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Serelam

Alprazolam

Tablet 0.5 mg Allopathic Benzodiazepine sedatives

Indications

Vestibular neuritis

Indication detailsView

Alprazolam is indicated in-

Anxiety disorder
Short term relief of anxiety
Anxiety associated with depression
Panic disorder, with or without agoraphobia.

Therapeutic classView

Benzodiazepine sedatives

PharmacologyView

Alprazolam is a triazole analog of the 1,4-benzodiazepine class of drugs. It is an anxiolytic with hypnotic and anticonvulsive properties. Alprazolam is presumed to produce its effects via interacting with the Gamma Aminobutyric Acid (GABA)- benzodiazepine receptor complex. Like all benzodiazepines, it causes a dose-related CNS depressant activity varying from mild impairment of task performance to hypnosis.

DosageView

Treatment should be initiated with a dose of 0.25 to 0.5 mg three times daily. Depending on the response, dose may be increased at intervals of 3 to 4 days in increments of no more than 1 mg/day. The maximum dose should not exceed 4 mg/day. Occasional patients with panic disorder may need as much as 10 mg a day to achieve a successful response and in these cases periodic reassessment and consideration of dosage adjustment is required.

Dosage should be individualized for maximum beneficial effect with the lowest possible dose. If side-effects occur at starting dose, dose may be lowered. When discontinuing therapy, dosage should be reduced gradually by no more than 0.5 mg every three days.

In elderly patients or in patients with advanced liver disease, the usual starting dose is 0.25 mg, two or three times daily and may be gradually increased if needed and tolerated.

Alprazolam 1 mg should be administered once daily, preferably in the morning by patients who are on multiple dosage regimens of Alprazolam 0.25/0.5 mg. The tablets should be taken intact, they should not be chewed, crushed, or broken.

Side effectsView

Side effects, if occur, are generally observed at the beginning of therapy and usually disappear upon continued medication. The most frequent side effects are drowsiness and light-headedness. The other side effects, that may occur include depression, headache, confusion, dry mouth, constipation, etc.

PrecautionsView

Because Alprazolam may produce psychological and physical dependence, the increment of dose or abrupt discontinuation of Alprazolam therapy should not be done without the physician's advice. The duration of therapy must be determined by the physicians. Alprazolam should be administered with caution to patients with hepatic or renal disease, chronic pulmonary insufficiency, or sleep apnea.

InteractionsView

The CNS-depressant action of Alprazolam may be aggravated by concomitant use of other psychotropic drugs, anticonvulsants, antihistaminics, alcohol and oral ontraceptives.

Pregnancy & lactationView

Alprazolam has been categorized in pregnancy category D; that means, it should be avoided in pregnancy. Like other benzodiazepines, Alprazolam is assumed to be excreted in breast milk. Therefore, nursing should not be undertaken by mothers who must use Alprazolam.

Pediatric usageView

The safety and effectiveness of Alprazolam in individuals below 18 years of age have not been established.

Overdose effectsView

Manifestations of Alprazolam overdosage include somnolence, confusion, impaired coordination, diminished reflexes, and coma. In such cases of overdosage general supportive measures should be employed along with immediate gastric lavage.

StorageView

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Serelam

Alprazolam

Tablet 0.25 mg Allopathic Benzodiazepine sedatives

Indications

Vestibular neuritis

Indication detailsView

Alprazolam is indicated in-

Anxiety disorder
Short term relief of anxiety
Anxiety associated with depression
Panic disorder, with or without agoraphobia.

Therapeutic classView

Benzodiazepine sedatives

PharmacologyView

Alprazolam is a triazole analog of the 1,4-benzodiazepine class of drugs. It is an anxiolytic with hypnotic and anticonvulsive properties. Alprazolam is presumed to produce its effects via interacting with the Gamma Aminobutyric Acid (GABA)- benzodiazepine receptor complex. Like all benzodiazepines, it causes a dose-related CNS depressant activity varying from mild impairment of task performance to hypnosis.

DosageView

Treatment should be initiated with a dose of 0.25 to 0.5 mg three times daily. Depending on the response, dose may be increased at intervals of 3 to 4 days in increments of no more than 1 mg/day. The maximum dose should not exceed 4 mg/day. Occasional patients with panic disorder may need as much as 10 mg a day to achieve a successful response and in these cases periodic reassessment and consideration of dosage adjustment is required.

Dosage should be individualized for maximum beneficial effect with the lowest possible dose. If side-effects occur at starting dose, dose may be lowered. When discontinuing therapy, dosage should be reduced gradually by no more than 0.5 mg every three days.

In elderly patients or in patients with advanced liver disease, the usual starting dose is 0.25 mg, two or three times daily and may be gradually increased if needed and tolerated.

Alprazolam 1 mg should be administered once daily, preferably in the morning by patients who are on multiple dosage regimens of Alprazolam 0.25/0.5 mg. The tablets should be taken intact, they should not be chewed, crushed, or broken.

Side effectsView

Side effects, if occur, are generally observed at the beginning of therapy and usually disappear upon continued medication. The most frequent side effects are drowsiness and light-headedness. The other side effects, that may occur include depression, headache, confusion, dry mouth, constipation, etc.

PrecautionsView

Because Alprazolam may produce psychological and physical dependence, the increment of dose or abrupt discontinuation of Alprazolam therapy should not be done without the physician's advice. The duration of therapy must be determined by the physicians. Alprazolam should be administered with caution to patients with hepatic or renal disease, chronic pulmonary insufficiency, or sleep apnea.

InteractionsView

The CNS-depressant action of Alprazolam may be aggravated by concomitant use of other psychotropic drugs, anticonvulsants, antihistaminics, alcohol and oral ontraceptives.

Pregnancy & lactationView

Alprazolam has been categorized in pregnancy category D; that means, it should be avoided in pregnancy. Like other benzodiazepines, Alprazolam is assumed to be excreted in breast milk. Therefore, nursing should not be undertaken by mothers who must use Alprazolam.

Pediatric usageView

The safety and effectiveness of Alprazolam in individuals below 18 years of age have not been established.

Overdose effectsView

Manifestations of Alprazolam overdosage include somnolence, confusion, impaired coordination, diminished reflexes, and coma. In such cases of overdosage general supportive measures should be employed along with immediate gastric lavage.

StorageView

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Serelose

Lactulose

Oral Solution 3.35 gm/5 ml Allopathic Osmotic purgatives

Indications

Osmotic laxative

Indication detailsView

Constipation (Chronic Constipation): In every case of chronic constipation, initial treatment should consist of a diet rich in fiber (vegetables, salads, fruits etc.) a generous amount of liquids and much physical exercise. Lactulose is only to be taken when these measures prove insufficient.

Intestinal flora disturbances:

In damaged to intestinal flora (e.g. following long-term antibiotic treatment)
gall bladder diseases
intestinal diseases ( Colitis, Diverticulosis, Megacolon)

Increased blood ammonia levels (hyper ammoniemia in hepatopathy, portal-systemic encephalopathy)

Therapeutic classView

Osmotic purgatives

PharmacologyView

Lactulose is a synthetic disaccharide. Lactulose is metabolized in the colon by the saccharolytic bacteria, producing low molecular weight organic acids (mainly lactic acid), which lowers the pH of the colon contents, promote the retention of water by an osmotic effect; thus increasing peristaltic activity. Lactulose is minimally absorbed; therefore, the pharmacokinetics of the absorbed material are not relevant to the principal therapeutic action.

DosageView

In constipation ( chronic constipation):

Adults: Initially 3-6 tea-spoons daily, In long-term therapy 1½-6 tea-spoons daily
Children up to 14 years: Initially 3 tea-spoons daily, In long-term therapy 1-2 tea-spoons daily
Infants and toddlers: Initially 1-2 tea-spoons daily, In long-term therapy 1 tea-spoon daily

In damaged intestinal flora:

Adults: 1-2 tea-spoons daily
Children: 1 tea-spoon daily

For reduction of blood ammonia level:

Hyper-ammoniemia in hepatopathy: a maximum of 18-30 tea-spoons daily.
In portal systemic encephalopathy: hourly doses of 6-9 tea-spoons of Lactulose solution may be used to induce the rapid laxation. When the laxative effect has been achieved, the dose may then be reduced.

Side effectsView

Occasionally flatulence, cramp and abdominal discomfort can occur at the beginning of treatment; this is rapidly eliminated by reducing the dose. Overdose can result in diarrhoea. In abuse, loss of electrolytes (primarily potassium).

ContraindicationsView

Hypersensitivity to either galactose and or lactose; galactose-free diet, gastro-cardial symptom complex, suspected intestinal obstruction.

PrecautionsView

Lactulose should be administered with care to patients who are intolerant to lactulose. The dose used in the treatment of (pre) coma hepaticum is usually much higher and may need to be taken into consideration for diabetics.

InteractionsView

There is no significant drug interactions with lactulose. The glycosidic effect of cardiac glycosides can be intensified by potassium deficiency in abuse.

Pregnancy & lactationView

US FDA Pregnancy Category of Lactulose is B. Studies show that Lactulose has no adverse effects. Decisions regarding use during pregnancy and lactation must be made by registered physician.

Overdose effectsView

There have been no reports of accidental overdosage. In the event of acute overdosage it is expected that diarrhoea and abdominal cramps would be the major symptoms.

StorageView

Keep in a dry place away from light and heat. Keep out of the reach of children.

Seren

Fluoxetine Hydrochloride

Capsule 20 mg Allopathic Phenothiazine related drugs

Indications

Obsessive-compulsive disorder (OCD)

Indication detailsView

Fluoxetine is indicated for the treatment of-

depressive illness
bulimia nervosa
obsessive compulsive disorder.

