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Nevirax
Nirmatrelvir + Ritonavir
Nevirax
Nirmatrelvir + Ritonavir
Indication detailsView
Indicated for mild-to-moderate COVID-19 positive adult and pediatric patients (12 years of age and older weighing at least 40 kg), who are at high risk for progression to severe COVID-19, including hospitalization or death.
PharmacologyView
This inhibits the main protease (Mpro) of the SARS-CoV-2. This main protease (Mpro) is also referred as 3C-like protease (3CLpro) or nsp5 protease. This inhibition of Mpro hampers the peptidomimetic activity of SARS-CoV-2. Ritonavir is an HIV-1 protease inhibitor but is not active against SARS-CoV-2 Mpro. Ritonavir inhibits the CYP3A mediated metabolism of Nirmatrelvir, resulting in increased plasma concentrations of Nirmatrelvir
DosageView
Nirmatrelvir must be co-administered with Ritonavir. Initiate this treatment as soon as possible after diagnosis of COVID-19 and within 3-5 days of symptom onset. Administer orally with or without food.
Dosage: 300 mg Nirmatrelvir (two 150 mg tablets) with 100 mg Ritonavir (one 100 mg tablet), with all three tablets taken together twice daily for 5 days.
Missed Dose: If the patient misses a dose of this within 8 hours of the time it is usually taken, the patient should take it as soon as possible and resume the normal dosing schedule. If the patient misses a dose by more than 8 hours, the patient should not take the missed dose and instead take the next dose at the regularly scheduled time. The patient should not double the dose to make up for a missed dose.
Dosage: 300 mg Nirmatrelvir (two 150 mg tablets) with 100 mg Ritonavir (one 100 mg tablet), with all three tablets taken together twice daily for 5 days.
Missed Dose: If the patient misses a dose of this within 8 hours of the time it is usually taken, the patient should take it as soon as possible and resume the normal dosing schedule. If the patient misses a dose by more than 8 hours, the patient should not take the missed dose and instead take the next dose at the regularly scheduled time. The patient should not double the dose to make up for a missed dose.
Side effectsView
Adverse events (incidence >1% and subject difference) were dysgeusia, diarrhea, hypertension, and myalgia.
ContraindicationsView
- History of clinically significant hypersensitivity reactions to the active ingredients (Nirmatrelvir or Ritonavir) or any other components.
- Co-administration with drugs highly dependent on CYP3A for clearance and for which elevated concentrations are associated with serious and/or life-threatening reactions.
- Co-administration with potent CYP3A inducers where significantly reduced Nirmatrelvir or Ritonavir plasma concentrations may be associated with the potential for loss of virologic response and possible resistance.
PrecautionsView
The concomitant use of this tablet and certain other drugs may result in potentially significant drug interactions. Consult the full prescribing information prior to and during treatment for potential drug interactions.
Hepatotoxicity: Hepatic transaminase elevations, clinical hepatitis, and jaundice have occurred in patients receiving Ritonavir.
HIV-1 Drug Resistance: This tablet use may lead to a risk of HIV-1 developing resistance to HIV protease inhibitors in individuals with uncontrolled or undiagnosed HIV-1 infection.
Hepatotoxicity: Hepatic transaminase elevations, clinical hepatitis, and jaundice have occurred in patients receiving Ritonavir.
HIV-1 Drug Resistance: This tablet use may lead to a risk of HIV-1 developing resistance to HIV protease inhibitors in individuals with uncontrolled or undiagnosed HIV-1 infection.
InteractionsView
Co-administration of this tablet with drugs highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events is contraindicated. Co-administration with other CYP3A substrates may require a dose adjustment or additional monitoring. Nirmatrelvir and Ritonavir are CYP3A substrates; therefore, drugs that induce CYP3A may decrease Nirmatrelvir and Ritonavir plasma concentrations and reduce this tablet therapeutic effect.
Pregnancy & lactationView
This is not recommended during pregnancy and in people who can become pregnant and who are not using contraception. Breastfeeding should be interrupted during treatment. These recommendations are because laboratory studies in animals suggest that high doses of this may impact the growth of the fetus. This drug should be used during pregnancy only if clearly needed and the benefit outweighs the risk to the fetus; use of oral solution is not recommended.
Pediatric usageView
Pediatric Use: This tablet is not authorized for use in pediatric patients younger than 12 years of age or weighing less than 40 kg. The safety and effectiveness of this tablet have not been established in pediatric patients.
Geriatric Use: Clinical studies of this tablet include subjects 65 years of age and older and their data contributes to the overall assessment of safety and efficacy.
Renal Impairment: No dosage adjustment is needed in patients with mild renal impairment. In patients with moderate renal impairment (eGFR >30 to <60 mL/min), reduce the dose of This tablet to 150 mg Nirmatrelvir and 100 mg Ritonavir twice daily for 5 days. This tablet is not recommended in patients with severe renal impairment (eGFR <30 mL/min).
Hepatic Impairment: No dosage adjustment of this tablet is needed for patients with either mild (Child-Pugh Class A) or moderate (Child-Pugh Class B) hepatic impairment. This tablet is not recommended in patients with severe hepatic impairment (Child-Pugh Class C).
Geriatric Use: Clinical studies of this tablet include subjects 65 years of age and older and their data contributes to the overall assessment of safety and efficacy.
Renal Impairment: No dosage adjustment is needed in patients with mild renal impairment. In patients with moderate renal impairment (eGFR >30 to <60 mL/min), reduce the dose of This tablet to 150 mg Nirmatrelvir and 100 mg Ritonavir twice daily for 5 days. This tablet is not recommended in patients with severe renal impairment (eGFR <30 mL/min).
Hepatic Impairment: No dosage adjustment of this tablet is needed for patients with either mild (Child-Pugh Class A) or moderate (Child-Pugh Class B) hepatic impairment. This tablet is not recommended in patients with severe hepatic impairment (Child-Pugh Class C).
Overdose effectsView
Treatment of an overdose of this tablet should consist of general supportive measures including monitoring of vital signs and observation of the clinical status of the patient. There is no specific antidote for overdose with this tablet.
StorageView
Do not store above 30°C. Keep in a dry place. Protect from light and keep out of the reach of children.
Nevola
Desvenlafaxine
Nevola
Desvenlafaxine
Indications
Depression
Indication detailsView
Desvenlafaxine, a serotonin and norepinephrine reuptake inhibitor (SNRI), is indicated for the treatment of major depressive disorder (MDD). The efficacy of Desvenlafaxine has been established in four short-term (8-week, placebo-controlled studies) and two maintenance studies in adult outpatients who met DSM-IV criteria for major depressive disorder.
Therapeutic classView
Serotonin-norepinephrine reuptake inhibitor (SNRI)
PharmacologyView
Desvenlafaxine is the principal active metabolite of venlafaxine. The exact mechanism is unknown, but is thought to be related to the potentiation of serotonin and norepinephrine in the CNS, through inhibition of their reuptake.
DosageView
The recommended dose for Desvenlafaxine is 50 mg once daily, with or without food. The 50 mg dose is both a starting dose and the therapeutic dose. Desvenlafaxine should be taken at approximately the same time each day. Tablets must be swallowed whole with fluid and not divided, crushed, chewed, or dissolved.
In clinical studies, doses of 10 mg to 400 mg per day were studied. In clinical studies, doses of 50 mg to 400 mg per day were shown to be effective, although no additional benefit was demonstrated at doses greater than 50 mg per day and adverse reactions and discontinuations were more frequent at higher doses.
The 25 mg per day dose is intended for a gradual reduction in dose when discontinuing treatment. When discontinuing therapy, gradual dose reduction is recommended whenever possible to minimize discontinuation symptoms
In clinical studies, doses of 10 mg to 400 mg per day were studied. In clinical studies, doses of 50 mg to 400 mg per day were shown to be effective, although no additional benefit was demonstrated at doses greater than 50 mg per day and adverse reactions and discontinuations were more frequent at higher doses.
The 25 mg per day dose is intended for a gradual reduction in dose when discontinuing treatment. When discontinuing therapy, gradual dose reduction is recommended whenever possible to minimize discontinuation symptoms
Side effectsView
Suicidal thinking/ behaviour, HTN, mydriasis, seizure, hyponatraemia, interstitial lung disease and eosinophilic pneumonia; nausea, dizziness, insomnia, hyperhidrosis, constipation, somnolence, decreased appetite, anxiety, sexual function disorders in males (e.g. anorgasmia, decreased libido, abnormal orgasm, delayed ejaculation, erectile dysfunction, ejaculation disorder, ejaculation failure, sexual dysfunction).
ContraindicationsView
Concurrent use or within 14 days of discontinuing MAOIs (e.g. linezolid, IV methylene blue). Initiation of MAOI at least 7 days after discontinuing desvenlafaxine.
PrecautionsView
Patient with pre-existing HTN or other conditions that may be compromised by increased BP, raised intraocular pressure, personal or family history of mania or hypomania; CV, cerebrovascular or lipid metabolism disorders; seizure disorder. Avoid abrupt withdrawal. Renal and moderate to severe hepatic impairment. Pregnancy and lactation.
InteractionsView
Increased risk of bleeding with aspirin or other NSAIDs, warfarin and other anticoagulants.
Pregnancy & lactationView
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Pediatric usageView
Hepatic impairment (Moderate to severe): 50 mg daily. Max: 100 mg once daily.
Renal Impairment:
Renal Impairment:
- CrCl <30 or ESRD: 25 mg daily or 50 mg every other day. Supplemental doses should not be given after dialysis.
- CrCl (30-50): Max 50 mg once daily.
StorageView
Store between 20-25° C.
