质子泵和质子泵抑制剂研究进展

胃壁细胞H^ ,K^＋－ATP酶是一种质子泵，能特异性地将H^ 泵入胃腔，形成胃内高酸状态。质子泵抑制剂（PPI）为苯丙咪唑替代物，在体内转化为活性物质－－次磺酰胺，后者与H^ ,K^ －ATP酶共价结合，从而抑制该酶活性，抑制胃酸分泌，是治疗各种酸相关性疾病的首选药物。旧一代PPI如奥美拉唑，兰索拉唑和泮托拉唑的药代动力学个体差异大，与其他药物作用明显，起效时间慢，而新一代PPI如雷贝拉唑、伊索美拉唑起效快，抑酸效果更好，尤其在治疗胃食管反流性疾病（GERD）方面疗效更佳。

Progress in proton pump and proton pump inhibitor

Gastric acid pump,H +,K + ATPase,is a proton pump which transports H + into gastric lumen,resulting in the formulation of a high proton gradient across the plasma membrane of parietal cells.PPIs are substituted benzimidazoles and convert to active sulfenamide.In acidic environment,it covalently combines with H +,K + ATPase and therefore blocks acid secretion.PPIs are now generally considered the drugs of choice for treatment of patients with various acid related diseases.First generation PPIs(omerprazole,lansoprazole and pantoprazole) exhibit substantial interpatient variability in pharmacokinetics and may have significant interactions with other drugs.These drugs also have a relatively slow onset of pharmacological action.Compared with the older generations,the new generation PPIs,rabeprazole and esomeprazole,achieve more rapid and profound inhibition of acid secretion,especially in the treatment of GERD.