.
Side effectsView
Short courses of Methylprednisolone are usually well-tolerated with few, mild side effects. Long term, high doses of Methyiprednisoione may produce predictable and potentially serious side effects. Whenever possible, the lowest effective doses of Methylprednisolone should be used for the shortest length of time to minimize side effects. Alternate day dosing also can help reduce side effects. Side effects of Methylprednisolone and other corticosteroids range from mild annoyances to serious irreversible bodily damage. Side effects include fluid retention, weight gain, high blood pressure, potassium loss, headache, muscle weakness, hair growth on the face, glaucoma, cataracts, peptic ulceration, growth retardation in children, convulsions, and psychic disturbances including depression, euphoria, insomnia etc. Prolonged use of Methylprednisolone can depress the ability of the body's adrenal glands to produce corticosteroids. Abruptly stopping Methylprednisolone in these individuals can cause symptoms of corticosteroid insufficiency, with accompanying nausea, vomiting, and even shock. Therefore, withdrawal of Methylprednisolone usually is accomplished by gradually lowering the dose. Gradually tapering Methylprednisolone not only minimizes the symptoms of corticosteroid insufficiency, it also reduces the risk of an abrupt flare of the disease being treated.
ContraindicationsView
Systemic fungal infections arid known hypersensitivity to components.
PrecautionsView
Adrenocortical insufficiency may persist for months after discontinuation of therapy; therefore, in any situation of stress occurring during that period, hormone therapy should be reinstituted. Since mineralocorticoid secretion may be impaired, salt and/or a mineralocorticoid should be administered concurrently. There is an enhanced effect of corticosteroids on patients with hypothyroidism and in those with cirrhosis. Corticosteroids should be used cautiously in patients with ocular herpes simplex because of possible corneal perforation. Aspirin should be used cautiously in conjunction with corticosteroids in hypoprothrombinemia. The growth and development of infants and children on prolonged corticosteroid therapy should be carefully observed.
InteractionsView
Erythromycin, Clarithromycin, Phenobarbital, Phenytoin, Rifampin and Ketoconazole inhibit the metabolism of Methylprednisolone. Estrogens, including With control pills, can increase the effect of corticosteroids by 50%. Cyclosporin reduces the metabolism of Methylprednisolone. while Methylprednisolone reduces the metabolism of Cyclosporin. Methylprednisolone may increase or decrease the effect of blood thinners (e.g. Warfarin). For all these Interactions, the dose of Methylprednisolone may need to be lowered.
Pregnancy & lactationView
Pregnancy category C. Dregs should be given only if the potential benefit justifies the potential risk te the foetus. Mefhyiprednisofone has not been adequately evaluated in nursing mothers.
Overdose effectsView
Report of acute toxicity and/or death following an overdose of glucocorticoid ere rare. No specific antidote is available; treatment is supportive and symptomatic. Serum electrolytes should be monitored.
StorageView
Store in a cool and dry place, away from light. Keep out of reach of children.
Solupred
Methylprednisolone
Solupred
Methylprednisolone
Indications
Rheumatic disorders
Indication detailsView
Endocrine Disorders: Primary or Secondary Adrenocortical Insufficiency, Congenital Adrenal Hyperplasia, Nonsuppurative Thyroiditis, Hypercalcemia associated with Cancer.
Rheumatic Disorders: Rheumatoid Arthritis. Juvenile Rheumatoid Arthritis, Ankylosing Spondylitis, Acute and Subacute Bursitis, Synovitis of Osteoarthritis, Acute nonspecific Tenosynovitis, Post-traumatic Osteoarthritis, Psoriatic Arthritis, Epicondylitis, Acute Gouty Arthritis.
Collagen Diseases: Systemic lupus Erythematosus, Systemic Dermatomyositis and Acute Rheumatic Carditis.
Dermatologic Diseases: Bullous Dermatitis Herpetiformis, Severe Erythema Multiforme (Stevens-Johnson syndrome), Severe Seborrheic Dermatitis, Exfoliative Dermatitis, Mycosis Fungoides, Pemphigus, Severe Psoriasis.
Allergy: Seasonal or Perennial Allergic Rhinitis, Drug hypersensitivity reactions, Serum Sickness, Contact Dermatitis, Bronchial Asthma and Atopic Dermatitis;
Ophthalmic Diseases: Allergic Corneal Ulcers, Herpes Zoster Ophthalmicus, Anterior segment inflammation, Sympathetic Ophthalmia, Keratitis, Optic Neuritis, Allergic Conjunctivitis, Chorioretinitis, iritis end iridocyclitis.
Respiratory Diseases: Symptomatic sarcoidosis, Loeffler's syndrome not manageable by other means, berylliosis, Aspiration Pneumonitis.
Hematological Disorders: Idiopathic Thrombocytopenic Purpura in adults, Secondary Thrombocytopenia in adults, Acquired (Autoimmune) Hemolytic Anemia, Erythroblastopenia, Congenital (Erythroid) Hypoplastic Anemia.
Neoplastic Diseases: For palliative management of Leukemias and Lymphomas in adults, Acute leukemia of childhood.
Edematous States: To induce a diuresis or remission of Proteinuria in the Nephrotic Syndrome, without Uremia, of the idiopathic type or that due to Lupus Erythematosus.
Gastrointestinal Disease: To tide the patient over a critical period of the disease in Ulcerative Colitis & Regional Enteritis.
CNS Disease: Acute Exacerbations of Multiple Sclerosis.
Rheumatic Disorders: Rheumatoid Arthritis. Juvenile Rheumatoid Arthritis, Ankylosing Spondylitis, Acute and Subacute Bursitis, Synovitis of Osteoarthritis, Acute nonspecific Tenosynovitis, Post-traumatic Osteoarthritis, Psoriatic Arthritis, Epicondylitis, Acute Gouty Arthritis.
Collagen Diseases: Systemic lupus Erythematosus, Systemic Dermatomyositis and Acute Rheumatic Carditis.
Dermatologic Diseases: Bullous Dermatitis Herpetiformis, Severe Erythema Multiforme (Stevens-Johnson syndrome), Severe Seborrheic Dermatitis, Exfoliative Dermatitis, Mycosis Fungoides, Pemphigus, Severe Psoriasis.
Allergy: Seasonal or Perennial Allergic Rhinitis, Drug hypersensitivity reactions, Serum Sickness, Contact Dermatitis, Bronchial Asthma and Atopic Dermatitis;
Ophthalmic Diseases: Allergic Corneal Ulcers, Herpes Zoster Ophthalmicus, Anterior segment inflammation, Sympathetic Ophthalmia, Keratitis, Optic Neuritis, Allergic Conjunctivitis, Chorioretinitis, iritis end iridocyclitis.
Respiratory Diseases: Symptomatic sarcoidosis, Loeffler's syndrome not manageable by other means, berylliosis, Aspiration Pneumonitis.
Hematological Disorders: Idiopathic Thrombocytopenic Purpura in adults, Secondary Thrombocytopenia in adults, Acquired (Autoimmune) Hemolytic Anemia, Erythroblastopenia, Congenital (Erythroid) Hypoplastic Anemia.
Neoplastic Diseases: For palliative management of Leukemias and Lymphomas in adults, Acute leukemia of childhood.
Edematous States: To induce a diuresis or remission of Proteinuria in the Nephrotic Syndrome, without Uremia, of the idiopathic type or that due to Lupus Erythematosus.
Gastrointestinal Disease: To tide the patient over a critical period of the disease in Ulcerative Colitis & Regional Enteritis.
CNS Disease: Acute Exacerbations of Multiple Sclerosis.
Therapeutic classView
Glucocorticoids
PharmacologyView
Pharmacodynamic properties: Methylprednisolone Is a potent anti-inflammatory agent with the capacity to profoundly inhibit the immune system. Glucocorticoids primarily bind to and activate intracellular glucocorticoid receptors that being activated bind to promoter regions of DMA (which may activate or suppress transcription) and activate transcription factors that result in inactivation of genes through deacetylation of histones. Methylprednisolone influences the kidney and fluid & electrolyte balance, lipid,
protein, and carbohydrate metabolism, skeletal muscle, the cardiovascular system, the immune system, the nervous system, and the endocrine system.
Pharmacokinetic properties: The absolute bioavailability of Methylprednisclone is generally high (82% to 89%) following oral administration and rapidly absorbed and the maximum plasma concentration is achieved around 1.5 to 2.3 hours across doses following oral administration in normal healthy adults. Methylprednisolone is widely distributed into the tissues and its volume of distribution is 41-61.5 liter. It crosses the Wood-brain barrier and the placental barrier and is secreted in breast milk. The plasma protein binding of Methylprednisolone in humans is approximately 77%. Methylprednisolone is metabolized in the liver to inactive metabolites. No dosing adjustments are necessary for renal failure. Methylprednisolone is haemodializable.
protein, and carbohydrate metabolism, skeletal muscle, the cardiovascular system, the immune system, the nervous system, and the endocrine system.
Pharmacokinetic properties: The absolute bioavailability of Methylprednisclone is generally high (82% to 89%) following oral administration and rapidly absorbed and the maximum plasma concentration is achieved around 1.5 to 2.3 hours across doses following oral administration in normal healthy adults. Methylprednisolone is widely distributed into the tissues and its volume of distribution is 41-61.5 liter. It crosses the Wood-brain barrier and the placental barrier and is secreted in breast milk. The plasma protein binding of Methylprednisolone in humans is approximately 77%. Methylprednisolone is metabolized in the liver to inactive metabolites. No dosing adjustments are necessary for renal failure. Methylprednisolone is haemodializable.
DosageView
The usual range is 2-48 mg daily in divided doses, depending on the specific disease being treated.
As anti-inflammatory or immunosuppressive initial dosage: As anti-inflammatory or immunosuppressive, the initial dosage of Methylprednisolone tablets may vary from 4-48 mg per day depending on the specific disease entity being treated, in situations of less severity lower doses will generally suffice while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory dirtied response, Methylprednisolone should be discontinued and the patient transferred to other appropriate therapy. It should be emphasized that dosage requirements are variable and must be Individualized on the basis of the disease under treatment and the response of the patient.
As anti-inflammatory or immunosuppressive maintenance dosage: After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.
Multiple Sclerosis: In the treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of Methylprednisolone for a week followed by 64 mg every other day for 1 month have been shown to be effective.
Methylprednisolone 4 mg tablet can be used to treat and to control severe allergy end dermatitis following the guideline listed below to minimize the steroid withdrawal syndromes:
The following should be kept in mind when considering alternate-day therapy:
As anti-inflammatory or immunosuppressive initial dosage: As anti-inflammatory or immunosuppressive, the initial dosage of Methylprednisolone tablets may vary from 4-48 mg per day depending on the specific disease entity being treated, in situations of less severity lower doses will generally suffice while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory dirtied response, Methylprednisolone should be discontinued and the patient transferred to other appropriate therapy. It should be emphasized that dosage requirements are variable and must be Individualized on the basis of the disease under treatment and the response of the patient.
As anti-inflammatory or immunosuppressive maintenance dosage: After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.
Multiple Sclerosis: In the treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of Methylprednisolone for a week followed by 64 mg every other day for 1 month have been shown to be effective.
Methylprednisolone 4 mg tablet can be used to treat and to control severe allergy end dermatitis following the guideline listed below to minimize the steroid withdrawal syndromes:
- Day 1: 2 tablets before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
- Day 2: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
- Day 3: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 1 tablet at bedtime
- Day 4: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet at bedtime
- Day 5: 1 tablet before breakfast + 1 tablet at bedtime
- Day 6: 1 tablet before breakfast
The following should be kept in mind when considering alternate-day therapy:
- Basic principles and indications for corticosteroid therapy should be applied.
- Alternate-day therapy is a therapeutic technique primarily designed for pefienis in whom long-term pharmacologic corticoid therapy is anticipated.
- In less severe disease processes in which corticoid therapy is indicated, it may be possible to initiate treatment with alternate-day therapy. More severe disease state usually will require daily divided high dose therapy for initiai control of the disease process. The initial suppressive dose level should be continued until a satisfactory clinical response is obtained, usually four to ten days in the case of many allergic and collagen diseases.
Side effectsView
Short courses of Methylprednisolone are usually well-tolerated with few, mild side effects. Long term, high doses of Methyiprednisoione may produce predictable and potentially serious side effects. Whenever possible, the lowest effective doses of Methylprednisolone should be used for the shortest length of time to minimize side effects. Alternate day dosing also can help reduce side effects. Side effects of Methylprednisolone and other corticosteroids range from mild annoyances to serious irreversible bodily damage. Side effects include fluid retention, weight gain, high blood pressure, potassium loss, headache, muscle weakness, hair growth on the face, glaucoma, cataracts, peptic ulceration, growth retardation in children, convulsions, and psychic disturbances including depression, euphoria, insomnia etc. Prolonged use of Methylprednisolone can depress the ability of the body's adrenal glands to produce corticosteroids. Abruptly stopping Methylprednisolone in these individuals can cause symptoms of corticosteroid insufficiency, with accompanying nausea, vomiting, and even shock. Therefore, withdrawal of Methylprednisolone usually is accomplished by gradually lowering the dose. Gradually tapering Methylprednisolone not only minimizes the symptoms of corticosteroid insufficiency, it also reduces the risk of an abrupt flare of the disease being treated.
ContraindicationsView
Systemic fungal infections arid known hypersensitivity to components.
PrecautionsView
Adrenocortical insufficiency may persist for months after discontinuation of therapy; therefore, in any situation of stress occurring during that period, hormone therapy should be reinstituted. Since mineralocorticoid secretion may be impaired, salt and/or a mineralocorticoid should be administered concurrently. There is an enhanced effect of corticosteroids on patients with hypothyroidism and in those with cirrhosis. Corticosteroids should be used cautiously in patients with ocular herpes simplex because of possible corneal perforation. Aspirin should be used cautiously in conjunction with corticosteroids in hypoprothrombinemia. The growth and development of infants and children on prolonged corticosteroid therapy should be carefully observed.
InteractionsView
Erythromycin, Clarithromycin, Phenobarbital, Phenytoin, Rifampin and Ketoconazole inhibit the metabolism of Methylprednisolone. Estrogens, including With control pills, can increase the effect of corticosteroids by 50%. Cyclosporin reduces the metabolism of Methylprednisolone. while Methylprednisolone reduces the metabolism of Cyclosporin. Methylprednisolone may increase or decrease the effect of blood thinners (e.g. Warfarin). For all these Interactions, the dose of Methylprednisolone may need to be lowered.
Pregnancy & lactationView
Pregnancy category C. Dregs should be given only if the potential benefit justifies the potential risk te the foetus. Mefhyiprednisofone has not been adequately evaluated in nursing mothers.
Overdose effectsView
Report of acute toxicity and/or death following an overdose of glucocorticoid ere rare. No specific antidote is available; treatment is supportive and symptomatic. Serum electrolytes should be monitored.
StorageView
Store in a cool and dry place, away from light. Keep out of reach of children.
Solupred
Methylprednisolone
Solupred
Methylprednisolone
Indications
Rheumatic disorders
Indication detailsView
Endocrine Disorders: Primary or Secondary Adrenocortical Insufficiency, Congenital Adrenal Hyperplasia, Nonsuppurative Thyroiditis, Hypercalcemia associated with Cancer.
Rheumatic Disorders: Rheumatoid Arthritis. Juvenile Rheumatoid Arthritis, Ankylosing Spondylitis, Acute and Subacute Bursitis, Synovitis of Osteoarthritis, Acute nonspecific Tenosynovitis, Post-traumatic Osteoarthritis, Psoriatic Arthritis, Epicondylitis, Acute Gouty Arthritis.
Collagen Diseases: Systemic lupus Erythematosus, Systemic Dermatomyositis and Acute Rheumatic Carditis.
Dermatologic Diseases: Bullous Dermatitis Herpetiformis, Severe Erythema Multiforme (Stevens-Johnson syndrome), Severe Seborrheic Dermatitis, Exfoliative Dermatitis, Mycosis Fungoides, Pemphigus, Severe Psoriasis.
Allergy: Seasonal or Perennial Allergic Rhinitis, Drug hypersensitivity reactions, Serum Sickness, Contact Dermatitis, Bronchial Asthma and Atopic Dermatitis;
Ophthalmic Diseases: Allergic Corneal Ulcers, Herpes Zoster Ophthalmicus, Anterior segment inflammation, Sympathetic Ophthalmia, Keratitis, Optic Neuritis, Allergic Conjunctivitis, Chorioretinitis, iritis end iridocyclitis.
Respiratory Diseases: Symptomatic sarcoidosis, Loeffler's syndrome not manageable by other means, berylliosis, Aspiration Pneumonitis.
Hematological Disorders: Idiopathic Thrombocytopenic Purpura in adults, Secondary Thrombocytopenia in adults, Acquired (Autoimmune) Hemolytic Anemia, Erythroblastopenia, Congenital (Erythroid) Hypoplastic Anemia.
Neoplastic Diseases: For palliative management of Leukemias and Lymphomas in adults, Acute leukemia of childhood.
