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质子泵抑制剂的分类及药理学特性

         

摘要

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 ifrst choice of acid-related disorders such as peptic ulcer and gastro-esophageal relfux disease or non-steroidal anti-inlfammatory 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 brielfy introduced so as to promote their rational use in clinic.%选择性抑制胃壁细胞上H+/K+-ATP酶的药物--质子泵抑制剂已成为一代新型抑酸药物,是目前治疗酸相关疾病(消化性溃疡、反流性食管炎等)以及非甾体类抗炎药相关胃肠病变的首选药物。自1988年第一个质子泵抑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抑制剂有5个。尽管各个质子泵抑制剂拥有共同的苯并咪唑内核及吡啶环的化学结构,但它们在药代动力学和药效学上仍有细微差异。本文就国内已上市的质子泵抑制剂的药理学特性作一简要概述,以期促进质子泵抑制剂在临床上的合理选用。

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