Nevola
Desvenlafaxine
Nevola
Desvenlafaxine
Indications
Depression
Indication detailsView
Desvenlafaxine, a serotonin and norepinephrine reuptake inhibitor (SNRI), is indicated for the treatment of major depressive disorder (MDD). The efficacy of Desvenlafaxine has been established in four short-term (8-week, placebo-controlled studies) and two maintenance studies in adult outpatients who met DSM-IV criteria for major depressive disorder.
Therapeutic classView
Serotonin-norepinephrine reuptake inhibitor (SNRI)
PharmacologyView
Desvenlafaxine is the principal active metabolite of venlafaxine. The exact mechanism is unknown, but is thought to be related to the potentiation of serotonin and norepinephrine in the CNS, through inhibition of their reuptake.
DosageView
The recommended dose for Desvenlafaxine is 50 mg once daily, with or without food. The 50 mg dose is both a starting dose and the therapeutic dose. Desvenlafaxine should be taken at approximately the same time each day. Tablets must be swallowed whole with fluid and not divided, crushed, chewed, or dissolved.
In clinical studies, doses of 10 mg to 400 mg per day were studied. In clinical studies, doses of 50 mg to 400 mg per day were shown to be effective, although no additional benefit was demonstrated at doses greater than 50 mg per day and adverse reactions and discontinuations were more frequent at higher doses.
The 25 mg per day dose is intended for a gradual reduction in dose when discontinuing treatment. When discontinuing therapy, gradual dose reduction is recommended whenever possible to minimize discontinuation symptoms
In clinical studies, doses of 10 mg to 400 mg per day were studied. In clinical studies, doses of 50 mg to 400 mg per day were shown to be effective, although no additional benefit was demonstrated at doses greater than 50 mg per day and adverse reactions and discontinuations were more frequent at higher doses.
The 25 mg per day dose is intended for a gradual reduction in dose when discontinuing treatment. When discontinuing therapy, gradual dose reduction is recommended whenever possible to minimize discontinuation symptoms
Side effectsView
Suicidal thinking/ behaviour, HTN, mydriasis, seizure, hyponatraemia, interstitial lung disease and eosinophilic pneumonia; nausea, dizziness, insomnia, hyperhidrosis, constipation, somnolence, decreased appetite, anxiety, sexual function disorders in males (e.g. anorgasmia, decreased libido, abnormal orgasm, delayed ejaculation, erectile dysfunction, ejaculation disorder, ejaculation failure, sexual dysfunction).
ContraindicationsView
Concurrent use or within 14 days of discontinuing MAOIs (e.g. linezolid, IV methylene blue). Initiation of MAOI at least 7 days after discontinuing desvenlafaxine.
PrecautionsView
Patient with pre-existing HTN or other conditions that may be compromised by increased BP, raised intraocular pressure, personal or family history of mania or hypomania; CV, cerebrovascular or lipid metabolism disorders; seizure disorder. Avoid abrupt withdrawal. Renal and moderate to severe hepatic impairment. Pregnancy and lactation.
InteractionsView
Increased risk of bleeding with aspirin or other NSAIDs, warfarin and other anticoagulants.
Pregnancy & lactationView
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Pediatric usageView
Hepatic impairment (Moderate to severe): 50 mg daily. Max: 100 mg once daily.
Renal Impairment:
Renal Impairment:
- CrCl <30 or ESRD: 25 mg daily or 50 mg every other day. Supplemental doses should not be given after dialysis.
- CrCl (30-50): Max 50 mg once daily.
StorageView
Store between 20-25° C.
Nevralip
Alpha Lipoic Acid
Nevralip
Alpha Lipoic Acid
Indication detailsView
This tablet has potent antioxidant and neurotrophic properties. This helps you cope with the pain caused by:
- Peripheral and diabetic neuropathies
- Sciatica, backache, cervical syndrome, carpal tunnel syndrome
- Migraine headaches
PharmacologyView
α-Lipoic Acid is a substance which can be naturally found in animal and plant tissues and maintains its activity both in aqueous cell compartments and in those lipid membrane ones. Chromium Picolinate is a biologically active organic Chromium. Selenium and Zinc are essential minerals. It contains Vitamins of the B group, including the Vitamin B1 (Thiamine), also known as Antineuritic Vitamin.
Medical Pharmaquality is a dietary supplement containing an antioxidant combination with 600 mg alpha lipoic acid, trace elements (selenium, zinc and picolino chromium) and vitamins (B1, B5, B6, biotin and vitamin E) that have strong anti-inflammatory effects and neurotrophic properties. Alpha lipoic acid, zinc, selenium, picoline chromium and vitamin E help protect cells from oxidative stress. peripheral nerves (neuritis), protects the nervous system from degenerative phenomena. Picolinate chromium, zinc and biotin can help regulate glucose levels. Medical Pharmaquality can contribute to the relief of discomfort due to peripheral and diabetic neuropathies, sciatica, back pain, cervical syndrome, carpal tunnel syndrome, migraines. The retard form of this (prolonged-release) tablet ensures effectiveness with just one tablet per day.
Medical Pharmaquality is a dietary supplement containing an antioxidant combination with 600 mg alpha lipoic acid, trace elements (selenium, zinc and picolino chromium) and vitamins (B1, B5, B6, biotin and vitamin E) that have strong anti-inflammatory effects and neurotrophic properties. Alpha lipoic acid, zinc, selenium, picoline chromium and vitamin E help protect cells from oxidative stress. peripheral nerves (neuritis), protects the nervous system from degenerative phenomena. Picolinate chromium, zinc and biotin can help regulate glucose levels. Medical Pharmaquality can contribute to the relief of discomfort due to peripheral and diabetic neuropathies, sciatica, back pain, cervical syndrome, carpal tunnel syndrome, migraines. The retard form of this (prolonged-release) tablet ensures effectiveness with just one tablet per day.
DosageView
It is recommended to take 1 tablet daily, preferably on an empty stomach.
ContraindicationsView
Contraindicated in people receiving treatment for diabetes.
PrecautionsView
The Food Supplements should not be understood as a substitute for a varied and balanced diet and a healthy lifestyle. Do not exceed the recommended daily dose. Keep out of reach of children under 3 years of age. Do not take in case of hypersensitivity or allergy to one or more components. Before the possible use of the product, if you should be in treatment with hypoglycaemic pharmaceuticals, please consult with your own physician.
Nevrona
Vitamin B1, B6 & B12
Nevrona
Vitamin B1, B6 & B12
Indications
Vitamin B deficiencies
Indication detailsView
Vitamin B1, B6 & B12 is indicated for the treatment of vitamin B1, B6 & B12 deficiency syndrome. It is also indicated for the supportive treatment of neuritis & non-inflammatory diseases of the nerves, e.g.- Diabetic neuropathy, Peripheral neuralgin, Lumbago, Myalgia, Optic neuritis, Sciatica, Facial neuralgia, Intercostal neuralgia, Spinal pain.
Therapeutic classView
Specific combined vitamin preparations
PharmacologyView
Vitamin B1 converts carbohydrates, fatty acids and amino acids into energy, promotes healthy nerves, improves mood, strengthens the heart. Vitamin B6 forms RBCs, helps cells to make proteins, manufactures neurotransmitters e.g. serotonin and releases stored forms of energy, helps to prevent CVS diseases and stroke, helps to lift depression and eases insomnia. Vitamin B12 is essential for cell replication and important for RBC production, prevents anemia, helps to prevent depression, reduces nerve pain, numbness, tingling and lowers the risk of heart diseases.
The vitamin ingredients are absorbed well in per oral reception. It is widely distributed to most tissues and appears in breast milk. Within the cell, thiamine is mostly present as diphosphate. Thiamine is not stored to any appreciable extent in the body and amounts in excess of the body’s requirements are excreted in the urine as unchanged thiamine or as metabolites. Pyridoxine, pyridoxal and pyridoxamine are readily absorbed from the GIT following oral administration and are converted to the active forms of pyridoxal phosphate an pyridoxamine phosphate. They are stored mainly in liver where there is oxidation to 4-pyridoxic acid and other inactive metabolites, which are excreted in urine. As the dose increases, proportionally greater amounts are excreted unchanged in the urine.
The vitamin ingredients are absorbed well in per oral reception. It is widely distributed to most tissues and appears in breast milk. Within the cell, thiamine is mostly present as diphosphate. Thiamine is not stored to any appreciable extent in the body and amounts in excess of the body’s requirements are excreted in the urine as unchanged thiamine or as metabolites. Pyridoxine, pyridoxal and pyridoxamine are readily absorbed from the GIT following oral administration and are converted to the active forms of pyridoxal phosphate an pyridoxamine phosphate. They are stored mainly in liver where there is oxidation to 4-pyridoxic acid and other inactive metabolites, which are excreted in urine. As the dose increases, proportionally greater amounts are excreted unchanged in the urine.
DosageView
Tablet: 1-3 Tablets per day or as advised by the physician.
Injection:
Injection:
- In severe (acute) cases: 1 injection daily until the acute symptoms subside or taken as advised by the physician.
- In mild cases: 1 injection 2-3 times per week. Ampoules are preferably injected intramuscularly.
Side effectsView
Generally well tolerated but allergic reactions may be observed in few cases.
ContraindicationsView
Vitamin B1, Vitamin B6 and Vitamin B12 is contraindicated in patients on levodopa therapy, and in patients with hypersensitivity to any of the ingredients of the preparation.
PrecautionsView
Cyanocobalamin should not be given in patients with subacute degeneration of the spinal cord. Cyanocobalamin is not suitable form of vitamin B12 for the treatment of optic neuropathies associated with raised plasma concentrations of cyanocobalamin.
InteractionsView
No drug interaction has been reported yet.
Pregnancy & lactationView
Oral tablet form is recommended but due to the presence of benzyl alcohol, injection is not recommended during pregnancy & lactation.
