Review article: the pharmacology of rabeprazole
Review article: the pharmacology of rabeprazole
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综述文章：雷贝拉唑的药理学
DOI：
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发表时间：
1999
影响因子：
7.6
通讯作者：
Roy E. Pounder
中科院分区：
文献类型：
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作者：
MP Williams;Roy E. Pounder
雷帕霉素钠是一种新型的取代苯并咪唑类质子泵抑制剂，与现有的质子泵抑制剂有几个不同之处。体外和动物研究表明，雷贝拉唑是比奥美拉唑更强效的H+，K+-ATP酶和酸分泌抑制剂，是比奥美拉唑、兰索拉唑或泮托拉唑更快速的质子泵抑制剂。这可能反映了雷贝拉唑在壁细胞小管中的更快激活。在人体研究中，每日一次给予5-40 mg雷贝拉唑以剂量依赖性方式抑制胃酸分泌。在健康志愿者和消化性溃疡病或胃食管反流病患者中进行的单次和重复给药研究中，20 mg每日一次给药可持续显著降低24 h胃内酸度。与奥美拉唑20 mg相比，雷贝拉唑20 mg给药第1天胃内酸度显著降低。与其他质子泵抑制剂一样，雷贝拉唑对幽门螺杆菌具有体外抗菌活性，对该微生物的活性高于兰索拉唑或奥美拉唑。除了抑制细菌脲酶活性外，雷贝拉唑还与H.幽门。需要临床试验来评估这些发现的临床重要性，以及评估雷贝拉唑的潜在优势是否会为酸相关疾病患者带来临床获益。
Rabeprazole sodium is a new substituted benzimidazole proton pump inhibitor with several differences compared with existing proton pump inhibitors. In vitro and animal studies have demonstrated that rabeprazole is a more potent inhibitor of H+,K+‐ATPase and acid secretion than omeprazole, and is a more rapid inhibitor of proton pumps than omeprazole, lansoprazole, or pantoprazole. This probably reflects rabeprazole’s faster activation in the parietal cell canaliculus. In human studies, once‐daily doses of 5–40 mg of rabeprazole inhibit gastric acid secretion in a dose‐dependent fashion. A once‐daily dose of 20 mg has consistently achieved profound decreases in 24‐h intragastric acidity in single and repeat dosing studies, in healthy volunteers and patients with either peptic ulcer disease or gastro‐oesophageal reflux disease. Significantly greater decreases in intragastric acidity are achieved on day 1 of dosing with rabeprazole 20 mg than with omeprazole 20 mg. As with other proton pump inhibitors, rabeprazole has in vitro antibacterial activity against Helicobacter pylori, with greater activity against this organism than either lansoprazole or omeprazole. In addition to inhibiting bacterial urease activity, rabeprazole binds to several molecules on H. pylori. Clinical trials are needed to assess the clinical importance of these findings, as well as to assess whether the potential advantages of rabeprazole result in clinical benefit for patients with acid‐related diseases.