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法莫替丁(Famotidine,FT)是一个新的抗H_2-受体拮抗剂。离体和整体实验证明,该药对毒蕈碱、烟碱、组胺H_1或交感神经α和β受体无拮抗作用。离体实验还证明FT抑制H_2-受体的强度(用游离碱分子相比较)比西咪替丁(CT)强20倍,比雷尼替丁(RT)强7.5倍。离体实验中观察到FT是竞争性抑制H_2受体。一、药效学研究健康人和消化性溃疡病人口服FT 10和20mg,对夜间的胃酸分泌和用氨乙吡唑或四肽胃泌素刺激的胃酸分泌的抑制率为60和80%。病人每小时的基础胃酸分泌量≥5
Famotidine (FT) is a new anti-H 2 -receptor antagonist. In vitro and in vivo experiments show that the drug has no antagonistic effect on muscarinic, nicotine, histamine H 1 or sympathetic α and β receptors. In vitro experiments also demonstrated that FT inhibits the intensity of H 2 -receptors (compared with the free base molecule) 20 times stronger than cimetidine (CT) and 7.5 times stronger than ranitidine (RT). FT was observed in vitro to competitively inhibit H 2 receptors. Pharmacodynamic Studies Oral FT 10 and 20 mg administered to healthy and peptic ulcer patients showed 60 and 80% inhibition of gastric acid secretion during the night and gastric acid secretion stimulated with either acephate or tetrapeptide gastrin. The patient’s basic gastric acid secretion per hour ≥ 5