Overdose effectsView
No overdosage symptoms are to be expected in the recommended dosage. If there is known overdose then treatment is symptomatic & supportive.
StorageView
Keep out of reach of children. Store in a cool (below 25°C temperature) and dry place, protected from light.
New Orsa-A
Oral Rehydration Salt [Powder]
New Orsa-A
Oral Rehydration Salt [Powder]
Indication detailsView
Oral Rehydration Salt replacement of fluid and electrolyte loss due to-
- Acute diarrhea
- Vomiting
- Dehydration
Therapeutic classView
Oral electrolytes preparations
PharmacologyView
This is the preparation of oral rehydration salt. It is composed of anhydrous glucose, sodium chloride, potassium chloride and sodium citrate (as dihydrate). This is a single formulation of glucose based oral rehydration salt to treat or prevent dehydration from diarrhea of any etiology, including cholera and in individuals of any age. This also prevents acidosis due to electrolyte imbalance.
DosageView
Daily dose should be equivalent to patients' fluid requirement for maintenance and replenishment of losses. During this therapy, mother should not stop breastfeeding to their child and normal food should be continued in case of adults.
Children less than 2 years: After each loose stool or vomiting 50-100 mL (10 to 20 teaspoonful) of prepared this.
Children 2 to 10 years: After each loose stool or vomiting 100-200 mL (1/2 to 1 glass) of prepared oral saline.
Adult and children above 10 years: After each loose stool or vomiting 200-400 mL (1 to 2 glass) of prepared this.
Children less than 2 years: After each loose stool or vomiting 50-100 mL (10 to 20 teaspoonful) of prepared this.
Children 2 to 10 years: After each loose stool or vomiting 100-200 mL (1/2 to 1 glass) of prepared oral saline.
Adult and children above 10 years: After each loose stool or vomiting 200-400 mL (1 to 2 glass) of prepared this.
AdministrationView
- Disperse the full contents of the sachet in 500 mL (1/2 liter) of pure drinking water.
- Do not mix the oral saline with hot water or heat the prepared solution.
- Discard the unused prepared oral saline after 12 hours of preparation.
PrecautionsView
Depressed renal function, severe continuing diarrhea or other critical fluid losses may need supplementation with parenteral fluids along with oral saline.
InteractionsView
There are no known drug interactions and none well documented.
StorageView
Do not store above 30°C temperature. Keep away from light and wet places. Keep out of reach of children.
Newage
Multivitamins & Multiminerals [A-Z prenatal preparation]
Newage
Multivitamins & Multiminerals [A-Z prenatal preparation]
Indications
Vitamin deficiency
Indication detailsView
This is indicated for use in improving the nutritional status of women throughout the pregnancy and in the postnatal period for both lactating and non-lactating mothers. This is also indicated in improving the nutritional status of women prior to conception.
Therapeutic classView
Iron, Vitamin & Mineral Combined preparation, Multi-vitamin & Multi-mineral combined preparations
PharmacologyView
This Multivitamins & Multiminerals is a preparation of comprehensive multiple vitamin and mineral supplement designed to meet the increased nutritional needs of pregnant or lactating women. Since pregnancy and lactation impose an increased demand for certain nutrients, added insurance of a complete multiple vitamin and nutrient supplement is recommended.
The special formulation of This Multivitamins & Multiminerals provides a wide spectrum of the essential nutrients needed for pregnant women, in a form that is gentle to the sensitive stomach. is a preparation of comprehensive multiple vitamin and mineral supplement designed to meet the increased nutritional needs of pregnant or lactating women. Since pregnancy and lactation impose an increased demand for certain nutrients, added insurance of a complete multiple vitamin and nutrient supplement is recommended. The special formulation of This Multivitamins & Multiminerals provides a wide spectrum of the essential nutrients needed for pregnant women, in a form that is gentle to the sensitive stomach.
The special formulation of This Multivitamins & Multiminerals provides a wide spectrum of the essential nutrients needed for pregnant women, in a form that is gentle to the sensitive stomach. is a preparation of comprehensive multiple vitamin and mineral supplement designed to meet the increased nutritional needs of pregnant or lactating women. Since pregnancy and lactation impose an increased demand for certain nutrients, added insurance of a complete multiple vitamin and nutrient supplement is recommended. The special formulation of This Multivitamins & Multiminerals provides a wide spectrum of the essential nutrients needed for pregnant women, in a form that is gentle to the sensitive stomach.
DosageView
One tablet daily or as directed by the physician.
Side effectsView
Allergic sensitization has been reported following oral administration of folic acid.
ContraindicationsView
This Multivitamins & Multiminerals is contraindicated in patients with a known hypersensitivity to any of the ingredients.
PrecautionsView
Folic acid in doses above 0.1 mg daily may obscure pernicious anemia in that hematological remission can occur while neurological manifestations remain progressive
Pregnancy & lactationView
Recommended.
Overdose effectsView
Accidental overdose of iron-containing products is a leading cause of fatal poisoning in children under 6. In case of accidental overdose, call a doctor or poison control center immediately.
Newcip
Ciprofloxacin
Newcip
Ciprofloxacin
Indications
Urinary tract infection
Indication detailsView
Ciprofloxacin is indicated for the treatment of Respiratory Tract Infections,Urinary tract infections, Pelvic Inflammatory Diseases, Infectious Diarrhea (Shigella dysenteriae, Vibrio cholera), Typhoid fever, Intra-abdominal infections, Prostatitis, Skin and Soft Tissue Infections, Bone and Joint Infections, Gonorrhea, Neutropenic patients with fever due to bacterial infection, Meningitis, Surgical prophylaxis.
Therapeutic classView
4-Quinolone preparations, Anti-diarrhoeal Antimicrobial drugs
PharmacologyView
Ciprofloxacin is a synthetic fluoroquinolone. It has bactericidal activity against a wide range of gram-positive and gram-negative organisms. It inhibits bacterial DNA synthesis by binding with the bacterial enzyme-DNA gyrase and topoisomerase IV which are responsible for DNA supercoiling.
DosageView
Tablet: Adult:
Extended-release tablet: In uncomplicated urinary tract infection (acute cystitis), the recommended dose of extended-release tablet is 1000 mg tablet once daily for three days.
For IV infusion:
- Respiratory Tract Infections: 500 to 750 mg twice daily (7 to 14 days)
- Urinary tract infections: 250 to 750 mg twice daily (3 to 10 days)
- Pelvic Inflammatory Diseases: 500 to 750 mg twice daily (14 days)
- Infectious Diarrhea (Shigella dysenteriae, Vibrio cholera): 500 mg twice daily (1 to 5 days)
- Typhoid fever: 500 mg twice daily (7 days)
- Intra-abdominal infections: 500 to 750 mg twice daily (5 to 14 days)
- Prostatitis: 500 to 750 mg twice daily (2 to 6 weeks)
- Skin and Soft Tissue Infections: 500 to 750 mg twice daily (7 to 14 days)
- Bone and Joint Infections: 500 to 750 mg twice daily (max. 3 months)
- Gonorrhea: 500 mg as a single dose
- Neutropenic patients with fever due to bacterial infection: 500 to 750 mg twice daily co-administered with appropriate antibacterials.
- Meningitis: 500 mg as a single dose.
- Surgical prophylaxis: 500 mg as a single dose, 60 minutes before the procedure.
Extended-release tablet: In uncomplicated urinary tract infection (acute cystitis), the recommended dose of extended-release tablet is 1000 mg tablet once daily for three days.
For IV infusion:
- Urinary Tract Infection: Mild to Moderate: 200 mg 12 hourly for 7-14 days; Severe or Complicated: 400 mg 12 hourly for 7-14 days
- Lower Respiratory Tract infection: Mild to Moderate: 400 mg 12 hourly for 7-14 days; Severe or Complicated: 400 mg 8 hourly for 7-14 days
- Nosocomial Pneumonia: Mild/Moderate/Severe: 400 mg 8 hourly for 10-14 days
- Skin and Skin Structure: Mild to Moderate: 400 mg 12 hourly for 7-14 days; Severe or Complicated: 400 mg 8 hourly for 7-14 days
- Bone and Joint Infection: Mild to Moderate: 400 mg 12 hourly for more than 4-6 weeks; Severe/Complicated: 400 mg 8 hourly for more than 4-6weeks
- Intraabdominal (Acute abdomen): Complicated: 400 mg 12 hourly for 7-14 days
- Acute Sinusitis: Mild/Moderate: 400 mg 12 hourly for 10 days
- Chronic Bacterial Prostatitis: Mild/Moderate: 400 mg 12 hourly for 28 Days.
AdministrationView
Instruction for the use of Ciprofloxacin IV infusion-
- Check the bag for minute leaks by squeezing the inner bag firmly. If leaks are found, or if seal is not intact, discard the solution.
- Do not use if the solution is cloudy or a precipitate is present.
- Do not use flexible bags in series connections.
- Close flow control clamp of administration set.
- Remove cover from port at bottom of bag.
- Insert piercing pin of administration set into port with a twisting motion until the pin is firmly seated.
- Suspend bag from hanger.
- Squeeze and release drip chamber to establish proper fluid level in chamber during infusion of Ciprofloxacin IV infusion.
- Open flow control clamp to expel air from set.Close clamp.
- Regulate rate of administration with flow control clamp
Side effectsView
Side effects include- nausea and other gastrointestinal disturbances, headache, dizziness, joint pain and skin rashes.
ContraindicationsView
It is contraindicated in patients who have known hypersensitivity to Ciprofloxacin or other quinolones.
PrecautionsView
Patients receiving Ciprofloxacin should be instructed to drink fluids liberally. It should be used with caution in patients with suspected or known CNS disorders such as epilepsy or other factors which predispose to seizures and convulsion. Avoid in patients with known QT prolongation, hypokalemia.
