Inhibitory cholinergic effects of esaprazole on gastric secretion and plasma gastrin levels in the dog.

Abstract

The effects of esaprazole, a novel antiulcer drug, on gastric acid secretion and plasma gastrin levels were investigated in dogs provided with a gastric fistula or Heidenhain pouch. Esaprazole affected in a different extent the tests performed on dogs with a gastric fistula. The greatest inhibitory effect was obtained against 2-deoxy-D-glucose-induced acid output and gastrin release. An intermediate inhibition by esaprazole was detected on bethanechol-evoked secretion, and the lowest activity was found versus histamine-stimulated secretion. All these responses were strongly inhibited by the antimuscarinic drug pirenzepine used as reference drug. Moreover, both esaprazole and pirenzepine prevented the acid secretory response to a test meal in dogs with a Heidenhain pouch, without significantly affecting plasma gastrin levels. The present results suggest that the depressant action of esaprazole on gastric secretion depends on its peripheral anticholinergic activity, consisting of a partial blockade of acid output and a main reduction of vagally mediated gastrin release. On the basis of these findings, the antiulcer activity of esaprazole might be in part ascribed to its inhibitory effects on gastric secretion.

• Authors: C Blandizzi, G Mengozzi, L Intorre, G Natale, G Soldani, M Del Tacca
• Journal: Pharmacology (Pharmacology) Vol. 46 Issue 4 Pg. 231-40 (Apr 1993) ISSN: 0031-7012 [Print] Switzerland
• PMID: 8483969 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Anti-Ulcer Agents
• Gastrins
• Piperazines
• esaprazole

Topics

• Animals
• Anti-Ulcer Agents (pharmacology)
• Dogs
• Female
• Gastric Acid (metabolism)
• Gastric Fistula
• Gastric Mucosa (drug effects, metabolism)
• Gastrins (blood, drug effects)
• Guinea Pigs
• Ileum (drug effects, metabolism)
• In Vitro Techniques
• Male
• Piperazines (pharmacology)
• Radioimmunoassay
• Rats
• Rats, Wistar