Esomeprazole

General information

Esomeprazole is the S-isomer of omeprazole. The pharmacology, pharmacokinetics, efficacy, and safety of esomeprazole have been reviewed [ ]. Esomeprazole produces acid control comparable to that of currently available proton pump inhibitors. It undergoes less hepatic metabolism than omeprazole, has an oral availability of 89% at a dose of 40 mg, and a half-life of 1.5 hours. Esomeprazole is well tolerated; its common adverse effects are diarrhea, headache, nausea, abdominal pain, respiratory infection, and sinusitis.

To assess symptom control, esomeprazole 20 mg on demand has been compared with placebo on demand (maximum of one dose a day) for 6 months in a multi-center, double-blind study in 342 endoscopy-negative patients with gastro-esophageal reflux disease [ ]. There was complete resolution of heartburn after 4 weeks of daily esomeprazole therapy. On-demand therapy with esomeprazole was significantly more effective than placebo in controlling symptoms. The frequencies of adverse effects and laboratory profiles were similar in the two groups when adjusted for the time spent in the study.

To examine the pharmacokinetics and pharmacodynamics of esomeprazole, 12 healthy men took once-daily esomeprazole 5, 10, or 20 mg, or omeprazole 20 mg for 5 days in a crossover study [ ]. The pharmacokinetics of esomeprazole were time- and dose-dependent. There was greater acid inhibition with esomeprazole than with omeprazole.

Drug studies