InteractionsView
Concurrent administration of Ciprofloxacin should be avoided with Magnesium or Aluminum containing antacids or sucralfate or with other products containing Calcium, Iron or Zinc. These products may be taken two hours after or six hours before Ciprofloxacin. Ciprofloxacin should not be taken concurrently with milk or other dairy products, since absorption of Ciprofloxacin may be significantly reduced. Dietary calcium is a part of a meal, however, does not significantly affect the absorption of Ciprofloxacin.
Pregnancy & lactationView
There are no adequate and well-controlled studies in pregnant women. Ciprofloxacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus and mother. Ciprofloxacin is excreted in human milk. Due to the potential risk of articular damage, Ciprofloxacin should not be used during lactation.
Pediatric usageView
Although effective in clinical trials, Ciprofloxacin is not a drug of first choice in pediatric population.
Overdose effectsView
Overdose following Ciprofloxacin administration may lead to seizures, hallucinations, confusion, abdominal discomfort, renal and hepatic impairment as well as crystalluria, haematuria, & reversible renal toxicity.
StorageView
Keep below 30°C temperature, protected from light & moisture. Keep out of the reach of children.
Newseas
Multivitamin & Cod Liver Oil
Newseas
Multivitamin & Cod Liver Oil
Indications
Vitamin deficiency
Indication detailsView
Multivitamin syrup with cod-liver oil is indicated for growing children-
- It helps in the development and proper functioning of their vital organs.
- It helps to prevent vitamin deficiency and restore lost vitality after illness, in case of lack of appetite or tiredness of growing children.
- It also increases immunity and helps to maintain healthy skin, hair, nail, teeth, bone, eye and nervous system.
- Increases the resistance against cough, cold, chest and bronchial troubles.
- Helps to optimize brain development.
- In adults it helps to treat and prevent chronic diseases like heart diseases, rheumatoid arthritis, COPD, cancer etc.
- In pregnant and nursing mother it helps in proper development of the baby.
Therapeutic classView
Specific combined vitamin preparations
PharmacologyView
This preparation contains 8 essential vitamins with Cod Liver Oil. This provides extra protection for the children. It ensures for getting enough vitamins for children that help them to be grown up strong & stay healthy. Cod Liver Oil contains Vitamin A, Vitamin D, EPA & DHA. Vitamin A is essential for the immune system, bone growth, night vision, cellular growth, testicular and ovarian function, Vitamin D is essential for the absorption and utilization of calcium, which is also required for skeletal growth. EPA and DHA; omega-3 fatty acids, which are converted in the body to produce prostaglandins that affect a wide variety of physiological processes due to their modulating effect on the action of hormones. Omega-3 fatty acids relieve the symptoms of osteoarthritis, rheumatoid arthritis which also enhances immune function and promotes healthy blood circulation. It is thought that EPA and DHA may reduce the risk of coronary heart disease. DHA seems essential for normal brain development in unborn babies.
DosageView
1-12 Months: 2.5 ml (½ teaspoon) daily
1-4 Years: 5 ml (1 teaspoon) daily
4 years up: 7.5 ml (1½ teaspoon) daily
Adult: 10 ml (2 teaspoons) daily.
This syrup can be taken with water or milk.
1-4 Years: 5 ml (1 teaspoon) daily
4 years up: 7.5 ml (1½ teaspoon) daily
Adult: 10 ml (2 teaspoons) daily.
This syrup can be taken with water or milk.
Side effectsView
Generally well tolerated. However, a few allergic reactions may be seen.
ContraindicationsView
This product is contraindicated in patients with a known hypersensitivity to any of the ingredients.
PrecautionsView
This medicine may accumulate in the body. So, should not be taken in overdose.
InteractionsView
Some drug interaction may occur with- Erythromycin, Conjugated estrogens, Sodium bicarbonate, Chloramphenicol etc.
Pregnancy & lactationView
Should be taken on physician's advice.
StorageView
Keep in cool and dry place and away from light. Keep away from children
NexCap
Esomeprazole
NexCap
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.
NexCap
Esomeprazole
NexCap
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.
Nexanib
Sorafenib Tosylate
Nexanib
Sorafenib Tosylate
Indications
Renal cell carcinoma
Indication detailsView
Hepatocellular Carcinoma: Sorafenib is indicated for the treatment of patients with unresectablehepatocellular carcinoma (HCC).
Renal Cell Carcinoma: Sorafenib is indicated for the treatment of patients with advanced renal cell carcinoma (RCC).
Renal Cell Carcinoma: Sorafenib is indicated for the treatment of patients with advanced renal cell carcinoma (RCC).
Therapeutic classView
Targeted Cancer Therapy
PharmacologyView
Sorafenib is a kinase inhibitor that decreases tumor cell proliferation in vitro. Sorafenib was shown to inhibit multiple intracellular (CRAF, BRAF and mutant BRAF) and cell surface kinases (KIT, FLT-3, RET, VEGFR-1, VEGFR-2, VEGFR-3, and PDGFR-ß). Several of these kinases are thought to be involved in tumor cell signaling, angiogenesis, and apoptosis. Sorafenib inhibited tumor growth and angiogenesis of human hepatocellular carcinoma and renal cell carcinoma, and several other human tumor xenografts in immunocompromised mice.
DosageView
Advanced renal cell carcinoma: 400 mg bid. May continue until patient is no longer responding or unacceptable toxicity occurs.
Hepatic Impairment: No safety data is available for use in patients with Child-Pugh C hepatic impairment.
Hepatic Impairment: No safety data is available for use in patients with Child-Pugh C hepatic impairment.
AdministrationView
Should be taken on an empty stomach. May be taken with a low or moderate fat meal. If the patient intends to have a high fat meal, sorafenib should be taken on an empty stomach at least 1 hr before or 2 hr after meals. Swallow whole, do not chew/crush.
Side effectsView
Rash and hand-foot skin reactions. Hypophosphataemia, hypertension, bleeding, tinnitus, depression and erectile dysfunction. Alopecia, pruritus, dry skin, erythema, acne, flushing, exfoliative dermatitis, hoarseness, GI disturbances, arthralgia, myalgia, asthenia, pain and peripheral neuropathy.
ContraindicationsView
Sorafenib is contraindicated in patients with known severe hypersensitivity to sorafenib or any other component of Sorafenib. Sorafenib in combination with carboplatin and paclitaxel is contraindicated in patients with squamous cell lung cancer
PrecautionsView
Interrupt teatment if patient develops cardiac infarction, ischaemia and/or bleeding fatalities. Regular monitoring of BP, CBC and platelet is recommended. Monitor INR in patients who are on treatment with warfarin. Adequate contraception should be used during and for at least 2 wk after stopping treatment. May need to discontinue treatment if severe or persistent hypertension occurs.
InteractionsView
Inducers of isoenzyme CYP3A4 e.g. carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampicin may decrease sorafenib plasma concentration. Coadmin with sorafenib may increase the plasma concentration of doxorubicin and irinotecan.
Pregnancy & lactationView
Pregnancy category D There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Overdose effectsView
There is no specific treatment for Sorafenib overdose. The highest dose of Sorafenib studied clinically is 800 mg twice daily. The adverse reactions observed at this dose were primarily diarrhea and dermatologic. No information is available on symptoms of acute overdose in animals because of the saturation of absorption in oral acute toxicity studies conducted in animals. In cases of suspected overdose, Sorafenib should be withheld and supportive care instituted.
StorageView
Store at 25° C.
Nexataf
Tenofovir Alafenamide
Nexataf
Tenofovir Alafenamide
Indications
Liver disease
Indication detailsView
Tenofovir Alafenamide is a hepatitis B virus (HBV) nucleoside analog reverse transcriptase inhibitor and is indicated for the treatment of chronic hepatitis B virus infection in adults with compensated liver disease.
Therapeutic classView
Hepatic viral infections (Hepatitis B)
PharmacologyView
Tenofovir alafenamide is a phosphonamidate prodrug of tenofovir (2'-deoxyadenosine monophosphate analog). Tenofovir alafenamide as a lipophilic cell-permeant compound enters primary hepatocytes by passive diffusion and by the hepatic uptake transporters OATP1B1 and OATP1B3. Tenofovir alafenamide is then converted to tenofovir through hydrolysis primarily by carboxylesterase 1 (CES1) in primary hepatocytes. Intracellular tenofovir is subsequently phosphorylated by cellular kinases to the pharmacologically active metabolite tenofovir diphosphate. Tenofovir diphosphate inhibits HBV replication through incorporation into viral DNA by the HBV reverse transcriptase, which results in DNA chain-termination.
Tenofovir diphosphate is a weak inhibitor of mammalian DNA polymerases that include mitochondrial DNA polymerase γ and there is no evidence of toxicity to mitochondria in cell culture.
Tenofovir diphosphate is a weak inhibitor of mammalian DNA polymerases that include mitochondrial DNA polymerase γ and there is no evidence of toxicity to mitochondria in cell culture.
DosageView
Testing Prior To Initiation Of Tenofovir Alafenamide: Prior to initiation of Tenofovir Alafenamide, patients should be tested for HIV-1 infection. Tenofovir Alafenamide alone should not be used in patients with HIV infection
It is recommended that serum creatinine, serum phosphorous, estimated creatinine clearance, urine glucose, and urine protein be assessed before initiating Tenofovir Alafenamide and during therapy in all patients as clinically appropriate
Recommended Dosage In Adults: The recommended dosage of Tenofovir Alafenamide is 25 mg (one tablet) taken orally once daily with food
It is recommended that serum creatinine, serum phosphorous, estimated creatinine clearance, urine glucose, and urine protein be assessed before initiating Tenofovir Alafenamide and during therapy in all patients as clinically appropriate
Recommended Dosage In Adults: The recommended dosage of Tenofovir Alafenamide is 25 mg (one tablet) taken orally once daily with food
Side effectsView
The following adverse reactions are discussed in other sections of the labeling:
- Lactic Acidosis/Severe Hepatomegaly with Steatosis
- Severe Acute Exacerbation of Hepatitis B
- New Onset or Worsening of Renal Impairment
ContraindicationsView
None
InteractionsView
Tenofovir is a substrate of P-glycoprotein (P-gp) and BCRP. Drugs that strongly affect P-gp and BCRP activity may lead to changes in Tenofovir absorption. Consult the full prescribing information prior to and during treatment for potential drug drug interactions.
