Prakash A, Faulds D
Adis International Limited, Auckland, New Zealand.
Drugs. 1998 Feb;55(2):261-7; discussion 268. doi: 10.2165/00003495-199855020-00009.
Rabeprazole is a proton pump inhibitor with antisecretory properties. In vitro animal experiments have indicated that the inhibition of the proton pump by rabeprazole is partially reversible. Rabeprazole has 2- to 10-fold greater antisecretory activity than omeprazole in vitro. However, it dissociates more readily from H+,K(+)-ATPase than omeprazole, resulting in a shorter duration of action. In comparative clinical trials rabeprazole was significantly more effective than placebo, famotidine or ranitidine and as effective as omeprazole in the treatment of patients with erosive or ulcerative gastro-oesophageal reflux disease or gastric or duodenal ulcers. Healing rates with rabeprazole were independent of Helicobacter pylori status. Rabeprazole in combination with either clarithromycin and metronidazole or clarithromycin and amoxicillin or amoxicillin and metronidazole or clarithromycin for 7 days produced eradication of H. pylori in 100, 95, 90 and 63% of patients. The tolerability profile of rabeprazole 20mg once daily was similar to that of famotidine 20mg twice daily, ranitidine 150mg 4 times daily or omeprazole 20mg once daily in comparative trials. The adverse events reported with once daily administration of rabeprazole 20mg include malaise, nausea, diarrhoea, headache, dizziness and skin eruptions in 0.7 to 2.2% of patients.
雷贝拉唑是一种具有抗分泌特性的质子泵抑制剂。体外动物实验表明,雷贝拉唑对质子泵的抑制作用部分可逆。在体外,雷贝拉唑的抗分泌活性比奥美拉唑高2至10倍。然而,它比奥美拉唑更容易从H⁺,K⁺-ATP酶上解离,导致作用持续时间较短。在比较性临床试验中,雷贝拉唑在治疗糜烂性或溃疡性胃食管反流病或胃或十二指肠溃疡患者时,明显比安慰剂、法莫替丁或雷尼替丁更有效,且与奥美拉唑效果相当。雷贝拉唑的愈合率与幽门螺杆菌感染状况无关。雷贝拉唑与克拉霉素和甲硝唑或克拉霉素和阿莫西林或阿莫西林和甲硝唑或克拉霉素联合使用7天,分别使100%、95%、90%和63%的患者根除幽门螺杆菌。在比较性试验中,每日一次服用20mg雷贝拉唑的耐受性与每日两次服用20mg法莫替丁、每日四次服用150mg雷尼替丁或每日一次服用20mg奥美拉唑相似。每日一次服用20mg雷贝拉唑报告的不良事件包括0.7%至2.2%的患者出现不适、恶心、腹泻、头痛、头晕和皮疹。