Therapeutic classView

Phenothiazine related drugs

PharmacologyView

Fluoxetine has been shown to selectively inhibit the reuptake of serotonin at the presynaptic neuronal membrane which causes increased synaptic concentration of serotonin in the CNS. This result in numerous functional changes associated with enhanced serotonergic neurotransmission. Fluoxetine appears to have no effect on the reuptake of norepinephrine and dopamine and does not exhibit anticholinergic, antihistaminic or α1 adrenergic blocking activity at usual therapeutic doses.

DosageView

Initial treatment: Recent studies suggest that 20 mg/day of Fluoxetine may be sufficient to obtain satisfactory antidepressant response. Consequently, a dose of 20 mg/day administered in the morning is recommended as the initial dose.

A dose increase may be considered after several weeks if no clinical improvement is observed. Dosage above 20 mg/day, should be administered on a bid schedule (i.e. morning and noon) and should not exceed a maximum dose of 80 mg/day. As with other antidepressants, the full antidepressant effect may be delayed until 4 weeks of treatment or longer. As with many other medications, a lower or less frequent dosage should be used in patients with renal and/or hepatic impairment.

A lower or less frequent dosage should also be considered for patients, such as elderly, with concurrent disease or on multiple medication. A recommended maximum dose for elderly patients is 60 mg per day.

Maintenance treatment: It is generally agreed among expert psychopharmacologists that acute episode of depression requires several months or longer sustained pharmacologic therapy. Fluoxetine is also used in dosage of 60 mg daily for the management of bulimia nervosa.

Use in children: The use of Fluoxetine in children is not recommended as safety and efficacy have not been established.

Side effectsView

Gastrointestinal: Nausea, vomiting, dyspepsia, dry mouth, and diarrhoea.

Neurological: Anxiety, nervousness, insomnia/ drowsiness and fatigue.

Others: Excessive sweating, pruritus, skin rashes associated with liver, kidney and lung involvement. It has therefore been advised that Fluoxetine therapy should be discontinued in any patient who develops a skin rash.

ContraindicationsView

Fluoxetine Hydrochloride is contraindicated in patients known to be hypersensitive to it.

Monoamine oxidase inhibitors: There have been reports of serious, sometimes fatal reactions (including hyperthermia, rigidity, myoclonus, autonomic instability with possible rapid fluctuations of vital signs and changes of mental status that include extreme agitation progressing to delirium and coma) in patients receiving Fluoxetine in combination with monoamine oxidase inhibitors (MAOIs), and in patients who have recently discontinued Fluoxetine and are then started on MAOIs. Some cases presented with features resembling neuroleptic malignant syndrome. Therefore, Fluoxetine should not be used in combination with MAOI, or within 14 days of discontinuing therapy with MAOI. Since Fluoxetine and its major metabolites have very long elimination half-lives, at least 5 weeks should be allowed after stopping Fluoxetine and before starting MAOI.

PrecautionsView

As Fluoxetine undergoes hepatic metabolism and renal excretion, it should be used with caution and in reduced doses in patients with impaired hepatic or renal function. Because of its epileptogenic effect, it should be used with caution in patients with epilepsy or a history of such disorders. Fluoxetine may alter glycaemic control and therefore caution is also warranted in diabetic subjects. Depressed patients with suicidal tendencies should be carefully supervised during treatment. Fluoxetine is not usually considered a suitable form of therapy for the depressive component of bipolar (manic depressive) illness as mania may be precipitated.

InteractionsView

MAO inhibitors: Sometimes serious fatal reactions have been reported with concomitant use.
Antidepressants: There have been greater than two fold increases of previously stable plasma levels of other antidepressants.
Lithium: There have been reports of increased or decreased lithium levels when used concomitantly with Fluoxetine.
Antipsychotics: Elevation of blood levels of haloperidol and clozapine has been observed in patients receiving concomitant Fluoxetine.
Anticonvulsants: Patients on stable dose of phenytoin and carbamazepine have developed elevated plasma anticonvulsant concentrations and clinical anticonvulsant toxicity following initiation of concomitant fluoxetine treatment.
CNS active drugs: Caution is advised if concomitant administration of Fluoxetine is required.

Pregnancy & lactationView

In animal studies, no teratogenicity or harmful effect was found. Because animal reproductive studies are not always predictive of human responses, Fluoxetine should be used in pregnancy only if clearly needed. As Fluoxetine is excreted in human milk, caution should be exercised when Fluoxetine is administered to nursing women.

StorageView

Protect from light & moisture. Keep in cool & dry place. Store below 30°C. Keep all the medicines out of the reach of children.

Seretide

Salmeterol + Fluticasone Propionate

Inhalation Capsule 50 mcg+100 mcg Allopathic Long-acting selective β-adrenoceptor stimulants

Indications

COPD

Indication detailsView

This is indicated in the regular treatment of asthma where use of a combination product (long-acting β2-agonist and inhaled corticosteroid) is appropriate:

patients not adequately controlled with inhaled corticosteroids and 'as needed' inhaled short acting β2-agonist or
patients already adequately controlled on both inhaled corticosteroid and long-acting β2-agonist.

Therapeutic classView

Long-acting selective β-adrenoceptor stimulants, Respiratory corticosteroids

PharmacologyView

Salmeterol Xinafoate is a selective, long acting beta-2 agonist used in the treatment of asthma and other forms of diffuse airways obstruction. Fluticasone Propionate is a corticosteroid with mainly glucocorticoid activity. Fluticasone Propionate is stated to exert a topical effect on the lungs without systematic effects at usual dose.

Salmeterol protects against symptoms, Fluticasone Propionate improves lung function and prevents exacerbations of the condition. This preparation can offer a more convenient regime for patients on concurrent β-agonist and inhaled corticosteroid therapy. The respective mechanisms of action of both drugs are discussed below:

Salmeterol: Salmeterol is a selective long-acting (12 hour) beta-2-adrenoceptor agonist with a long side chain which binds to the exo-site of the receptor.

Fluticasone Propionate: Fluticasone Propionate given by inhalation at recommended doses has a potent glucocorticoid anti-inflammatory action within the lungs, resulting in reduced symptoms and exacerbaions of asthma, without the adverse effects observed when corticosteroids are administered systemically.

DosageView

Inhalation Aerosol:

Adults and adolescents 12 years and older: 2 puffs of 25 µg Salmeterol and 50 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 125 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 250 µg Fluticasone Propionate twice daily.
Children (4-12 years): 2 puffs of 25 µg salmeterol and 50 µg Fluticasone Propionate twice daily.

Inhalation Powder in Capsule (For Asthma):

Adult and Adolescent (12 Years and Older): Salmeterol 50 µg & Fluticasone 100 µg or Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart).
The recommended starting dosages for Salmeterol 50 µg & Fluticasone 100 µg & Salmeterol 50 µg & Fluticasone 250 µg for patients aged 12 years and older are based upon patients asthma severity.
The maximum recommended dosage is Salmeterol 50 µg & Fluticasone 500 µg twice daily.
Pediatric Patients (4 to 11 Years): For patients with asthma who are not controlled on an inhaled corticosteroid, the dosage is Salmeterol 50 µg & Fluticasone 100 µg twice daily (morning and evening, approximately 12 hours apart).

Inhalation Powder in Capsule (For COPD): Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart). Rinsing the mouth after each inhalation is advised.

Inhalation Powder in Maxhaler (For Asthma): This is a moulded plastic device containing a foil strip with 60 regularly placed blisters containing pre-dispensed inhalation powder. Patients should be made aware that Maxhaler must be used daily for optimum benefit, even when asymptomatic.

Adults and Adolescents (12 years and older)-

50/100 Maxhaler: One Inhalation twice daily
50/250 Maxhaler: One Inhalation twice daily
50/500 Maxhaler: One Inhalation twice daily

Children (4 years and older)-

50/100 Maxhaler: One Inhalation twice daily. The maximum licensed dose of fluticasone propionate delivered by this Maxhaler in children is 100 ug twice daily. There are no data available for use of this Maxhaler in children aged under 4 years.

Inhalation Powder in Maxhaler (For COPD):

Maxhaler: One Inhalation twice daily
Special patient groups: There is no need to adjust the dose in elderly patients or in those with renal impairment. There are no data available for use of this in patients with hepatic impairment.
Using the Maxhaler: This is a patient friendly, ready to use and easy to grip device. Use as per instructions for use.

AdministrationView

Using an Inhaler seems simple, but most patients do not know how to use it in the right way. If the Inhaler is used in the wrong way, less medicine can reach the lungs. Correct and regular use of the Inhaler will prevent or lessen the severity of asthma attacks.

Following simple steps can help to use Inhaler effectively (According to "National Asthma Guidelines for Medical Practitioners" published by Asthma Association):

Take off the cap.
Shake the inhaler (at least six times) vigorously before each use.
If the inhaler is new or if it has not been used for a week or more, shake it well and release one puff into the air to make sure that it works.
Breathe out as full as comfortably possible & hold the inhaler upright.
Place the actuator into mouth between the teeth and close lips around the mouthpiece.
While breathing deeply and slowly through the mouth, press down firmly add fully on the canister to release medicine.
Remove the inhaler from mouth. Continue holding breath for at least for 10 seconds or as long as it is comfortable.
If doctor has prescribed more than one inhalation per treatment, wait 1 minute between puffs (inhalations). Shake the inhaler well and repeat steps 4 to 7.
After use, replace the cap on the mouthpiece. After each treatment, rinse mouth with water.
Check your technique in front of a mirror from time to time, if you see a white mist during the inhalation, you may not have closed your lips properly around mouthpiece, or you may not be breathing in as you press the can. This indicates failure of technique. If this happens, repeat the procedure from step 4 carefully.

Instructions for Cleaning Inhaler: Clean your Inhaler at least once a week. Remove canister and rinse the plastic actuator and cap in warm water but do not put the metal canister into water. Dry the actuator and cap thoroughly and gently replace the metal canister into the actuator with a twisting motion. Put the cap on the mouthpiece.

