Effects of a proton pump inhibitor, omeprazole, on gastric secretion and gastric and duodenal ulcers or erosions in rats

Effects of a proton pump inhibitor, omeprazole, on gastric secretion and gastric and duodenal ulcers or erosions in rats
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质子泵抑制剂奥美拉唑对大鼠胃分泌以及胃和十二指肠溃疡或糜烂的影响

DOI:
10.1007/bf01296212
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发表时间:
1984
影响因子:
3.1
通讯作者:
S. Okabe
S. Okabe
中科院分区:
医学3区
文献类型:
--
作者:
O. Yamamoto;Yukiko Okada;S. Okabe

文献摘要

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研究了质子泵抑制剂奥美拉唑对大鼠胃分泌和胃、十二指肠溃疡或糜烂的影响。奥美拉唑,经尿道给药,剂量依赖性地抑制幽门结扎大鼠的胃分泌(体积,酸和胃蛋白酶输出)。给药后,100 mg/kg奥美拉唑的抗分泌活性持续14 h。口服或十二指肠内给予10-100 mg/kg奥美拉唑均可明显抑制急性诱发的胃溃疡或糜烂,例如Shay溃疡、浸水应激、消炎痛、阿司匹林或泼尼松龙诱发的糜烂。奥美拉唑以3-10 mg/kg经口给药也可有效抑制美吡唑引起的十二指肠溃疡和胃糜烂的发展。奥美拉唑重复给药(200 mg/kg/天,分两次给药,持续14天)可显著加速乙酸诱导的胃溃疡的自发愈合。奥美拉唑抑制急性溃疡发展和加速既存溃疡愈合的机制似乎主要是由于其强效和持久的抗分泌活性。奥美拉唑的最大抑制反应和ED_(50)值均与西咪替丁相当或超过西咪替丁。
The effects of omeprazole, a proton pump inhibitor, on gastric secretion and gastric or duodenal ulcers or erosions in rats were studied. Omeprazole, given intraduodenally, dose-dependently inhibited the gastric secretion (volume, acid and pepsin output) of pylorus-ligated rats. The antisecretory activity of omeprazole at 100 mg/kg persisted for 14 hr after treatment. Acutely induced gastric ulcers or erosions such as Shay ulcers, water-immersion stress-, indomethacin-, aspirin-, or prednisolone-induced erosions were all markedly inhibited by oral or intraduodenal administration of 10–100 mg/kg of omeprazole. The development of duodenal ulcers and gastric erosions caused by mepirizole was also potently inhibited by omeprazole at 3–10 mg/kg given orally. Repeated administration of omeprazole, 200 mg/kg/day in two divided doses for 14 days, significantly accelerated the spontaneous healing of acetic acid-induced gastric ulcers. The mechanism by which omeprazole inhibits the development of acute ulcers and accelerates healing of preexisting ulcers appears to be mainly due to its potent and longlasting antisecretory activity. The antisecretory and antiulcer activities of omeprazole are equal to or exceed those of cimetidine, both in the maximum inhibitory response and ED50values.