Esmosim

Generic composition: Esomeprazole

General Introduction

Esomeprazole is an S-enantiomer of omeprazole, claimed to have higher oral bioavailability and produce better control of gastric pH than omeprazole.

Therapeutic category

• Proton pump inhibitors

Dosage forms available

• ESMOSIM 20mg Tablets
• ESMOSIM 40mg Tablets

Mechanism of action

• Like all other PPIs, it blocks the enzyme H⁺-K⁺ATPase in the wall of the stomach thereby suppressing acid production and helps in healing of ulcers.

Pharmacokinetics

• Absorption: Peak plasma concentration occur at approximately 1.5 hours after oral administration, esomeprazole is decreased by 43% to 53% after food intake compared to fasting conditions, 97% plasma protein bound
• Metabolism: extensively metabolized in liver by cytochrome P450 enzyme
• Elimination: 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 feces.
• Half-life: 1-1.5 hours

Uses

• GERD
• Dyspepsia
• Gastritis
• Peptic ulcer
• Zollinger-Ellison Syndrome
• Heartburn

 Dose

• 1 tablet to be taken once a day in empty stomach
• 20-40mg once daily for 4-8 weeks for healing erosive esophaigitis, peptic ulcer, 20mg once daily as a maintenance dose,
• 20mg once daily for up to 4 weeks for GERD and can be additionally taken up to 4 weeks,
• 10 days of triple therapy with esomeprazole 40 mg once daily, amoxicillin 1g and clarithromycin 500 mg twice daily for eradication of H. Pylori

Side effects

• The most frequently occurring adverse events were headache, diarrhea, nausea, flatulence, abdominal pain and constipation.

 Contraindications

• Hypersensitivity to esomeprazole or to substituted benzimidazoles.

Precautions

• Because treatment with esomeprazole may alleviate symptoms and delay diagnosis, patients on long-term treatment should be kept under regular surveillance.
• Caution should be exercised in pregnant and nursing mothers.

Drug interaction

• Atazanavir: Plasma concentrations may be reduced by esomeprazole, decreasing the efficacy.
• Diazepam: Plasma concentrations may be increased by esomeprazole; however, the increase not likely to be clinically important.
• Drugs dependent on gastric pH for bioavailability (eg, ampicillin, cyanocobalamin, digoxin, iron salts, ketoconazole) – Absorption of these drugs may be affected.
• Warfarin: Risk of bleeding may be increased