Esomep^®

Esomep is a preparation of Esomeprazole which is the S-isomer of Omeprazole, a proton pump inhibitor, weak base in nature and is concentrated and converted to the active form in the highly acidic environment of the intracellular canaliculi within the parietal cell, where it inhibits the enzyme H⁺/K⁺-ATPase, the acid pump. This effect on the final step of the gastric acid formation process is dose-dependent and provides for highly effective inhibition of both basal and stimulated acid secretion, irrespective of the stimulus.

No Data

Esomep is indicated for:
Treatment of gastroesophageal reflux disease (GERD)
- Healing of erosive esophagitis
- Maintenance of healing of erosive esophagitis
- Symptomatic treatment of gastroesophageal reflux disease (GERD)
Risk reduction of NSAID-associated gastric ulcer
- Healing of gastric ulcers associated with NSAID therapy
- Prevention of gastric and duodenal ulcers associated with NSAID
H. pylori eradication to reduce the risk of duodenal ulcer recurrence
- Healing of H. pylori associated duodenal ulcer
- Prevention of relapse of peptic ulcers in patient with H. pylori associated
Pathological hypersecretory conditions including Zollinger-Ellison Syndrome

Route of administration: Esomep can be taken by oral and parenteral route.

Esomep tablet and capsule
The recommended adult dosages outlined in the table below. Esomep tablet and capsule should be taken one hour before meal.

*The majority of patients are healed within 4 to 8 weeks. For patients who do not heal after 4-8 weeks, an additional 4-8 weeks of treatment may be considered.
** Controlled studies did not extend beyond six months.
***If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
+ Doses over 1 mg/kg/day have not been studied.

Direction for use of intravenous injection: Solution for injection should be prepared by adding 5 ml 0.9% w/v Sodium Chloride BP into the vial containing the powder. The reconstituted solution for injection is clear and colorless to very slightly yellow. The reconstituted solution should be given as an intravenous injection over a period of at least 3 minutes. Half of the IV injection should be used when 20 mg is to be administrated. Use only freshly prepared solution. The reconstituted solution should be stored at room temperature (below 250C) and should be administered within 12 hours after reconstitution. No refrigeration is required.

Esomep IV injection for GERD patients with Erosive Esophagitis (EE)

Patients with impaired hepatic function: No dosage adjustment is necessary in patients with mild to moderate liver impairment. For patients with severe liver impairment a dose of 20 mg of esomeprazole should not be exceeded.

Patients with renal impairment: No dose adjustment is necessary in patients with impaired renal function.

Use in pregnancy and lactation
Pregnancy: Esomeprazole is pregnancy category B drug. Animal studies have revealed no teratogenic effects. No sufficient clinical data is available on exposed pregnancies for esomeprazole. So, caution should be exercised when prescribing to pregnant women.

Lactation: It is not known whether esomeprazole is excreted in human breast milk. Therefore esomeprazole should not be used during breastfeeding.

Use in children and adolescents
The safety and effectiveness of esomeprazole have not been established in patients less than 1 month of age.

Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy. When gastric ulcer is suspected or present, malignancy should be excluded, as treatment with esomeprazole may alleviate symptoms and delay diagnosis. When prescribing esomeprazole for eradication of H. pylori possible drug interactions for all components in the triple therapy should be considered.

The most common side effects of esomeprazole are nausea, vomiting, abdominal pain, flatulence, diarrhoea, constipation and headache. Less frequent side effects include dry mouth, peripheral edema, dizziness, sleep disturbances, fatigue, paraesthesia, arthralgia, myalgia, rash, and pruritus. Other side effects reported rarely or very rarely include taste disturbance, stomatitis, hepatitis, jaundice, hypersensitivity reactions (including anaphylaxis, bronchospasm), fever, depression, hallucinations, confusion, gynaecomastia, interstitial nephritis, hyponatraemia, blood disorders (including leucopenia, leucocytosis, pancytopenia, thrombocytopenia), visual disturbances, sweating, photosensitivity, alopecia, Stevens-Johnson syndrome, and toxic epidermal necrolysis.

Esomeprazole is contraindicated in patients with known hypersensitivity to esomeprazole or any components of this product.

Drug interaction with medications: Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin). Coadministration of atazanavir with esomeprazole is expected to substantially decrease atazanavir plasma concentrations and thereby reduce its therapeutic effect. Esomeprazole inhibits CYP2C19, the major esomeprazole metabolising enzyme. Thus, when esomeprazole is combined with drugs metabolised by CYP2C19, such as diazepam, citalopram, imipramine, clomipramine and phenytoin, the plasma concentrations of these drugs may be increased and a dose reduction could be needed.

Drug interaction with food and others: Not applicable.

There is very limited experience to date with deliberate overdose. The symptoms described in connection with 280 mg were gastrointestinal symptoms and weakness. Single doses of 80 mg esomeprazole were uneventful. No specific antidote is known. Esomeprazole is extensively plasma protein bound and is therefore not readily dialyzable. As in any case Of overdose, treatment should be symptomatic and general supportive measures should be utilised.

No Data

Esomep^® capsule and tablet: Store in a cool & dry place. Protect from light.
Esomep^® IV injection: Store in a cool (below 30°C) & dry place. Protect from light.

Esomep 20 mg tablet: Each enteric coated tablet contains Esomeprazole 20 mg as Magnesium Trihydrate USP.
Esomep 40 mg tablet: Each enteric coated tablet contains Esomeprazole 40 mg as Magnesium Trihydrate USP.
Esomep 20 mg capsule: Each capsule contains Esomeprazole 20 mg as Magnesium Trihydrate USP as enteric coated pellets.
Esomep 40 mg capsule: Each capsule contains Esomeprazole 40 mg as Magnesium Trihydrate USP as enteric coated pellets.
Esomep 40 mg IV injection: Each vial contains Lyophilized Esomeprazole 40 mg as Sodium INN.

Storage
Store in a cool (below 25°C) and dry place protected from light. Keep away from the reach of children.

Packing
Esomep 20 mg tablet: Carton of 50 tablets in blister.
Esomep 40 mg tablet: Carton of 30 tablets in blister.
Esomep 20 mg capsule: Carton of 50 capsules in blister.
Esomep 40 mg capsule: Carton of 40 capsules in blister.
Esomep 40 mg IV injection: Carton containing 1 vial of 40 mg Lyophilized Esomeprazole, 1 ampoule of 5 ml Salinor@(0.9% w/v Sodium Chloride BP) as diluent.
Esomep 40 mg IV injection manufactured by Popular Pharmaceuticals Ltd. (Only API Part) for Advanced Chemical Industries Limited.