Informational only — Not medical advice. Always consult a licensed healthcare provider.

Shasthya স্বাস্থ্য · Health, made simple
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Community data Updated 2 months ago
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Indications

Gastroesophageal Reflux Disease Peptic Ulcer Dyspepsia Helicobacter Pylori Infection

Esomium is used to relieve chronic heartburn and other symptoms of GERD, and to heal and then maintain healing of erosive esophagitis. It is also given together with amoxicillin and clarithromycin to help eradicate *Helicobacter pylori* infection in patients with duodenal ulcer disease. Other uses include Zollinger-Ellison syndrome, acid-related dyspepsia, and duodenal and gastric ulcers.

⚠️ Always consult a registered physician before taking any medicine.

Pharmacology

Esomeprazole is a proton pump inhibitor. It reduces stomach acid by specifically blocking the H+/K+-ATPase enzyme (the proton pump) in the parietal cells of the stomach lining. Esomeprazole is the S-isomer of omeprazole, and it was the first single optical isomer of a proton pump inhibitor. It gives better acid control than the racemic proton pump inhibitors.

Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration, peak plasma levels (Cmax) are reached at about 1.5 hours (Tmax). Cmax rises in proportion to the dose, and the area under the plasma concentration-time curve (AUC) increases three-fold when the dose goes from 20 mg to 40 mg. With repeated once-daily dosing, systemic bioavailability is about 90%, compared with 64% after a single dose. Food reduces the AUC after a single dose by 33-53% compared with fasting. So esomeprazole should be taken at least one hour before meals.

Distribution: About 97% of esomeprazole is bound to plasma proteins. This binding stays constant across the concentration range of 2 to 20 mmol/L. In healthy volunteers, the apparent volume of distribution at steady state is about 16 L.

Metabolism: Esomeprazole is extensively metabolised in the liver by the cytochrome P450 (CYP) enzyme system. Its metabolites have no anti-secretory activity. Most of the metabolism depends on the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The rest depends on CYP3A4, which forms the sulphone metabolite.

Excretion: The plasma elimination half-life of esomeprazole is about 1 to 1.5 hours. Less than 1% of the parent drug is excreted in urine. About 80% of an oral dose is excreted in urine as inactive metabolites, and the remainder is found as inactive metabolites in faeces.

Combination therapy with antimicrobials: Esomeprazole magnesium 40 mg once daily is given together with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. During this triple combination, the mean steady-state AUC and Cmax of esomeprazole increase by 70% and 18%, respectively, compared with esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are much the same whether they are given in the triple combination or alone. The mean AUC and Cmax of 14-hydroxyclarithromycin do rise, by 19% and 22%, during triple therapy compared with clarithromycin alone. This rise in exposure to 14-hydroxyclarithromycin is not considered clinically significant.

Pregnancy & Breastfeeding

Pregnancy: There isn't enough well-controlled research on esomeprazole use in pregnant women, though animal studies have not shown any effect on fetal development.

Breastfeeding: It is not known whether esomeprazole passes into breast milk. If a doctor decides the medicine is essential, breastfeeding should be stopped while taking it.

⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.

Dosage Reference

⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.

Adults: For oral dosage forms, healing of erosive esophagitis is achieved with 20 mg or 40 mg once daily for 4 to 8 weeks, and most patients heal within that period. For patients who do not heal after 4 to 8 weeks, an additional 4 to 8 weeks of treatment may be considered. Maintenance of healing of erosive esophagitis uses 20 mg once daily, though clinical studies did not extend beyond 6 months. Symptomatic GERD is treated with 20 mg once daily for 4 weeks, and if symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered. For Helicobacter Pylori eradication using triple therapy to reduce the risk of duodenal ulcer recurrence, Esomeprazole 40 mg once daily is given for 10 days together with Amoxicillin 1000 mg twice daily for 10 days and Clarithromycin 500 mg twice daily for 10 days. For Zollinger-Ellison Syndrome, the dose is 20 to 80 mg once daily, adjusted individually, with treatment continued as long as clinically indicated. Acid related dyspepsia is treated with 20 to 40 mg once daily for 2 to 4 weeks according to response. Duodenal ulcer is treated with 20 mg once daily for 2 to 4 weeks. Gastric ulcer is treated with 20 to 40 mg once daily for 4 to 8 weeks. For IV injection or IV infusion in GERD with erosive esophagitis, adult patients aged 18 years and above receive 20 mg or 40 mg once daily, given as an IV injection over more than 3 minutes or as an IV infusion over 10 to 30 minutes. In pediatric patients aged 1 year to 17 years, those with body weight under 55 kg receive 10 mg once daily, and those with body weight of 55 kg or more receive 20 mg once daily. Pediatric patients aged 1 month to under 1 year receive 0.5 mg per kg once daily, given as an IV infusion over 10 to 30 minutes. For risk reduction of rebleeding of gastric or duodenal ulcers following therapeutic endoscopy in adults, adult patients aged 18 years and above receive 80 mg as an IV infusion over 30 minutes, followed by a continuous infusion of 8 mg per hour for a total treatment duration of 72 hours.

Side Effects & Interactions

Side Effects

No side-effect data recorded yet.