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机构地区:[1]上海交通大学医学院附属仁济医院药剂科,上海200001
出 处:《药学服务与研究》2014年第1期14-17,共4页Pharmaceutical Care and Research
摘 要:依普沙坦是一种高选择性的血管紧张素Ⅱ-1型(AT1)受体拮抗剂.单次口服后达峰时间(tmax)为1~2.5 h,血浆蛋白质结合率高达98%;多次口服600mg/d,消除半衰期(t12)为20 h,平均稳态分布容积(Vss)为308 L.随机、双盲、多中心临床试验结果表明,依普沙坦的降压效果与依那普利、尼群地平、缬沙坦和替米沙坦相似,对收缩压的降低作用强于氯沙坦;对高血压病人的卒中二级预防作用优于尼群地平,而且依普沙坦对年龄≥50岁的新诊断为高血压的病人,在降压的同时还可适当改善他们的认知功能.病人对依普沙坦的耐受性较好,持续干咳的发生率明显低于依那普利.Eprosartan is a highly selective angiotensin Ⅱ type 1 (AT1) receptor blocker (ARB). Peak plasma concentra lion (ARB) of eprosartan could be achieved in 1 2.5 h (tmax) after a single oral dose. Its plasma protein binding rate could be as high as 98%. The mean terminal elimination half-life (t1/2) was 20 h following multiple oral administration of eprosartan (600 mg/d), and its mean steady-slate volume of distrihution was 308 L. Many double blind, randomized, multi centre trials showed that eprosartan could produce greater reduction of systolic Mood pressure (SBP) than that of losartan, and its pressurelowering effects were similar to those of enalapril, nitrendipine, valsartan and telmisartan. Its secondary stroke prevention effect on patients with hypertension was superior to that of nitrendipine. Furthermore, eprosartan could also modestly improve cognitive function of patients ≥ 50 years old with newly diagnosed hypertension in a large observational study. Generally, eprosartan was well tolerated in clinical trials and patients had a lower incidence of persistent dry cough, as compared with those patients taking enalapril.
关 键 词:依普沙坦 血管紧张素受体拮抗剂 抗高血压药 临床研究 综述 ANGIOTENSIN Ⅱ receptor BLOCKER (ARB)
分 类 号:R544.1[医药卫生—心血管疾病] R972.4[医药卫生—内科学]
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