Peptic Ulcer Research Today is a free monthly online journal that collates and summarizes the latest research about Peptic Ulcer, including details on helicobacter pylori, diet, symptoms, treatment.

Pharmacodynamic comparison of pantoprazole enantiomers: inhibition of acid-related lesions and acid secretion in rats and guinea-pigs.

Cao H, Wang MW, Sun LX, Ikejima T, Hu ZQ, Zhao WH

Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang, China.

Pantoprazole is an irreversible proton pump inhibitor that is administered as a racemic mixture clinically. The effects of pantoprazole sodium (PAN.Na) enantiomers on acid-related lesions were compared using models of pylorus ligation induced ulcer, histamine induced ulcer and reflux oesophagitis in rats and guinea-pigs. Compared with (+)-PAN.Na and (+/-)-PAN.Na, (-)-PAN.Na showed much stronger inhibitory effects on pylorus ligation induced and histamine induced ulcers, but similar effects on reflux oesophagitis. The doses of (-)-PAN.Na, (+)-PAN.Na and (+/-)-PAN.Na required for 50% inhibition (ID50) of acid-related lesions were 1.28, 5.03 and 3.40 mg kg(-1) against pylorus ligation induced ulcer, 1.20, 4.28 and 3.15 mg kg(-1) against histamine induced ulcer, and 2.92, 3.56 and 3.70 mg kg(-1) against reflux oesophagitis, respectively. The inhibitory effects of PAN.Na enantiomers on basal gastric acid output were compared in rats with acute fistula. In contrast to inhibitory rates of 89.3% and 83.6% on gastric acid output by (-)-PAN.Na and (+/-)-PAN.Na at 1.5 mg kg(-1), (+)-PAN.Na had an inhibitory rate of only 24.7% at the same dose. The above results indicate that (-)-PAN.Na is more potent than (+)-PAN.Na at inhibiting acid-related lesions owing to its stronger inhibition of acid secretion.

Published 22 June 2005 in J Pharm Pharmacol, 57(7): 923-7.
Full-text of this article is available online (may require subscription).

© 2004-2008 Peptic Ulcer Research Today. All Rights Reserved.