Edematous States: To induce a diuresis or remission of Proteinuria in the Nephrotic Syndrome, without Uremia, of the idiopathic type or that due to Lupus Erythematosus.
Gastrointestinal Disease: To tide the patient over a critical period of the disease in Ulcerative Colitis & Regional Enteritis.
CNS Disease: Acute Exacerbations of Multiple Sclerosis.
Rheumatic Disorders: Rheumatoid Arthritis. Juvenile Rheumatoid Arthritis, Ankylosing Spondylitis, Acute and Subacute Bursitis, Synovitis of Osteoarthritis, Acute nonspecific Tenosynovitis, Post-traumatic Osteoarthritis, Psoriatic Arthritis, Epicondylitis, Acute Gouty Arthritis.
Collagen Diseases: Systemic lupus Erythematosus, Systemic Dermatomyositis and Acute Rheumatic Carditis.
Dermatologic Diseases: Bullous Dermatitis Herpetiformis, Severe Erythema Multiforme (Stevens-Johnson syndrome), Severe Seborrheic Dermatitis, Exfoliative Dermatitis, Mycosis Fungoides, Pemphigus, Severe Psoriasis.
Allergy: Seasonal or Perennial Allergic Rhinitis, Drug hypersensitivity reactions, Serum Sickness, Contact Dermatitis, Bronchial Asthma and Atopic Dermatitis;
Ophthalmic Diseases: Allergic Corneal Ulcers, Herpes Zoster Ophthalmicus, Anterior segment inflammation, Sympathetic Ophthalmia, Keratitis, Optic Neuritis, Allergic Conjunctivitis, Chorioretinitis, iritis end iridocyclitis.
Respiratory Diseases: Symptomatic sarcoidosis, Loeffler's syndrome not manageable by other means, berylliosis, Aspiration Pneumonitis.
Hematological Disorders: Idiopathic Thrombocytopenic Purpura in adults, Secondary Thrombocytopenia in adults, Acquired (Autoimmune) Hemolytic Anemia, Erythroblastopenia, Congenital (Erythroid) Hypoplastic Anemia.
Neoplastic Diseases: For palliative management of Leukemias and Lymphomas in adults, Acute leukemia of childhood.
Edematous States: To induce a diuresis or remission of Proteinuria in the Nephrotic Syndrome, without Uremia, of the idiopathic type or that due to Lupus Erythematosus.
Gastrointestinal Disease: To tide the patient over a critical period of the disease in Ulcerative Colitis & Regional Enteritis.
CNS Disease: Acute Exacerbations of Multiple Sclerosis.
Therapeutic classView
Glucocorticoids
PharmacologyView
Pharmacodynamic properties: Methylprednisolone Is a potent anti-inflammatory agent with the capacity to profoundly inhibit the immune system. Glucocorticoids primarily bind to and activate intracellular glucocorticoid receptors that being activated bind to promoter regions of DMA (which may activate or suppress transcription) and activate transcription factors that result in inactivation of genes through deacetylation of histones. Methylprednisolone influences the kidney and fluid & electrolyte balance, lipid,
protein, and carbohydrate metabolism, skeletal muscle, the cardiovascular system, the immune system, the nervous system, and the endocrine system.
Pharmacokinetic properties: The absolute bioavailability of Methylprednisclone is generally high (82% to 89%) following oral administration and rapidly absorbed and the maximum plasma concentration is achieved around 1.5 to 2.3 hours across doses following oral administration in normal healthy adults. Methylprednisolone is widely distributed into the tissues and its volume of distribution is 41-61.5 liter. It crosses the Wood-brain barrier and the placental barrier and is secreted in breast milk. The plasma protein binding of Methylprednisolone in humans is approximately 77%. Methylprednisolone is metabolized in the liver to inactive metabolites. No dosing adjustments are necessary for renal failure. Methylprednisolone is haemodializable.
protein, and carbohydrate metabolism, skeletal muscle, the cardiovascular system, the immune system, the nervous system, and the endocrine system.
Pharmacokinetic properties: The absolute bioavailability of Methylprednisclone is generally high (82% to 89%) following oral administration and rapidly absorbed and the maximum plasma concentration is achieved around 1.5 to 2.3 hours across doses following oral administration in normal healthy adults. Methylprednisolone is widely distributed into the tissues and its volume of distribution is 41-61.5 liter. It crosses the Wood-brain barrier and the placental barrier and is secreted in breast milk. The plasma protein binding of Methylprednisolone in humans is approximately 77%. Methylprednisolone is metabolized in the liver to inactive metabolites. No dosing adjustments are necessary for renal failure. Methylprednisolone is haemodializable.
DosageView
The usual range is 2-48 mg daily in divided doses, depending on the specific disease being treated.
As anti-inflammatory or immunosuppressive initial dosage: As anti-inflammatory or immunosuppressive, the initial dosage of Methylprednisolone tablets may vary from 4-48 mg per day depending on the specific disease entity being treated, in situations of less severity lower doses will generally suffice while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory dirtied response, Methylprednisolone should be discontinued and the patient transferred to other appropriate therapy. It should be emphasized that dosage requirements are variable and must be Individualized on the basis of the disease under treatment and the response of the patient.
As anti-inflammatory or immunosuppressive maintenance dosage: After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.
Multiple Sclerosis: In the treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of Methylprednisolone for a week followed by 64 mg every other day for 1 month have been shown to be effective.
Methylprednisolone 4 mg tablet can be used to treat and to control severe allergy end dermatitis following the guideline listed below to minimize the steroid withdrawal syndromes:
The following should be kept in mind when considering alternate-day therapy:
As anti-inflammatory or immunosuppressive initial dosage: As anti-inflammatory or immunosuppressive, the initial dosage of Methylprednisolone tablets may vary from 4-48 mg per day depending on the specific disease entity being treated, in situations of less severity lower doses will generally suffice while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory dirtied response, Methylprednisolone should be discontinued and the patient transferred to other appropriate therapy. It should be emphasized that dosage requirements are variable and must be Individualized on the basis of the disease under treatment and the response of the patient.
As anti-inflammatory or immunosuppressive maintenance dosage: After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.
Multiple Sclerosis: In the treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of Methylprednisolone for a week followed by 64 mg every other day for 1 month have been shown to be effective.
Methylprednisolone 4 mg tablet can be used to treat and to control severe allergy end dermatitis following the guideline listed below to minimize the steroid withdrawal syndromes:
- Day 1: 2 tablets before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
- Day 2: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
- Day 3: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 1 tablet at bedtime
- Day 4: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet at bedtime
- Day 5: 1 tablet before breakfast + 1 tablet at bedtime
- Day 6: 1 tablet before breakfast
The following should be kept in mind when considering alternate-day therapy:
- Basic principles and indications for corticosteroid therapy should be applied.
- Alternate-day therapy is a therapeutic technique primarily designed for pefienis in whom long-term pharmacologic corticoid therapy is anticipated.
- In less severe disease processes in which corticoid therapy is indicated, it may be possible to initiate treatment with alternate-day therapy. More severe disease state usually will require daily divided high dose therapy for initiai control of the disease process. The initial suppressive dose level should be continued until a satisfactory clinical response is obtained, usually four to ten days in the case of many allergic and collagen diseases.
Side effectsView
Short courses of Methylprednisolone are usually well-tolerated with few, mild side effects. Long term, high doses of Methyiprednisoione may produce predictable and potentially serious side effects. Whenever possible, the lowest effective doses of Methylprednisolone should be used for the shortest length of time to minimize side effects. Alternate day dosing also can help reduce side effects. Side effects of Methylprednisolone and other corticosteroids range from mild annoyances to serious irreversible bodily damage. Side effects include fluid retention, weight gain, high blood pressure, potassium loss, headache, muscle weakness, hair growth on the face, glaucoma, cataracts, peptic ulceration, growth retardation in children, convulsions, and psychic disturbances including depression, euphoria, insomnia etc. Prolonged use of Methylprednisolone can depress the ability of the body's adrenal glands to produce corticosteroids. Abruptly stopping Methylprednisolone in these individuals can cause symptoms of corticosteroid insufficiency, with accompanying nausea, vomiting, and even shock. Therefore, withdrawal of Methylprednisolone usually is accomplished by gradually lowering the dose. Gradually tapering Methylprednisolone not only minimizes the symptoms of corticosteroid insufficiency, it also reduces the risk of an abrupt flare of the disease being treated.
ContraindicationsView
Systemic fungal infections arid known hypersensitivity to components.
PrecautionsView
Adrenocortical insufficiency may persist for months after discontinuation of therapy; therefore, in any situation of stress occurring during that period, hormone therapy should be reinstituted. Since mineralocorticoid secretion may be impaired, salt and/or a mineralocorticoid should be administered concurrently. There is an enhanced effect of corticosteroids on patients with hypothyroidism and in those with cirrhosis. Corticosteroids should be used cautiously in patients with ocular herpes simplex because of possible corneal perforation. Aspirin should be used cautiously in conjunction with corticosteroids in hypoprothrombinemia. The growth and development of infants and children on prolonged corticosteroid therapy should be carefully observed.
InteractionsView
Erythromycin, Clarithromycin, Phenobarbital, Phenytoin, Rifampin and Ketoconazole inhibit the metabolism of Methylprednisolone. Estrogens, including With control pills, can increase the effect of corticosteroids by 50%. Cyclosporin reduces the metabolism of Methylprednisolone. while Methylprednisolone reduces the metabolism of Cyclosporin. Methylprednisolone may increase or decrease the effect of blood thinners (e.g. Warfarin). For all these Interactions, the dose of Methylprednisolone may need to be lowered.
Pregnancy & lactationView
Pregnancy category C. Dregs should be given only if the potential benefit justifies the potential risk te the foetus. Mefhyiprednisofone has not been adequately evaluated in nursing mothers.
Overdose effectsView
Report of acute toxicity and/or death following an overdose of glucocorticoid ere rare. No specific antidote is available; treatment is supportive and symptomatic. Serum electrolytes should be monitored.
StorageView
Store in a cool and dry place, away from light. Keep out of reach of children.
Solupred
Methylprednisolone Sodium Succcinate
Solupred
Methylprednisolone Sodium Succcinate
Indications
Vestibular neuritis
Indication detailsView
Methylprednisolone Sodium Succinate IM/IV is indicated in the following conditions:
Endocrine disorder: Primary or secondary adrenocortical insufficiency, acute adrenocortical insufficiency, shock unresponsive to conventional, congenital adrenal hyperplasia, Nonsuppurative thyroiditis. Hypercalcemia associated with cancer.
Rheumatic disorder: Rheumatoid arthritis, including juvenile rheumatoid arthritis, acute and subacute bursitis, epicondylitis, acute nonspecific tenosynovitis, acute gouty arthritis, psoriatic arthritis, ankylosing spondylitis.
Collagen disease: During an exacerbation or as maintenance therapy in selected cases of systemic lupus erythematosus; acute rheumatic carditis, systemic dermatomyositis (polymyositis).
Dermatological disease: Pemphigus, severe erythema multiforme (Stevens-Johnson syndrome), exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe psoriasis, mycosis fungoides.
Allergic states: Controls bronchial asthma, contact dermatitis, atopic dermatitis, serum sickness, seasonal or perennial allergic rhinitis, drug hypersensitivity reaction, urticarial transfusion reactions, acute noninfectious laryngeal edema (epinephrine is the drug of first choice), anaphylactic reactions.
Ophthalmic disease: Severe acute and chronic allergic and inflammatory processes involving the eye, such as: herpes zoster ophthalmicus, iritis, iridocyclitis, chorioretinitis, diffuse posterior uveitis and chroiditis, optic neuritis, sympathetic ophthalmia, anterior segment inflammation, allergic conjunctivitis, allergic corneal marginal ulcers, keratitis.
Gastrointestinal disease: To tide the patient over a critical period of the disease in: ulcerative colitis (systemic therapy), regional enteritis (systemic therapy), Crohn’s disease.
Respiratory disease: Symptomatic sarcoidosis, berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculosis chemotherapy, Loafer syndrome not manageable by other means, aspiration pneumonitis.
Hematologic disorder: Acquired (autoimmune) hemolytic anemia, idiopathic thrombocytopenic purpura in adults (IV only, IM administration is contraindicated), erythroblastopenia (RBC anemia), congenital (erythroid) hypoplastic anemia, secondary thrombocytopenia in adults.
Neoplastic disease: For palliative management of: leukemias and lymphoma in adults, acute leukemia of childhood.
Edematous state: To induce diuresis or remission of proteinuria in the nephrotic syndrome, without uremia of the idiopathic type or that due to lupus erythematosus.
Miscellaneous: Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculosis chemotherapy. Trichinosis with neurologic or myocardial involvement.
Endocrine disorder: Primary or secondary adrenocortical insufficiency, acute adrenocortical insufficiency, shock unresponsive to conventional, congenital adrenal hyperplasia, Nonsuppurative thyroiditis. Hypercalcemia associated with cancer.
Rheumatic disorder: Rheumatoid arthritis, including juvenile rheumatoid arthritis, acute and subacute bursitis, epicondylitis, acute nonspecific tenosynovitis, acute gouty arthritis, psoriatic arthritis, ankylosing spondylitis.
Collagen disease: During an exacerbation or as maintenance therapy in selected cases of systemic lupus erythematosus; acute rheumatic carditis, systemic dermatomyositis (polymyositis).
Dermatological disease: Pemphigus, severe erythema multiforme (Stevens-Johnson syndrome), exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe psoriasis, mycosis fungoides.
Allergic states: Controls bronchial asthma, contact dermatitis, atopic dermatitis, serum sickness, seasonal or perennial allergic rhinitis, drug hypersensitivity reaction, urticarial transfusion reactions, acute noninfectious laryngeal edema (epinephrine is the drug of first choice), anaphylactic reactions.
Ophthalmic disease: Severe acute and chronic allergic and inflammatory processes involving the eye, such as: herpes zoster ophthalmicus, iritis, iridocyclitis, chorioretinitis, diffuse posterior uveitis and chroiditis, optic neuritis, sympathetic ophthalmia, anterior segment inflammation, allergic conjunctivitis, allergic corneal marginal ulcers, keratitis.
Gastrointestinal disease: To tide the patient over a critical period of the disease in: ulcerative colitis (systemic therapy), regional enteritis (systemic therapy), Crohn’s disease.
Respiratory disease: Symptomatic sarcoidosis, berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculosis chemotherapy, Loafer syndrome not manageable by other means, aspiration pneumonitis.
Hematologic disorder: Acquired (autoimmune) hemolytic anemia, idiopathic thrombocytopenic purpura in adults (IV only, IM administration is contraindicated), erythroblastopenia (RBC anemia), congenital (erythroid) hypoplastic anemia, secondary thrombocytopenia in adults.
Neoplastic disease: For palliative management of: leukemias and lymphoma in adults, acute leukemia of childhood.
Edematous state: To induce diuresis or remission of proteinuria in the nephrotic syndrome, without uremia of the idiopathic type or that due to lupus erythematosus.
Miscellaneous: Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculosis chemotherapy. Trichinosis with neurologic or myocardial involvement.
Therapeutic classView
Glucocorticoids
PharmacologyView
Methylprednisolone, a naturally occurring glucocorticoid (hydrocortisone and cortisone), which has also salt-retaining properties, is used as replacement therapy in adrenocortical deficiency states. This synthetic analog is primarily used for its potent anti-inflammatory effects in disorders of many organ systems. The intravenous injection of Methylprednisolone Sodium Succinate, demonstrable effects are evident within one hour and persist for a variable period. Excretion of the administered dose is nearly complete within 12 hours. Thus, if constantly high blood levels are required, injections should be made every 4 to 6 hours. This preparation is also rapidly absorbed when administered intramuscularly and is excreted in a pattern similar to that observed after intravenous injection. Its anti-inflammatory potency is greater than prednisolone in the ratio of 5 to 4. It has only minimal mineralocorticoid properties and has less tendency than prednisolone to induce sodium and water retention. It influences carbohydrate, protein, fat and purine metabolism, electrolyte and water balance, and the functional capacities of the cardiovascular system, the kidney, the skeletal muscle, nervous system and other organs and tissues. It exerts a suppressive effect on the immune response.
DosageView
Methylprednisolone may be administered by IM or IV or by IV infusion. To administer by IM or IV injection, prepare solution as direction for reconstitution. The desired dose may be administered intravenously over a period of several minutes. When high dose therapy is desired, the recommended dose of Methylprednisolone Sodium Succinate for Injection, USP is 30 mg/kg administered intravenously over at least 30 minutes. This dose may be repeated every 4 to 6 hours for 48 hours. In general, high-dose corticosteroid therapy should be continued only until the patient’s condition has stabilized usually not beyond 48 to 72 hours.
Although adverse effects associated with high dose short-term corticoid therapy are uncommon, peptic ulceration may occur. Prophylactic antacid therapy may be indicated.
