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H2受体拮抗剂法莫替丁对大鼠的抗分泌及抗溃疡作用:与雷尼替丁的比较。

Antisecretory and antiulcer effect of the H2-receptor antagonist famotidine in the rat: comparison with ranitidine.

作者信息

Scarpignato C, Tramacere R, Zappia L

机构信息

Institute of Pharmacology, School of Medicine and Dentistry, Maggiore University Hospital, University of Parma, Italy.

出版信息

Br J Pharmacol. 1987 Sep;92(1):153-9. doi: 10.1111/j.1476-5381.1987.tb11307.x.

Abstract

1 The effects of the new H2-receptor antagonist famotidine, administered orally, on gastric secretion and emptying as well as on experimentally-induced gastric and duodenal ulcers were studied in the rat. Ranitidine was used as a reference compound. 2 Both compounds inhibited acid secretion in a dose-dependent manner. Calculated ED50 values were 0.80 and 6.84 mg kg-1 for famotidine and ranitidine, respectively. However, the duration of the antisecretory action was the same for both drugs. 3 The effect of the two drugs, administered at equiactive antisecretory doses, on gastric emptying was different. Ranitidine significantly accelerated the emptying rate whereas famotidine had no effect. 4 Famotidine reduced, in a dose-dependent manner, ulcer incidence in stomachs of dimaprit-treated rats and in duodena of cysteamine-treated animals with a potency respectively 2 and 7 times higher than that of ranitidine. 5 Famotidine is therefore an effective antisecretory and untiulcer compound. Its potency, but not its efficacy, is higher than that of ranitidine. Moreover, the duration of the antisecretory action is virtually the same for both drugs.

摘要

1 在大鼠中研究了口服新型H2受体拮抗剂法莫替丁对胃酸分泌、胃排空以及实验性诱导的胃溃疡和十二指肠溃疡的影响。雷尼替丁用作对照化合物。2 两种化合物均以剂量依赖性方式抑制胃酸分泌。法莫替丁和雷尼替丁的计算ED50值分别为0.80和6.84 mg kg-1。然而,两种药物的抗分泌作用持续时间相同。3 以等效抗分泌剂量给药的两种药物对胃排空的影响不同。雷尼替丁显著加快排空速率,而法莫替丁无此作用。4 法莫替丁以剂量依赖性方式降低了用二甲普利处理的大鼠胃和用半胱胺处理的动物十二指肠中的溃疡发生率,其效力分别比雷尼替丁高2倍和7倍。5 因此,法莫替丁是一种有效的抗分泌和抗溃疡化合物。其效力高于雷尼替丁,但疗效相同。此外,两种药物的抗分泌作用持续时间实际上相同。

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Histamine H2-antagonists modify gastric emptying in the rat.组胺H2拮抗剂可改变大鼠的胃排空。
Br J Pharmacol. 1982 Nov;77(3):443-8. doi: 10.1111/j.1476-5381.1982.tb09316.x.

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