Esomeprazole for acid peptic disorders.
OBJECTIVE
To review the pharmacology, pharmacokinetics, clinical efficacy, and safety of esomeprazole, a new proton-pump inhibitor (PPI).


METHODS
A MEDLINE search (1966-March 2001) was conducted for relevant literature using the terms esomeprazole, Nexium, and H199/18. Abstracts from the XXXII Nordic Meeting of Gastroenterology and journal articles provided by AstraZeneca were reviewed.


METHODS
All available studies on the pharmacology, pharmacokinetics, clinical efficacy, and safety of esomeprazole were reviewed.


RESULTS
Esomeprazole is a new PPI and is the S-isomer of racemic omeprazole. Esomeprazole has demonstrated acid control comparable to that of the other PPIs currently available. Esomeprazole undergoes less hepatic metabolism compared with omeprazole, and thus may result in less interpatient variability among slow and fast metabolizers of CYP2C19. The oral bioavailability of esomeprazole is approximately 89% with a dose of 40 mg, and the half-life is approximately 1.5 hours. Esomeprazole is effective in the healing of erosive esophagitis, with a rate of healing at week 8 of 93.7% (p < 0.001). In maintenance therapy of healed erosive esophagitis, esomeprazole maintained healing rates >90% (6-mo trial). Esomeprazole is comparable with omeprazole (both in combination with appropriate antibiotics) in the eradication of Helicobacter pylori, with eradication rates of 89.7% and 87.8%, respectively. The drug is well tolerated. The few adverse effects associated with esomeprazole are diarrhea, headache, nausea, abdominal pain, respiratory infection, and sinusitis.


CONCLUSIONS
Esomeprazole is a safe and effective PPI. It is effective in the treatment of peptic ulcer disease and gastroesophageal reflux disease.
Kale-Pradhan
Pramodini B
PB
Department of Pharmacy Practice, Wayne State University, Detroit, MI 48236-2148, USA. Pkale@wizard.pharm.wayne.edu
Landry
Heather K
HK
Sypula
William T
WT
D000042:Absorption; D000897:Anti-Ulcer Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D064098:Esomeprazole; D004942:Esophagitis, Peptic / Q000188:drug therapy*; D006801:Humans; D016239:MEDLINE; D009853:Omeprazole / Q000031:analogs & derivatives / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D016896:Treatment Outcome
D000897:Anti-Ulcer Agents; D009853:Omeprazole; D064098:Esomeprazole