In other indications, the initial dosage will vary from 10 to 40 mg of Methylprednisolone depending on the clinical problem being treated. The larger doses may be required for short-term management of severe, acute conditions. The initial dose usually should be given intravenously over a period of several minutes. Subsequent doses may be given intravenously or intramuscularly at intervals dictated by the patient’s response and clinical condition. Corticoid therapy is an adjunct to, and not a replacement for conventional therapy.
Dosage must be decreased or discontinued gradually when the drug has been administered for more than a few days. If a period of spontaneous remission occurs in a chronic condition, treatment should be discontinued. Routine laboratory studies, such as urinalysis, two-hour postprandial blood sugar, determination of blood pressure and body weight, and a chest X-ray should be made at regular intervals during prolonged therapy. Upper GI X-rays are desirable in patients with an ulcer history or significant dyspepsia.
In pediatric patients, the initial dose of Methylprednisolone may vary depending on the specific disease being treated. The initial dose is 0.11-1.6 mg/day in three or four divided doses. Dosage may be reduced for infants and children but should be governed more by the severity of the condition and response of the patient than by age or size but it should not be less than 0.5 mg per kg every 24 hours.
In the treatment of acute exacerbations of multiple sclerosis daily doses is 160 mg daily for 3 days. Methylprednisolone powder for injection/infusion should be given as an intravenous infusion over at least 30 minutes.
Although adverse effects associated with high dose short-term corticoid therapy are uncommon, peptic ulceration may occur. Prophylactic antacid therapy may be indicated.
In other indications, the initial dosage will vary from 10 to 40 mg of Methylprednisolone depending on the clinical problem being treated. The larger doses may be required for short-term management of severe, acute conditions. The initial dose usually should be given intravenously over a period of several minutes. Subsequent doses may be given intravenously or intramuscularly at intervals dictated by the patient’s response and clinical condition. Corticoid therapy is an adjunct to, and not a replacement for conventional therapy.
Dosage must be decreased or discontinued gradually when the drug has been administered for more than a few days. If a period of spontaneous remission occurs in a chronic condition, treatment should be discontinued. Routine laboratory studies, such as urinalysis, two-hour postprandial blood sugar, determination of blood pressure and body weight, and a chest X-ray should be made at regular intervals during prolonged therapy. Upper GI X-rays are desirable in patients with an ulcer history or significant dyspepsia.
In pediatric patients, the initial dose of Methylprednisolone may vary depending on the specific disease being treated. The initial dose is 0.11-1.6 mg/day in three or four divided doses. Dosage may be reduced for infants and children but should be governed more by the severity of the condition and response of the patient than by age or size but it should not be less than 0.5 mg per kg every 24 hours.
In the treatment of acute exacerbations of multiple sclerosis daily doses is 160 mg daily for 3 days. Methylprednisolone powder for injection/infusion should be given as an intravenous infusion over at least 30 minutes.
Side effectsView
Fluid and Electrolyte Disturbances: Sodium retention, fluid retention, congestive heart failure in susceptible patients, potassium loss, hypokalemic alkalosis, hypertension.
Musculoskeletal: Muscle weakness, steroid myopathy, loss of muscle mass, severe arthralgia, vertebral compression fractures, aseptic necrosis of femoral and humeral heads, pathologic fracture of long bones, osteoporosis.
Gastrointestinal: Peptic ulcer with possible perforation and hemorrhage, pancreatitis, abdominal distention, and ulcerative esophagitis.
Dermatologic: Impaired wound healing, thin fragile skin, petechiae and ecchymoses, facial erythema, increased sweating, may suppress reactions to skin tests.
Neurological: Increased intracranial pressure with papilledema (pseudo-tumor cerebri) usually after treatment, convulsions, vertigo, headache.
Endocrine: Development of Cushingoid state, suppression of growth in children, secondary adrenocortical and pituitary unresponsiveness, particularly in times of stress, as in trauma, surgery or illness, menstrual irregularities, decreased carbohydrate tolerance, manifestations of latent diabetes mellitus, increased requirements for insulin or oral hypoglycemic agents in diabetics.
Ophthalmic: Posterior subcapsular cataracts, increased intraocular pressure, glaucoma, exophthalmos.
Others: Negative nitrogen balance due to protein catabolism.
The following additional adverse reactions are related to parenteral corticosteroid therapy: hyperpigmentation or hypopigmentation, subcutaneous and cutaneous atrophy, sterile abscess, anaphylactic reaction with or without circulatory collapse, cardiac arrest, bronchospasm, urticaria, nausea and vomiting, cardiac arrhythmias; hypotension or hypertension.
Musculoskeletal: Muscle weakness, steroid myopathy, loss of muscle mass, severe arthralgia, vertebral compression fractures, aseptic necrosis of femoral and humeral heads, pathologic fracture of long bones, osteoporosis.
Gastrointestinal: Peptic ulcer with possible perforation and hemorrhage, pancreatitis, abdominal distention, and ulcerative esophagitis.
Dermatologic: Impaired wound healing, thin fragile skin, petechiae and ecchymoses, facial erythema, increased sweating, may suppress reactions to skin tests.
Neurological: Increased intracranial pressure with papilledema (pseudo-tumor cerebri) usually after treatment, convulsions, vertigo, headache.
Endocrine: Development of Cushingoid state, suppression of growth in children, secondary adrenocortical and pituitary unresponsiveness, particularly in times of stress, as in trauma, surgery or illness, menstrual irregularities, decreased carbohydrate tolerance, manifestations of latent diabetes mellitus, increased requirements for insulin or oral hypoglycemic agents in diabetics.
Ophthalmic: Posterior subcapsular cataracts, increased intraocular pressure, glaucoma, exophthalmos.
Others: Negative nitrogen balance due to protein catabolism.
The following additional adverse reactions are related to parenteral corticosteroid therapy: hyperpigmentation or hypopigmentation, subcutaneous and cutaneous atrophy, sterile abscess, anaphylactic reaction with or without circulatory collapse, cardiac arrest, bronchospasm, urticaria, nausea and vomiting, cardiac arrhythmias; hypotension or hypertension.
ContraindicationsView
Methylprednisolone Sterile Powder is contraindicated:
- In systemic fungal infections and patients with known hypersensitivity to the product and its constituents.
- For intrathecal administration. Reports of severe medical events have been associated with this route of administration.
- Intramuscular corticosteroid preparations are contraindicated for idiopathic thrombocytopenic purpura.
PrecautionsView
Methylprednisolone, like many other steroid formulations, is sensitive to heat. Therefore, it should not be autoclaved when it is desirable to sterilize the exterior of the vial. The lowest possible dose of corticosteroid should be used to control the condition under treatment. When reduction in dosage is possible, the reduction should be gradual. Since complications of treatment with glucocorticoids are dependent on the size of the dose and the duration of treatment a risk/benefit decision must be made in each individual case as to dose and duration of treatment and as to whether daily or intermittent therapy should be used. For chronic conditions, discontinuation of corticosteroids may result in clinical improvement.
InteractionsView
- Aminoglutethimide may lead to a loss of corticosteroid-induced adrenal suppression.
- Amphotericin B injection and potassium-depleting agents- When corticosteroids are administered concomitantly with potassium-depleting agents (i.e., amphotericin B, diuretics), patients should be observed closely for the development of hypokalemia.
- Macrolide antibiotics have been reported to cause a significant decrease in corticosteroid clearance.
- Anticholinesterases- Concomitant use of anticholinesterase agents and corticosteroids may produce severe weakness in patients with myasthenia gravis. If possible, anticholinesterase agents should be withdrawn at least 24 hours before initiating corticosteroid therapy.
- Anticoagulants, oral- Coadministration of corticosteroids and warfarin usually results in inhibition of response to warfarin, although there have been some conflicting reports.
- Antidiabetics- Because corticosteroids may increase blood glucose concentrations, dosage adjustments of antidiabetic agents may be required.
- Antitubercular drugs- Serum concentrations of isoniazid may be decreased.
- Cholestyramine may increase the clearance of corticosteroids.
- Cyclosporine Increased activity of both cyclosporine and corticosteroids may occur when the two are used concurrently. Convulsions have been reported with this concurrent use.
- Digitalis glycosides- Patients on digitalis glycosides may be at increased risk of arrhythmias due to hypokalemia.
- Estrogens, including oral contraceptives- Estrogens may decrease the hepatic metabolism of certain corticosteroids, thereby increasing their effect.
- Hepatic Enzyme Inhibitors- Drugs which inhibit cytochrome P450 3A4 have the potential to result in increased plasma concentrations of corticosteroids.
- Ketoconazole has been reported to significantly decrease the metabolism of certain corticosteroids by up to 60%, leading to an increased risk of corticosteroid side effects.
- Nonsteroidal anti-inflammatory agents (NSAIDs)- Concomitant use of aspirin and corticosteroids increases the risk of gastrointestinal side effects.
- Skin tests- Corticosteroids may suppress reactions to skin tests.
- Vaccines- Patients on prolonged corticosteroid therapy may exhibit a diminished response to toxoids and live or inactivated vaccines due to inhibition of antibody response.
Pregnancy & lactationView
Pregnancy: Corticosteroids have been shown to be teratogenic in many species when given in doses equivalent to the human dose. There are no adequate and well-controlled studies in pregnant women. Corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Infants born to mothers who have received corticosteroids during pregnancy should be carefully observed for signs of hypoadrenalism.
Lactation: Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Because of the potential for serious adverse reactions in nursing infants from corticosteroids, a decision should be made whether to continue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Lactation: Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Because of the potential for serious adverse reactions in nursing infants from corticosteroids, a decision should be made whether to continue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric usageView
Pediatric Use: The adverse effects of corticosteroids in pediatric patients are similar to those in adults. Like adults, pediatric patients should be carefully observed with frequent measurements of blood pressure, weight, height, intraocular pressure and clinical evaluation for the presence of infection, psychosocial disturbances, thromboembolism, peptic ulcers, cataracts and osteoporosis. Pediatric patients who are treated with corticosteroids by any route, including systemically administered corticosteroids, may experience a decrease in their growth velocity. In order to minimize the potential growth effects of corticosteroids, pediatric patients should be titrated to the lowest effective dose.
Geriatric Use: Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, refecting the greater frequency of decreased hepatic, renal or cardiac function and of concomitant disease or other drug therapy.
Overdose effectsView
Treatment of acute over dosage is by supportive and symptomatic therapy. For chronic over dosage in the face of severe disease requiring continuous steroid therapy, the dosage of the corticosteroid may be reduced only temporarily or alternate day treatment may be introduced.
ReconstitutionView
Directions for Reconstitution-
- Remove protective plastic flip-of seal.
- Cleanse stopper with a suitable germicide.
- Aseptically add 8 mL Water for Injection BP for the 500 mg vial or 16 ml for 1 gm vial by means of a syringe into the vial.
- Agitate to effect solution to dissolve the powder content.
- Invert vial. Insert the needle through the target area of stopper until the tip is just visible. Withdraw dose.
StorageView
Protect from light. Store at controlled room temperature 20° to 25°C. Store solution at controlled room temperature 20° to 25°C.Use solution within 48 hours after mixing.
Solupred
Methylprednisolone Sodium Succcinate
Solupred
Methylprednisolone Sodium Succcinate
Indications
Vestibular neuritis
Indication detailsView
Methylprednisolone Sodium Succinate IM/IV is indicated in the following conditions:
Endocrine disorder: Primary or secondary adrenocortical insufficiency, acute adrenocortical insufficiency, shock unresponsive to conventional, congenital adrenal hyperplasia, Nonsuppurative thyroiditis. Hypercalcemia associated with cancer.
Rheumatic disorder: Rheumatoid arthritis, including juvenile rheumatoid arthritis, acute and subacute bursitis, epicondylitis, acute nonspecific tenosynovitis, acute gouty arthritis, psoriatic arthritis, ankylosing spondylitis.
Collagen disease: During an exacerbation or as maintenance therapy in selected cases of systemic lupus erythematosus; acute rheumatic carditis, systemic dermatomyositis (polymyositis).
Dermatological disease: Pemphigus, severe erythema multiforme (Stevens-Johnson syndrome), exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe psoriasis, mycosis fungoides.
Allergic states: Controls bronchial asthma, contact dermatitis, atopic dermatitis, serum sickness, seasonal or perennial allergic rhinitis, drug hypersensitivity reaction, urticarial transfusion reactions, acute noninfectious laryngeal edema (epinephrine is the drug of first choice), anaphylactic reactions.
Ophthalmic disease: Severe acute and chronic allergic and inflammatory processes involving the eye, such as: herpes zoster ophthalmicus, iritis, iridocyclitis, chorioretinitis, diffuse posterior uveitis and chroiditis, optic neuritis, sympathetic ophthalmia, anterior segment inflammation, allergic conjunctivitis, allergic corneal marginal ulcers, keratitis.
Gastrointestinal disease: To tide the patient over a critical period of the disease in: ulcerative colitis (systemic therapy), regional enteritis (systemic therapy), Crohn’s disease.
Respiratory disease: Symptomatic sarcoidosis, berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculosis chemotherapy, Loafer syndrome not manageable by other means, aspiration pneumonitis.
Hematologic disorder: Acquired (autoimmune) hemolytic anemia, idiopathic thrombocytopenic purpura in adults (IV only, IM administration is contraindicated), erythroblastopenia (RBC anemia), congenital (erythroid) hypoplastic anemia, secondary thrombocytopenia in adults.
Neoplastic disease: For palliative management of: leukemias and lymphoma in adults, acute leukemia of childhood.
Edematous state: To induce diuresis or remission of proteinuria in the nephrotic syndrome, without uremia of the idiopathic type or that due to lupus erythematosus.
Miscellaneous: Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculosis chemotherapy. Trichinosis with neurologic or myocardial involvement.
Endocrine disorder: Primary or secondary adrenocortical insufficiency, acute adrenocortical insufficiency, shock unresponsive to conventional, congenital adrenal hyperplasia, Nonsuppurative thyroiditis. Hypercalcemia associated with cancer.
Rheumatic disorder: Rheumatoid arthritis, including juvenile rheumatoid arthritis, acute and subacute bursitis, epicondylitis, acute nonspecific tenosynovitis, acute gouty arthritis, psoriatic arthritis, ankylosing spondylitis.
Collagen disease: During an exacerbation or as maintenance therapy in selected cases of systemic lupus erythematosus; acute rheumatic carditis, systemic dermatomyositis (polymyositis).
Dermatological disease: Pemphigus, severe erythema multiforme (Stevens-Johnson syndrome), exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe psoriasis, mycosis fungoides.
Allergic states: Controls bronchial asthma, contact dermatitis, atopic dermatitis, serum sickness, seasonal or perennial allergic rhinitis, drug hypersensitivity reaction, urticarial transfusion reactions, acute noninfectious laryngeal edema (epinephrine is the drug of first choice), anaphylactic reactions.
Ophthalmic disease: Severe acute and chronic allergic and inflammatory processes involving the eye, such as: herpes zoster ophthalmicus, iritis, iridocyclitis, chorioretinitis, diffuse posterior uveitis and chroiditis, optic neuritis, sympathetic ophthalmia, anterior segment inflammation, allergic conjunctivitis, allergic corneal marginal ulcers, keratitis.
Gastrointestinal disease: To tide the patient over a critical period of the disease in: ulcerative colitis (systemic therapy), regional enteritis (systemic therapy), Crohn’s disease.
Respiratory disease: Symptomatic sarcoidosis, berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculosis chemotherapy, Loafer syndrome not manageable by other means, aspiration pneumonitis.
Hematologic disorder: Acquired (autoimmune) hemolytic anemia, idiopathic thrombocytopenic purpura in adults (IV only, IM administration is contraindicated), erythroblastopenia (RBC anemia), congenital (erythroid) hypoplastic anemia, secondary thrombocytopenia in adults.
Neoplastic disease: For palliative management of: leukemias and lymphoma in adults, acute leukemia of childhood.
Edematous state: To induce diuresis or remission of proteinuria in the nephrotic syndrome, without uremia of the idiopathic type or that due to lupus erythematosus.
Miscellaneous: Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculosis chemotherapy. Trichinosis with neurologic or myocardial involvement.
Therapeutic classView
Glucocorticoids
PharmacologyView
Methylprednisolone, a naturally occurring glucocorticoid (hydrocortisone and cortisone), which has also salt-retaining properties, is used as replacement therapy in adrenocortical deficiency states. This synthetic analog is primarily used for its potent anti-inflammatory effects in disorders of many organ systems. The intravenous injection of Methylprednisolone Sodium Succinate, demonstrable effects are evident within one hour and persist for a variable period. Excretion of the administered dose is nearly complete within 12 hours. Thus, if constantly high blood levels are required, injections should be made every 4 to 6 hours. This preparation is also rapidly absorbed when administered intramuscularly and is excreted in a pattern similar to that observed after intravenous injection. Its anti-inflammatory potency is greater than prednisolone in the ratio of 5 to 4. It has only minimal mineralocorticoid properties and has less tendency than prednisolone to induce sodium and water retention. It influences carbohydrate, protein, fat and purine metabolism, electrolyte and water balance, and the functional capacities of the cardiovascular system, the kidney, the skeletal muscle, nervous system and other organs and tissues. It exerts a suppressive effect on the immune response.