Side effectsView

As this preparation contains Salmeterol and Fluticasone Propionate, the type and severity of adverse reactions associated with each of the compounds may be expected. There is no incidence of additional adverse events following concurrent administration of the two compounds. Adverse events, which have been associated with Salmeterol or Fluticasone Propionate, are given below.

Salmeterol: The pharmacological side effects of beta-2-agonist treatment, such as tremor, subjective palpitations and headache, have been reported, but tend to be transient and reduce with regular therapy. Cardiac arrhythmia (including atrial fibrillation, supraventricular tachycardia and extra systoles) may occur, usually in susceptible patients. There have been reports of arthralgia and hypersensitivity reactions, including rash, oedema and angioedema. There have been reports of oropharyngeal irritation. There have been rare reports of muscle cramps.

Fluticasone propionate: Hoarseness and candidiasis (thrush) of the mouth and throat can occur in some patients. Cutaneous hypersensitivity reactions have been reported. Rare cases of facial and oropharyngeal oedema have been reported. Both hoarseness and incidence of candidiasis may be relieved by gargling with water after use of Salmeterol/ Fluticasone Propionate Inhaler.

ContraindicationsView

This is contraindicated in patients with a history of hypersensitivity to any of the ingredients.

PrecautionsView

Consideration should be given to additional corticosteroid therapies, and to including administration of antibiotics if an infection is present. As with all inhaled medication containing corticosteroids, this preparation should be administered with caution in patients with active or quiescent pulmonary tuberculosis. This preparation should be administered with caution in patients with thyrotoxicosis.

InteractionsView

Both non-selective and selective β-blockers should be avoided in patients with asthma, unless there are compelling reasons for their use. Due to the very low plasma concentrations achieved after inhaled dosing clinically significant drug interactions are unlikely. Care should be taken when co-administering known strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir), as there is potential for increased systemic exposure to Fluticasone Propionate.

Pregnancy & lactationView

Administration of drugs during pregnancy and lactation should only be considered if the expected benefit to the mother is greater than any possible risk to the foetus or child. There is insufficient experience of the use of Salmeterol Xinafoate and Fluticasone Propionate in human pregnancy and lactation. There are no data available for human breast milk.

Pediatric usageView

Orally inhaled corticosteroids may cause a reduction in growth velocity when administered to paediatric patients. The long-term effects of this reduction including the impact of final adult height are unknown.

StorageView

Pressurised canister, do not puncture, break or incinerate even when apparently empty. Avoid storage in direct sunlight or heat. Store below 30°C. Keep away from eyes. Keep away from children.

Seretide

Salmeterol + Fluticasone Propionate

Inhaler (25 mcg+250 mcg)/puff Allopathic Long-acting selective β-adrenoceptor stimulants

Indications

COPD

Indication detailsView

This is indicated in the regular treatment of asthma where use of a combination product (long-acting β2-agonist and inhaled corticosteroid) is appropriate:

patients not adequately controlled with inhaled corticosteroids and 'as needed' inhaled short acting β2-agonist or
patients already adequately controlled on both inhaled corticosteroid and long-acting β2-agonist.

Therapeutic classView

Long-acting selective β-adrenoceptor stimulants, Respiratory corticosteroids

PharmacologyView

Salmeterol Xinafoate is a selective, long acting beta-2 agonist used in the treatment of asthma and other forms of diffuse airways obstruction. Fluticasone Propionate is a corticosteroid with mainly glucocorticoid activity. Fluticasone Propionate is stated to exert a topical effect on the lungs without systematic effects at usual dose.

Salmeterol protects against symptoms, Fluticasone Propionate improves lung function and prevents exacerbations of the condition. This preparation can offer a more convenient regime for patients on concurrent β-agonist and inhaled corticosteroid therapy. The respective mechanisms of action of both drugs are discussed below:

Salmeterol: Salmeterol is a selective long-acting (12 hour) beta-2-adrenoceptor agonist with a long side chain which binds to the exo-site of the receptor.

Fluticasone Propionate: Fluticasone Propionate given by inhalation at recommended doses has a potent glucocorticoid anti-inflammatory action within the lungs, resulting in reduced symptoms and exacerbaions of asthma, without the adverse effects observed when corticosteroids are administered systemically.

DosageView

Inhalation Aerosol:

Adults and adolescents 12 years and older: 2 puffs of 25 µg Salmeterol and 50 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 125 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 250 µg Fluticasone Propionate twice daily.
Children (4-12 years): 2 puffs of 25 µg salmeterol and 50 µg Fluticasone Propionate twice daily.

Inhalation Powder in Capsule (For Asthma):

Adult and Adolescent (12 Years and Older): Salmeterol 50 µg & Fluticasone 100 µg or Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart).
The recommended starting dosages for Salmeterol 50 µg & Fluticasone 100 µg & Salmeterol 50 µg & Fluticasone 250 µg for patients aged 12 years and older are based upon patients asthma severity.
The maximum recommended dosage is Salmeterol 50 µg & Fluticasone 500 µg twice daily.
Pediatric Patients (4 to 11 Years): For patients with asthma who are not controlled on an inhaled corticosteroid, the dosage is Salmeterol 50 µg & Fluticasone 100 µg twice daily (morning and evening, approximately 12 hours apart).

Inhalation Powder in Capsule (For COPD): Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart). Rinsing the mouth after each inhalation is advised.

Inhalation Powder in Maxhaler (For Asthma): This is a moulded plastic device containing a foil strip with 60 regularly placed blisters containing pre-dispensed inhalation powder. Patients should be made aware that Maxhaler must be used daily for optimum benefit, even when asymptomatic.

Adults and Adolescents (12 years and older)-

50/100 Maxhaler: One Inhalation twice daily
50/250 Maxhaler: One Inhalation twice daily
50/500 Maxhaler: One Inhalation twice daily

Children (4 years and older)-

50/100 Maxhaler: One Inhalation twice daily. The maximum licensed dose of fluticasone propionate delivered by this Maxhaler in children is 100 ug twice daily. There are no data available for use of this Maxhaler in children aged under 4 years.

Inhalation Powder in Maxhaler (For COPD):

Maxhaler: One Inhalation twice daily
Special patient groups: There is no need to adjust the dose in elderly patients or in those with renal impairment. There are no data available for use of this in patients with hepatic impairment.
Using the Maxhaler: This is a patient friendly, ready to use and easy to grip device. Use as per instructions for use.

AdministrationView

Using an Inhaler seems simple, but most patients do not know how to use it in the right way. If the Inhaler is used in the wrong way, less medicine can reach the lungs. Correct and regular use of the Inhaler will prevent or lessen the severity of asthma attacks.

Following simple steps can help to use Inhaler effectively (According to "National Asthma Guidelines for Medical Practitioners" published by Asthma Association):

Take off the cap.
Shake the inhaler (at least six times) vigorously before each use.
If the inhaler is new or if it has not been used for a week or more, shake it well and release one puff into the air to make sure that it works.
Breathe out as full as comfortably possible & hold the inhaler upright.
Place the actuator into mouth between the teeth and close lips around the mouthpiece.
While breathing deeply and slowly through the mouth, press down firmly add fully on the canister to release medicine.
Remove the inhaler from mouth. Continue holding breath for at least for 10 seconds or as long as it is comfortable.
If doctor has prescribed more than one inhalation per treatment, wait 1 minute between puffs (inhalations). Shake the inhaler well and repeat steps 4 to 7.
After use, replace the cap on the mouthpiece. After each treatment, rinse mouth with water.
Check your technique in front of a mirror from time to time, if you see a white mist during the inhalation, you may not have closed your lips properly around mouthpiece, or you may not be breathing in as you press the can. This indicates failure of technique. If this happens, repeat the procedure from step 4 carefully.

Instructions for Cleaning Inhaler: Clean your Inhaler at least once a week. Remove canister and rinse the plastic actuator and cap in warm water but do not put the metal canister into water. Dry the actuator and cap thoroughly and gently replace the metal canister into the actuator with a twisting motion. Put the cap on the mouthpiece.

Side effectsView

As this preparation contains Salmeterol and Fluticasone Propionate, the type and severity of adverse reactions associated with each of the compounds may be expected. There is no incidence of additional adverse events following concurrent administration of the two compounds. Adverse events, which have been associated with Salmeterol or Fluticasone Propionate, are given below.

Salmeterol: The pharmacological side effects of beta-2-agonist treatment, such as tremor, subjective palpitations and headache, have been reported, but tend to be transient and reduce with regular therapy. Cardiac arrhythmia (including atrial fibrillation, supraventricular tachycardia and extra systoles) may occur, usually in susceptible patients. There have been reports of arthralgia and hypersensitivity reactions, including rash, oedema and angioedema. There have been reports of oropharyngeal irritation. There have been rare reports of muscle cramps.

Fluticasone propionate: Hoarseness and candidiasis (thrush) of the mouth and throat can occur in some patients. Cutaneous hypersensitivity reactions have been reported. Rare cases of facial and oropharyngeal oedema have been reported. Both hoarseness and incidence of candidiasis may be relieved by gargling with water after use of Salmeterol/ Fluticasone Propionate Inhaler.

ContraindicationsView

This is contraindicated in patients with a history of hypersensitivity to any of the ingredients.

PrecautionsView

Consideration should be given to additional corticosteroid therapies, and to including administration of antibiotics if an infection is present. As with all inhaled medication containing corticosteroids, this preparation should be administered with caution in patients with active or quiescent pulmonary tuberculosis. This preparation should be administered with caution in patients with thyrotoxicosis.

InteractionsView

Both non-selective and selective β-blockers should be avoided in patients with asthma, unless there are compelling reasons for their use. Due to the very low plasma concentrations achieved after inhaled dosing clinically significant drug interactions are unlikely. Care should be taken when co-administering known strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir), as there is potential for increased systemic exposure to Fluticasone Propionate.

