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H2受体拮抗剂必须在夜间给药吗?一项关于新型H2受体拮抗剂SKF 94482抗分泌特性的研究,该拮抗剂对日间胃酸度有显著影响。

Do H2 receptor antagonists have to be given at night? A study of the antisecretory profile of SKF 94482, a new H2 receptor antagonist which has a profound effect on daytime acidity.

作者信息

Chiverton S G, Burget D W, Hunt R H

机构信息

Division of Gastroenterology, McMaster University Medical Center, Hamilton, Ontario, Canada.

出版信息

Gut. 1989 May;30(5):594-9. doi: 10.1136/gut.30.5.594.

DOI:10.1136/gut.30.5.594
PMID:2567265
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1434200/
Abstract

Evening dosing has become standard for H2 receptor antagonists, because available agents inhibit nocturnal basal acid secretion more effectively than daytime stimulated secretion. We studied the optimal time of administration of a new high affinity long acting H2 receptor antagonist, SKF 94482, for the suppression of intragastric acidity using intragastric telemetry. Sixteen healthy subjects received SKF 94482 200 mg or placebo at 07:30, 17:30, and 21:30 h during four separate studies. Time (h) above pH 4 was (mean (SD] 1.1 (1.2) on placebo, 7.8 (5.0) on SKF 94482 given at 07:30, 5.75 (3.6) on SKF 94482 given at 17:30, and 6.1 (2.9) when given at 21:30. All treatment regimens were effective in increasing time above pH 4 (p less than 0.01). The efficacy of the morning dose of SKF 94482 indicates that the best time to give H2 receptor antagonists depends on their pharmacological properties.

摘要

由于现有药物抑制夜间基础胃酸分泌比白天刺激胃酸分泌更有效,因此晚间给药已成为H2受体拮抗剂的标准给药方式。我们使用胃内遥测技术研究了新型高亲和力长效H2受体拮抗剂SKF 94482抑制胃内酸度的最佳给药时间。在四项单独的研究中,16名健康受试者在07:30、17:30和21:30分别接受200 mg的SKF 94482或安慰剂。安慰剂组pH值高于4的时间(小时)为(均值(标准差))1.1(1.2),07:30给予SKF 94482时为7.8(5.0),17:30给予SKF 94482时为5.75(3.6),21:30给予时为6.1(2.9)。所有治疗方案在延长pH值高于4的时间方面均有效(p<0.01)。SKF 94482早晨给药的疗效表明,给予H2受体拮抗剂的最佳时间取决于其药理特性。

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本文引用的文献

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Experimental gastric carcinogenesis in the rat: effects of hypergastrinemia and acid secretion.大鼠实验性胃癌发生:高胃泌素血症和胃酸分泌的影响
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Ranitidine 150 mg twice daily vs 300 mg nightly in treatment of duodenal ulcers.雷尼替丁每日两次,每次150毫克与每晚300毫克治疗十二指肠溃疡的对比研究。
Lancet. 1984 Aug 4;2(8397):274-6. doi: 10.1016/s0140-6736(84)90312-x.
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Effect of omeprazole and cimetidine on duodenal ulcer. A double-blind comparative trial.奥美拉唑与西咪替丁对十二指肠溃疡的疗效。一项双盲对照试验。
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Large single daily dose of histamine H2 receptor antagonist for duodenal ulcer. How much and when? A clinical pharmacological study.十二指肠溃疡大剂量组胺H2受体拮抗剂每日单次给药:剂量与时间?一项临床药理学研究
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