洛沙坦的临床药物动力学。

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西卡哒,Gehr TW, Ghosh年代

洛沙坦的临床药物动力学。

Pharmacokinet。2005; 44 (8): 797 - 814。

PubMed ID

16029066 (在PubMed

]

文摘

洛沙坦是第一个没有兴奋剂性质可用口服血管紧张素受体拮抗剂。口服后,洛沙坦迅速吸收,达到最大浓度post-administration 1 - 2小时。洛沙坦剂量的口服后大约14%转化为药物活性E 3174代谢物。E 3174是10 - 40倍更有效比母体化合物和估计终端半衰期范围从6到9个小时。洛沙坦和E 3174的药物代谢动力学情况是线性的,dose-proportional不显著改变和重复的管理。推荐的洛沙坦50毫克/天的剂量可以不考虑食品管理。没有临床显著影响的年龄,性别或种族在洛沙坦的药物代谢动力学情况,不需要剂量调整患者的轻度肝损害或不同程度的肾功能不全。洛沙坦,或其E 3174代谢物,在血液透析过程中并不会被删除。洛沙坦的主要代谢途径是由细胞色素P450 (CYP) 3 a4, 2 c9和2 c10同功酶。洛沙坦具有良好药物之间的相互作用,总的来说,就是明证缺乏临床相关的这种药物之间的相互作用和CYP450的一系列抑制剂和刺激器系统。 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.

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药物

洛沙坦

药物酶

药物	酶	类	生物	药理作用	行动
洛沙坦	细胞色素P450 2 c9	蛋白质	人类	未知的	底物	细节
洛沙坦	细胞色素P450 3 a4	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	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