Sergel MUPS 40 mg

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: 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.

Paediatric use: The safety and effectiveness of esomeprazole in paediatric patients have not been established.

Geriatric use: No overall differences in safety and efficacy have been observed between elderly and younger people. Other clinical experience reported so far hasn't found differences in response either. Still, greater sensitivity in some older people cannot be ruled out.

Hepatic insufficiency: No dose adjustment is recommended for patients with mild to moderate hepatic insufficiency. In severe hepatic insufficiency, however, the dose should not go above 20 mg once daily.

Renal insufficiency: The pharmacokinetics of Esomep in patients with renal impairment are not expected to differ from those in healthy volunteers, because less than 1% of Esomep is excreted unchanged in the urine.

A single oral dose of Esomep at 510 mg/kg, which is about 103 times the human dose on a body surface area basis, was lethal to rats. The main signs of acute toxicity were reduced motor activity, changes in respiratory frequency, tremor, ataxia and intermittent clonic convulsions.

There have been no reports of overdose with Esomep, and no specific antidote is known. Esomep is extensively protein bound, so dialysis is not expected to remove it. If an overdose does happen, treatment should be symptomatic and supportive. As with any overdose, the possibility that more than one drug was taken should be considered.

Keep Esomeprazole in a dry place at a temperature not above 30°C. Protect it from light and moisture. Keep it out of reach of children.