The anti-secretory and anti-ulcer activities of esomeprazole in comparison with omeprazole in the stomach of rats and rabbits.
Proton pump inhibitors (PPIs) are widely used to treat hyperacid secretion and stomach ulcers. The study investigated the anti-secretory and anti-ulcer effects of esomeprazole, the S-isomer of omeprazole on dimaprit, histamine and dibutyryl adenosine 3, 5 cyclic monophosphate (dbcAMP)-evoked gastric acid secretion, acidified ethanol (AE) and indomethacin (INDO)-induced haemorrhagic lesions and on prostaglandin E2 (PGE2) level in the rat in vivo and rabbit in vitro preparations. The effect of omeprazole was also investigated for comparison. Dimaprit-induced acid secretion was significantly (P < 0.05) inhibited by both PPIs in a dose-dependent manner. In the isolated rabbit gastric glands, both PPIs elicited marked reductions in histamine- and dbcAMP-evoked acid secretion with similar potency. The lesions induced by either AE or INDO were significantly (P < 0.05) reduced in the presence of either esomeprazole or omeprazole compared to control values. Increasing doses of esomeprazole before AE treatment resulted in a marked degree of cytoprotection and an elevation in the concentration of bound PGE2 in the stomach tissue homogenate. The results show that esomeprazole and omeprazole were equally effective against gastric haemorrhagic lesions induced by either AE or INDO and in inhibiting dimaprit-, dbcAMP- and histamine-induced gastric acid secretion in the rat and rabbit stomach both in vivo and in vitro. The gastro-protective effect of esomeprazole was found to be proportional to the bound PGE2 levels in the glandular area of the stomach.
Faculty of Medicine & Health Sciences, UAE University, P.O. Box-17666, Al Ain, United Arab Emirates. sbastaki@uaeu.ac.ae
Salim M A
SM
Bastaki
Irwin S
IS
Chandranath
Jaipaul
J
Singh
D000632:Aminopyrine / Q000378:metabolism; D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000494:pharmacology*; D003994:Bucladesine / Q000494:pharmacology; D002247:Carbon Isotopes; D017259:Dimaprit / Q000494:pharmacology; D015232:Dinoprostone / Q000378:metabolism; D064098:Esomeprazole; D005260:Female; D005744:Gastric Acid / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D006632:Histamine / Q000494:pharmacology; D007213:Indomethacin / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008297:Male; D009853:Omeprazole / Q000008:administration & dosage / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D013270:Stomach / Q000187:drug effects* / Q000473:pathology
D000897:Anti-Ulcer Agents; D002247:Carbon Isotopes; D000632:Aminopyrine; D003994:Bucladesine; D006632:Histamine; D015232:Dinoprostone; D009853:Omeprazole; D064098:Esomeprazole; D007213:Indomethacin; D017259:Dimaprit