Pregnancy & lactationView
Before you take Tenofovir Alafenamide, tell your healthcare provider about all of your medical conditions, including if you are pregnant or plan to become pregnant. It is not known if Tenofovir Alafenamide will harm your unborn baby. Tell your healthcare provider if you become pregnant during treatment with Tenofovir Alafenamide.
Pregnancy Registry: There is a pregnancy registry for women who take antiviral medicines during pregnancy. The purpose of this registry is to collect information about the health of you and your baby. Talk with your healthcare provider about how you can take part in this registry.
Pregnancy Registry: There is a pregnancy registry for women who take antiviral medicines during pregnancy. The purpose of this registry is to collect information about the health of you and your baby. Talk with your healthcare provider about how you can take part in this registry.
Pediatric usageView
Pediatric Use: Safety and effectiveness of Tenofovir Alafenamide in pediatric patients less than 18 years of age have not been established.
Geriatric Use: Clinical trials of Tenofovir Alafenamide did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.
Renal Impairment: No dosage adjustment of Tenofovir Alafenamide is required in patients with mild, moderate, or severe renal impairment. Tenofovir Alafenamide is not recommended in patients with end stage renal disease (estimated creatinine clearance below 15 mL per minute)
Hepatic Impairment: No dosage adjustment of Tenofovir Alafenamide is required in patients with mild hepatic impairment (Child-Pugh A). The safety and efficacy of Tenofovir Alafenamide in patients with decompensated cirrhosis (Child-Pugh B or C) have not been established; therefore Tenofovir Alafenamide is not recommended in patients with decompensated (Child-Pugh B or C) hepatic impairment
Geriatric Use: Clinical trials of Tenofovir Alafenamide did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.
Renal Impairment: No dosage adjustment of Tenofovir Alafenamide is required in patients with mild, moderate, or severe renal impairment. Tenofovir Alafenamide is not recommended in patients with end stage renal disease (estimated creatinine clearance below 15 mL per minute)
Hepatic Impairment: No dosage adjustment of Tenofovir Alafenamide is required in patients with mild hepatic impairment (Child-Pugh A). The safety and efficacy of Tenofovir Alafenamide in patients with decompensated cirrhosis (Child-Pugh B or C) have not been established; therefore Tenofovir Alafenamide is not recommended in patients with decompensated (Child-Pugh B or C) hepatic impairment
Overdose effectsView
If overdose occurs, monitor patient for evidence of toxicity. Treatment of overdosage with Tenofovir Alafenamide consists of general supportive measures including monitoring of vital signs as well as observation of the clinical status of the patient. Tenofovir is efficiently removed by hemodialysiswith an extraction coefficient of approximately 54%
StorageView
Store below 86°F (30°C). Keep in its original container. Keep the container tightly closed.
Nexcal-D
Calcium Carbonate [Coral source] + Vitamin D3
Nexcal-D
Calcium Carbonate [Coral source] + Vitamin D3
Indications
Rickets
Indication detailsView
This is indicated for the treatment & prevention of osteoporosis, osteomalacia, tetany, hypoparathyroidism, disorders of osteogenesis. Also used as supplement in case of inadequate intake of Calcium in childhood diet, rickets, pregnancy & lactation, elderly patients. Other indications include pancreatitis, phosphate binder in chronic renal failure etc.
Therapeutic classView
Specific mineral & vitamin combined preparations
PharmacologyView
This is a Calcium and Vitamin D3 preparation where Calcium Carbonate is sourced from coral origin. The Calcium Carbonate from Coral has a chemical structure that is very similar to the composition of human bone. Coral Calcium is similar to other sources but ensures better absorption. Vitamin D3 aids in the absorption of Calcium from GI tract and helps to maintain Calcium balance in the body.
DosageView
One tablet once or twice daily with plenty of water or as directed by the physician. Taking in full stomach ensures better absorption.
Side effectsView
Flatulence, diarrhoea, constipation, upper GI discomfort etc. are rare manifestation. Hypercalcaemia due to prolong use has rarely been reported.
ContraindicationsView
Hypersensitivity to any of the components, hypocalcaemia resulting from overdose of Vitamin D3, hyperparathyroidism, bone metastases, severe renal insufficiency, severe hypercalciuria, renal calculi etc.
PrecautionsView
In presence of mild hypercalciuria, careful monitoring with reduction of dose may be needed. Plasma and serum Calcium level should be monitored in mild to moderate renal impairment and also in case of long-term use. Patients with renal stones or with such previous history should also take precautions.
InteractionsView
Oral Calcium can reduce the absorption of tetracycline & fluoride preparations and minimum 3 hours time should be allowed between ingestion of these medications. Thiazide diuretics reduces the renal excretion of Calcium. Phenytoin, barbiturates, glucocorticoids may induce metabolism of Vitamin D3. Concomitant ingestion of certain foods like spinach, cereals, milk and its derivatives may reduce the intestinal uptake of Calcium.
Pregnancy & lactationView
This can be given to pregnant and lactating mothers as per recommendation of physician.
Overdose effectsView
At high doses it may result in nausea, vomiting, dizziness, anorexia, abdominal cramps, headache, constipation, irritability etc. Treatment includes cessation of therapy and adequate rehydration.
StorageView
Store at temperature of below 30°C, protect from light & moisture. Keep out of reach of children.
Nexcital
Escitalopram Oxalate
Nexcital
Escitalopram Oxalate
Indications
Trichotillomania
Indication detailsView
Escitalopram Oxalate is indicated in the-
- Treatment of major depressive episodes.
- Treatment of panic disorder with or without agoraphobia.
- Treatment of social anxiety disorder (social phobia).
- Treatment of generalised anxiety disorder.
- Treatment of obsessive-compulsive disorder.
Therapeutic classView
SSRIs & related anti-depressant drugs
PharmacologyView
Escitalopram is an orally administered selective serotonin reuptake inhibitor (SSRI). Escitalopram is the pure S-enantiomer of the racemic bicyclic phthalate derivative citalopram. Escitalopram is at least 100 fold more potent than the R-enantiomer with respect to inhibition of 5-HT reuptake. Escitalopram has no or very low affinity for serotonergic or other receptors including alpha- and beta-adrenergic Dopamine, Histamine, Muscarinic and benzodiazepine receptors.
DosageView
Safety of daily doses above 20 mg has not been demonstrated. Escitalopram Oxalate is administered as a single daily dose and may be taken with or without food.
Major depressive episodes: Usual dosage is 10 mg once daily. Depending on individual patient response, the dose may be increased to a maximum of 20 mg daily. Usually, 2-4 weeks are necessary to obtain an antidepressant response. After the symptoms resolve, treatment for at least 6 months is required for consolidation of the response.
Panic disorder with or without agoraphobia: An initial dose of 5 mg is recommended for the first week before increasing the dose to 10 mg daily. The dose may be further increased, up to a maximum of 20 mg daily, dependent on individual patient response. Maximum effectiveness is reached after about 3 months. The treatment lasts several months.
Social anxiety disorder: Usual dosage is 10 mg once daily. Usually, 2-4 weeks are necessary to obtain symptom relief. The dose may subsequently, depending on individual patient response, be decreased to 5 mg or increased to a maximum of 20 mg daily. Social anxiety disorder is a disease with a chronic course, and treatment for 12 weeks is recommended to consolidate response. Long-term treatment of responders has been studied for 6 months and can be considered on an individual basis to prevent relapse; treatment benefits should be re-evaluated at regular intervals. Social anxiety disorder is a well-defined diagnostic terminology of a specific disorder, which should not be confounded with excessive shyness. Pharmacotherapy is only indicated if the disorder interferes significantly with professional and social activities. The place of this treatment compared to cognitive behavioural therapy has not been assessed. Pharmacotherapy is part of an overall therapeutic strategy.
Generalised anxiety disorder: Initial dosage is 10 mg once daily. Depending on the individual patient response, the dose may be increased to a maximum of 20 mg daily. Long term treatment of responders has been studied for at least 6 months in patients receiving 20 mg/day. Treatment benefits and dose should be re-evaluated at regular intervals.
Obsessive-Compulsive Disorder: Initial dosage is 10 mg once daily. Depending on the individual patient response, the dose may be increased to a maximum of 20 mg daily. As OCD is a chronic disease, patients should be treated for a sufficient period to ensure that they are symptom-free. Treatment benefits and dose should be re-evaluated at regular intervals.
Major depressive episodes: Usual dosage is 10 mg once daily. Depending on individual patient response, the dose may be increased to a maximum of 20 mg daily. Usually, 2-4 weeks are necessary to obtain an antidepressant response. After the symptoms resolve, treatment for at least 6 months is required for consolidation of the response.
Panic disorder with or without agoraphobia: An initial dose of 5 mg is recommended for the first week before increasing the dose to 10 mg daily. The dose may be further increased, up to a maximum of 20 mg daily, dependent on individual patient response. Maximum effectiveness is reached after about 3 months. The treatment lasts several months.