DosageView
Methylprednisolone may be administered by IM or IV or by IV infusion. To administer by IM or IV injection, prepare solution as direction for reconstitution. The desired dose may be administered intravenously over a period of several minutes. When high dose therapy is desired, the recommended dose of Methylprednisolone Sodium Succinate for Injection, USP is 30 mg/kg administered intravenously over at least 30 minutes. This dose may be repeated every 4 to 6 hours for 48 hours. In general, high-dose corticosteroid therapy should be continued only until the patient’s condition has stabilized usually not beyond 48 to 72 hours.
Although adverse effects associated with high dose short-term corticoid therapy are uncommon, peptic ulceration may occur. Prophylactic antacid therapy may be indicated.
In other indications, the initial dosage will vary from 10 to 40 mg of Methylprednisolone depending on the clinical problem being treated. The larger doses may be required for short-term management of severe, acute conditions. The initial dose usually should be given intravenously over a period of several minutes. Subsequent doses may be given intravenously or intramuscularly at intervals dictated by the patient’s response and clinical condition. Corticoid therapy is an adjunct to, and not a replacement for conventional therapy.
Dosage must be decreased or discontinued gradually when the drug has been administered for more than a few days. If a period of spontaneous remission occurs in a chronic condition, treatment should be discontinued. Routine laboratory studies, such as urinalysis, two-hour postprandial blood sugar, determination of blood pressure and body weight, and a chest X-ray should be made at regular intervals during prolonged therapy. Upper GI X-rays are desirable in patients with an ulcer history or significant dyspepsia.
In pediatric patients, the initial dose of Methylprednisolone may vary depending on the specific disease being treated. The initial dose is 0.11-1.6 mg/day in three or four divided doses. Dosage may be reduced for infants and children but should be governed more by the severity of the condition and response of the patient than by age or size but it should not be less than 0.5 mg per kg every 24 hours.
In the treatment of acute exacerbations of multiple sclerosis daily doses is 160 mg daily for 3 days. Methylprednisolone powder for injection/infusion should be given as an intravenous infusion over at least 30 minutes.
Although adverse effects associated with high dose short-term corticoid therapy are uncommon, peptic ulceration may occur. Prophylactic antacid therapy may be indicated.
In other indications, the initial dosage will vary from 10 to 40 mg of Methylprednisolone depending on the clinical problem being treated. The larger doses may be required for short-term management of severe, acute conditions. The initial dose usually should be given intravenously over a period of several minutes. Subsequent doses may be given intravenously or intramuscularly at intervals dictated by the patient’s response and clinical condition. Corticoid therapy is an adjunct to, and not a replacement for conventional therapy.
Dosage must be decreased or discontinued gradually when the drug has been administered for more than a few days. If a period of spontaneous remission occurs in a chronic condition, treatment should be discontinued. Routine laboratory studies, such as urinalysis, two-hour postprandial blood sugar, determination of blood pressure and body weight, and a chest X-ray should be made at regular intervals during prolonged therapy. Upper GI X-rays are desirable in patients with an ulcer history or significant dyspepsia.
In pediatric patients, the initial dose of Methylprednisolone may vary depending on the specific disease being treated. The initial dose is 0.11-1.6 mg/day in three or four divided doses. Dosage may be reduced for infants and children but should be governed more by the severity of the condition and response of the patient than by age or size but it should not be less than 0.5 mg per kg every 24 hours.
In the treatment of acute exacerbations of multiple sclerosis daily doses is 160 mg daily for 3 days. Methylprednisolone powder for injection/infusion should be given as an intravenous infusion over at least 30 minutes.
Side effectsView
Fluid and Electrolyte Disturbances: Sodium retention, fluid retention, congestive heart failure in susceptible patients, potassium loss, hypokalemic alkalosis, hypertension.
Musculoskeletal: Muscle weakness, steroid myopathy, loss of muscle mass, severe arthralgia, vertebral compression fractures, aseptic necrosis of femoral and humeral heads, pathologic fracture of long bones, osteoporosis.
Gastrointestinal: Peptic ulcer with possible perforation and hemorrhage, pancreatitis, abdominal distention, and ulcerative esophagitis.
Dermatologic: Impaired wound healing, thin fragile skin, petechiae and ecchymoses, facial erythema, increased sweating, may suppress reactions to skin tests.
Neurological: Increased intracranial pressure with papilledema (pseudo-tumor cerebri) usually after treatment, convulsions, vertigo, headache.
Endocrine: Development of Cushingoid state, suppression of growth in children, secondary adrenocortical and pituitary unresponsiveness, particularly in times of stress, as in trauma, surgery or illness, menstrual irregularities, decreased carbohydrate tolerance, manifestations of latent diabetes mellitus, increased requirements for insulin or oral hypoglycemic agents in diabetics.
Ophthalmic: Posterior subcapsular cataracts, increased intraocular pressure, glaucoma, exophthalmos.
Others: Negative nitrogen balance due to protein catabolism.
The following additional adverse reactions are related to parenteral corticosteroid therapy: hyperpigmentation or hypopigmentation, subcutaneous and cutaneous atrophy, sterile abscess, anaphylactic reaction with or without circulatory collapse, cardiac arrest, bronchospasm, urticaria, nausea and vomiting, cardiac arrhythmias; hypotension or hypertension.
Musculoskeletal: Muscle weakness, steroid myopathy, loss of muscle mass, severe arthralgia, vertebral compression fractures, aseptic necrosis of femoral and humeral heads, pathologic fracture of long bones, osteoporosis.
Gastrointestinal: Peptic ulcer with possible perforation and hemorrhage, pancreatitis, abdominal distention, and ulcerative esophagitis.
Dermatologic: Impaired wound healing, thin fragile skin, petechiae and ecchymoses, facial erythema, increased sweating, may suppress reactions to skin tests.
Neurological: Increased intracranial pressure with papilledema (pseudo-tumor cerebri) usually after treatment, convulsions, vertigo, headache.
Endocrine: Development of Cushingoid state, suppression of growth in children, secondary adrenocortical and pituitary unresponsiveness, particularly in times of stress, as in trauma, surgery or illness, menstrual irregularities, decreased carbohydrate tolerance, manifestations of latent diabetes mellitus, increased requirements for insulin or oral hypoglycemic agents in diabetics.
Ophthalmic: Posterior subcapsular cataracts, increased intraocular pressure, glaucoma, exophthalmos.
Others: Negative nitrogen balance due to protein catabolism.
The following additional adverse reactions are related to parenteral corticosteroid therapy: hyperpigmentation or hypopigmentation, subcutaneous and cutaneous atrophy, sterile abscess, anaphylactic reaction with or without circulatory collapse, cardiac arrest, bronchospasm, urticaria, nausea and vomiting, cardiac arrhythmias; hypotension or hypertension.
ContraindicationsView
Methylprednisolone Sterile Powder is contraindicated:
- In systemic fungal infections and patients with known hypersensitivity to the product and its constituents.
- For intrathecal administration. Reports of severe medical events have been associated with this route of administration.
- Intramuscular corticosteroid preparations are contraindicated for idiopathic thrombocytopenic purpura.
PrecautionsView
Methylprednisolone, like many other steroid formulations, is sensitive to heat. Therefore, it should not be autoclaved when it is desirable to sterilize the exterior of the vial. The lowest possible dose of corticosteroid should be used to control the condition under treatment. When reduction in dosage is possible, the reduction should be gradual. Since complications of treatment with glucocorticoids are dependent on the size of the dose and the duration of treatment a risk/benefit decision must be made in each individual case as to dose and duration of treatment and as to whether daily or intermittent therapy should be used. For chronic conditions, discontinuation of corticosteroids may result in clinical improvement.
InteractionsView
- Aminoglutethimide may lead to a loss of corticosteroid-induced adrenal suppression.
- Amphotericin B injection and potassium-depleting agents- When corticosteroids are administered concomitantly with potassium-depleting agents (i.e., amphotericin B, diuretics), patients should be observed closely for the development of hypokalemia.
- Macrolide antibiotics have been reported to cause a significant decrease in corticosteroid clearance.
- Anticholinesterases- Concomitant use of anticholinesterase agents and corticosteroids may produce severe weakness in patients with myasthenia gravis. If possible, anticholinesterase agents should be withdrawn at least 24 hours before initiating corticosteroid therapy.
- Anticoagulants, oral- Coadministration of corticosteroids and warfarin usually results in inhibition of response to warfarin, although there have been some conflicting reports.
- Antidiabetics- Because corticosteroids may increase blood glucose concentrations, dosage adjustments of antidiabetic agents may be required.
- Antitubercular drugs- Serum concentrations of isoniazid may be decreased.
- Cholestyramine may increase the clearance of corticosteroids.
- Cyclosporine Increased activity of both cyclosporine and corticosteroids may occur when the two are used concurrently. Convulsions have been reported with this concurrent use.
- Digitalis glycosides- Patients on digitalis glycosides may be at increased risk of arrhythmias due to hypokalemia.
- Estrogens, including oral contraceptives- Estrogens may decrease the hepatic metabolism of certain corticosteroids, thereby increasing their effect.
- Hepatic Enzyme Inhibitors- Drugs which inhibit cytochrome P450 3A4 have the potential to result in increased plasma concentrations of corticosteroids.
- Ketoconazole has been reported to significantly decrease the metabolism of certain corticosteroids by up to 60%, leading to an increased risk of corticosteroid side effects.
- Nonsteroidal anti-inflammatory agents (NSAIDs)- Concomitant use of aspirin and corticosteroids increases the risk of gastrointestinal side effects.
- Skin tests- Corticosteroids may suppress reactions to skin tests.
- Vaccines- Patients on prolonged corticosteroid therapy may exhibit a diminished response to toxoids and live or inactivated vaccines due to inhibition of antibody response.
Pregnancy & lactationView
Pregnancy: Corticosteroids have been shown to be teratogenic in many species when given in doses equivalent to the human dose. There are no adequate and well-controlled studies in pregnant women. Corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Infants born to mothers who have received corticosteroids during pregnancy should be carefully observed for signs of hypoadrenalism.
Lactation: Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Because of the potential for serious adverse reactions in nursing infants from corticosteroids, a decision should be made whether to continue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Lactation: Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Because of the potential for serious adverse reactions in nursing infants from corticosteroids, a decision should be made whether to continue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric usageView
Pediatric Use: The adverse effects of corticosteroids in pediatric patients are similar to those in adults. Like adults, pediatric patients should be carefully observed with frequent measurements of blood pressure, weight, height, intraocular pressure and clinical evaluation for the presence of infection, psychosocial disturbances, thromboembolism, peptic ulcers, cataracts and osteoporosis. Pediatric patients who are treated with corticosteroids by any route, including systemically administered corticosteroids, may experience a decrease in their growth velocity. In order to minimize the potential growth effects of corticosteroids, pediatric patients should be titrated to the lowest effective dose.
Geriatric Use: Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, refecting the greater frequency of decreased hepatic, renal or cardiac function and of concomitant disease or other drug therapy.
Overdose effectsView
Treatment of acute over dosage is by supportive and symptomatic therapy. For chronic over dosage in the face of severe disease requiring continuous steroid therapy, the dosage of the corticosteroid may be reduced only temporarily or alternate day treatment may be introduced.
ReconstitutionView
Directions for Reconstitution-
- Remove protective plastic flip-of seal.
- Cleanse stopper with a suitable germicide.
- Aseptically add 8 mL Water for Injection BP for the 500 mg vial or 16 ml for 1 gm vial by means of a syringe into the vial.
- Agitate to effect solution to dissolve the powder content.
- Invert vial. Insert the needle through the target area of stopper until the tip is just visible. Withdraw dose.
StorageView
Protect from light. Store at controlled room temperature 20° to 25°C. Store solution at controlled room temperature 20° to 25°C.Use solution within 48 hours after mixing.
Solupred
Methylprednisolone Sodium Succcinate
Solupred
Methylprednisolone Sodium Succcinate
Indications
Vestibular neuritis
Indication detailsView
Methylprednisolone Sodium Succinate IM/IV is indicated in the following conditions:
Endocrine disorder: Primary or secondary adrenocortical insufficiency, acute adrenocortical insufficiency, shock unresponsive to conventional, congenital adrenal hyperplasia, Nonsuppurative thyroiditis. Hypercalcemia associated with cancer.
Rheumatic disorder: Rheumatoid arthritis, including juvenile rheumatoid arthritis, acute and subacute bursitis, epicondylitis, acute nonspecific tenosynovitis, acute gouty arthritis, psoriatic arthritis, ankylosing spondylitis.
Collagen disease: During an exacerbation or as maintenance therapy in selected cases of systemic lupus erythematosus; acute rheumatic carditis, systemic dermatomyositis (polymyositis).
Dermatological disease: Pemphigus, severe erythema multiforme (Stevens-Johnson syndrome), exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe psoriasis, mycosis fungoides.
Allergic states: Controls bronchial asthma, contact dermatitis, atopic dermatitis, serum sickness, seasonal or perennial allergic rhinitis, drug hypersensitivity reaction, urticarial transfusion reactions, acute noninfectious laryngeal edema (epinephrine is the drug of first choice), anaphylactic reactions.
Ophthalmic disease: Severe acute and chronic allergic and inflammatory processes involving the eye, such as: herpes zoster ophthalmicus, iritis, iridocyclitis, chorioretinitis, diffuse posterior uveitis and chroiditis, optic neuritis, sympathetic ophthalmia, anterior segment inflammation, allergic conjunctivitis, allergic corneal marginal ulcers, keratitis.
Gastrointestinal disease: To tide the patient over a critical period of the disease in: ulcerative colitis (systemic therapy), regional enteritis (systemic therapy), Crohn’s disease.
Respiratory disease: Symptomatic sarcoidosis, berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculosis chemotherapy, Loafer syndrome not manageable by other means, aspiration pneumonitis.
Hematologic disorder: Acquired (autoimmune) hemolytic anemia, idiopathic thrombocytopenic purpura in adults (IV only, IM administration is contraindicated), erythroblastopenia (RBC anemia), congenital (erythroid) hypoplastic anemia, secondary thrombocytopenia in adults.
Neoplastic disease: For palliative management of: leukemias and lymphoma in adults, acute leukemia of childhood.
Edematous state: To induce diuresis or remission of proteinuria in the nephrotic syndrome, without uremia of the idiopathic type or that due to lupus erythematosus.
Miscellaneous: Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculosis chemotherapy. Trichinosis with neurologic or myocardial involvement.
Endocrine disorder: Primary or secondary adrenocortical insufficiency, acute adrenocortical insufficiency, shock unresponsive to conventional, congenital adrenal hyperplasia, Nonsuppurative thyroiditis. Hypercalcemia associated with cancer.
Rheumatic disorder: Rheumatoid arthritis, including juvenile rheumatoid arthritis, acute and subacute bursitis, epicondylitis, acute nonspecific tenosynovitis, acute gouty arthritis, psoriatic arthritis, ankylosing spondylitis.
Collagen disease: During an exacerbation or as maintenance therapy in selected cases of systemic lupus erythematosus; acute rheumatic carditis, systemic dermatomyositis (polymyositis).
Dermatological disease: Pemphigus, severe erythema multiforme (Stevens-Johnson syndrome), exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe psoriasis, mycosis fungoides.
Allergic states: Controls bronchial asthma, contact dermatitis, atopic dermatitis, serum sickness, seasonal or perennial allergic rhinitis, drug hypersensitivity reaction, urticarial transfusion reactions, acute noninfectious laryngeal edema (epinephrine is the drug of first choice), anaphylactic reactions.
Ophthalmic disease: Severe acute and chronic allergic and inflammatory processes involving the eye, such as: herpes zoster ophthalmicus, iritis, iridocyclitis, chorioretinitis, diffuse posterior uveitis and chroiditis, optic neuritis, sympathetic ophthalmia, anterior segment inflammation, allergic conjunctivitis, allergic corneal marginal ulcers, keratitis.
Gastrointestinal disease: To tide the patient over a critical period of the disease in: ulcerative colitis (systemic therapy), regional enteritis (systemic therapy), Crohn’s disease.
Respiratory disease: Symptomatic sarcoidosis, berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculosis chemotherapy, Loafer syndrome not manageable by other means, aspiration pneumonitis.
Hematologic disorder: Acquired (autoimmune) hemolytic anemia, idiopathic thrombocytopenic purpura in adults (IV only, IM administration is contraindicated), erythroblastopenia (RBC anemia), congenital (erythroid) hypoplastic anemia, secondary thrombocytopenia in adults.
Neoplastic disease: For palliative management of: leukemias and lymphoma in adults, acute leukemia of childhood.
Edematous state: To induce diuresis or remission of proteinuria in the nephrotic syndrome, without uremia of the idiopathic type or that due to lupus erythematosus.
Miscellaneous: Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculosis chemotherapy. Trichinosis with neurologic or myocardial involvement.