Pregnancy & lactationView

Administration of drugs during pregnancy and lactation should only be considered if the expected benefit to the mother is greater than any possible risk to the foetus or child. There is insufficient experience of the use of Salmeterol Xinafoate and Fluticasone Propionate in human pregnancy and lactation. There are no data available for human breast milk.

Pediatric usageView

Orally inhaled corticosteroids may cause a reduction in growth velocity when administered to paediatric patients. The long-term effects of this reduction including the impact of final adult height are unknown.

StorageView

Pressurised canister, do not puncture, break or incinerate even when apparently empty. Avoid storage in direct sunlight or heat. Store below 30°C. Keep away from eyes. Keep away from children.

Seretide

Salmeterol + Fluticasone Propionate

Inhaler (25 mcg+125 mcg)/puff Allopathic Long-acting selective β-adrenoceptor stimulants

Indications

COPD

Indication detailsView

This is indicated in the regular treatment of asthma where use of a combination product (long-acting β2-agonist and inhaled corticosteroid) is appropriate:

patients not adequately controlled with inhaled corticosteroids and 'as needed' inhaled short acting β2-agonist or
patients already adequately controlled on both inhaled corticosteroid and long-acting β2-agonist.

Therapeutic classView

Long-acting selective β-adrenoceptor stimulants, Respiratory corticosteroids

PharmacologyView

Salmeterol Xinafoate is a selective, long acting beta-2 agonist used in the treatment of asthma and other forms of diffuse airways obstruction. Fluticasone Propionate is a corticosteroid with mainly glucocorticoid activity. Fluticasone Propionate is stated to exert a topical effect on the lungs without systematic effects at usual dose.

Salmeterol protects against symptoms, Fluticasone Propionate improves lung function and prevents exacerbations of the condition. This preparation can offer a more convenient regime for patients on concurrent β-agonist and inhaled corticosteroid therapy. The respective mechanisms of action of both drugs are discussed below:

Salmeterol: Salmeterol is a selective long-acting (12 hour) beta-2-adrenoceptor agonist with a long side chain which binds to the exo-site of the receptor.

Fluticasone Propionate: Fluticasone Propionate given by inhalation at recommended doses has a potent glucocorticoid anti-inflammatory action within the lungs, resulting in reduced symptoms and exacerbaions of asthma, without the adverse effects observed when corticosteroids are administered systemically.

DosageView

Inhalation Aerosol:

Adults and adolescents 12 years and older: 2 puffs of 25 µg Salmeterol and 50 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 125 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 250 µg Fluticasone Propionate twice daily.
Children (4-12 years): 2 puffs of 25 µg salmeterol and 50 µg Fluticasone Propionate twice daily.

Inhalation Powder in Capsule (For Asthma):

Adult and Adolescent (12 Years and Older): Salmeterol 50 µg & Fluticasone 100 µg or Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart).
The recommended starting dosages for Salmeterol 50 µg & Fluticasone 100 µg & Salmeterol 50 µg & Fluticasone 250 µg for patients aged 12 years and older are based upon patients asthma severity.
The maximum recommended dosage is Salmeterol 50 µg & Fluticasone 500 µg twice daily.
Pediatric Patients (4 to 11 Years): For patients with asthma who are not controlled on an inhaled corticosteroid, the dosage is Salmeterol 50 µg & Fluticasone 100 µg twice daily (morning and evening, approximately 12 hours apart).

Inhalation Powder in Capsule (For COPD): Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart). Rinsing the mouth after each inhalation is advised.

Inhalation Powder in Maxhaler (For Asthma): This is a moulded plastic device containing a foil strip with 60 regularly placed blisters containing pre-dispensed inhalation powder. Patients should be made aware that Maxhaler must be used daily for optimum benefit, even when asymptomatic.

Adults and Adolescents (12 years and older)-

50/100 Maxhaler: One Inhalation twice daily
50/250 Maxhaler: One Inhalation twice daily
50/500 Maxhaler: One Inhalation twice daily

Children (4 years and older)-

50/100 Maxhaler: One Inhalation twice daily. The maximum licensed dose of fluticasone propionate delivered by this Maxhaler in children is 100 ug twice daily. There are no data available for use of this Maxhaler in children aged under 4 years.

Inhalation Powder in Maxhaler (For COPD):

Maxhaler: One Inhalation twice daily
Special patient groups: There is no need to adjust the dose in elderly patients or in those with renal impairment. There are no data available for use of this in patients with hepatic impairment.
Using the Maxhaler: This is a patient friendly, ready to use and easy to grip device. Use as per instructions for use.

AdministrationView

Using an Inhaler seems simple, but most patients do not know how to use it in the right way. If the Inhaler is used in the wrong way, less medicine can reach the lungs. Correct and regular use of the Inhaler will prevent or lessen the severity of asthma attacks.

Following simple steps can help to use Inhaler effectively (According to "National Asthma Guidelines for Medical Practitioners" published by Asthma Association):

Take off the cap.
Shake the inhaler (at least six times) vigorously before each use.
If the inhaler is new or if it has not been used for a week or more, shake it well and release one puff into the air to make sure that it works.
Breathe out as full as comfortably possible & hold the inhaler upright.
Place the actuator into mouth between the teeth and close lips around the mouthpiece.
While breathing deeply and slowly through the mouth, press down firmly add fully on the canister to release medicine.
Remove the inhaler from mouth. Continue holding breath for at least for 10 seconds or as long as it is comfortable.
If doctor has prescribed more than one inhalation per treatment, wait 1 minute between puffs (inhalations). Shake the inhaler well and repeat steps 4 to 7.
After use, replace the cap on the mouthpiece. After each treatment, rinse mouth with water.
Check your technique in front of a mirror from time to time, if you see a white mist during the inhalation, you may not have closed your lips properly around mouthpiece, or you may not be breathing in as you press the can. This indicates failure of technique. If this happens, repeat the procedure from step 4 carefully.

Instructions for Cleaning Inhaler: Clean your Inhaler at least once a week. Remove canister and rinse the plastic actuator and cap in warm water but do not put the metal canister into water. Dry the actuator and cap thoroughly and gently replace the metal canister into the actuator with a twisting motion. Put the cap on the mouthpiece.

Side effectsView

As this preparation contains Salmeterol and Fluticasone Propionate, the type and severity of adverse reactions associated with each of the compounds may be expected. There is no incidence of additional adverse events following concurrent administration of the two compounds. Adverse events, which have been associated with Salmeterol or Fluticasone Propionate, are given below.

Salmeterol: The pharmacological side effects of beta-2-agonist treatment, such as tremor, subjective palpitations and headache, have been reported, but tend to be transient and reduce with regular therapy. Cardiac arrhythmia (including atrial fibrillation, supraventricular tachycardia and extra systoles) may occur, usually in susceptible patients. There have been reports of arthralgia and hypersensitivity reactions, including rash, oedema and angioedema. There have been reports of oropharyngeal irritation. There have been rare reports of muscle cramps.

Fluticasone propionate: Hoarseness and candidiasis (thrush) of the mouth and throat can occur in some patients. Cutaneous hypersensitivity reactions have been reported. Rare cases of facial and oropharyngeal oedema have been reported. Both hoarseness and incidence of candidiasis may be relieved by gargling with water after use of Salmeterol/ Fluticasone Propionate Inhaler.

ContraindicationsView

This is contraindicated in patients with a history of hypersensitivity to any of the ingredients.

PrecautionsView

Consideration should be given to additional corticosteroid therapies, and to including administration of antibiotics if an infection is present. As with all inhaled medication containing corticosteroids, this preparation should be administered with caution in patients with active or quiescent pulmonary tuberculosis. This preparation should be administered with caution in patients with thyrotoxicosis.

InteractionsView

Both non-selective and selective β-blockers should be avoided in patients with asthma, unless there are compelling reasons for their use. Due to the very low plasma concentrations achieved after inhaled dosing clinically significant drug interactions are unlikely. Care should be taken when co-administering known strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir), as there is potential for increased systemic exposure to Fluticasone Propionate.

Pregnancy & lactationView

Administration of drugs during pregnancy and lactation should only be considered if the expected benefit to the mother is greater than any possible risk to the foetus or child. There is insufficient experience of the use of Salmeterol Xinafoate and Fluticasone Propionate in human pregnancy and lactation. There are no data available for human breast milk.

Pediatric usageView

Orally inhaled corticosteroids may cause a reduction in growth velocity when administered to paediatric patients. The long-term effects of this reduction including the impact of final adult height are unknown.

StorageView

Pressurised canister, do not puncture, break or incinerate even when apparently empty. Avoid storage in direct sunlight or heat. Store below 30°C. Keep away from eyes. Keep away from children.

Seretide

Salmeterol + Fluticasone Propionate

Inhaler (25 mcg+50 mcg)/puff Allopathic Long-acting selective β-adrenoceptor stimulants

Indications

COPD

Indication detailsView

This is indicated in the regular treatment of asthma where use of a combination product (long-acting β2-agonist and inhaled corticosteroid) is appropriate:

patients not adequately controlled with inhaled corticosteroids and 'as needed' inhaled short acting β2-agonist or
patients already adequately controlled on both inhaled corticosteroid and long-acting β2-agonist.

Therapeutic classView

Long-acting selective β-adrenoceptor stimulants, Respiratory corticosteroids

PharmacologyView

Salmeterol Xinafoate is a selective, long acting beta-2 agonist used in the treatment of asthma and other forms of diffuse airways obstruction. Fluticasone Propionate is a corticosteroid with mainly glucocorticoid activity. Fluticasone Propionate is stated to exert a topical effect on the lungs without systematic effects at usual dose.

Salmeterol protects against symptoms, Fluticasone Propionate improves lung function and prevents exacerbations of the condition. This preparation can offer a more convenient regime for patients on concurrent β-agonist and inhaled corticosteroid therapy. The respective mechanisms of action of both drugs are discussed below:

Salmeterol: Salmeterol is a selective long-acting (12 hour) beta-2-adrenoceptor agonist with a long side chain which binds to the exo-site of the receptor.

