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血管紧张素Ⅱ受体阻滞剂(AngⅡ RAS)是一类新型抗高血压药物。其中的洛沙坦(Losartan)是第一个进入临床的有效制剂,其钾盐由Merch公司开发,1995年在美国上市。国外对该药的研究资源较丰富,应用经验也较成熟。现对其药理作用、药物动力学、临床应用以及安全性作简要介绍。一、药理作用 AngⅡRAS分为肽类和非肽类,每类又可分为选择性AT_1(亚型AngⅡ)受体阻滞剂和AT_2受体阻滞剂。洛沙坦属于非肽类,是高亲和力的亚型AT_1受体阻滞剂。它通过与AT_1受体跨膜区内的氨基酸相互作用,并占据其螺旋状空间而阻止AngⅡ与AT_1受体的结合,从而在受体水平阻断了AngⅡ的心血管
Angiotensin Ⅱ receptor blocker (Ang Ⅱ RAS) is a new class of antihypertensive drugs. Among them, Losartan is the first effective formulation to enter the clinic. Its potassium salt was developed by Merch Company and was listed in the United States in 1995. Abroad, the research resources of the drug is rich, more mature application experience. Now its pharmacological effects, pharmacokinetics, clinical applications and safety brief. First, the pharmacological effects Ang Ⅱ RAS is divided into peptides and non-peptides, each class can be divided into selective AT_1 (subtype Ang Ⅱ) receptor blockers and AT 2 receptor blockers. Losartan is a non-peptide, high-affinity subtype AT_1 receptor blocker. It interacts with amino acids in the transmembrane region of the AT1 receptor and occupies its helical space and blocks the binding of AngII to the AT1 receptor, thereby blocking AngII cardiovascular at the receptor level