Therapeutic classView
Glucocorticoids
PharmacologyView
Methylprednisolone, a naturally occurring glucocorticoid (hydrocortisone and cortisone), which has also salt-retaining properties, is used as replacement therapy in adrenocortical deficiency states. This synthetic analog is primarily used for its potent anti-inflammatory effects in disorders of many organ systems. The intravenous injection of Methylprednisolone Sodium Succinate, demonstrable effects are evident within one hour and persist for a variable period. Excretion of the administered dose is nearly complete within 12 hours. Thus, if constantly high blood levels are required, injections should be made every 4 to 6 hours. This preparation is also rapidly absorbed when administered intramuscularly and is excreted in a pattern similar to that observed after intravenous injection. Its anti-inflammatory potency is greater than prednisolone in the ratio of 5 to 4. It has only minimal mineralocorticoid properties and has less tendency than prednisolone to induce sodium and water retention. It influences carbohydrate, protein, fat and purine metabolism, electrolyte and water balance, and the functional capacities of the cardiovascular system, the kidney, the skeletal muscle, nervous system and other organs and tissues. It exerts a suppressive effect on the immune response.
DosageView
Methylprednisolone may be administered by IM or IV or by IV infusion. To administer by IM or IV injection, prepare solution as direction for reconstitution. The desired dose may be administered intravenously over a period of several minutes. When high dose therapy is desired, the recommended dose of Methylprednisolone Sodium Succinate for Injection, USP is 30 mg/kg administered intravenously over at least 30 minutes. This dose may be repeated every 4 to 6 hours for 48 hours. In general, high-dose corticosteroid therapy should be continued only until the patient’s condition has stabilized usually not beyond 48 to 72 hours.
Although adverse effects associated with high dose short-term corticoid therapy are uncommon, peptic ulceration may occur. Prophylactic antacid therapy may be indicated.
In other indications, the initial dosage will vary from 10 to 40 mg of Methylprednisolone depending on the clinical problem being treated. The larger doses may be required for short-term management of severe, acute conditions. The initial dose usually should be given intravenously over a period of several minutes. Subsequent doses may be given intravenously or intramuscularly at intervals dictated by the patient’s response and clinical condition. Corticoid therapy is an adjunct to, and not a replacement for conventional therapy.
Dosage must be decreased or discontinued gradually when the drug has been administered for more than a few days. If a period of spontaneous remission occurs in a chronic condition, treatment should be discontinued. Routine laboratory studies, such as urinalysis, two-hour postprandial blood sugar, determination of blood pressure and body weight, and a chest X-ray should be made at regular intervals during prolonged therapy. Upper GI X-rays are desirable in patients with an ulcer history or significant dyspepsia.
In pediatric patients, the initial dose of Methylprednisolone may vary depending on the specific disease being treated. The initial dose is 0.11-1.6 mg/day in three or four divided doses. Dosage may be reduced for infants and children but should be governed more by the severity of the condition and response of the patient than by age or size but it should not be less than 0.5 mg per kg every 24 hours.
In the treatment of acute exacerbations of multiple sclerosis daily doses is 160 mg daily for 3 days. Methylprednisolone powder for injection/infusion should be given as an intravenous infusion over at least 30 minutes.
Although adverse effects associated with high dose short-term corticoid therapy are uncommon, peptic ulceration may occur. Prophylactic antacid therapy may be indicated.
In other indications, the initial dosage will vary from 10 to 40 mg of Methylprednisolone depending on the clinical problem being treated. The larger doses may be required for short-term management of severe, acute conditions. The initial dose usually should be given intravenously over a period of several minutes. Subsequent doses may be given intravenously or intramuscularly at intervals dictated by the patient’s response and clinical condition. Corticoid therapy is an adjunct to, and not a replacement for conventional therapy.
Dosage must be decreased or discontinued gradually when the drug has been administered for more than a few days. If a period of spontaneous remission occurs in a chronic condition, treatment should be discontinued. Routine laboratory studies, such as urinalysis, two-hour postprandial blood sugar, determination of blood pressure and body weight, and a chest X-ray should be made at regular intervals during prolonged therapy. Upper GI X-rays are desirable in patients with an ulcer history or significant dyspepsia.
In pediatric patients, the initial dose of Methylprednisolone may vary depending on the specific disease being treated. The initial dose is 0.11-1.6 mg/day in three or four divided doses. Dosage may be reduced for infants and children but should be governed more by the severity of the condition and response of the patient than by age or size but it should not be less than 0.5 mg per kg every 24 hours.
In the treatment of acute exacerbations of multiple sclerosis daily doses is 160 mg daily for 3 days. Methylprednisolone powder for injection/infusion should be given as an intravenous infusion over at least 30 minutes.
Side effectsView
Fluid and Electrolyte Disturbances: Sodium retention, fluid retention, congestive heart failure in susceptible patients, potassium loss, hypokalemic alkalosis, hypertension.
Musculoskeletal: Muscle weakness, steroid myopathy, loss of muscle mass, severe arthralgia, vertebral compression fractures, aseptic necrosis of femoral and humeral heads, pathologic fracture of long bones, osteoporosis.
Gastrointestinal: Peptic ulcer with possible perforation and hemorrhage, pancreatitis, abdominal distention, and ulcerative esophagitis.
Dermatologic: Impaired wound healing, thin fragile skin, petechiae and ecchymoses, facial erythema, increased sweating, may suppress reactions to skin tests.
Neurological: Increased intracranial pressure with papilledema (pseudo-tumor cerebri) usually after treatment, convulsions, vertigo, headache.
Endocrine: Development of Cushingoid state, suppression of growth in children, secondary adrenocortical and pituitary unresponsiveness, particularly in times of stress, as in trauma, surgery or illness, menstrual irregularities, decreased carbohydrate tolerance, manifestations of latent diabetes mellitus, increased requirements for insulin or oral hypoglycemic agents in diabetics.
Ophthalmic: Posterior subcapsular cataracts, increased intraocular pressure, glaucoma, exophthalmos.
Others: Negative nitrogen balance due to protein catabolism.
The following additional adverse reactions are related to parenteral corticosteroid therapy: hyperpigmentation or hypopigmentation, subcutaneous and cutaneous atrophy, sterile abscess, anaphylactic reaction with or without circulatory collapse, cardiac arrest, bronchospasm, urticaria, nausea and vomiting, cardiac arrhythmias; hypotension or hypertension.
Musculoskeletal: Muscle weakness, steroid myopathy, loss of muscle mass, severe arthralgia, vertebral compression fractures, aseptic necrosis of femoral and humeral heads, pathologic fracture of long bones, osteoporosis.
Gastrointestinal: Peptic ulcer with possible perforation and hemorrhage, pancreatitis, abdominal distention, and ulcerative esophagitis.
Dermatologic: Impaired wound healing, thin fragile skin, petechiae and ecchymoses, facial erythema, increased sweating, may suppress reactions to skin tests.
Neurological: Increased intracranial pressure with papilledema (pseudo-tumor cerebri) usually after treatment, convulsions, vertigo, headache.
Endocrine: Development of Cushingoid state, suppression of growth in children, secondary adrenocortical and pituitary unresponsiveness, particularly in times of stress, as in trauma, surgery or illness, menstrual irregularities, decreased carbohydrate tolerance, manifestations of latent diabetes mellitus, increased requirements for insulin or oral hypoglycemic agents in diabetics.
Ophthalmic: Posterior subcapsular cataracts, increased intraocular pressure, glaucoma, exophthalmos.
Others: Negative nitrogen balance due to protein catabolism.
The following additional adverse reactions are related to parenteral corticosteroid therapy: hyperpigmentation or hypopigmentation, subcutaneous and cutaneous atrophy, sterile abscess, anaphylactic reaction with or without circulatory collapse, cardiac arrest, bronchospasm, urticaria, nausea and vomiting, cardiac arrhythmias; hypotension or hypertension.
ContraindicationsView
Methylprednisolone Sterile Powder is contraindicated:
- In systemic fungal infections and patients with known hypersensitivity to the product and its constituents.
- For intrathecal administration. Reports of severe medical events have been associated with this route of administration.
- Intramuscular corticosteroid preparations are contraindicated for idiopathic thrombocytopenic purpura.
PrecautionsView
Methylprednisolone, like many other steroid formulations, is sensitive to heat. Therefore, it should not be autoclaved when it is desirable to sterilize the exterior of the vial. The lowest possible dose of corticosteroid should be used to control the condition under treatment. When reduction in dosage is possible, the reduction should be gradual. Since complications of treatment with glucocorticoids are dependent on the size of the dose and the duration of treatment a risk/benefit decision must be made in each individual case as to dose and duration of treatment and as to whether daily or intermittent therapy should be used. For chronic conditions, discontinuation of corticosteroids may result in clinical improvement.
InteractionsView
- Aminoglutethimide may lead to a loss of corticosteroid-induced adrenal suppression.
- Amphotericin B injection and potassium-depleting agents- When corticosteroids are administered concomitantly with potassium-depleting agents (i.e., amphotericin B, diuretics), patients should be observed closely for the development of hypokalemia.
- Macrolide antibiotics have been reported to cause a significant decrease in corticosteroid clearance.
- Anticholinesterases- Concomitant use of anticholinesterase agents and corticosteroids may produce severe weakness in patients with myasthenia gravis. If possible, anticholinesterase agents should be withdrawn at least 24 hours before initiating corticosteroid therapy.
- Anticoagulants, oral- Coadministration of corticosteroids and warfarin usually results in inhibition of response to warfarin, although there have been some conflicting reports.
- Antidiabetics- Because corticosteroids may increase blood glucose concentrations, dosage adjustments of antidiabetic agents may be required.
- Antitubercular drugs- Serum concentrations of isoniazid may be decreased.
- Cholestyramine may increase the clearance of corticosteroids.
- Cyclosporine Increased activity of both cyclosporine and corticosteroids may occur when the two are used concurrently. Convulsions have been reported with this concurrent use.
- Digitalis glycosides- Patients on digitalis glycosides may be at increased risk of arrhythmias due to hypokalemia.
- Estrogens, including oral contraceptives- Estrogens may decrease the hepatic metabolism of certain corticosteroids, thereby increasing their effect.
- Hepatic Enzyme Inhibitors- Drugs which inhibit cytochrome P450 3A4 have the potential to result in increased plasma concentrations of corticosteroids.
- Ketoconazole has been reported to significantly decrease the metabolism of certain corticosteroids by up to 60%, leading to an increased risk of corticosteroid side effects.
- Nonsteroidal anti-inflammatory agents (NSAIDs)- Concomitant use of aspirin and corticosteroids increases the risk of gastrointestinal side effects.
- Skin tests- Corticosteroids may suppress reactions to skin tests.
- Vaccines- Patients on prolonged corticosteroid therapy may exhibit a diminished response to toxoids and live or inactivated vaccines due to inhibition of antibody response.
Pregnancy & lactationView
Pregnancy: Corticosteroids have been shown to be teratogenic in many species when given in doses equivalent to the human dose. There are no adequate and well-controlled studies in pregnant women. Corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Infants born to mothers who have received corticosteroids during pregnancy should be carefully observed for signs of hypoadrenalism.
Lactation: Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Because of the potential for serious adverse reactions in nursing infants from corticosteroids, a decision should be made whether to continue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Lactation: Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Because of the potential for serious adverse reactions in nursing infants from corticosteroids, a decision should be made whether to continue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric usageView
Pediatric Use: The adverse effects of corticosteroids in pediatric patients are similar to those in adults. Like adults, pediatric patients should be carefully observed with frequent measurements of blood pressure, weight, height, intraocular pressure and clinical evaluation for the presence of infection, psychosocial disturbances, thromboembolism, peptic ulcers, cataracts and osteoporosis. Pediatric patients who are treated with corticosteroids by any route, including systemically administered corticosteroids, may experience a decrease in their growth velocity. In order to minimize the potential growth effects of corticosteroids, pediatric patients should be titrated to the lowest effective dose.
Geriatric Use: Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, refecting the greater frequency of decreased hepatic, renal or cardiac function and of concomitant disease or other drug therapy.
Overdose effectsView
Treatment of acute over dosage is by supportive and symptomatic therapy. For chronic over dosage in the face of severe disease requiring continuous steroid therapy, the dosage of the corticosteroid may be reduced only temporarily or alternate day treatment may be introduced.
ReconstitutionView
Directions for Reconstitution-
- Remove protective plastic flip-of seal.
- Cleanse stopper with a suitable germicide.
- Aseptically add 8 mL Water for Injection BP for the 500 mg vial or 16 ml for 1 gm vial by means of a syringe into the vial.
- Agitate to effect solution to dissolve the powder content.
- Invert vial. Insert the needle through the target area of stopper until the tip is just visible. Withdraw dose.
StorageView
Protect from light. Store at controlled room temperature 20° to 25°C. Store solution at controlled room temperature 20° to 25°C.Use solution within 48 hours after mixing.
Solurin
Solifenacin Succinate
Solurin
Solifenacin Succinate
Indications
Urinary frequency and urgency
Indication detailsView
Symptomatic treatment of urge incontinence and/or increased urinary frequency and urgency as may occur in patients with overactive bladder syndrome.
Therapeutic classView
Anticholinergics (antimuscarinics)/ Anti-spasmodics, BPH/ Urinary retention/ Urinary incontinence
PharmacologyView
Solifenacin is a competitive muscarinic receptor antagonist. It has the highest affinity for M3, M1, and M2 muscarinic receptors. 80% of the muscarinic receptors in the bladder are M2, while 20% are M3. Solifenacin's antagonism of the M3 receptor prevents contraction of the detrusor muscle, while antagonism of the M2 receptor may prevent contraction of smooth muscle in the bladder.
DosageView
The recommended dose for adults and the elderly: Solifenacin Succinate 5 mg once daily. If needed, the dose may be increased to Solifenacin Succinate 10 mg once daily.
Use in children: Safety and effectiveness in children have not yet been established. Therefore, Solifenacin Succinate should not be used in children.
Use in children: Safety and effectiveness in children have not yet been established. Therefore, Solifenacin Succinate should not be used in children.
Side effectsView
Due to the pharmacological effect of Solifenacin, it may cause anticholinergic undesirable effects of (in general) mild or moderate severity. The frequency of anticholinergic undesirable effects is dose related. The most commonly reported adverse reactionwith Solifenacin is dry mouth. It occurred in 11% of patients treated with 5 mg once daily, in 22% of patients treated with 10 mg once daily and in 4% of placebo-treated patients. The severity of dry mouth was generally mild and only occasionally led to discontinuation of treatment. In general,medicinal product compliance was very high (approximately 99%) and approximately 90% of the patients treated with Solifenacin completed the full study period of 12 weeks treatment.
- Gastrointestinal disorders: very common- dry mouth, common-constipation, nausea, dyspepsia, abdominal pain, uncommon- gastroesophageal reflux diseases, dry throat, rare- colonic obstruction, faecal impaction, very rare- vomiting.
- Infections and infestations: uncommonurinary tract infection, cystitis.
- nervous system disorders: uncommon- somnolence, dysgeusia, very rare-dizziness, headache.
- psychiatric disorders: very rare- hallucinations.
- eye disorders: common- blurred vision, uncommon- dry eyes.
- General disorders and administration site conditions: uncommon- fatigue, peripheral oedema.
- Respiratory, thoracic and mediastinal disorders: uncommon nasal dryness.
- skin and subcutaneous tissue disorders: uncommon- dry skin, very rare- pruritus, rash, urticaria.
- renal and urinary disorders: uncommon- difficulty in micturition, rare- urinary retention.
ContraindicationsView
Solifenacin is contraindicated in patients with hypersensitivity to solifenacin or to any of the excipients. It is also contraindicated in myasthenia gravis, urinary retention, uncontrolled narrow angle glaucoma, severe gastro-intestinal condition (including toxic megacolon), patients undergoing haemodialysis, patients with severe hepatic impairment, patients with severe renal impairment or moderate hepatic impairment and on treatment with a strong CYP3A4 inhibitor, e.g. ketoconazole.
PrecautionsView
Other causes of frequent urination (heart failure or renal disease) should be assessed before treatment with Solifenacin Succinate. If urinary tract infection is present, an appropriate antibacterial therapy should be started. Solifenacin Succinate should be used with caution in patients with: clinically significant bladder outflow obstruction at risk of urinary retention, gastrointestinal obstructive disorders, risk of decreased gastrointestinal motility, severe renal impairment (creatinine clearance 30 ml/min), moderate hepatic impairment (Child-Pugh score of 7 to 9) and doses should not exceed 5 mg for these patients. Caution should be taken in concomitant use of a potent CYP3A4 inhibitor e.g. Ketoconazole, hiatus hernia/ gastroesophageal reflux and/or who are concurrently taking medicinal products (such as Bisphosphonates) that can cause or exacerbate oesophagitis, autonomic neuropathy. Safety and efficacy have not yet been established in patients with a neurogenic cause for detrusor overactivity. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product. The maximum effect of Solifenacin Succinate can be determined after 4 weeks at the earliest.
