Relative efficacies of gastric proton pump inhibitors: Their clinical and pharmacological basis

Citation
W. Kromer et al., Relative efficacies of gastric proton pump inhibitors: Their clinical and pharmacological basis, PHARMACOL, 59(2), 1999, pp. 57-77
Citations number
165
Categorie Soggetti
Pharmacology & Toxicology
Journal title
PHARMACOLOGY
ISSN journal
00317012 → ACNP
Volume
59
Issue
2
Year of publication
1999
Pages
57 - 77
Database
ISI
SICI code
0031-7012(199908)59:2<57:REOGPP>2.0.ZU;2-F
Abstract
The present review will verify by intra-study rank orders, and their compar ison between studies, that the different gastric proton pump inhibitors (PP Is) display similar dose-response relationships with similar potencies and efficacies on a milligram basis, i.e., at the same milligram doses. This is in line with their basic pharmacology which suggests that, primarily, the serum AUCs of the free pro-drugs and their chemical activation half lives a t pH 1 relative to their serum elimination half lives determine the efficac ies of PPIs. According to the literature, these drug characteristics are si milar for all PPIs. Although PPIs have been introduced into the therapy of acute peptic ulcer disease at different daily, oral doses of 20 mg (omepraz ole and rabeprazole), 30 mg (lansoprazole) and 40 mg (pantoprazole), the da ta suggest that the optimal dose of lansoprazole, omeprazole and pantoprazo le, with respect to the acute treatment of peptic ulcers and moderate to se vere gastroesophageal reflux disease (GERD), is about 30-40 mg daily. The d ata base of rebeprazole appears to be too small at present to make any defi nite statement. Lower daily doses of the PPIs of about 15-20 mg are suffici ent in less severe cases of GERD and in maintenance therapy. It appears tha t different dose recommendations were based on different strategies to bala nce optimal drug dosage and safety, rather than on real differences in mill igram-related efficacies.