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尼扎替丁。对其药效学和药代动力学特性及其在消化性溃疡疾病中的治疗应用的初步综述。

Nizatidine. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in peptic ulcer disease.

作者信息

Price A H, Brogden R N

机构信息

ADIS Drug Information Services, Auckland, New Zealand.

出版信息

Drugs. 1988 Nov;36(5):521-39. doi: 10.2165/00003495-198836050-00002.

Abstract

Nizatidine is an H2-receptor antagonist which in animal studies was more active on a weight-for-weight basis than cimetidine in inhibiting basal and stimulated gastric acid secretion. Similarly, studies in humans have confirmed that nizatidine is a potent inhibitor of basal, nocturnal and stimulated gastric acid secretion. As might be expected at this stage of its development, published therapeutic experience with nizatidine is limited. Nevertheless, multicentre therapeutic trials have shown that nizatidine 300mg at bedtime or 150mg twice daily is significantly more effective than placebo for healing active duodenal ulcer, and is apparently as effective as standard doses of ranitidine in increasing the rate of healing of both duodenal and gastric ulcers, and as effective as a standard dose of cimetidine in active duodenal ulcer. When used prophylactically a single 150mg dose of nizatidine at night produces a decrease in the incidence of ulcer recurrence compared with placebo, and a similar rate of decrease to that achieved with ranitidine 150mg. Nizatidine is well tolerated. Unlike cimetidine it does not have any antiandrogenic effects or alter the hepatic metabolism of drugs. However, only wider clinical experience with nizatidine can accurately determine its relative efficacy and tolerability compared with other antiulcer therapy. Thus, early clinical experience suggests that nizatidine is a useful alternative to the histamine H2-receptor antagonists presently in clinical use.

摘要

尼扎替丁是一种H2受体拮抗剂,在动物研究中,按单位体重计算,它在抑制基础胃酸分泌和刺激胃酸分泌方面比西咪替丁更具活性。同样,人体研究证实,尼扎替丁是基础胃酸、夜间胃酸和刺激胃酸分泌的有效抑制剂。在其研发的这个阶段,正如预期的那样,已发表的关于尼扎替丁的治疗经验有限。然而,多中心治疗试验表明,睡前服用300mg尼扎替丁或每日两次服用150mg尼扎替丁在治愈活动性十二指肠溃疡方面比安慰剂显著更有效,而且在提高十二指肠溃疡和胃溃疡的愈合率方面显然与标准剂量的雷尼替丁一样有效,在治疗活动性十二指肠溃疡方面与标准剂量的西咪替丁一样有效。预防性使用时,与安慰剂相比,每晚单次服用150mg尼扎替丁可降低溃疡复发率,降低率与服用150mg雷尼替丁相似。尼扎替丁耐受性良好。与西咪替丁不同,它没有任何抗雄激素作用,也不会改变药物的肝代谢。然而,只有通过更广泛的临床经验才能准确确定它与其他抗溃疡疗法相比的相对疗效和耐受性。因此,早期临床经验表明,尼扎替丁是目前临床使用的组胺H2受体拮抗剂的一种有用替代品。

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