Fluticasone Propionate: Fluticasone Propionate given by inhalation at recommended doses has a potent glucocorticoid anti-inflammatory action within the lungs, resulting in reduced symptoms and exacerbaions of asthma, without the adverse effects observed when corticosteroids are administered systemically.

DosageView

Inhalation Aerosol:

Adults and adolescents 12 years and older: 2 puffs of 25 µg Salmeterol and 50 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 125 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 250 µg Fluticasone Propionate twice daily.
Children (4-12 years): 2 puffs of 25 µg salmeterol and 50 µg Fluticasone Propionate twice daily.

Inhalation Powder in Capsule (For Asthma):

Adult and Adolescent (12 Years and Older): Salmeterol 50 µg & Fluticasone 100 µg or Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart).
The recommended starting dosages for Salmeterol 50 µg & Fluticasone 100 µg & Salmeterol 50 µg & Fluticasone 250 µg for patients aged 12 years and older are based upon patients asthma severity.
The maximum recommended dosage is Salmeterol 50 µg & Fluticasone 500 µg twice daily.
Pediatric Patients (4 to 11 Years): For patients with asthma who are not controlled on an inhaled corticosteroid, the dosage is Salmeterol 50 µg & Fluticasone 100 µg twice daily (morning and evening, approximately 12 hours apart).

Inhalation Powder in Capsule (For COPD): Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart). Rinsing the mouth after each inhalation is advised.

Inhalation Powder in Maxhaler (For Asthma): This is a moulded plastic device containing a foil strip with 60 regularly placed blisters containing pre-dispensed inhalation powder. Patients should be made aware that Maxhaler must be used daily for optimum benefit, even when asymptomatic.

Adults and Adolescents (12 years and older)-

50/100 Maxhaler: One Inhalation twice daily
50/250 Maxhaler: One Inhalation twice daily
50/500 Maxhaler: One Inhalation twice daily

Children (4 years and older)-

50/100 Maxhaler: One Inhalation twice daily. The maximum licensed dose of fluticasone propionate delivered by this Maxhaler in children is 100 ug twice daily. There are no data available for use of this Maxhaler in children aged under 4 years.

Inhalation Powder in Maxhaler (For COPD):

Maxhaler: One Inhalation twice daily
Special patient groups: There is no need to adjust the dose in elderly patients or in those with renal impairment. There are no data available for use of this in patients with hepatic impairment.
Using the Maxhaler: This is a patient friendly, ready to use and easy to grip device. Use as per instructions for use.

AdministrationView

Using an Inhaler seems simple, but most patients do not know how to use it in the right way. If the Inhaler is used in the wrong way, less medicine can reach the lungs. Correct and regular use of the Inhaler will prevent or lessen the severity of asthma attacks.

Following simple steps can help to use Inhaler effectively (According to "National Asthma Guidelines for Medical Practitioners" published by Asthma Association):

Take off the cap.
Shake the inhaler (at least six times) vigorously before each use.
If the inhaler is new or if it has not been used for a week or more, shake it well and release one puff into the air to make sure that it works.
Breathe out as full as comfortably possible & hold the inhaler upright.
Place the actuator into mouth between the teeth and close lips around the mouthpiece.
While breathing deeply and slowly through the mouth, press down firmly add fully on the canister to release medicine.
Remove the inhaler from mouth. Continue holding breath for at least for 10 seconds or as long as it is comfortable.
If doctor has prescribed more than one inhalation per treatment, wait 1 minute between puffs (inhalations). Shake the inhaler well and repeat steps 4 to 7.
After use, replace the cap on the mouthpiece. After each treatment, rinse mouth with water.
Check your technique in front of a mirror from time to time, if you see a white mist during the inhalation, you may not have closed your lips properly around mouthpiece, or you may not be breathing in as you press the can. This indicates failure of technique. If this happens, repeat the procedure from step 4 carefully.

Instructions for Cleaning Inhaler: Clean your Inhaler at least once a week. Remove canister and rinse the plastic actuator and cap in warm water but do not put the metal canister into water. Dry the actuator and cap thoroughly and gently replace the metal canister into the actuator with a twisting motion. Put the cap on the mouthpiece.

Side effectsView

As this preparation contains Salmeterol and Fluticasone Propionate, the type and severity of adverse reactions associated with each of the compounds may be expected. There is no incidence of additional adverse events following concurrent administration of the two compounds. Adverse events, which have been associated with Salmeterol or Fluticasone Propionate, are given below.

Salmeterol: The pharmacological side effects of beta-2-agonist treatment, such as tremor, subjective palpitations and headache, have been reported, but tend to be transient and reduce with regular therapy. Cardiac arrhythmia (including atrial fibrillation, supraventricular tachycardia and extra systoles) may occur, usually in susceptible patients. There have been reports of arthralgia and hypersensitivity reactions, including rash, oedema and angioedema. There have been reports of oropharyngeal irritation. There have been rare reports of muscle cramps.

Fluticasone propionate: Hoarseness and candidiasis (thrush) of the mouth and throat can occur in some patients. Cutaneous hypersensitivity reactions have been reported. Rare cases of facial and oropharyngeal oedema have been reported. Both hoarseness and incidence of candidiasis may be relieved by gargling with water after use of Salmeterol/ Fluticasone Propionate Inhaler.

ContraindicationsView

This is contraindicated in patients with a history of hypersensitivity to any of the ingredients.

PrecautionsView

Consideration should be given to additional corticosteroid therapies, and to including administration of antibiotics if an infection is present. As with all inhaled medication containing corticosteroids, this preparation should be administered with caution in patients with active or quiescent pulmonary tuberculosis. This preparation should be administered with caution in patients with thyrotoxicosis.

InteractionsView

Both non-selective and selective β-blockers should be avoided in patients with asthma, unless there are compelling reasons for their use. Due to the very low plasma concentrations achieved after inhaled dosing clinically significant drug interactions are unlikely. Care should be taken when co-administering known strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir), as there is potential for increased systemic exposure to Fluticasone Propionate.

Pregnancy & lactationView

Administration of drugs during pregnancy and lactation should only be considered if the expected benefit to the mother is greater than any possible risk to the foetus or child. There is insufficient experience of the use of Salmeterol Xinafoate and Fluticasone Propionate in human pregnancy and lactation. There are no data available for human breast milk.

Pediatric usageView

Orally inhaled corticosteroids may cause a reduction in growth velocity when administered to paediatric patients. The long-term effects of this reduction including the impact of final adult height are unknown.

StorageView

Pressurised canister, do not puncture, break or incinerate even when apparently empty. Avoid storage in direct sunlight or heat. Store below 30°C. Keep away from eyes. Keep away from children.

Seretide

Salmeterol + Fluticasone Propionate

Inhalation Capsule 50 mcg+500 mcg Allopathic Long-acting selective β-adrenoceptor stimulants

Indications

COPD

Indication detailsView

This is indicated in the regular treatment of asthma where use of a combination product (long-acting β2-agonist and inhaled corticosteroid) is appropriate:

patients not adequately controlled with inhaled corticosteroids and 'as needed' inhaled short acting β2-agonist or
patients already adequately controlled on both inhaled corticosteroid and long-acting β2-agonist.

Therapeutic classView

Long-acting selective β-adrenoceptor stimulants, Respiratory corticosteroids

PharmacologyView

Salmeterol Xinafoate is a selective, long acting beta-2 agonist used in the treatment of asthma and other forms of diffuse airways obstruction. Fluticasone Propionate is a corticosteroid with mainly glucocorticoid activity. Fluticasone Propionate is stated to exert a topical effect on the lungs without systematic effects at usual dose.

Salmeterol protects against symptoms, Fluticasone Propionate improves lung function and prevents exacerbations of the condition. This preparation can offer a more convenient regime for patients on concurrent β-agonist and inhaled corticosteroid therapy. The respective mechanisms of action of both drugs are discussed below:

Salmeterol: Salmeterol is a selective long-acting (12 hour) beta-2-adrenoceptor agonist with a long side chain which binds to the exo-site of the receptor.

Fluticasone Propionate: Fluticasone Propionate given by inhalation at recommended doses has a potent glucocorticoid anti-inflammatory action within the lungs, resulting in reduced symptoms and exacerbaions of asthma, without the adverse effects observed when corticosteroids are administered systemically.

DosageView

Inhalation Aerosol:

Adults and adolescents 12 years and older: 2 puffs of 25 µg Salmeterol and 50 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 125 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 250 µg Fluticasone Propionate twice daily.
Children (4-12 years): 2 puffs of 25 µg salmeterol and 50 µg Fluticasone Propionate twice daily.

Inhalation Powder in Capsule (For Asthma):

Adult and Adolescent (12 Years and Older): Salmeterol 50 µg & Fluticasone 100 µg or Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart).
The recommended starting dosages for Salmeterol 50 µg & Fluticasone 100 µg & Salmeterol 50 µg & Fluticasone 250 µg for patients aged 12 years and older are based upon patients asthma severity.
The maximum recommended dosage is Salmeterol 50 µg & Fluticasone 500 µg twice daily.
Pediatric Patients (4 to 11 Years): For patients with asthma who are not controlled on an inhaled corticosteroid, the dosage is Salmeterol 50 µg & Fluticasone 100 µg twice daily (morning and evening, approximately 12 hours apart).

Inhalation Powder in Capsule (For COPD): Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart). Rinsing the mouth after each inhalation is advised.

Inhalation Powder in Maxhaler (For Asthma): This is a moulded plastic device containing a foil strip with 60 regularly placed blisters containing pre-dispensed inhalation powder. Patients should be made aware that Maxhaler must be used daily for optimum benefit, even when asymptomatic.

Adults and Adolescents (12 years and older)-

50/100 Maxhaler: One Inhalation twice daily
50/250 Maxhaler: One Inhalation twice daily
50/500 Maxhaler: One Inhalation twice daily

Children (4 years and older)-

50/100 Maxhaler: One Inhalation twice daily. The maximum licensed dose of fluticasone propionate delivered by this Maxhaler in children is 100 ug twice daily. There are no data available for use of this Maxhaler in children aged under 4 years.

