质子泵克制剂的分类及药理学特性作者:陈坚来源:《上海医药》第 21 期 摘 要 选择性克制胃壁细胞上 H+/K+-ATP——酶的药品质子泵克制剂已成为一代新型抑酸药品,是现在治疗酸有关疾病(消化性溃疡、反流性食管炎等)以及非甾体类抗炎药有关胃肠病变的首选药品。自 1988 年第一种质子泵克制剂奥美拉唑上市以来,全球共相继上市了兰索拉唑、泮托拉唑、雷贝拉唑、埃索美拉唑等 8 个品种,而现在国内上市的质子泵克制剂有 5 个。尽管各个质子泵克制剂拥有共同的苯并咪唑内核及吡啶环的化学构造,但它们在药代动力学和药效学上仍有细微差别。本文就国内已上市的质子泵克制剂的药理学特性作一简要概述,以期增进质子泵克制剂在临床上的合理选用。 核心词 质子泵克制剂 酸有关疾病 药代动力学 药效学 中图分类号:R975.2 文献标记码:A 文章编号:1006-1533()21-0003-05 The classification and pharmacological characteristics of proton pump inhibitors Chen Jian* (Division of Gastroenterology , Huashan Hospital , Fudan University , Shanghai 40 ,China) Abstract Proton pump inhibitors bind covalently to the gastric H+/K+-ATPase via disulfide bond. Proton pump inhibitors are the most potent anti-secretary agent for gastric acid and they are the first choice of acid-related disorders such as peptic ulcer and gastro-esophageal reflux disease or non-steroidal anti-inflammatory drugs-induced gastrointestinal lesions. Omeprazole is the first proton pump inhibitor marketed in 1988 , followed by pantoprazole , lansoprazole , rabeprazole ,esomeprazole , revaprazan , ilaprazole and dexlansoprazole. Though these proton pump inhibitors share the core structures of benzimidazole and pyridine , they possess a little bit difference in pharmacokinetics and pharmacodynamics. Pharmacological characteristics of some proton pump inhibitors marketed in China are briefly introduced so as to promote their rational use in clinic. Key words proton pump inhibitors ; acid-related ...