Medical Department I, Gastroenterology, University Hospital, Fetscherstrasse 74, 01307 Dresden, Germany.
Expert Rev Clin Immunol. 2005 Nov;1(4):511-27. doi: 10.1586/1744666X.1.4.511.
Esomeprazole (S-omeprazole), an enantiomer of the racemate omeprazole, is the first proton pump inhibitor to be developed as an isomer. This confers improved pharmacokinetics and pharmacodynamics compared with the racemate R/S-omeprazole. The difference in the pharmacokinetics of esomeprazole compared with omeprazole and the R-isomer is due to reductions in total body clearance and first-pass metabolism in the liver. Pharmacodynamic studies showed that esomeprazole 40 mg provides greater intragastric acid control than respective doses of all the other proton pump inhibitors on the market. Several well-designed clinical trials, employing both endoscopic and symptomatic response criteria, have compared the efficacy of esomeprazole with that of other proton pump inhibitors in the management of gastroesophageal reflux disease patients, and in the eradication of Helicobacter pylori. In addition, the efficacy of esomeprazole for the healing and prevention of nonsteroidal anti-inflammatory drug-associated dyspeptic symptoms and ulcers has been established. The aim of this review is to provide an overview of the pharmacokinetics, pharmacodynamics and consequent clinical importance of esomeprazole in the treatment of acid-related disorders.
埃索美拉唑(S-埃索美拉唑)是消旋体奥美拉唑的对映异构体,是第一个作为异构体开发的质子泵抑制剂。与消旋体 R/S-奥美拉唑相比,它具有更好的药代动力学和药效学。与奥美拉唑和 R-异构体相比,埃索美拉唑的药代动力学差异是由于全身清除率和肝脏首过代谢的降低。药效学研究表明,埃索美拉唑 40mg 比市场上所有其他质子泵抑制剂的相应剂量更能控制胃酸。几项精心设计的临床试验,采用内镜和症状缓解标准,比较了埃索美拉唑与其他质子泵抑制剂在治疗胃食管反流病患者和根除幽门螺杆菌方面的疗效。此外,埃索美拉唑在治疗非甾体抗炎药相关消化不良症状和溃疡方面的疗效也已得到证实。本文旨在综述埃索美拉唑在治疗酸相关疾病中的药代动力学、药效学及其临床重要性。