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法莫替丁。药效学和药代动力学特性及其在消化性溃疡疾病和佐林格-埃利森综合征治疗应用的初步综述。

Famotidine. Pharmacodynamic and pharmacokinetic properties and a preliminary review of its therapeutic use in peptic ulcer disease and Zollinger-Ellison syndrome.

作者信息

Campoli-Richards D M, Clissold S P

出版信息

Drugs. 1986 Sep;32(3):197-221. doi: 10.2165/00003495-198632030-00001.

Abstract

Famotidine is a new histamine H2-receptor antagonist. On a weight basis, famotidine is 20 times more potent than cimetidine and 7.5 times more potent than ranitidine in inhibiting basal and pentagastrin-stimulated gastric acid secretion in humans. Therapeutic trials have shown that famotidine 20 mg twice daily or 40 mg at bedtime may be an effective alternative to standard doses of cimetidine for healing gastric ulcers and to standard doses of cimetidine and ranitidine for healing duodenal ulcers. When used prophylactically, a single 20 mg dose of famotidine at night decreases the incidence of duodenal ulcer recurrence (versus placebo). However, further study is needed to clarify the comparative efficacy of the H2-receptor antagonists, in particular as maintenance therapy for healed peptic ulcer. Preliminary results in a few patients with Zollinger-Ellison syndrome indicate that famotidine, alone or in combination with an anticholinergic agent, gives good control of gastric acid hyperacidity with no evidence of biochemical or haematological toxicity. Famotidine appears to be well tolerated. Unlike cimetidine, it does not have antiandrogenic effects or alter hepatic metabolism of drugs. However, wider clinical experience with famotidine is needed to accurately determine its relative tolerability compared with other anti-ulcer drugs. Thus, famotidine appears to be a suitable and well tolerated alternative to cimetidine and ranitidine for healing peptic ulcers, but wider clinical experience is needed to assess its relative efficacy and tolerability in the long term maintenance treatment of patients with healed ulcers as well as in patients with Zollinger-Ellison syndrome.

摘要

法莫替丁是一种新型组胺H2受体拮抗剂。按重量计算,法莫替丁在抑制人体基础胃酸分泌和五肽胃泌素刺激的胃酸分泌方面,比西咪替丁强20倍,比雷尼替丁强7.5倍。治疗试验表明,每日两次服用20毫克法莫替丁或睡前服用40毫克法莫替丁,对于治疗胃溃疡而言,可能是标准剂量西咪替丁的有效替代药物;对于治疗十二指肠溃疡而言,可能是标准剂量西咪替丁和雷尼替丁的有效替代药物。预防性使用时,夜间单次服用20毫克法莫替丁可降低十二指肠溃疡复发率(与安慰剂相比)。然而,需要进一步研究以阐明H2受体拮抗剂的相对疗效,尤其是作为愈合消化性溃疡的维持疗法。少数佐林格-埃利森综合征患者的初步结果表明,法莫替丁单独使用或与抗胆碱能药物联合使用,能很好地控制胃酸过多,且无生化或血液学毒性迹象。法莫替丁似乎耐受性良好。与西咪替丁不同,它没有抗雄激素作用,也不会改变药物的肝脏代谢。然而,需要更广泛的临床经验来准确确定其与其他抗溃疡药物相比的相对耐受性。因此,法莫替丁似乎是治疗消化性溃疡的西咪替丁和雷尼替丁的合适且耐受性良好的替代药物,但需要更广泛的临床经验来评估其在愈合溃疡患者以及佐林格-埃利森综合征患者长期维持治疗中的相对疗效和耐受性。

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