Social anxiety disorder: Usual dosage is 10 mg once daily. Usually, 2-4 weeks are necessary to obtain symptom relief. The dose may subsequently, depending on individual patient response, be decreased to 5 mg or increased to a maximum of 20 mg daily. Social anxiety disorder is a disease with a chronic course, and treatment for 12 weeks is recommended to consolidate response. Long-term treatment of responders has been studied for 6 months and can be considered on an individual basis to prevent relapse; treatment benefits should be re-evaluated at regular intervals. Social anxiety disorder is a well-defined diagnostic terminology of a specific disorder, which should not be confounded with excessive shyness. Pharmacotherapy is only indicated if the disorder interferes significantly with professional and social activities. The place of this treatment compared to cognitive behavioural therapy has not been assessed. Pharmacotherapy is part of an overall therapeutic strategy.
Generalised anxiety disorder: Initial dosage is 10 mg once daily. Depending on the individual patient response, the dose may be increased to a maximum of 20 mg daily. Long term treatment of responders has been studied for at least 6 months in patients receiving 20 mg/day. Treatment benefits and dose should be re-evaluated at regular intervals.
Obsessive-Compulsive Disorder: Initial dosage is 10 mg once daily. Depending on the individual patient response, the dose may be increased to a maximum of 20 mg daily. As OCD is a chronic disease, patients should be treated for a sufficient period to ensure that they are symptom-free. Treatment benefits and dose should be re-evaluated at regular intervals.
AdministrationView
Escitalopram should generally be administered once daily, morning or evening with or without food.
Side effectsView
SSRIs are less sedating and have fewer antimuscarinic and cardiotoxic effects than tricyclic antidepressants. Side-effects of the SSRIs include gastrointestinal effects (dose-related and fairly common include nausea, vomiting, dyspepsia, abdominal pain, diarrhoea, constipation), anorexia with weight loss (increased appetite and weight gain also reported) and hypersensitivity reactions including rash, urticaria, angioedema, anaphylaxis, arthralgia, myalgia, and photosensitivity; other side-effects include dry mouth, nervousness, anxiety, headache, insomnia, tremor, dizziness, asthenia, hallucinations, drowsiness, convulsions, galactorrhoea, sexual dysfunction, urinary retention, sweating, hypomania or mania, movement disorders and dyskinesias, visual disturbances.
ContraindicationsView
Escitalopram is contraindicated in patients with known hypersensitivity to Escitalopram or Citalopram or any of the inactive ingredients of the drug product. Concomitant use of escitalopram in patients taking monoamine oxidase/pimozide is contraindicated.
PrecautionsView
SSRIs should be used with caution in patients with epilepsy (avoid if poorly controlled, discontinue if convulsions develop), concurrent electroconvulsive therapy (prolonged seizures reported with fluoxetine), history of mania, cardiac disease, diabetes mellitus, angle-closure glaucoma, concomitant use of drugs that increase risk of bleeding, history of bleeding disorders (especially gastro-lntestinal bleeding), hepatic and renal impairment.
InteractionsView
As SSRI or related antidepressants should not be started until 2 weeks after stopping an MAOI. Conversely, an MAOI should not. be started until at least a week after an SSRI or related antidepressant has been stopped (2 weeks in the case of paroxetine and sertraline, at least 5 weeks in the case of fluoxetine).
Pregnancy & lactationView
When treating a pregnant woman with Escitalopram during the third trimester, the physician should carefully consider the potential risks and benefits of treatment. It is excreted in human breast milk. The decision whether to continue or discontinue either nursing or Escitalopram therapy should take into account the risk of citalopram exposure for the infant and the benefits Escitalopram treatment for the mother.
Pediatric usageView
Elderly patients (>65 years of age): Initial dosage is 5 mg once daily. Depending on the individual patient response the dose may be increased to 10 mg daily. The efficacy of escitalopram in social anxiety disorder has not been studied in elderly patients.
Children and adolescents (<18 years): Escitalopram Oxalate should not be used in the treatment of children and adolescents under the age of 18 years.
Reduced renal function: Dosage adjustment is not necessary in patients with mild or moderate renal impairment. Caution is advised in patients with severely reduced renal function (CLCR less than 30 ml/min).
Reduced hepatic function: An initial dose of 5 mg daily for the first two weeks of treatment is recommended in patients with mild or moderate hepatic impairment. Depending on individual patient response, the dose may be increased to 10 mg daily. Caution and extra careful dose titration is advised in patients with severely reduced hepatic function.
Poor metabolizers of CYP2C19: For patients who are known to be poor metabolisers with respect to CYP2C19, an initial dose of 5 mg daily during the first two weeks of treatment is recommended. Depending on individual patient response, the dose may be increased to 10 mg daily. Discontinuation symptoms seen when stopping treatment. Abrupt discontinuation should be avoided.
When stopping treatment with escitalopram the dose should be gradually reduced over a period of at least one to two weeks in order to reduce the risk of discontinuation symptoms. If intolerable symptoms occur following a decrease in the dose or upon discontinuation of treatment, then resuming the previously prescribed dose may be considered. Subsequently, the physician may continue decreasing the dose, but at a more gradual rate.
Children and adolescents (<18 years): Escitalopram Oxalate should not be used in the treatment of children and adolescents under the age of 18 years.
Reduced renal function: Dosage adjustment is not necessary in patients with mild or moderate renal impairment. Caution is advised in patients with severely reduced renal function (CLCR less than 30 ml/min).
Reduced hepatic function: An initial dose of 5 mg daily for the first two weeks of treatment is recommended in patients with mild or moderate hepatic impairment. Depending on individual patient response, the dose may be increased to 10 mg daily. Caution and extra careful dose titration is advised in patients with severely reduced hepatic function.
Poor metabolizers of CYP2C19: For patients who are known to be poor metabolisers with respect to CYP2C19, an initial dose of 5 mg daily during the first two weeks of treatment is recommended. Depending on individual patient response, the dose may be increased to 10 mg daily. Discontinuation symptoms seen when stopping treatment. Abrupt discontinuation should be avoided.
When stopping treatment with escitalopram the dose should be gradually reduced over a period of at least one to two weeks in order to reduce the risk of discontinuation symptoms. If intolerable symptoms occur following a decrease in the dose or upon discontinuation of treatment, then resuming the previously prescribed dose may be considered. Subsequently, the physician may continue decreasing the dose, but at a more gradual rate.
Overdose effectsView
Symptoms: Symptoms seen in a reported overdose of escitalopram include symptoms mainly related to the central nervous system (ranging from dizziness, tremor, and agitation to rare cases of serotonin syndrome, convulsion, and coma), the gastrointestinal system (nausea/vomiting), and the cardiovascular system (hypotension, tachycardia, QT interval, prolongation, and arrhythmia) and electrolyte/fluid balance conditions (hypokalaemia, hyponatremia).
Management: There is no specific antidote. Establish and maintain an airway, ensure adequate oxygenation and respiratory function. Gastric lavage and the use of activated charcoal should be considered. Gastric lavage should be carried out as soon as possible after oral ingestion. Cardiac and vital signs monitoring are recommended along with general symptomatic supportive measures. ECG monitoring is advised in case of overdose, in patients with congestive heart failure/bradyarrhythmias, in patients using concomitant medications that prolong the QT-interval, or in patients with altered metabolism, e.g. liver impairment.
Management: There is no specific antidote. Establish and maintain an airway, ensure adequate oxygenation and respiratory function. Gastric lavage and the use of activated charcoal should be considered. Gastric lavage should be carried out as soon as possible after oral ingestion. Cardiac and vital signs monitoring are recommended along with general symptomatic supportive measures. ECG monitoring is advised in case of overdose, in patients with congestive heart failure/bradyarrhythmias, in patients using concomitant medications that prolong the QT-interval, or in patients with altered metabolism, e.g. liver impairment.
StorageView
Store below 30°C temperature and protect from light & moisture. Keep the medicine out of the reach of children.
Nexcital
Escitalopram Oxalate
Nexcital
Escitalopram Oxalate
Indications
Trichotillomania
Indication detailsView
Escitalopram Oxalate is indicated in the-
- Treatment of major depressive episodes.
- Treatment of panic disorder with or without agoraphobia.
- Treatment of social anxiety disorder (social phobia).
- Treatment of generalised anxiety disorder.
- Treatment of obsessive-compulsive disorder.
Therapeutic classView
SSRIs & related anti-depressant drugs
PharmacologyView
Escitalopram is an orally administered selective serotonin reuptake inhibitor (SSRI). Escitalopram is the pure S-enantiomer of the racemic bicyclic phthalate derivative citalopram. Escitalopram is at least 100 fold more potent than the R-enantiomer with respect to inhibition of 5-HT reuptake. Escitalopram has no or very low affinity for serotonergic or other receptors including alpha- and beta-adrenergic Dopamine, Histamine, Muscarinic and benzodiazepine receptors.
DosageView
Safety of daily doses above 20 mg has not been demonstrated. Escitalopram Oxalate is administered as a single daily dose and may be taken with or without food.
Major depressive episodes: Usual dosage is 10 mg once daily. Depending on individual patient response, the dose may be increased to a maximum of 20 mg daily. Usually, 2-4 weeks are necessary to obtain an antidepressant response. After the symptoms resolve, treatment for at least 6 months is required for consolidation of the response.
Panic disorder with or without agoraphobia: An initial dose of 5 mg is recommended for the first week before increasing the dose to 10 mg daily. The dose may be further increased, up to a maximum of 20 mg daily, dependent on individual patient response. Maximum effectiveness is reached after about 3 months. The treatment lasts several months.
Social anxiety disorder: Usual dosage is 10 mg once daily. Usually, 2-4 weeks are necessary to obtain symptom relief. The dose may subsequently, depending on individual patient response, be decreased to 5 mg or increased to a maximum of 20 mg daily. Social anxiety disorder is a disease with a chronic course, and treatment for 12 weeks is recommended to consolidate response. Long-term treatment of responders has been studied for 6 months and can be considered on an individual basis to prevent relapse; treatment benefits should be re-evaluated at regular intervals. Social anxiety disorder is a well-defined diagnostic terminology of a specific disorder, which should not be confounded with excessive shyness. Pharmacotherapy is only indicated if the disorder interferes significantly with professional and social activities. The place of this treatment compared to cognitive behavioural therapy has not been assessed. Pharmacotherapy is part of an overall therapeutic strategy.