Inhalation Powder in Maxhaler (For COPD):

Maxhaler: One Inhalation twice daily
Special patient groups: There is no need to adjust the dose in elderly patients or in those with renal impairment. There are no data available for use of this in patients with hepatic impairment.
Using the Maxhaler: This is a patient friendly, ready to use and easy to grip device. Use as per instructions for use.

AdministrationView

Using an Inhaler seems simple, but most patients do not know how to use it in the right way. If the Inhaler is used in the wrong way, less medicine can reach the lungs. Correct and regular use of the Inhaler will prevent or lessen the severity of asthma attacks.

Following simple steps can help to use Inhaler effectively (According to "National Asthma Guidelines for Medical Practitioners" published by Asthma Association):

Take off the cap.
Shake the inhaler (at least six times) vigorously before each use.
If the inhaler is new or if it has not been used for a week or more, shake it well and release one puff into the air to make sure that it works.
Breathe out as full as comfortably possible & hold the inhaler upright.
Place the actuator into mouth between the teeth and close lips around the mouthpiece.
While breathing deeply and slowly through the mouth, press down firmly add fully on the canister to release medicine.
Remove the inhaler from mouth. Continue holding breath for at least for 10 seconds or as long as it is comfortable.
If doctor has prescribed more than one inhalation per treatment, wait 1 minute between puffs (inhalations). Shake the inhaler well and repeat steps 4 to 7.
After use, replace the cap on the mouthpiece. After each treatment, rinse mouth with water.
Check your technique in front of a mirror from time to time, if you see a white mist during the inhalation, you may not have closed your lips properly around mouthpiece, or you may not be breathing in as you press the can. This indicates failure of technique. If this happens, repeat the procedure from step 4 carefully.

Instructions for Cleaning Inhaler: Clean your Inhaler at least once a week. Remove canister and rinse the plastic actuator and cap in warm water but do not put the metal canister into water. Dry the actuator and cap thoroughly and gently replace the metal canister into the actuator with a twisting motion. Put the cap on the mouthpiece.

Side effectsView

As this preparation contains Salmeterol and Fluticasone Propionate, the type and severity of adverse reactions associated with each of the compounds may be expected. There is no incidence of additional adverse events following concurrent administration of the two compounds. Adverse events, which have been associated with Salmeterol or Fluticasone Propionate, are given below.

Salmeterol: The pharmacological side effects of beta-2-agonist treatment, such as tremor, subjective palpitations and headache, have been reported, but tend to be transient and reduce with regular therapy. Cardiac arrhythmia (including atrial fibrillation, supraventricular tachycardia and extra systoles) may occur, usually in susceptible patients. There have been reports of arthralgia and hypersensitivity reactions, including rash, oedema and angioedema. There have been reports of oropharyngeal irritation. There have been rare reports of muscle cramps.

Fluticasone propionate: Hoarseness and candidiasis (thrush) of the mouth and throat can occur in some patients. Cutaneous hypersensitivity reactions have been reported. Rare cases of facial and oropharyngeal oedema have been reported. Both hoarseness and incidence of candidiasis may be relieved by gargling with water after use of Salmeterol/ Fluticasone Propionate Inhaler.

ContraindicationsView

This is contraindicated in patients with a history of hypersensitivity to any of the ingredients.

PrecautionsView

Consideration should be given to additional corticosteroid therapies, and to including administration of antibiotics if an infection is present. As with all inhaled medication containing corticosteroids, this preparation should be administered with caution in patients with active or quiescent pulmonary tuberculosis. This preparation should be administered with caution in patients with thyrotoxicosis.

InteractionsView

Both non-selective and selective β-blockers should be avoided in patients with asthma, unless there are compelling reasons for their use. Due to the very low plasma concentrations achieved after inhaled dosing clinically significant drug interactions are unlikely. Care should be taken when co-administering known strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir), as there is potential for increased systemic exposure to Fluticasone Propionate.

Pregnancy & lactationView

Administration of drugs during pregnancy and lactation should only be considered if the expected benefit to the mother is greater than any possible risk to the foetus or child. There is insufficient experience of the use of Salmeterol Xinafoate and Fluticasone Propionate in human pregnancy and lactation. There are no data available for human breast milk.

Pediatric usageView

Orally inhaled corticosteroids may cause a reduction in growth velocity when administered to paediatric patients. The long-term effects of this reduction including the impact of final adult height are unknown.

StorageView

Pressurised canister, do not puncture, break or incinerate even when apparently empty. Avoid storage in direct sunlight or heat. Store below 30°C. Keep away from eyes. Keep away from children.

Seretide

Salmeterol + Fluticasone Propionate

Inhalation Capsule 50 mcg+250 mcg Allopathic Long-acting selective β-adrenoceptor stimulants

Indications

COPD

Indication detailsView

This is indicated in the regular treatment of asthma where use of a combination product (long-acting β2-agonist and inhaled corticosteroid) is appropriate:

patients not adequately controlled with inhaled corticosteroids and 'as needed' inhaled short acting β2-agonist or
patients already adequately controlled on both inhaled corticosteroid and long-acting β2-agonist.

Therapeutic classView

Long-acting selective β-adrenoceptor stimulants, Respiratory corticosteroids

PharmacologyView

Salmeterol Xinafoate is a selective, long acting beta-2 agonist used in the treatment of asthma and other forms of diffuse airways obstruction. Fluticasone Propionate is a corticosteroid with mainly glucocorticoid activity. Fluticasone Propionate is stated to exert a topical effect on the lungs without systematic effects at usual dose.

Salmeterol protects against symptoms, Fluticasone Propionate improves lung function and prevents exacerbations of the condition. This preparation can offer a more convenient regime for patients on concurrent β-agonist and inhaled corticosteroid therapy. The respective mechanisms of action of both drugs are discussed below:

Salmeterol: Salmeterol is a selective long-acting (12 hour) beta-2-adrenoceptor agonist with a long side chain which binds to the exo-site of the receptor.

Fluticasone Propionate: Fluticasone Propionate given by inhalation at recommended doses has a potent glucocorticoid anti-inflammatory action within the lungs, resulting in reduced symptoms and exacerbaions of asthma, without the adverse effects observed when corticosteroids are administered systemically.

DosageView

Inhalation Aerosol:

Adults and adolescents 12 years and older: 2 puffs of 25 µg Salmeterol and 50 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 125 µg Fluticasone Propionate twice daily or 2 puffs of 25 µg Salmeterol and 250 µg Fluticasone Propionate twice daily.
Children (4-12 years): 2 puffs of 25 µg salmeterol and 50 µg Fluticasone Propionate twice daily.

Inhalation Powder in Capsule (For Asthma):

Adult and Adolescent (12 Years and Older): Salmeterol 50 µg & Fluticasone 100 µg or Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart).
The recommended starting dosages for Salmeterol 50 µg & Fluticasone 100 µg & Salmeterol 50 µg & Fluticasone 250 µg for patients aged 12 years and older are based upon patients asthma severity.
The maximum recommended dosage is Salmeterol 50 µg & Fluticasone 500 µg twice daily.
Pediatric Patients (4 to 11 Years): For patients with asthma who are not controlled on an inhaled corticosteroid, the dosage is Salmeterol 50 µg & Fluticasone 100 µg twice daily (morning and evening, approximately 12 hours apart).

Inhalation Powder in Capsule (For COPD): Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart). Rinsing the mouth after each inhalation is advised.

Inhalation Powder in Maxhaler (For Asthma): This is a moulded plastic device containing a foil strip with 60 regularly placed blisters containing pre-dispensed inhalation powder. Patients should be made aware that Maxhaler must be used daily for optimum benefit, even when asymptomatic.

Adults and Adolescents (12 years and older)-

50/100 Maxhaler: One Inhalation twice daily
50/250 Maxhaler: One Inhalation twice daily
50/500 Maxhaler: One Inhalation twice daily

Children (4 years and older)-

50/100 Maxhaler: One Inhalation twice daily. The maximum licensed dose of fluticasone propionate delivered by this Maxhaler in children is 100 ug twice daily. There are no data available for use of this Maxhaler in children aged under 4 years.

Inhalation Powder in Maxhaler (For COPD):

Maxhaler: One Inhalation twice daily
Special patient groups: There is no need to adjust the dose in elderly patients or in those with renal impairment. There are no data available for use of this in patients with hepatic impairment.
Using the Maxhaler: This is a patient friendly, ready to use and easy to grip device. Use as per instructions for use.

AdministrationView

Using an Inhaler seems simple, but most patients do not know how to use it in the right way. If the Inhaler is used in the wrong way, less medicine can reach the lungs. Correct and regular use of the Inhaler will prevent or lessen the severity of asthma attacks.

Following simple steps can help to use Inhaler effectively (According to "National Asthma Guidelines for Medical Practitioners" published by Asthma Association):

Take off the cap.
Shake the inhaler (at least six times) vigorously before each use.
If the inhaler is new or if it has not been used for a week or more, shake it well and release one puff into the air to make sure that it works.
Breathe out as full as comfortably possible & hold the inhaler upright.
Place the actuator into mouth between the teeth and close lips around the mouthpiece.
While breathing deeply and slowly through the mouth, press down firmly add fully on the canister to release medicine.
Remove the inhaler from mouth. Continue holding breath for at least for 10 seconds or as long as it is comfortable.
If doctor has prescribed more than one inhalation per treatment, wait 1 minute between puffs (inhalations). Shake the inhaler well and repeat steps 4 to 7.
After use, replace the cap on the mouthpiece. After each treatment, rinse mouth with water.
Check your technique in front of a mirror from time to time, if you see a white mist during the inhalation, you may not have closed your lips properly around mouthpiece, or you may not be breathing in as you press the can. This indicates failure of technique. If this happens, repeat the procedure from step 4 carefully.