InteractionsView
Concomitant medication with other medicinal products with anticholinergic properties may result in more pronounced therapeutic effects and undesirable effects. An interval of approximately one week should be allowed after stopping treatment with Solifenacin Succinate before commencing other anticholinergic therapy. The therapeutic effect of Solifenacin may be reduced by concomitant administration of cholinergic receptor agonists. Solifenacin can reduce the effect of medicinal products that stimulate the motility of the gastrointestinal tract, such as Metoclopramide and Cisapride. In vitro studies have demonstrated that at therapeutic concentrations, Solifenacin does not inhibit CYP1A1/2, 2C9, 2C19, 2D6, or 3A4 derived from human liver microsomes. Therefore, Solifenacin is unlikely to alter the clearance of drugs metabolized by these CYP enzymes. Solifenacin is metabolized by CYP3A4. Simultaneous administration of Ketoconazole (200 mg/day), a potent CYP3A4 inhibitor, resulted in a two-fold increase of the AUC of Solifenacin, while Ketoconazole at a dose of 400 mg/day resulted in a three-fold increase of the AUC of Solifenacin. Therefore, the maximum dose of Solifenacin Succinate should be restricted to 5 mg when used simultaneously with Ketoconazole or therapeutic doses of other potent CYP3A4 inhibitors (e.g. Ritonavir, Nelfinavir, Itraconazole).
Simultaneous treatment of Solifenacin and a potent CYP3A4 inhibitor is contra-indicated in patients with severe renal impairment or moderate hepatic impairment. The effects of enzyme induction on the pharmacokinetics of Solifenacin and its metabolites have not been studied as well as the effect of higher affinity CYP3A4 substrates on Solifenacin exposure. Since Solifenacin is metabolised by CYP3A4, pharmacokinetic interactions are possible with other CYP3A4 substrates with higher affinity (e.g. Verapamil, Diltiazem) and CYP3A4 inducers (e.g. Rifampicin, Phenytoin, Carbamazepine).
Effect of Solifenacin on the pharmacokinetics of other medicinal products:
Simultaneous treatment of Solifenacin and a potent CYP3A4 inhibitor is contra-indicated in patients with severe renal impairment or moderate hepatic impairment. The effects of enzyme induction on the pharmacokinetics of Solifenacin and its metabolites have not been studied as well as the effect of higher affinity CYP3A4 substrates on Solifenacin exposure. Since Solifenacin is metabolised by CYP3A4, pharmacokinetic interactions are possible with other CYP3A4 substrates with higher affinity (e.g. Verapamil, Diltiazem) and CYP3A4 inducers (e.g. Rifampicin, Phenytoin, Carbamazepine).
Effect of Solifenacin on the pharmacokinetics of other medicinal products:
- Oral Contraceptives: Intake of Solifenacin showed no pharmacokinetic interaction on combined oral contraceptives (Ethinylestradiol/Levonorgestrel).
- Warfarin: Intake of Solifenacin did not alter the pharmacokinetics of R-warfarin or S-warfarin or their effect on prothrombin time.
- Digoxin: Intake of Solifenacin showed no effect on the pharmacokinetics of digoxin.
- Effects on ability to drive and use machines: Since Solifenacin, like other anticholinergics may cause blurred vision and, uncommonly, somnolence and fatigue, the ability to drive and use machines may be negatively affected.
Pregnancy & lactationView
No clinical data are available from women who became pregnant while taking Solifenacin. Animal studies do not indicate direct harmful effects on fertility, embryonal / foetal development or parturition. The potential risk for humans is unknown. Caution should be exercised when prescribing to pregnant women. No data on the excretion of Solifenacin in human milk are available. In mice, Solifenacin and/or its metabolites was excreted in milk, and caused a dose dependent failure to thrive in neonatal mice. The use of Solifenacin should therefore be avoided during breast-feeding.
Pediatric usageView
Patients with renal impairment: No dose adjustment is necessary for patients with mild to moderate renal impairment (creatinine clearance >30 ml/min). Patients with severe renal impairment (creatinine clearance <30 ml/min) should be treated with caution and receive no more than 5 mg once daily.
Patients with hepatic impairment: No dose adjustment is necessary for patients with mild hepatic impairment. Patients with moderate hepatic impairment (Child-Pugh score of 7 to 9) should be treated with caution and receive no more than 5 mg once daily.
Potent inhibitors of cytochrome P450 3A4: The maximum dose of Solifenacin Succinate should be limited to 5 mg when treated simultaneously with Ketoconazole or therapeutic doses of other potent CYP3A4 inhibitors e.g. Ritonavir, Nelfinavir, Itraconazole. Solifenacin Succinate tablet should be taken orally and should be swallowed whole with liquids. It can be taken with or without food.
Patients with hepatic impairment: No dose adjustment is necessary for patients with mild hepatic impairment. Patients with moderate hepatic impairment (Child-Pugh score of 7 to 9) should be treated with caution and receive no more than 5 mg once daily.
Potent inhibitors of cytochrome P450 3A4: The maximum dose of Solifenacin Succinate should be limited to 5 mg when treated simultaneously with Ketoconazole or therapeutic doses of other potent CYP3A4 inhibitors e.g. Ritonavir, Nelfinavir, Itraconazole. Solifenacin Succinate tablet should be taken orally and should be swallowed whole with liquids. It can be taken with or without food.
Overdose effectsView
Over dosage with Solifenacin Succinate can potentially result in severe anticholinergic effects. The highest dose of Solifenacin Succinate accidentally given to a single patient was 280 mg in a 5 hour period, resulting in mental status changes not requiring hospitalization. In the event of overdose with Solifenacin Succinate, the patient should be treated with activated charcoal. Gastric lavage is useful if performed within 1 hour, but vomiting should not be induced. As for other anticholinergics, symptoms can be treated as follows:
- Severe central anticholinergic effects such as hallucinations or pronounced excitation: treat with physostigmine or carbachol.
- Convulsions or pronounced excitation: treat with benzodiazepines.
- Respiratory insufficiency: treat with artificial respiration.
- Tachycardia: treat with beta-blockers.
- Urinary retention: treat with catheterisation.
- Mydriasis: treat with pilocarpine eye drops and/or place patient in a dark room.
StorageView
Store in a cool and dry place, protected from light.
Solurin
Solifenacin Succinate
Solurin
Solifenacin Succinate
Indications
Urinary frequency and urgency
Indication detailsView
Symptomatic treatment of urge incontinence and/or increased urinary frequency and urgency as may occur in patients with overactive bladder syndrome.
Therapeutic classView
Anticholinergics (antimuscarinics)/ Anti-spasmodics, BPH/ Urinary retention/ Urinary incontinence
PharmacologyView
Solifenacin is a competitive muscarinic receptor antagonist. It has the highest affinity for M3, M1, and M2 muscarinic receptors. 80% of the muscarinic receptors in the bladder are M2, while 20% are M3. Solifenacin's antagonism of the M3 receptor prevents contraction of the detrusor muscle, while antagonism of the M2 receptor may prevent contraction of smooth muscle in the bladder.
DosageView
The recommended dose for adults and the elderly: Solifenacin Succinate 5 mg once daily. If needed, the dose may be increased to Solifenacin Succinate 10 mg once daily.
Use in children: Safety and effectiveness in children have not yet been established. Therefore, Solifenacin Succinate should not be used in children.
Use in children: Safety and effectiveness in children have not yet been established. Therefore, Solifenacin Succinate should not be used in children.
Side effectsView
Due to the pharmacological effect of Solifenacin, it may cause anticholinergic undesirable effects of (in general) mild or moderate severity. The frequency of anticholinergic undesirable effects is dose related. The most commonly reported adverse reactionwith Solifenacin is dry mouth. It occurred in 11% of patients treated with 5 mg once daily, in 22% of patients treated with 10 mg once daily and in 4% of placebo-treated patients. The severity of dry mouth was generally mild and only occasionally led to discontinuation of treatment. In general,medicinal product compliance was very high (approximately 99%) and approximately 90% of the patients treated with Solifenacin completed the full study period of 12 weeks treatment.
- Gastrointestinal disorders: very common- dry mouth, common-constipation, nausea, dyspepsia, abdominal pain, uncommon- gastroesophageal reflux diseases, dry throat, rare- colonic obstruction, faecal impaction, very rare- vomiting.
- Infections and infestations: uncommonurinary tract infection, cystitis.
- nervous system disorders: uncommon- somnolence, dysgeusia, very rare-dizziness, headache.
- psychiatric disorders: very rare- hallucinations.
- eye disorders: common- blurred vision, uncommon- dry eyes.
- General disorders and administration site conditions: uncommon- fatigue, peripheral oedema.
- Respiratory, thoracic and mediastinal disorders: uncommon nasal dryness.
- skin and subcutaneous tissue disorders: uncommon- dry skin, very rare- pruritus, rash, urticaria.
- renal and urinary disorders: uncommon- difficulty in micturition, rare- urinary retention.
ContraindicationsView
Solifenacin is contraindicated in patients with hypersensitivity to solifenacin or to any of the excipients. It is also contraindicated in myasthenia gravis, urinary retention, uncontrolled narrow angle glaucoma, severe gastro-intestinal condition (including toxic megacolon), patients undergoing haemodialysis, patients with severe hepatic impairment, patients with severe renal impairment or moderate hepatic impairment and on treatment with a strong CYP3A4 inhibitor, e.g. ketoconazole.
PrecautionsView
Other causes of frequent urination (heart failure or renal disease) should be assessed before treatment with Solifenacin Succinate. If urinary tract infection is present, an appropriate antibacterial therapy should be started. Solifenacin Succinate should be used with caution in patients with: clinically significant bladder outflow obstruction at risk of urinary retention, gastrointestinal obstructive disorders, risk of decreased gastrointestinal motility, severe renal impairment (creatinine clearance 30 ml/min), moderate hepatic impairment (Child-Pugh score of 7 to 9) and doses should not exceed 5 mg for these patients. Caution should be taken in concomitant use of a potent CYP3A4 inhibitor e.g. Ketoconazole, hiatus hernia/ gastroesophageal reflux and/or who are concurrently taking medicinal products (such as Bisphosphonates) that can cause or exacerbate oesophagitis, autonomic neuropathy. Safety and efficacy have not yet been established in patients with a neurogenic cause for detrusor overactivity. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product. The maximum effect of Solifenacin Succinate can be determined after 4 weeks at the earliest.
InteractionsView
Concomitant medication with other medicinal products with anticholinergic properties may result in more pronounced therapeutic effects and undesirable effects. An interval of approximately one week should be allowed after stopping treatment with Solifenacin Succinate before commencing other anticholinergic therapy. The therapeutic effect of Solifenacin may be reduced by concomitant administration of cholinergic receptor agonists. Solifenacin can reduce the effect of medicinal products that stimulate the motility of the gastrointestinal tract, such as Metoclopramide and Cisapride. In vitro studies have demonstrated that at therapeutic concentrations, Solifenacin does not inhibit CYP1A1/2, 2C9, 2C19, 2D6, or 3A4 derived from human liver microsomes. Therefore, Solifenacin is unlikely to alter the clearance of drugs metabolized by these CYP enzymes. Solifenacin is metabolized by CYP3A4. Simultaneous administration of Ketoconazole (200 mg/day), a potent CYP3A4 inhibitor, resulted in a two-fold increase of the AUC of Solifenacin, while Ketoconazole at a dose of 400 mg/day resulted in a three-fold increase of the AUC of Solifenacin. Therefore, the maximum dose of Solifenacin Succinate should be restricted to 5 mg when used simultaneously with Ketoconazole or therapeutic doses of other potent CYP3A4 inhibitors (e.g. Ritonavir, Nelfinavir, Itraconazole).
Simultaneous treatment of Solifenacin and a potent CYP3A4 inhibitor is contra-indicated in patients with severe renal impairment or moderate hepatic impairment. The effects of enzyme induction on the pharmacokinetics of Solifenacin and its metabolites have not been studied as well as the effect of higher affinity CYP3A4 substrates on Solifenacin exposure. Since Solifenacin is metabolised by CYP3A4, pharmacokinetic interactions are possible with other CYP3A4 substrates with higher affinity (e.g. Verapamil, Diltiazem) and CYP3A4 inducers (e.g. Rifampicin, Phenytoin, Carbamazepine).
Effect of Solifenacin on the pharmacokinetics of other medicinal products:
Simultaneous treatment of Solifenacin and a potent CYP3A4 inhibitor is contra-indicated in patients with severe renal impairment or moderate hepatic impairment. The effects of enzyme induction on the pharmacokinetics of Solifenacin and its metabolites have not been studied as well as the effect of higher affinity CYP3A4 substrates on Solifenacin exposure. Since Solifenacin is metabolised by CYP3A4, pharmacokinetic interactions are possible with other CYP3A4 substrates with higher affinity (e.g. Verapamil, Diltiazem) and CYP3A4 inducers (e.g. Rifampicin, Phenytoin, Carbamazepine).
Effect of Solifenacin on the pharmacokinetics of other medicinal products:
- Oral Contraceptives: Intake of Solifenacin showed no pharmacokinetic interaction on combined oral contraceptives (Ethinylestradiol/Levonorgestrel).
- Warfarin: Intake of Solifenacin did not alter the pharmacokinetics of R-warfarin or S-warfarin or their effect on prothrombin time.
- Digoxin: Intake of Solifenacin showed no effect on the pharmacokinetics of digoxin.
- Effects on ability to drive and use machines: Since Solifenacin, like other anticholinergics may cause blurred vision and, uncommonly, somnolence and fatigue, the ability to drive and use machines may be negatively affected.
Pregnancy & lactationView
No clinical data are available from women who became pregnant while taking Solifenacin. Animal studies do not indicate direct harmful effects on fertility, embryonal / foetal development or parturition. The potential risk for humans is unknown. Caution should be exercised when prescribing to pregnant women. No data on the excretion of Solifenacin in human milk are available. In mice, Solifenacin and/or its metabolites was excreted in milk, and caused a dose dependent failure to thrive in neonatal mice. The use of Solifenacin should therefore be avoided during breast-feeding.
Pediatric usageView
Patients with renal impairment: No dose adjustment is necessary for patients with mild to moderate renal impairment (creatinine clearance >30 ml/min). Patients with severe renal impairment (creatinine clearance <30 ml/min) should be treated with caution and receive no more than 5 mg once daily.
Patients with hepatic impairment: No dose adjustment is necessary for patients with mild hepatic impairment. Patients with moderate hepatic impairment (Child-Pugh score of 7 to 9) should be treated with caution and receive no more than 5 mg once daily.
Potent inhibitors of cytochrome P450 3A4: The maximum dose of Solifenacin Succinate should be limited to 5 mg when treated simultaneously with Ketoconazole or therapeutic doses of other potent CYP3A4 inhibitors e.g. Ritonavir, Nelfinavir, Itraconazole. Solifenacin Succinate tablet should be taken orally and should be swallowed whole with liquids. It can be taken with or without food.
Patients with hepatic impairment: No dose adjustment is necessary for patients with mild hepatic impairment. Patients with moderate hepatic impairment (Child-Pugh score of 7 to 9) should be treated with caution and receive no more than 5 mg once daily.
Potent inhibitors of cytochrome P450 3A4: The maximum dose of Solifenacin Succinate should be limited to 5 mg when treated simultaneously with Ketoconazole or therapeutic doses of other potent CYP3A4 inhibitors e.g. Ritonavir, Nelfinavir, Itraconazole. Solifenacin Succinate tablet should be taken orally and should be swallowed whole with liquids. It can be taken with or without food.
Overdose effectsView
Over dosage with Solifenacin Succinate can potentially result in severe anticholinergic effects. The highest dose of Solifenacin Succinate accidentally given to a single patient was 280 mg in a 5 hour period, resulting in mental status changes not requiring hospitalization. In the event of overdose with Solifenacin Succinate, the patient should be treated with activated charcoal. Gastric lavage is useful if performed within 1 hour, but vomiting should not be induced. As for other anticholinergics, symptoms can be treated as follows:
- Severe central anticholinergic effects such as hallucinations or pronounced excitation: treat with physostigmine or carbachol.
- Convulsions or pronounced excitation: treat with benzodiazepines.
- Respiratory insufficiency: treat with artificial respiration.
- Tachycardia: treat with beta-blockers.
- Urinary retention: treat with catheterisation.
- Mydriasis: treat with pilocarpine eye drops and/or place patient in a dark room.
StorageView
Store in a cool and dry place, protected from light.
Solvit-B
Vitamin B complex
Solvit-B
Vitamin B complex
Indications
Vitamin B deficiencies
Indication detailsView
Vitamin-B complex is indicated for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi Vitamin-B complex is indicated for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi
Therapeutic classView
Specific combined vitamin preparations
PharmacologyView
Vitamin-B complex contains the most important members of the vitamin B group in pure form and in therapeutically balanced proportions. The members of the vitamin B group contained in Vitamin-B complex are components of enzyme systems that regulate various stages of carbohydrate, fat and protein metabolism, each of the components playing a specific biological role. Deficiency of B vitamin causes glossitis, stomatitis, cheilosis, polyneuritis, beriberi, pellagra and vascularisation of cornea.