Generalised anxiety disorder: Initial dosage is 10 mg once daily. Depending on the individual patient response, the dose may be increased to a maximum of 20 mg daily. Long term treatment of responders has been studied for at least 6 months in patients receiving 20 mg/day. Treatment benefits and dose should be re-evaluated at regular intervals.
Obsessive-Compulsive Disorder: Initial dosage is 10 mg once daily. Depending on the individual patient response, the dose may be increased to a maximum of 20 mg daily. As OCD is a chronic disease, patients should be treated for a sufficient period to ensure that they are symptom-free. Treatment benefits and dose should be re-evaluated at regular intervals.
Major depressive episodes: Usual dosage is 10 mg once daily. Depending on individual patient response, the dose may be increased to a maximum of 20 mg daily. Usually, 2-4 weeks are necessary to obtain an antidepressant response. After the symptoms resolve, treatment for at least 6 months is required for consolidation of the response.
Panic disorder with or without agoraphobia: An initial dose of 5 mg is recommended for the first week before increasing the dose to 10 mg daily. The dose may be further increased, up to a maximum of 20 mg daily, dependent on individual patient response. Maximum effectiveness is reached after about 3 months. The treatment lasts several months.
Social anxiety disorder: Usual dosage is 10 mg once daily. Usually, 2-4 weeks are necessary to obtain symptom relief. The dose may subsequently, depending on individual patient response, be decreased to 5 mg or increased to a maximum of 20 mg daily. Social anxiety disorder is a disease with a chronic course, and treatment for 12 weeks is recommended to consolidate response. Long-term treatment of responders has been studied for 6 months and can be considered on an individual basis to prevent relapse; treatment benefits should be re-evaluated at regular intervals. Social anxiety disorder is a well-defined diagnostic terminology of a specific disorder, which should not be confounded with excessive shyness. Pharmacotherapy is only indicated if the disorder interferes significantly with professional and social activities. The place of this treatment compared to cognitive behavioural therapy has not been assessed. Pharmacotherapy is part of an overall therapeutic strategy.
Generalised anxiety disorder: Initial dosage is 10 mg once daily. Depending on the individual patient response, the dose may be increased to a maximum of 20 mg daily. Long term treatment of responders has been studied for at least 6 months in patients receiving 20 mg/day. Treatment benefits and dose should be re-evaluated at regular intervals.
Obsessive-Compulsive Disorder: Initial dosage is 10 mg once daily. Depending on the individual patient response, the dose may be increased to a maximum of 20 mg daily. As OCD is a chronic disease, patients should be treated for a sufficient period to ensure that they are symptom-free. Treatment benefits and dose should be re-evaluated at regular intervals.
AdministrationView
Escitalopram should generally be administered once daily, morning or evening with or without food.
Side effectsView
SSRIs are less sedating and have fewer antimuscarinic and cardiotoxic effects than tricyclic antidepressants. Side-effects of the SSRIs include gastrointestinal effects (dose-related and fairly common include nausea, vomiting, dyspepsia, abdominal pain, diarrhoea, constipation), anorexia with weight loss (increased appetite and weight gain also reported) and hypersensitivity reactions including rash, urticaria, angioedema, anaphylaxis, arthralgia, myalgia, and photosensitivity; other side-effects include dry mouth, nervousness, anxiety, headache, insomnia, tremor, dizziness, asthenia, hallucinations, drowsiness, convulsions, galactorrhoea, sexual dysfunction, urinary retention, sweating, hypomania or mania, movement disorders and dyskinesias, visual disturbances.
ContraindicationsView
Escitalopram is contraindicated in patients with known hypersensitivity to Escitalopram or Citalopram or any of the inactive ingredients of the drug product. Concomitant use of escitalopram in patients taking monoamine oxidase/pimozide is contraindicated.
PrecautionsView
SSRIs should be used with caution in patients with epilepsy (avoid if poorly controlled, discontinue if convulsions develop), concurrent electroconvulsive therapy (prolonged seizures reported with fluoxetine), history of mania, cardiac disease, diabetes mellitus, angle-closure glaucoma, concomitant use of drugs that increase risk of bleeding, history of bleeding disorders (especially gastro-lntestinal bleeding), hepatic and renal impairment.
InteractionsView
As SSRI or related antidepressants should not be started until 2 weeks after stopping an MAOI. Conversely, an MAOI should not. be started until at least a week after an SSRI or related antidepressant has been stopped (2 weeks in the case of paroxetine and sertraline, at least 5 weeks in the case of fluoxetine).
Pregnancy & lactationView
When treating a pregnant woman with Escitalopram during the third trimester, the physician should carefully consider the potential risks and benefits of treatment. It is excreted in human breast milk. The decision whether to continue or discontinue either nursing or Escitalopram therapy should take into account the risk of citalopram exposure for the infant and the benefits Escitalopram treatment for the mother.
Pediatric usageView
Elderly patients (>65 years of age): Initial dosage is 5 mg once daily. Depending on the individual patient response the dose may be increased to 10 mg daily. The efficacy of escitalopram in social anxiety disorder has not been studied in elderly patients.
Children and adolescents (<18 years): Escitalopram Oxalate should not be used in the treatment of children and adolescents under the age of 18 years.
Reduced renal function: Dosage adjustment is not necessary in patients with mild or moderate renal impairment. Caution is advised in patients with severely reduced renal function (CLCR less than 30 ml/min).
Reduced hepatic function: An initial dose of 5 mg daily for the first two weeks of treatment is recommended in patients with mild or moderate hepatic impairment. Depending on individual patient response, the dose may be increased to 10 mg daily. Caution and extra careful dose titration is advised in patients with severely reduced hepatic function.
Poor metabolizers of CYP2C19: For patients who are known to be poor metabolisers with respect to CYP2C19, an initial dose of 5 mg daily during the first two weeks of treatment is recommended. Depending on individual patient response, the dose may be increased to 10 mg daily. Discontinuation symptoms seen when stopping treatment. Abrupt discontinuation should be avoided.
When stopping treatment with escitalopram the dose should be gradually reduced over a period of at least one to two weeks in order to reduce the risk of discontinuation symptoms. If intolerable symptoms occur following a decrease in the dose or upon discontinuation of treatment, then resuming the previously prescribed dose may be considered. Subsequently, the physician may continue decreasing the dose, but at a more gradual rate.
Children and adolescents (<18 years): Escitalopram Oxalate should not be used in the treatment of children and adolescents under the age of 18 years.
Reduced renal function: Dosage adjustment is not necessary in patients with mild or moderate renal impairment. Caution is advised in patients with severely reduced renal function (CLCR less than 30 ml/min).
Reduced hepatic function: An initial dose of 5 mg daily for the first two weeks of treatment is recommended in patients with mild or moderate hepatic impairment. Depending on individual patient response, the dose may be increased to 10 mg daily. Caution and extra careful dose titration is advised in patients with severely reduced hepatic function.
Poor metabolizers of CYP2C19: For patients who are known to be poor metabolisers with respect to CYP2C19, an initial dose of 5 mg daily during the first two weeks of treatment is recommended. Depending on individual patient response, the dose may be increased to 10 mg daily. Discontinuation symptoms seen when stopping treatment. Abrupt discontinuation should be avoided.
When stopping treatment with escitalopram the dose should be gradually reduced over a period of at least one to two weeks in order to reduce the risk of discontinuation symptoms. If intolerable symptoms occur following a decrease in the dose or upon discontinuation of treatment, then resuming the previously prescribed dose may be considered. Subsequently, the physician may continue decreasing the dose, but at a more gradual rate.
Overdose effectsView
Symptoms: Symptoms seen in a reported overdose of escitalopram include symptoms mainly related to the central nervous system (ranging from dizziness, tremor, and agitation to rare cases of serotonin syndrome, convulsion, and coma), the gastrointestinal system (nausea/vomiting), and the cardiovascular system (hypotension, tachycardia, QT interval, prolongation, and arrhythmia) and electrolyte/fluid balance conditions (hypokalaemia, hyponatremia).
Management: There is no specific antidote. Establish and maintain an airway, ensure adequate oxygenation and respiratory function. Gastric lavage and the use of activated charcoal should be considered. Gastric lavage should be carried out as soon as possible after oral ingestion. Cardiac and vital signs monitoring are recommended along with general symptomatic supportive measures. ECG monitoring is advised in case of overdose, in patients with congestive heart failure/bradyarrhythmias, in patients using concomitant medications that prolong the QT-interval, or in patients with altered metabolism, e.g. liver impairment.
Management: There is no specific antidote. Establish and maintain an airway, ensure adequate oxygenation and respiratory function. Gastric lavage and the use of activated charcoal should be considered. Gastric lavage should be carried out as soon as possible after oral ingestion. Cardiac and vital signs monitoring are recommended along with general symptomatic supportive measures. ECG monitoring is advised in case of overdose, in patients with congestive heart failure/bradyarrhythmias, in patients using concomitant medications that prolong the QT-interval, or in patients with altered metabolism, e.g. liver impairment.
StorageView
Store below 30°C temperature and protect from light & moisture. Keep the medicine out of the reach of children.
Nexdex
Dexlansoprazole
Nexdex
Dexlansoprazole
Indications
Oesophagitis
Indication detailsView
Healing of Erosive Esophagitis: Dexlansoprazole is indicated for the healing of all grades of erosive esophagitis (EE) for up to 8 weeks.