Instructions for Cleaning Inhaler: Clean your Inhaler at least once a week. Remove canister and rinse the plastic actuator and cap in warm water but do not put the metal canister into water. Dry the actuator and cap thoroughly and gently replace the metal canister into the actuator with a twisting motion. Put the cap on the mouthpiece.

Side effectsView

As this preparation contains Salmeterol and Fluticasone Propionate, the type and severity of adverse reactions associated with each of the compounds may be expected. There is no incidence of additional adverse events following concurrent administration of the two compounds. Adverse events, which have been associated with Salmeterol or Fluticasone Propionate, are given below.

Salmeterol: The pharmacological side effects of beta-2-agonist treatment, such as tremor, subjective palpitations and headache, have been reported, but tend to be transient and reduce with regular therapy. Cardiac arrhythmia (including atrial fibrillation, supraventricular tachycardia and extra systoles) may occur, usually in susceptible patients. There have been reports of arthralgia and hypersensitivity reactions, including rash, oedema and angioedema. There have been reports of oropharyngeal irritation. There have been rare reports of muscle cramps.

Fluticasone propionate: Hoarseness and candidiasis (thrush) of the mouth and throat can occur in some patients. Cutaneous hypersensitivity reactions have been reported. Rare cases of facial and oropharyngeal oedema have been reported. Both hoarseness and incidence of candidiasis may be relieved by gargling with water after use of Salmeterol/ Fluticasone Propionate Inhaler.

ContraindicationsView

This is contraindicated in patients with a history of hypersensitivity to any of the ingredients.

PrecautionsView

Consideration should be given to additional corticosteroid therapies, and to including administration of antibiotics if an infection is present. As with all inhaled medication containing corticosteroids, this preparation should be administered with caution in patients with active or quiescent pulmonary tuberculosis. This preparation should be administered with caution in patients with thyrotoxicosis.

InteractionsView

Both non-selective and selective β-blockers should be avoided in patients with asthma, unless there are compelling reasons for their use. Due to the very low plasma concentrations achieved after inhaled dosing clinically significant drug interactions are unlikely. Care should be taken when co-administering known strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir), as there is potential for increased systemic exposure to Fluticasone Propionate.

Pregnancy & lactationView

Administration of drugs during pregnancy and lactation should only be considered if the expected benefit to the mother is greater than any possible risk to the foetus or child. There is insufficient experience of the use of Salmeterol Xinafoate and Fluticasone Propionate in human pregnancy and lactation. There are no data available for human breast milk.

Pediatric usageView

Orally inhaled corticosteroids may cause a reduction in growth velocity when administered to paediatric patients. The long-term effects of this reduction including the impact of final adult height are unknown.

StorageView

Pressurised canister, do not puncture, break or incinerate even when apparently empty. Avoid storage in direct sunlight or heat. Store below 30°C. Keep away from eyes. Keep away from children.

Sergel

Esomeprazole

Oral Powder 20 mg Allopathic

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 (C_max) occur at approximately 1.5 hours (T_max). The C_maxincreases 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.

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.

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.

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.

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.

Sergel

Esomeprazole

Tablet (Enteric Coated) 40 mg Allopathic

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 (C_max) occur at approximately 1.5 hours (T_max). The C_maxincreases 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.

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.

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.

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.

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.

Sergel

Esomeprazole

Tablet (Enteric Coated) 20 mg Allopathic

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 (C_max) occur at approximately 1.5 hours (T_max). The C_maxincreases 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.

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.

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.

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.

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.

Sergel

Esomeprazole

IV Injection 40 mg/vial Allopathic

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 (C_max) occur at approximately 1.5 hours (T_max). The C_maxincreases 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.

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.

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.

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.

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.

Sergel

Esomeprazole

Capsule (Delayed Release) 40 mg Allopathic

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 (C_max) occur at approximately 1.5 hours (T_max). The C_maxincreases 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.

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.

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.

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.

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.

Sergel

Esomeprazole

Capsule (Delayed Release) 20 mg Allopathic

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 (C_max) occur at approximately 1.5 hours (T_max). The C_maxincreases 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.

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.

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.

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.

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.

Sergel MUPS

Esomeprazole (MUPS tablet)

MUPS Tablet 40 mg Allopathic

Indication detailsView

Esomeprazole MUPS tablet is indicated in:

Gastro-esophageal Reflux Disease (GERD).
Risk reduction in NSAID associated gastric ulcer.
H. pylori eradication (Triple therapy).
Zollinger-Ellison syndrome and idiopathic hypersecretion.

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.

DosageView

Erosive esophagitis-

Adult (≥18 years): 40 mg once daily for 4 weeks.
Children & adolescents (12-18 years): 40 mg once daily for 4 weeks.

Maintenance of healing of erosive esophagitis-

Adult (≥18 years): 20 mg once daily.
Children & adolescents (12-18 years): 20 mg once daily.

Risk reduction in NSAID associated gastric ulcer-

Adult (≥18 years): 20 mg once daily for 4-8 weeks.

H. pylori eradication (Esomeprazole MUPS tablet with 1000 mg Amoxicillin and 500 mg Clarithromycin)-

Adult (≥18 years): 20 mg twice daily for 7 days.
Children & adolescents (12-18 years): 20 mg twice daily for 7 days.

Zollinger-Ellison syndrome and idiopathic hypersecretion-

Adult (≥18 years): 40-80 mg twice daily.

Children 1-11 years:

Erosive esophagitis: Weight <20 kg: 10 mg once daily for 8 weeks. Weight ≥20 kg: 10 mg or 20 mg once daily for 8 weeks
Maintenance of healing of erosive esophagitis: 10 mg once daily

Children below the age of 1 year: Esomeprazole MUPS tablet is not approved for use in children younger than 1 year.

AdministrationView

Esomeprazole MUPS tablets should be swallowed whole with liquid. The tablets should not be chewed or crushed. If required, the tablets can also be dispersed in half a glass of non-carbonated water (mineral water is not suitable). No other liquids should be used. Stir until the tablets disintegrate and drink the liquid with the pellets immediately or within 30 minutes. Rinse the glass with half a glass of water and drink. The pellets must not be chewed or crushed.

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

Esomeprazole should be used carefully if the patient has severe liver dysfunction and severe renal impairment. Taking a proton pump inhibitor like Esomeprazole may slightly increase the risk of hip, wrist and spine fracture, particularly when it is taken over a period of more than one year.

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 anddiazepam, 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

The manufacturer advises caution. It is not known if Esomeprazole or its metabolites appear in human breast milk.

StorageView

Store in a cool & dry place below 25ºC, protect from light. Keep out of reach of children.

Sergel MUPS

Esomeprazole (MUPS tablet)

MUPS Tablet 20 mg Allopathic

Indication detailsView

Esomeprazole MUPS tablet is indicated in:

Gastro-esophageal Reflux Disease (GERD).
Risk reduction in NSAID associated gastric ulcer.
H. pylori eradication (Triple therapy).
Zollinger-Ellison syndrome and idiopathic hypersecretion.

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.

DosageView

Erosive esophagitis-

Adult (≥18 years): 40 mg once daily for 4 weeks.
Children & adolescents (12-18 years): 40 mg once daily for 4 weeks.

Maintenance of healing of erosive esophagitis-

Adult (≥18 years): 20 mg once daily.
Children & adolescents (12-18 years): 20 mg once daily.

Risk reduction in NSAID associated gastric ulcer-

Adult (≥18 years): 20 mg once daily for 4-8 weeks.

H. pylori eradication (Esomeprazole MUPS tablet with 1000 mg Amoxicillin and 500 mg Clarithromycin)-

Adult (≥18 years): 20 mg twice daily for 7 days.
Children & adolescents (12-18 years): 20 mg twice daily for 7 days.

Zollinger-Ellison syndrome and idiopathic hypersecretion-

Adult (≥18 years): 40-80 mg twice daily.

Children 1-11 years:

Erosive esophagitis: Weight <20 kg: 10 mg once daily for 8 weeks. Weight ≥20 kg: 10 mg or 20 mg once daily for 8 weeks
Maintenance of healing of erosive esophagitis: 10 mg once daily

Children below the age of 1 year: Esomeprazole MUPS tablet is not approved for use in children younger than 1 year.

AdministrationView

Esomeprazole MUPS tablets should be swallowed whole with liquid. The tablets should not be chewed or crushed. If required, the tablets can also be dispersed in half a glass of non-carbonated water (mineral water is not suitable). No other liquids should be used. Stir until the tablets disintegrate and drink the liquid with the pellets immediately or within 30 minutes. Rinse the glass with half a glass of water and drink. The pellets must not be chewed or crushed.

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

Esomeprazole should be used carefully if the patient has severe liver dysfunction and severe renal impairment. Taking a proton pump inhibitor like Esomeprazole may slightly increase the risk of hip, wrist and spine fracture, particularly when it is taken over a period of more than one year.

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 anddiazepam, 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

The manufacturer advises caution. It is not known if Esomeprazole or its metabolites appear in human breast milk.

StorageView

Store in a cool & dry place below 25ºC, protect from light. Keep out of reach of children.

Seridol

Paracetamol

Tablet 500 mg Allopathic Non opioid analgesics

Indications

Toothache

Indication detailsView

Paracetamol is indicated for fever, common cold and influenza, headache, toothache, earache, bodyache, myalgia, neuralgia, dysmenorrhoea, sprains, colic pain, back pain, post-operative pain, postpartum pain, inflammatory pain and post vaccination pain in children. It is also indicated for rheumatic & osteoarthritic pain and stiffness of joints.

