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雷尼替丁。对其药效学、药代动力学特性以及在消化性溃疡疾病和其他相关疾病中的治疗应用的最新综述。

Ranitidine. An updated review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in peptic ulcer disease and other allied diseases.

作者信息

Grant S M, Langtry H D, Brogden R N

机构信息

ADIS Drug Information Services, Auckland, New Zealand.

出版信息

Drugs. 1989 Jun;37(6):801-70. doi: 10.2165/00003495-198937060-00003.

Abstract

Ranitidine, a histamine H2-receptor antagonist, is now well established as a potent inhibitor of gastric acid secretion effective in the treatment and prophylaxis of gastrointestinal lesions aggravated by gastric acid secretion. Therapeutic trials involving several thousands of patients with peptic ulcer disease confirm that ranitidine 300mg daily administered orally in single or divided doses is at least as effective as cimetidine 800 to 1000mg daily in increasing the rate of healing of duodenal and gastric ulcers. Similar dosages of ranitidine have been shown to relieve the symptoms of reflux oesophagitis and heal or prevent gastrointestinal damage caused by ulcerogenic drugs. Ranitidine 150mg orally at night maintains ulcer healing in the long term. Ranitidine has also demonstrated good results in the treatment of Zollinger-Ellison syndrome and in the prevention of aspiration pneumonitis when given prior to surgery and to pregnant women at full term. It may also have a place in the management of acute upper gastrointestinal bleeding and in the prevention of stress ulcers in the intensive care setting, although these areas require further investigation. Ranitidine has been used safely in obstetric patients during labour, in children, the elderly, and in patients with renal impairment when given in appropriate dosages. The drug is very well tolerated and is only infrequently associated with serious adverse reactions or clinically significant drug interactions. Even at high dosages, ranitidine appears devoid of antiandrogenic effects. Ranitidine is clearly comparable or superior to most other antiulcer agents in the treatment and prevention of a variety of gastrointestinal disorders associated with gastric acid secretion. With its favourable efficacy and tolerability profiles, ranitidine must be considered a first-line agent when suppression of gastric acid secretion is indicated.

摘要

雷尼替丁是一种组胺H2受体拮抗剂,现已被公认为是一种有效的胃酸分泌抑制剂,可有效治疗和预防因胃酸分泌而加重的胃肠道病变。涉及数千名消化性溃疡病患者的治疗试验证实,每日口服300mg雷尼替丁,单次或分次给药,在提高十二指肠溃疡和胃溃疡愈合率方面至少与每日800至1000mg西咪替丁同样有效。已证明雷尼替丁的类似剂量可缓解反流性食管炎的症状,并治愈或预防由致溃疡药物引起的胃肠道损伤。每晚口服150mg雷尼替丁可长期维持溃疡愈合。雷尼替丁在治疗卓-艾综合征以及在手术前和足月孕妇中预防吸入性肺炎方面也取得了良好效果。在急性上消化道出血的管理和重症监护环境中预防应激性溃疡方面,雷尼替丁可能也有一席之地,尽管这些领域需要进一步研究。雷尼替丁在分娩期间的产科患者、儿童、老年人以及肾功能不全患者中以适当剂量使用时是安全的。该药物耐受性良好,很少与严重不良反应或具有临床意义的药物相互作用相关。即使在高剂量下,雷尼替丁似乎也没有抗雄激素作用。在治疗和预防与胃酸分泌相关的各种胃肠道疾病方面,雷尼替丁显然与大多数其他抗溃疡药物相当或更优。鉴于其良好的疗效和耐受性,当需要抑制胃酸分泌时,雷尼替丁必须被视为一线药物。

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