Maintenance of Healed Erosive Esophagitis: Dexlansoprazole is indicated to maintain healing of EE and relief of heartburn for up to 6 months.
Symptomatic Non-Erosive Gastroesophageal Reflux Disease: Dexlansoprazole is indicated for the treatment of heartburn associated with symptomatic non-erosive Gastroesophageal Reflux Disease (GERD) for 4 weeks.
Maintenance of Healed Erosive Esophagitis: Dexlansoprazole is indicated to maintain healing of EE and relief of heartburn for up to 6 months.
Symptomatic Non-Erosive Gastroesophageal Reflux Disease: Dexlansoprazole is indicated for the treatment of heartburn associated with symptomatic non-erosive Gastroesophageal Reflux Disease (GERD) for 4 weeks.
Therapeutic classView
Proton Pump Inhibitor
PharmacologyView
Dexlansoprazole delayed-release capsule is a Proton Pump Inhibitor (PPI) which suppresses gastric acid secretion by specific inhibition of the (H+/K+)-ATPase in the gastric parietal cell. By acting specifically on the proton pump, Dexlansoprazole blocks the final step of acid production. It is the R-enantiomer of lansoprazole (A racemic mixture of the R- and S-enantiomers). Dexlansoprazole is supplied as a Dual Delayed Release (DDR) formulation in a capsule for oral administration. This capsule contains a mixture of two types of enteric coated granules with different pH-dependent dissolution profiles. The dual delayed release formulation in dexlansoprazole, plasma concentration-time profile with two distinct peaks; the first peak occurs 1 to 2 hours after administration, followed by a second peak within 4 to 5 hours. After oral administration, mean Cmax and AUC value of Dexlansoprazole increased approximately dose proportionally. Dexlansoprazole is extensively metabolized in the liver and excreated by urine.
DosageView
Dexlansoprazole dosing recommendations-
- Maintenance of Healed erosive esophagitis and relief of heartburn: 30 mg Once daily
- Symptomatic Non-Erosive GERD: 30 mg Once daily for 4 weeks
- Healing of erosive esophagitis: 60 mg Once daily for up to 8 weeks
AdministrationView
Dexlansoprazole can be taken without regard to food. It should be swallowed whole.
Alternatively, Dexlansoprazole capsules can be administered as follows:
If a capsule is missed at its usual time, it should be taken as soon as possible. But if it is too close to the time of the next dose, only the prescribed dose should be taken at the appointed time. A double dose should not be taken.
Alternatively, Dexlansoprazole capsules can be administered as follows:
- Open capsule
- Sprinkle intact granules on one tablespoon
- Swallow immediately.
If a capsule is missed at its usual time, it should be taken as soon as possible. But if it is too close to the time of the next dose, only the prescribed dose should be taken at the appointed time. A double dose should not be taken.
Side effectsView
Common side effects: Diarrhea, abdominal pain, nausea, vomiting & flatulence.
ContraindicationsView
Dexlansoprazole is contraindicated in patients with known hypersensitivity to any component of the formulation.
PrecautionsView
Gastric Malignancy, Clostridium difficile Associated Diarrhea, Bone fracture, Hypomagnesemia, and concomitant use of Dexlansoprazole with Methotrexate.
InteractionsView
With medicine: Atazanavir, Warfarin, Tacrolimus, Clopidogrel & Methotrexate. With food & others: No data available.
Pregnancy & lactationView
Pregnancy Category B. There is no adequate and well-controlled studies with Dexlansoprazole in pregnant women. There is no adequate and well-controlled studies with Dexlansoprazole in Lactating mother.
Pediatric usageView
Use in children & adolescents: Safety and effectiveness of Dexlansoprazole in patients below 12 years age have not been established.
Geriatric use: No dose adjustment is necessary for elderly patients.
Renal impairment: No dose adjustment of Dexlansoprazole is necessary for patients with renal
impairment.
Hepatic impairment: No dose adjustment for Dexlansoprazole is necessary for patients with mild hepatic impairment. A maximum daily dose of Dexlansoprazole 30 mg should be considered for patients with moderate hepatic impairment.
Geriatric use: No dose adjustment is necessary for elderly patients.
Renal impairment: No dose adjustment of Dexlansoprazole is necessary for patients with renal
impairment.
Hepatic impairment: No dose adjustment for Dexlansoprazole is necessary for patients with mild hepatic impairment. A maximum daily dose of Dexlansoprazole 30 mg should be considered for patients with moderate hepatic impairment.
Overdose effectsView
There have been no reports of a significant overdose of Dexlansoprazole. Multiple doses of Dexlansoprazole 120 mg and a single dose of Dexlansoprazole 300 mg did not result in death or other severe adverse events.
StorageView
Store below 30°C temperature & in a dry place, protected from light. Keep all medicines out of reach of children.
Nexdex
Dexlansoprazole
Nexdex
Dexlansoprazole
Indications
Oesophagitis
Indication detailsView
Healing of Erosive Esophagitis: Dexlansoprazole is indicated for the healing of all grades of erosive esophagitis (EE) for up to 8 weeks.
Maintenance of Healed Erosive Esophagitis: Dexlansoprazole is indicated to maintain healing of EE and relief of heartburn for up to 6 months.
Symptomatic Non-Erosive Gastroesophageal Reflux Disease: Dexlansoprazole is indicated for the treatment of heartburn associated with symptomatic non-erosive Gastroesophageal Reflux Disease (GERD) for 4 weeks.
Maintenance of Healed Erosive Esophagitis: Dexlansoprazole is indicated to maintain healing of EE and relief of heartburn for up to 6 months.
Symptomatic Non-Erosive Gastroesophageal Reflux Disease: Dexlansoprazole is indicated for the treatment of heartburn associated with symptomatic non-erosive Gastroesophageal Reflux Disease (GERD) for 4 weeks.
Therapeutic classView
Proton Pump Inhibitor
PharmacologyView
Dexlansoprazole delayed-release capsule is a Proton Pump Inhibitor (PPI) which suppresses gastric acid secretion by specific inhibition of the (H+/K+)-ATPase in the gastric parietal cell. By acting specifically on the proton pump, Dexlansoprazole blocks the final step of acid production. It is the R-enantiomer of lansoprazole (A racemic mixture of the R- and S-enantiomers). Dexlansoprazole is supplied as a Dual Delayed Release (DDR) formulation in a capsule for oral administration. This capsule contains a mixture of two types of enteric coated granules with different pH-dependent dissolution profiles. The dual delayed release formulation in dexlansoprazole, plasma concentration-time profile with two distinct peaks; the first peak occurs 1 to 2 hours after administration, followed by a second peak within 4 to 5 hours. After oral administration, mean Cmax and AUC value of Dexlansoprazole increased approximately dose proportionally. Dexlansoprazole is extensively metabolized in the liver and excreated by urine.
DosageView
Dexlansoprazole dosing recommendations-
- Maintenance of Healed erosive esophagitis and relief of heartburn: 30 mg Once daily
- Symptomatic Non-Erosive GERD: 30 mg Once daily for 4 weeks
- Healing of erosive esophagitis: 60 mg Once daily for up to 8 weeks
AdministrationView
Dexlansoprazole can be taken without regard to food. It should be swallowed whole.
Alternatively, Dexlansoprazole capsules can be administered as follows:
If a capsule is missed at its usual time, it should be taken as soon as possible. But if it is too close to the time of the next dose, only the prescribed dose should be taken at the appointed time. A double dose should not be taken.
Alternatively, Dexlansoprazole capsules can be administered as follows:
- Open capsule
- Sprinkle intact granules on one tablespoon
- Swallow immediately.
If a capsule is missed at its usual time, it should be taken as soon as possible. But if it is too close to the time of the next dose, only the prescribed dose should be taken at the appointed time. A double dose should not be taken.
Side effectsView
Common side effects: Diarrhea, abdominal pain, nausea, vomiting & flatulence.
ContraindicationsView
Dexlansoprazole is contraindicated in patients with known hypersensitivity to any component of the formulation.
PrecautionsView
Gastric Malignancy, Clostridium difficile Associated Diarrhea, Bone fracture, Hypomagnesemia, and concomitant use of Dexlansoprazole with Methotrexate.
InteractionsView
With medicine: Atazanavir, Warfarin, Tacrolimus, Clopidogrel & Methotrexate. With food & others: No data available.
Pregnancy & lactationView
Pregnancy Category B. There is no adequate and well-controlled studies with Dexlansoprazole in pregnant women. There is no adequate and well-controlled studies with Dexlansoprazole in Lactating mother.
Pediatric usageView
Use in children & adolescents: Safety and effectiveness of Dexlansoprazole in patients below 12 years age have not been established.
Geriatric use: No dose adjustment is necessary for elderly patients.
Renal impairment: No dose adjustment of Dexlansoprazole is necessary for patients with renal
impairment.
Hepatic impairment: No dose adjustment for Dexlansoprazole is necessary for patients with mild hepatic impairment. A maximum daily dose of Dexlansoprazole 30 mg should be considered for patients with moderate hepatic impairment.
Geriatric use: No dose adjustment is necessary for elderly patients.
Renal impairment: No dose adjustment of Dexlansoprazole is necessary for patients with renal
impairment.
Hepatic impairment: No dose adjustment for Dexlansoprazole is necessary for patients with mild hepatic impairment. A maximum daily dose of Dexlansoprazole 30 mg should be considered for patients with moderate hepatic impairment.
Overdose effectsView
There have been no reports of a significant overdose of Dexlansoprazole. Multiple doses of Dexlansoprazole 120 mg and a single dose of Dexlansoprazole 300 mg did not result in death or other severe adverse events.
StorageView
Store below 30°C temperature & in a dry place, protected from light. Keep all medicines out of reach of children.
Nexe
Esomeprazole
Nexe
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.
Nexe
Esomeprazole
Nexe
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.