氯沙坦的临床药代动力学。

文章的细节

引用

复制到剪贴板

西卡·达，盖尔·TW，高希·S

氯沙坦的临床药代动力学。

临床药典杂志，2005;44(8):797-814。

PubMed ID

16029066 (PubMed视图

］

摘要

氯沙坦是第一种口服无激动剂性质的血管紧张素受体拮抗剂。口服给药后，氯沙坦被迅速吸收，给药后1-2小时达到最大浓度。口服给药后，约14%的氯沙坦剂量转化为具有药理活性的e3174代谢物。e3174的药效是其母体化合物的10- 40倍，其半衰期估计为6 - 9小时。氯沙坦和e3174的药代动力学是线性的，剂量成正比的，不因重复给药而发生实质性变化。氯沙坦的推荐剂量为50mg /天，可以不考虑食物。年龄、性别、种族对氯沙坦药代动力学无明显临床影响，轻度肝功能损害或不同程度肾功能不全患者无需调整剂量。氯沙坦或其e3174代谢物在血液透析过程中不被去除。氯沙坦的主要代谢途径是细胞色素P450 (CYP) 3A4, 2C9和2C10同工酶。总的来说，氯沙坦具有良好的药物-药物相互作用，这可以从该药与一系列CYP450系统抑制剂和刺激剂之间缺乏临床相关的相互作用中得到证明。 Losartan does not have a drug-drug interaction with hydrochlorothiazide, warfarin or digoxin. Losartan should be avoided in pregnancy, as is the case with all other angiotensin-receptor antagonists. When given in the second and third trimester of pregnancy, losartan is often associated with serious fetal toxicity. Losartan is a competitive antagonist that causes a parallel rightward shift of the concentration-contractile response curve to angiotensin-II, while E 3174 is a noncompetitive "insurmountable" antagonist of angiotensin-II. The maximum recommended daily dose of losartan is 100mg, which can be given as a once-daily dose or by splitting the same total daily dose into two doses. Losartan reduces blood pressure comparably to other angiotensin-receptor antagonists. Losartan has been extensively studied relative to end-organ protection, with studies having been conducted in diabetic nephropathy, heart failure, post-myocardial infarction and hypertensive patients with left ventricular hypertrophy. The results of these studies have been sufficiently positive to support a more widespread use of angiotensin-receptor antagonists in the setting of various end-organ diseases. Losartan, like other angiotensin-receptor antagonists, is devoid of significant adverse effects.

引用本文的药物库数据

药物

洛沙坦

药物酶

药物	酶	种类	生物	药理作用	行动
洛沙坦	细胞色素P450 2C9	蛋白质	人类	未知的	底物	细节
洛沙坦	细胞色素P450 3A4	蛋白质	人类	未知的	底物 抑制剂	细节

药物载体

药物	航空公司	种类	生物	药理作用	行动
洛沙坦	血清白蛋白	蛋白质	人类	未知的	底物	细节