Therapeutic classView

Non opioid analgesics

PharmacologyView

Paracetamol has analgesic and antipyretic properties with weak anti-inflammatory activity. Paracetamol (Acetaminophen) is thought to act primarily in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1, COX-2, and COX-3 enzymes involved in prostaglandin (PG) synthesis. Paracetamol is a para aminophenol derivative, has analgesic and antipyretic properties with weak anti-inflammatory activity. Paracetamol is one of the most widely used, safest and fast acting analgesic. It is well tolerated and free from various side effects of aspirin.

DosageView

Tablet:

Adult: 1-2 tablets every 4 to 6 hours up to a maximum of 4 gm (8 tablets) daily.
Children (6-12 years): ½ to 1 tablet 3 to 4 times daily. For long term treatment it is wise not to exceed the dose beyond 2.6 gm/day.

Extended Release Tablet:

Adults & Children over 12 years: Two tablets, swallowed whole, every 6 to 8 hours (maximum of 6 tablets in any 24 hours).The tablet must not be crushed.

Syrup/Suspension:

Children under 3 months: 10 mg/kg body weight (reduce to 5 mg/kg if jaundiced) 3 to 4 times daily.
3 months to below 1 year: ½ to 1 teaspoonful 3 to 4 times daily.
1-5 years: 1 -2 teaspoonful 3 to 4 times daily.
6-12 years: 2-A teaspoonful 3 to 4 times daily.
Adults: 4-8 teaspoonful 3 to 4 times daily.

Suppository:

Children 3-12 months: 60-120 mg,4 times daily.
Children 1-5 years: 125-250 mg 4 times daily.
Children 6-12 years: 250-500 mg 4 times daily.
Adults & children over 12 years: 0.5-1 gm 4 times daily.

Paediatric Drop:

Children Upto 3 months: 0.5 ml (40 mg)
4 to 11 months: 1.0 ml (80 mg)
7 to 2 years: 1.5 ml (120 mg). Do not exceed more than 5 dose daily for a maximum of 5 days.

Paracetamol tablet with actizorb technology: It dissolves up to five times faster than standard Paracetamol tablets. It is a fast acting and safe analgesic with marked antipyretic property. It is specially suitable for patients who, for any reason, can not tolerate aspirin or other analgesics.

Adults and children (aged 12 years and over): Take 1 to 2 Tablets every four to six hours as needed. Do not take more than 8 caplets in 24 hours.
Children (7 to 11 years): Take ½-1 Tablet every four to six hours as needed. Do not take more than 4 caplets in 24 hours. Not recommended in children under 7 years.

Side effectsView

Side effects of paracetamol are usually mild, though haematological reactions including thrombocytopenia, leucopenia, pancytopenia, neutropenia, and agranulocytosis have been reported. Pancreatitis, skin rashes, and other allergic reactions occur occasionally.

ContraindicationsView

It is contraindicated in known hypersensitivity to Paracetamol.

PrecautionsView

Paracetamol should be given with caution to patients with impaired kidney or liver function. Paracetamol should be given with care to patients taking other drugs that affect the liver.

InteractionsView

Patients who have taken barbiturates, tricyclic antidepressants and alcohol may show diminished ability to metabolise large doses of Paracetamol. Alcohol can increase the hepatotoxicity of Paracetamol overdosage. Chronic ingestion of anticonvulsants or oral steroid contraceptives induce liver enzymes and may prevent attainment of therapeutic Paracetamol levels by increasing first-pass metabolism or clearance.

Pregnancy & lactationView

Pregnancy category B according to USFDA. This drug should be used during pregnancy only if clearly needed

Overdose effectsView

Symptoms of Paracetamol overdose in the first 24 hours are pallor, nausea, vomiting, anorexia and abdominal pain. Liver damage may become apparent 12-48 hours after ingestion. Abnormalities of glucose metabolism and metabolic acidosis may occur.

StorageView

Keep in a dry place away from light and heat. Keep out of the reach of children.

Serifen

Dexibuprofen

Tablet 400 mg Allopathic Drugs for Osteoarthritis

Indications

Rheumatic disorders

Indication detailsView

Dexibuprofen is indicated in-

The relief of sign and symptoms of osteoarthritis.
Indicated in rheumatoidal disorders such as osseous rheumatism, ankylosing spondilitis, juvenile arthritis, muscular rheumatism, degenerative joint diseases
Acute symptomatic treatment of painful menstruation (primary dysmenorrhoea)
Common headache and fever
Symptomatic treatment of mild to moderate pain, such as muscle pain, headache and dental pain
As an adjuvant with common cold and influenza associated with headache.

Therapeutic classView

Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)

PharmacologyView

Dexibuprofen (S (+)-ibuprofen) is considered as the pharmacologically active enantiomer of racemic ibuprofen. Like racemic ibuprofen, Dexibuprofen is a non-steroidal anti-inflammatory drug with analgesic action. Like ibuprofen, Dexibuprofen acts by inhibiting prostaglandin synthesis.

Pharmacokinetics: Dexibuprofen is absorbed primarily from the small intestine. After metabolic transformation in the liver (hydroxylation, carboxylation) the pharmacologically inactive metabolites are completely excreted, mainly by the kidneys (90%), but also in the bile. The elimination half-life is 1.8-3.5 hours; the plasma protein binding is about 99%. Maximum plasma levels are reached about 2 hours after oral administration. The administration of dexibuprofen with a meal delays the time to reach maximum concentrations (from 2.1 hours after fasting conditions to 2.8 hours after non-fasting conditions) and decreases the maximum plasma concentrations (from 20.6 to 18.1 mcg/ml, which is of no clinical relevance), but has no effect on the extent of absorption.

DosageView

The dosage must be adjusted to the seriousness of the syndrome and the complaints of the patient. During chronic pain, the dosage must be adapted to the lowest effective dose.

The recommended dosage: 600-900 mg Dexibuprofen per day, at 2-3 divided doses. The dosage can be raised temporarily up to 1200 mg Dexibuprofen per day in patients with acute disorders or exacerbations. The maximum daily dose is 1200 mg.

At dysmenorrhea: A dosage of 600 up to 900 mg Dexibuprofen per day, at a divided dose.

Side effectsView

Clinical experience has shown that adverse effects of Dexibuprofen are similar to those of racemic ibuprofen. Common side-effects are dyspepsia, diarrhea, fatigue, and headache, nausea, vomiting, abdominal pain, hypersensitivity reactions - bleeding, ulcer.

ContraindicationsView

Dexibuprofen is contraindicated in patients with previous history of hypersensitivity to Dexibuprofen, or another NSAID, or any other component of the product. Patients, who experience attack of asthma, arouse bronchospasm, acute rhinitis, urticaria or edema after use of similar drugs (e.g. aspirin or other NSAID's). It is also contraindicated in patients with active or suspected hemorrhage, Crohn's disease or ulcerative colitis, patients with serious heart diseases, kidney function impairment (GFR <30ml/min), and liver function impairment.

PrecautionsView

Dexibuprofen should be used with particular caution in patients with bronchial asthma or other chronic diseases of the pulmonary tract as well as in persons prone to allergy. The drug should be used in patients with hepatic, renal or cardiac insufficiency and with hypertension not responding to any treatment. Consultation with a doctor is recommended for patients with systemic lupus or with other autoimmunological disease before beginning therapy using the drug. Dexibuprofen should be used with extreme cautions in active and suspected hemorrhagic conditions such as gastro-duodenal ulcers, ulcerative colitis, Crohn's disease, alcoholism. Allergic reactions to the drug may appear even for the first-time user and in such case, it should immediately be stopped.

InteractionsView

The reported drug interactions of Dexibuprofen are similar to that of racemic mixture of ibuprofen. Drug interactions is noticed with simultaneous use of anticoagulant, hydantoine and sulfonamide, ticlopidine, lithium, other NSAID's, ACE inhibitors, beta blockers, cyclosporine, tacrolimus, corticosteroids, digoxin, methotrexate, pentoxyfiline, phenytoine, probenecid, sulfinpyrazon, sulfonylurea, thiazide and thiazide type diuretics, and zidovudine.

Pregnancy & lactationView

Pregnancy: Although no teratogennic impact has been observed in the animal-experimental research with dexibuprofen or ibuprofen, the use should be avoided during the pregnancy. However, animal reproduction studies are not always predictive of human response. Because of the known effects of nonsteroidal anti-inflammatory drugs on the fetal cardiovascular system (closure of ductus arteriosus), use during late pregnancy should be avoided.

Lactation: Studies at people have shown that racimic ibuprofen proceed in small to negligible degree in mother milk. So, Dexibuprofen should be used with cautions in nursing mothers.

Pediatric usageView

Hepatic impairment: Patients with mild to moderate liver function impairments must start with low amounts, and must closely be monitored. Dexibuprofen should not be used in patients with serious liver function impairments.

Renal impairment: The start amount must be reduced at patients with mild to moderate kidney function impairments. Dexibuprofen cannot be used patients with serious kidney function impairments.

Children Dose: Although Dexibuprofen is not licensed for use in children under 18 years of age in the UK, some countries permit such use. For example, in Switzerland, Dexibuprofen has been given to children aged 6 years and over at a dose of 10 to 15 mg/kg daily in 2-4 divided doses.

For elderly people: Lowest effective dose is recommended. The dosage can be raised to adult dosage if well tolerated.

Overdose effectsView

Dexibuprofen has low acute toxicities. Symptoms of toxicity occur at doses between 80 and 100 mg/kg body weight. Mild symptoms are abdominal pain, nausea, vomiting, lethargy, headache, tinnitus and ataxia. Moderate to serious symptoms, such as flatulence, hypotension, hypothermia, metabolic acidosis, reduced kidney function, coma, and apnoea. The treatment must be symptomatic: there is no specific antidote. In case of large quantities of Dexibuprofen, activated charcoal should be administered. Vomiting can be induced only when life-threatening quantities of the substance ingested and the procedure can be carried out within 60 minutes after ingestion. Dialysis and hemodialysis are of little value as Dexibuprofen binds strongly to plasma protein.

StorageView

Do not store above 30°C. Keep away from light and out of the reach of children