DosageView
Tablet/ capsule: usual recommended dose is 1-2 tablet/capsule 3 times daily or as directed by the physician.
Syrup: 2-3 teaspoonful daily or as directed by the physician.
Injection: It is for intramuscular and intravenous administration. Usual recommended dose is 2 ml daily or as directed by the physician. In addition with Thiamine, Riboflavin, Nicotinamide, Pyridoxine; injectable dosage from contains D-Panthenol 5 mg.
Syrup: 2-3 teaspoonful daily or as directed by the physician.
Injection: It is for intramuscular and intravenous administration. Usual recommended dose is 2 ml daily or as directed by the physician. In addition with Thiamine, Riboflavin, Nicotinamide, Pyridoxine; injectable dosage from contains D-Panthenol 5 mg.
Side effectsView
Adverse reactions have been reported with specific vitamins and minerals, but generally at levels substantially higher than those in Vitamin-B complex. However, allergic and idiosyncratic reactions are possible at lower levels. Iron, even at the usual recommended level has been associated with gastrointestinal intolerance in some patients.
ContraindicationsView
Vitamin-B complex is contraindicated in patients hypersensitive to any of its components.
InteractionsView
As little as 5 mg pyridoxine daily can decrease the efficacy of levodopa in the treatment of parkinsonism. Therefore, Vitamin-B complex is not recommended for patients undergoing such therapy
Pregnancy & lactationView
It is safe to use Vitamin-B complex in pregnancy and lactation.
Solvit-M
Multivitamin & Multimineral
Solvit-M
Multivitamin & Multimineral
Indications
Vitamin deficiency
Indication detailsView
This is indicated for the treatment and/or prevention of vitamin and mineral deficiencies associated with restricted diets, improper food intake, alcoholism and decreased absorption. It is also indicated in patients with increased requirements for vitamins and minerals due to acute and chronic diseases, pregnancy, lactation, menopause, infections, during treatment with antibiotics, convalescence etc. To prevent the occurrence of serious birth defects periconceptional (from three months before conception up to the first trimester of pregnancy) supplementation with this tablet is required.
Therapeutic classView
Multi-vitamin & Multi-mineral combined preparations, Specific mineral & vitamin combined preparations
PharmacologyView
Vitamins and minerals are essential for normal metabolic functions including hematopoiesis. The members of vitamin B-group are components of enzyme system that regulate various stages of carbohydrate, fat and protein metabolism, each of the components playing a specific biological role. Vitamin C is involved in tissue repair and collagen formation. Vitamin A plays an essential role in the function of retina and is essential for growth and differentiation of epithelial tissue. Vitamin E is an antioxidant which preserves essential cellular constituents. Vitamin D is supplemented for prevention and cure of nutritional and metabolic rickets and for treatment of hypoparathyroidism. Iron, Copper, Manganese, Zinc serve as catalysts in enzyme systems which perform vital cellular functions.
DosageView
Orally one tablet daily for adult and children over 5 years of age or as directed by the physicians.
Side effectsView
Side effects have been reported with specific vitamins & minerals, but at level substantially higher than those in this tablet. Iron has been associated with gastrointestinal intolerance in some patients.
ContraindicationsView
This is contraindicated in patients hypersensitive to any of its components. This is not intended for treatment of severe specific deficiencies of vitamins or minerals. It is not recommended for patients undergoing treatment with levodopa as pyridoxine decreases the efficacy of levodopa. During the first trimester of pregnancy, larger doses of vitamin A (more than 10 tablets per day) may be teratogenic.
PrecautionsView
Not intended for treatment of pernicious anemia or other megaloblastic anemia where vitamin B12 is deficient.
Pregnancy & lactationView
During the first trimester of pregnancy, recommended daily dose should not be exceeded. Because larger doses of Vitamin-A (multiple tablets per day) may be teratogenic.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Solvitone
Vitamin B complex
Solvitone
Vitamin B complex
Indications
Vitamin B deficiencies
Indication detailsView
Vitamin-B complex is indicated for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi Vitamin-B complex is indicated for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi
Therapeutic classView
Specific combined vitamin preparations
PharmacologyView
Vitamin-B complex contains the most important members of the vitamin B group in pure form and in therapeutically balanced proportions. The members of the vitamin B group contained in Vitamin-B complex are components of enzyme systems that regulate various stages of carbohydrate, fat and protein metabolism, each of the components playing a specific biological role. Deficiency of B vitamin causes glossitis, stomatitis, cheilosis, polyneuritis, beriberi, pellagra and vascularisation of cornea.
DosageView
Tablet/ capsule: usual recommended dose is 1-2 tablet/capsule 3 times daily or as directed by the physician.
Syrup: 2-3 teaspoonful daily or as directed by the physician.
Injection: It is for intramuscular and intravenous administration. Usual recommended dose is 2 ml daily or as directed by the physician. In addition with Thiamine, Riboflavin, Nicotinamide, Pyridoxine; injectable dosage from contains D-Panthenol 5 mg.
Syrup: 2-3 teaspoonful daily or as directed by the physician.
Injection: It is for intramuscular and intravenous administration. Usual recommended dose is 2 ml daily or as directed by the physician. In addition with Thiamine, Riboflavin, Nicotinamide, Pyridoxine; injectable dosage from contains D-Panthenol 5 mg.
Side effectsView
Adverse reactions have been reported with specific vitamins and minerals, but generally at levels substantially higher than those in Vitamin-B complex. However, allergic and idiosyncratic reactions are possible at lower levels. Iron, even at the usual recommended level has been associated with gastrointestinal intolerance in some patients.
ContraindicationsView
Vitamin-B complex is contraindicated in patients hypersensitive to any of its components.
InteractionsView
As little as 5 mg pyridoxine daily can decrease the efficacy of levodopa in the treatment of parkinsonism. Therefore, Vitamin-B complex is not recommended for patients undergoing such therapy
Pregnancy & lactationView
It is safe to use Vitamin-B complex in pregnancy and lactation.
Som
Omeprazole
Som
Omeprazole
Indications
Zollinger-Ellison syndrome
Indication detailsView
Omeprazole is indicated for the treatment of-
- Gastric and duodenal ulcer
- NSAID-associated duodenal and gastric ulcer
- As prophylaxis in patients with a history of NSAID-associated duodenal and gastric ulcer
- Gastro-esophageal reflux disease
- Long-term management of acid reflux disease
- Acid-related dyspepsia
- Severe ulcerating reflux esophagitis
- Prophylaxis of acid aspiration during general anesthesia
- Zollinger-Ellison syndrome
- Helicobacter pylori-induced peptic ulcer.
Therapeutic classView
Proton Pump Inhibitor
PharmacologyView
Omeprazole, a substituted benzimidazole, is an inhibitor of gastric acid secretion. It inhibits gastric acid secretion by blocking hydrogen-potassium-adenosine triphosphatase (H+/K+ ATPase) enzyme system in the gastric parietal cell. After oral administration, the onset of the antisecretory effect occurs within one hour, with the maximum effect occurring within two hours and inhibition of secretion lasts up to 72 hours. When the drug is discontinued, secretory activity returns gradually, over 3 to 5 days.
DosageView
Oral-
IV Injection-
- Benign gastric and duodenal ulcer: 20 mg once daily for 4 weeks in duodenal ulceration, 8 weeks in gastric ulceration; in severe or recurrent cases, dose to be increased to 40 mg daily; maintenance dose for recurrent duodenal ulcer, 20 mg once daily; in prevention of relapse in duodenal ulcer, 10-20 mg daily.
- NSAID-associated duodenal or gastric ulcer: 20 mg once daily for 4 weeks, continued for further 4 weeks, if not fully healed. 20 mg once daily is used as prophylaxis in patients with a history of NSAID-associated duodenal or gastric ulcers.
- Gastro-esophageal reflux disease: 20 mg once daily for 4 weeks, continued for further 4-8 weeks, if not fully healed; 40 mg once daily has been given for 8 weeks in gastro-esophageal reflux disease, refractory to other treatment; maintenance dose is 20 mg once daily.
- Long-term management of acid reflux disease: 10-20 mg daily.
- Acid-related dyspepsia: 10-20 mg once daily for 2-4 weeks.
- Prophylaxis of acid aspiration: 40 mg on the preceding evening, then 40 mg 2-6 hours before surgery.
- Zollinger-Ellison syndrome: Initially 60 mg once daily; usual range 20-120 mg daily (If daily dose is more than 80 mg, 2 divided dose should be used).
- Helicobacter pylori eradication regimen in peptic ulcer disease: Omeprazole is recommended at a dose of 20 mg twice daily in association with antimicrobial agents as detailed below: Amoxicillin 500 mg and Metronidazole 400 mg both three times a day for one week, or Clarithromycin 250 mg and Metronidazole 400 mg both twice a day for one week, or Amoxicillin 1 g and Clarithromycin 500 mg both twice a day for one week.
- Paeditaric use in severe ulcerating reflux esophagitis (Child>1 year): If body-weight 10-20 kg, 10-20 -mg once daily for 4-12 weeks; if body-weight over 20 kg, 20-40 mg once daily for 4-12 weeks.
IV Injection-
- Prophylaxis of acid aspiration: Omeprazole 40 mg to be given slowly (over a period of 5 minutes) as an intravenous injection, one hour before surgery.
- Duodenal ulcer, gastric ulcer or reflux oesophagitis: In patients with duodenal ulcer, gastric ulcer or reflux oesophagitis where oral medication is inappropriate, Omeprazole IV 40 mg once daily is recommended.
- Zollinger- Ellison syndrome (ZES): In patients with Zollinger-Ellison Syndrome the recommended initial dose of Omeprazole given intravenously is 60 mg daily. Higher daily doses may be required and the dose should be adjusted individually. When doses exceed 60 mg daily, the dose should be divided & given twice daily.
AdministrationView
Direction for use of IV Injection: Omeprazole lyophilized powder and water for injection is for intravenous administration only and must not be given by any other route. Omeprazole IV injection should be given as a slow intravenous injection. The solution for IV injection is obtained by adding 10 ml water for injection to the vial containing powder. After reconstitution the injection should be given slowly over a period of at least 2 to 5 minutes at a maximum rate of 4 ml/minute. Use only freshly prepared solution. The solution should be used within 4 hours of reconstitution.
Direction for use of IV Infusion: Omeprazole IV infusion should be given as an intravenous infusion over a period of 20-30 minutes or more. The contents of one vial must be dissolved in 100 ml saline for infusion or 100 ml 5% Dextrose for infusion. The solution should be used within 12 hours when Omeprazole is dissolved in saline and within 6 hours when dissolved in 5% Dextrose. The reconstituted solution should not be mixed or co-administered in the same infusion set with any other drug.
Direction for use of IV Infusion: Omeprazole IV infusion should be given as an intravenous infusion over a period of 20-30 minutes or more. The contents of one vial must be dissolved in 100 ml saline for infusion or 100 ml 5% Dextrose for infusion. The solution should be used within 12 hours when Omeprazole is dissolved in saline and within 6 hours when dissolved in 5% Dextrose. The reconstituted solution should not be mixed or co-administered in the same infusion set with any other drug.
Side effectsView
Omeprazole is generally well tolerated. Nausea, abdominal colic, paresthesia, dizziness and headache have been stated to be generally mild and transient and not requiring a reduction in dosage.
ContraindicationsView
Omeprazole is contraindicated in patients with known hypersensitivity to any of the components of the formulation.
PrecautionsView
When gastric ulcer is suspected, the possibility of gastric malignancy should be excluded before treatment with Omeprazole is instituted, as treatment may alleviate the symptoms and delay diagnosis.
InteractionsView
Omeprazole can prolong the elimination of diazepam, warfarin and phenytoin. So, reduction of warfarin or phenytoin dose may be necessary when Omeprazole is added to the treatment. There is no evidence of an interaction of Omeprazole with theophylline, propranolol or antacids.
Pregnancy & lactationView
US FDA pregnancy category of Omeprazole is C. However, results from three prospective epidemiological studies indicate no adverse effects of Omeprazole on pregnancy or on the health of the fetus/newborn child. There is no information available on the passage of Omeprazole into breast milk or its effects on the neonate. Breast-feeding should, therefore, be discontinued, if the use of Omeprazole is considered essential.
StorageView
Keep in a dry place away from light and heat. Keep out of the reach of children.
Soma DS
Sulphamethoxazole + Trimethoprim
Soma DS
Sulphamethoxazole + Trimethoprim
Indications
Urinary tract infection
Indication detailsView
Cotrimoxazole is bactericidal in vitro to a wide range of Gram-positive and Gram-negative organisms, including Streptococcus, Staphylococcus, Pneumococcus, Neisseria, B. catarrhalis, Escherichia coli, Klebsiella, Proteus spp., Haemophilus, Salmonella, Shigella, Vibrio cholerae, Brucella, Pneumocystis carinii, Nocardia and Bordetella. A particularly high degree of activity is exhibited against Haemophilus influenzae, E. coli and Proteus spp., making Cotrimoxazole particularly suitable for the treatment of chronic bronchitis and urinary tract infections. Cotrimoxazole exerts its bactericidal action by the sequential blockade of two bacterial enzyme systems in the biosynthesis of Folinic acid in the micro-organisms. The synergy thus produced accounts for the high degree of bactericidal activity.
Indications are :
Indications are :
- Respiratory tract infections, including acute and chronic bronchitis (treatment and prophylaxis), bronchiectasis, lung abscess, lobar and broncho-pneumonia, Pneumocystis carinii pneumonitis, sinusitis and otitis media.
- Genito-urinary tract infections, including urethritis, acute and chronic cystitis, pyelonephritis, prostatitis and gonorrhoea.
- Gastro-intestinal tract infections, caused by Salmonella typhi and Salmonella paratyphi, including the chronic carrier state.
- Other infections, caused by a wide range of organisms confirmed to be susceptible to Cotrimoxazole and where the therapeutic benefits are considered to outweigh the possible occurrence of adverse events.
- Such infections include acute and chronic osteomyelitis, acute brucellosis, skin infections including pyoderma, abscesses and wound infections, septicaemia, bacillary dysentery and cholera (as an adjuvant to fluid and electrolyte replacement), nocardiosis and mycetoma.
Therapeutic classView
Anti-diarrhoeal Antimicrobial drugs, Sulphonamides & Trimethoprim
PharmacologyView
Cotrimoxazole having broad spectrum bactericidal activity against a wide range of gram-positive & gram-negative bacteria and some protozoa. Co-trimoxazole containing Trimethoprim and Sulphamethoxazole in a 1:5 combination exerts its bactericidal action by the sequential blockade of two bacterial enzyme systems in the biosynthesis of folinic acid in the microorganism.
DosageView
Cotrimoxazole double strength tablet: Over 12 years
- For mild to moderate infections: 1 tablet twice daily.
- For severe infections: 1.5 tablets twice daily.
- Long term therapy (>14 days): 0.5 tablet twice daily.
- Gonorrhoea: 2 tablets every 12 hours for two days or 2.5 tablets followed by a further dose of 2.5 tablets after 8 hours.
- For mild to moderate infections: 2 tablets twice daily.
- For severe infections: 2 tablets thrice daily.
- Long term therapy: (>14 days): 1 tablet twice daily.
- 6-12 years: 2 teaspoonful twice daily.
- 6 month-5 years: 1 teaspoonful twice daily.
- 6 weeks-6 months: 0.5 teaspoonful twice daily.
Side effectsView
The side effects like crystalluria, allergic reactions, haemolysis, thrombocytopenia, neutropenia, agranulocytosis etc. have been reported rarely with Sulphamethoxazole-Trimethoprim combination. Other side effects are less serious in nature such as malaise, headache, nausea and vomiting. These are normally transient and do not require withdrawal of treatment.
ContraindicationsView
- Hypersensitivity to trimethoprim or sulphonamides.
- Patients with documented megaloblastic anaemia due to folate deficiency.
- Patients showing marked liver parenchymal damage, blood dyscrasia, severe renal insufficiency, glucose 6-phosphate dehydrogenase deficiency.
PrecautionsView
Prolonged full dose treatment with sulfamethoxazole-trimethoprim combination is associated with the risk of macrocytic anaemia due to the drug’s interference in the conversion of Folic acid into Folinic acid. If this occurs, it can be reversed by giving Folinic acid. Care should be taken when giving this combination to diabetic patients receiving sulphonylurea drug for possible potentiation of action of sulphonylurea.
Pregnancy & lactationView
Pregnancy and during the nursing period, because sulphonamides pass the placenta and are excreted in the breast milk and may cause kernicterus.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Somarant
Suvorexant
Somarant
Suvorexant
Indications
Insomnia and sleep disturbances
Indication detailsView
Suvorexant is indicated for the treatment of insomnia, characterized by difculties with sleep onset and/or sleep maintenance.
Therapeutic classView
Miscellaneous sedatives & hypnotics
PharmacologyView
Suvorexant is a highly selective antagonist for orexin receptors OX1R and OX2R. The mechanism by which Suvorexant exerts its therapeutic efect in insomnia is presumed to be through antagonism of orexin receptors. The orexin neuropeptide signaling system is a central promoter of wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R is thought to suppress wake drive.
DosageView
Recommended dose is 10 mg, no more than once per night taken before 30 minutes of going to bed, with at least 7 hours remaining before the planned time of awakening. If the 10 mg dose is well-tolerated but not effective, the dose can be increased, not to exceed 20 mg once daily. Lowest dose effective should be used for the patient. Time to effect may be delayed if taken with or soon after a meal.
Side effectsView
Common side effects are Sleepiness during the day, Not thinking clearly, Act strangely, confused, or upset, Sleep-walking
ContraindicationsView
Do not use in patients with narcolepsy.
PrecautionsView
Daytime somnolence: Risk of impaired alertness and motor coordination, including impaired driving; risk increases with dose; caution patients taking 20 mg against next-day driving and other activities requiring complete mental alertness.
Need to evaluate for co-morbid diagnoses: Reevaluate if insomnia persists after 7 to 10 days of treatment.
Need to evaluate for co-morbid diagnoses: Reevaluate if insomnia persists after 7 to 10 days of treatment.
InteractionsView
CNS-Active Drugs: An additive effect on psychomotor performance was observed when a single dose of 40 mg of Suvorexant was co-administered with a single dose of 0.7 g/kg alcohol. Suvorexant does not afect alcohol concentrations and alcohol does not afect Suvorexant concentrations.
effect s of Other Drugs on Suvorexant: Strong (e.g., ketoconazole or itraconazole) and moderate (e.g., diltiazem) CYP3A inhibitors signifcantly increased Suvorexant exposure. Strong CYP3A inducers (e.g., rifampin) substantially decreases Suvorexant exposure.
effect s of Suvorexant on Other Drugs: Suvorexant is unlikely to cause clinically signifcant inhibition of human CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19 or CYP2D6. Chronic administration of Suvorexant is unlikely to induce the metabolism of drugs metabolized by major CYP isoforms.
effect s of Other Drugs on Suvorexant: Strong (e.g., ketoconazole or itraconazole) and moderate (e.g., diltiazem) CYP3A inhibitors signifcantly increased Suvorexant exposure. Strong CYP3A inducers (e.g., rifampin) substantially decreases Suvorexant exposure.
effect s of Suvorexant on Other Drugs: Suvorexant is unlikely to cause clinically signifcant inhibition of human CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19 or CYP2D6. Chronic administration of Suvorexant is unlikely to induce the metabolism of drugs metabolized by major CYP isoforms.
Pregnancy & lactationView
Pregnancy Category C. There is no adequate and well-controlled studies in pregnant women. Suvorexant should be used during pregnancy only if the potential beneft justifes the potential risk to the fetus.
StorageView
Store in dry and cool place, protect from light & keep away from children.
Somazin
Citicoline Sodium
Somazin
Citicoline Sodium
Indications
Parkinson’s disease
Indication detailsView
Citicoline Sodium is indicated in-
- Cerebrovascular disease e.g. ischemia due to stroke, where Citicoline accelerates the recovery of consciousness & overcoming motor deficit. Treatment within the first 24 hours after onset in patients with moderate to severe stroke increases the probability of complete recovery in 3 months.
- Cerebral insufficiency (e.g. dizziness, memory loss, poor concentration & disorientation) due to head trauma or brain injury.
- Cognitive dysfunction due to degenerative disease (Alzheimer's disease)
- Parkinson's disease: Citicoline has been shown to be effective as co-therapy for Parkinson's disease.
Therapeutic classView
CNS stimulant drugs
PharmacologyView
Citicoline is a naturally occurring substance that is an essential intermediate in the synthesis of structural phospholipids of cell membrane. Oral dose of Citicoline is metabolized to choline & cytidine. These then enter into the systemic circulation, cross the blood-brain barrier and recombine to form Citicoline within the central nervous system. Citicoline activates the biosynthesis of structural phospholipids in the neuronal membrane, promotes rapid repair of injured cell surface & mitochondrial membrane & increases the level of various neurotransmitters like acetylcholine & dopamine. Citicoline has neuroprotective effects in situations of hypoxia & ischemia, as well as improved learning & memory performance in animal models for the aging brain. Citicoline inhibits the activation of Phospholipase A2 to prevent apoptotic & necrotic cell death.
DosageView
Oral:
- Immediate treatment of stroke due to a clot (ischemic stroke): 500-2000 mg of Citicoline per day, start within 24 hours of stroke.
- For decline in thinking skills due to stroke: 1000-2000 mg of Citicoline per day.
- Chronic cerebrovascular disease: 1000 mg daily in divided dose with or between meals for ongoing disease of the blood vessels that serve the brain.
- 1 to 2 injections daily.
- Adjust dosage according to the severity.
- Can be administered through intramuscular (IM), or intravenous (IV) [ 3 to 5 minutes] route.
Side effectsView
Occasionally Citicoline may exert stimulating action of the parasympathetic system as well as a fleeting & discrete hypotensive effect.
ContraindicationsView
Patients with hypertonic of the parasympathetic nervous system.
PrecautionsView
In case of persistent intracranial hemorrhage, it is recommended not to exceed the dose of 1000 mg of Citicoline daily.
InteractionsView
Citicoline may enhance the effects of levodopa, carbidopa & entacapone. Citicoline must not be administered with products containing meclophenoxate.
Pregnancy & lactationView
There are no adequate & well controlled studies of Citicoline during pregnancy & lactation. Citicoline should be used during pregnancy & lactation only if the potential benefits justify the potential risks.
Pediatric usageView
Geriatric use: No dosage adjustment is required & the usual dose can be administered.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Somazin
Citicoline Sodium
Somazin
Citicoline Sodium
Indications
Parkinson’s disease
Indication detailsView
Citicoline Sodium is indicated in-
- Cerebrovascular disease e.g. ischemia due to stroke, where Citicoline accelerates the recovery of consciousness & overcoming motor deficit. Treatment within the first 24 hours after onset in patients with moderate to severe stroke increases the probability of complete recovery in 3 months.
- Cerebral insufficiency (e.g. dizziness, memory loss, poor concentration & disorientation) due to head trauma or brain injury.
- Cognitive dysfunction due to degenerative disease (Alzheimer's disease)
- Parkinson's disease: Citicoline has been shown to be effective as co-therapy for Parkinson's disease.
Therapeutic classView
CNS stimulant drugs
PharmacologyView
Citicoline is a naturally occurring substance that is an essential intermediate in the synthesis of structural phospholipids of cell membrane. Oral dose of Citicoline is metabolized to choline & cytidine. These then enter into the systemic circulation, cross the blood-brain barrier and recombine to form Citicoline within the central nervous system. Citicoline activates the biosynthesis of structural phospholipids in the neuronal membrane, promotes rapid repair of injured cell surface & mitochondrial membrane & increases the level of various neurotransmitters like acetylcholine & dopamine. Citicoline has neuroprotective effects in situations of hypoxia & ischemia, as well as improved learning & memory performance in animal models for the aging brain. Citicoline inhibits the activation of Phospholipase A2 to prevent apoptotic & necrotic cell death.
DosageView
Oral:
- Immediate treatment of stroke due to a clot (ischemic stroke): 500-2000 mg of Citicoline per day, start within 24 hours of stroke.
- For decline in thinking skills due to stroke: 1000-2000 mg of Citicoline per day.
- Chronic cerebrovascular disease: 1000 mg daily in divided dose with or between meals for ongoing disease of the blood vessels that serve the brain.
- 1 to 2 injections daily.
- Adjust dosage according to the severity.
- Can be administered through intramuscular (IM), or intravenous (IV) [ 3 to 5 minutes] route.
Side effectsView
Occasionally Citicoline may exert stimulating action of the parasympathetic system as well as a fleeting & discrete hypotensive effect.
ContraindicationsView
Patients with hypertonic of the parasympathetic nervous system.
PrecautionsView
In case of persistent intracranial hemorrhage, it is recommended not to exceed the dose of 1000 mg of Citicoline daily.
InteractionsView
Citicoline may enhance the effects of levodopa, carbidopa & entacapone. Citicoline must not be administered with products containing meclophenoxate.
Pregnancy & lactationView
There are no adequate & well controlled studies of Citicoline during pregnancy & lactation. Citicoline should be used during pregnancy & lactation only if the potential benefits justify the potential risks.
Pediatric usageView
Geriatric use: No dosage adjustment is required & the usual dose can be administered.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Somazole
Esomeprazole
Somazole
Esomeprazole
Indication detailsView
Esomeprazole is indicated:
- To relieve from chronic heartburn symptoms and other symptoms associated with GERD
- For the healing of erosive esophagitis
- For maintenance of healing of erosive esophagitis
- In combination with amoxicillin and clarithromycin for eradication of Helicobacter pylori infection in patients with duodenal ulcer disease.
- Zollinger-Ellison Syndrome
- Acid related Dyspepsia
- Duodenal & Gastric ulcer
PharmacologyView
Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole (S-isomer of omeprazole) is the first single optical isomer of proton pump inhibitor, provides better acid control than racemic proton pump inhibitors.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
DosageView
Healing of Erosive Esophagitis: 20 mg or 40 mg Once Daily for 4-8 Weeks. The majority of patients are healed within 4 to 8 weeks. For patients who don't heal after 4-8 weeks, an additional 4-8 weeks of treatment may be considered. Maintenance of Healing of Erosive
Esophagitis: 20 mg Once Daily (Clinical studies did not extend 6 months).
Symptomatic GERD: 20 mg Once Daily for 4 Weeks. If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
Helicobacter Pylori eradication: Triple Therapy to reduce the risk of Duodenal Ulcer recurrence-Esomeprazole 40 mg Once Daily for 10 days, Amoxicillin 1000 mg Twice Daily for 10 days, Clarithromycin 500 mg Twice Daily for 10 days.
Zollinger-Ellison Syndrome: The dose is 20-80 mg once daily. The dosage should be adjusted individually and treatment continued as long as clinically indicated.
Acid-related Dyspepsia: 20-40 mg once daily for 2-4 weeks according to the response.
Duodenal ulcer: 20 mg once daily for 2-4 weeks. Gastric ulcer: 20-40 mg once daily for 4-8 weeks.
Injection: The recommended adult dose is 40 mg Esomeprazole given once daily by intravenous injection (not less than 3 minutes) or intravenous infusion (10 to 30 minutes). Esomeprazole IV injection should not be administered concomitantly with any other medications through the same intravenous site. Treatment with Esomeprazole IV injection should be discontinued as soon as the patient is able to resume treatment with Esomeprazole delayed-release capsules. Safety and effectiveness in paediatric patients have not been established.
AdministrationView
Esomeprazole tablet or capsule: should be swallowed whole and taken one hour before a meal.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Side effectsView
The most frequently occurring adverse events reported with Esomeprazole include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth. There are no difference in types of related adverse events seen during maintenance treatment upto 12 months compared to short term treatment.
ContraindicationsView
Esomeprazole is contraindicated in-patient with known hypersensitivity to any of the formulation.
PrecautionsView
General: Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
InteractionsView
Esomeprazole is extensively metabolized in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that Esomeprazole is not likely to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and 3A4. No clinically relevant interactions with drugs metabolized by these CYP enzymes would be expected. Drug interaction studies have shown that Esomeprazole does not have any clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin or amoxicillin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Pregnancy & lactationView
There are no adequate and well-controlled studies in pregnant women. Animal studies have revealed no teratogenic effects. The excretion of esomeprazole in milk has not been studied. Breast-feeding should be therefore be discontinued if the use of esomeprazole is considered essential.
Pediatric usageView
Paediatric Use: Safety and effectiveness in paediatric patients have not been established.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Overdose effectsView
A single oral dose of Esomeprazole at 510 mg/kg (about 103 times the human dose on a body surface area basis), has been lethal to rats. The major signs of acute toxicity are reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. There have been no reports of overdose with Esomeprazole. No specific antidote for Esomeprazole is known. Since Esomeprazole is extensively protein bound, it is not expected to be removed by dialysis. In the event of overdosage, treatment should be symptomatic and supportive. As with the management of any overdose, the possibility of multiple drug ingestion should be considered.
ReconstitutionView
Infusion: Reconstitute one sterile single-dose vial of Esomeprazole IV Injection with 5 ml of the solvent (WFI) provided and further diluting the resulting solution within 0.9% Sodium Chloride solution or 5% Dextrose solution to make a final volume of 50 ml. The resultant infusion should be given intravenously over a period of 10-30 minutes. Chemical and physical in-use stability has been demonstrated for 12 hours after reconstitution with 0.9% Sodium Chloride solution or for 6 hours after reconstitution with 5% Dextrose solution. From a microbial point of view, the product should be used immediately. Any unused portion should be discarded.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of reach of children.
Somazole
Esomeprazole
Somazole
Esomeprazole
Indication detailsView
Esomeprazole is indicated:
- To relieve from chronic heartburn symptoms and other symptoms associated with GERD
- For the healing of erosive esophagitis
- For maintenance of healing of erosive esophagitis
- In combination with amoxicillin and clarithromycin for eradication of Helicobacter pylori infection in patients with duodenal ulcer disease.
- Zollinger-Ellison Syndrome
- Acid related Dyspepsia
- Duodenal & Gastric ulcer
PharmacologyView
Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole (S-isomer of omeprazole) is the first single optical isomer of proton pump inhibitor, provides better acid control than racemic proton pump inhibitors.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
DosageView
Healing of Erosive Esophagitis: 20 mg or 40 mg Once Daily for 4-8 Weeks. The majority of patients are healed within 4 to 8 weeks. For patients who don't heal after 4-8 weeks, an additional 4-8 weeks of treatment may be considered. Maintenance of Healing of Erosive
Esophagitis: 20 mg Once Daily (Clinical studies did not extend 6 months).
Symptomatic GERD: 20 mg Once Daily for 4 Weeks. If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
Helicobacter Pylori eradication: Triple Therapy to reduce the risk of Duodenal Ulcer recurrence-Esomeprazole 40 mg Once Daily for 10 days, Amoxicillin 1000 mg Twice Daily for 10 days, Clarithromycin 500 mg Twice Daily for 10 days.
Zollinger-Ellison Syndrome: The dose is 20-80 mg once daily. The dosage should be adjusted individually and treatment continued as long as clinically indicated.
Acid-related Dyspepsia: 20-40 mg once daily for 2-4 weeks according to the response.
Duodenal ulcer: 20 mg once daily for 2-4 weeks. Gastric ulcer: 20-40 mg once daily for 4-8 weeks.
Injection: The recommended adult dose is 40 mg Esomeprazole given once daily by intravenous injection (not less than 3 minutes) or intravenous infusion (10 to 30 minutes). Esomeprazole IV injection should not be administered concomitantly with any other medications through the same intravenous site. Treatment with Esomeprazole IV injection should be discontinued as soon as the patient is able to resume treatment with Esomeprazole delayed-release capsules. Safety and effectiveness in paediatric patients have not been established.
AdministrationView
Esomeprazole tablet or capsule: should be swallowed whole and taken one hour before a meal.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Side effectsView
The most frequently occurring adverse events reported with Esomeprazole include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth. There are no difference in types of related adverse events seen during maintenance treatment upto 12 months compared to short term treatment.
ContraindicationsView
Esomeprazole is contraindicated in-patient with known hypersensitivity to any of the formulation.
PrecautionsView
General: Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
InteractionsView
Esomeprazole is extensively metabolized in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that Esomeprazole is not likely to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and 3A4. No clinically relevant interactions with drugs metabolized by these CYP enzymes would be expected. Drug interaction studies have shown that Esomeprazole does not have any clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin or amoxicillin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Pregnancy & lactationView
There are no adequate and well-controlled studies in pregnant women. Animal studies have revealed no teratogenic effects. The excretion of esomeprazole in milk has not been studied. Breast-feeding should be therefore be discontinued if the use of esomeprazole is considered essential.
Pediatric usageView
Paediatric Use: Safety and effectiveness in paediatric patients have not been established.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Overdose effectsView
A single oral dose of Esomeprazole at 510 mg/kg (about 103 times the human dose on a body surface area basis), has been lethal to rats. The major signs of acute toxicity are reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. There have been no reports of overdose with Esomeprazole. No specific antidote for Esomeprazole is known. Since Esomeprazole is extensively protein bound, it is not expected to be removed by dialysis. In the event of overdosage, treatment should be symptomatic and supportive. As with the management of any overdose, the possibility of multiple drug ingestion should be considered.
ReconstitutionView
Infusion: Reconstitute one sterile single-dose vial of Esomeprazole IV Injection with 5 ml of the solvent (WFI) provided and further diluting the resulting solution within 0.9% Sodium Chloride solution or 5% Dextrose solution to make a final volume of 50 ml. The resultant infusion should be given intravenously over a period of 10-30 minutes. Chemical and physical in-use stability has been demonstrated for 12 hours after reconstitution with 0.9% Sodium Chloride solution or for 6 hours after reconstitution with 5% Dextrose solution. From a microbial point of view, the product should be used immediately. Any unused portion should be discarded.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of reach of children.