摘要
氯沙坦是第一个被研究开发的ＡＮＧⅡ受体拮抗剂。该药口服后吸收良好，生物利用度为３３％ ，大约１４％ 的氯沙坦在体内形成活性更强的羧酸代谢物Ｅ－３１７４。存在体内的ＡＮＧⅡ受体有ＡＴ１、ＡＴ２、ＡＴ３ 三种，其生理效应主要由ＡＴ１ 受体介导发生，可出现强烈的血管收缩及醛固酮释放等多种效应。氯沙坦是非肽类拮抗剂，能高效、特异地与ＡＴ１ 受体结合，有效地抑制ＡＴ１ 受体介导的所有生理效应，发挥舒张血管、降低外周阻力的作用，减少后负荷及交感神经的过度兴奋，有效地治疗高血压病及心力衰竭，同时能够逆转左室肥厚。与其他降压药相比，既无药源性踝部水肿、心率增加的反应，又无频繁咳嗽的不良作用，且临床效果满意、耐受性好，它将在高血压病的治疗中占据显著地位。
Losartan is the first of a new class of non peptide angiotensin Ⅱ receptor antagonists.This drug represents the prototype antagonist of the angiotensin Ⅱtype 1(AT1) receptor and does not possess significant affinity for the so called AT2 and AT3 receptors. Many studies with losartan have suggested that this agent produces inhibition of the renin angiotensin system comparable to that of angiotensin converting enzyme(ACE) inhibitors,without the bradykinin potentiating effects.Losartan has proved to be an orally effective antihypertensive agent with a long duration of action.A growing number of experimental studies have also shown that losartan inhibits neointimal proliferation and markedly reduces or prevents cardiovascular hypertrophy/remodeling and cardiac failure mediated by activation of the renin angiotensin system. After oral and intravenous dosing terminal plasma half life is about 2 h for losartan,and 6~7 h for its active metaotite E 3174.Average bioavailability is 33%.This drug is well tolerated.It is certain that losartan does not cause a dry cough and angioneurotic oedema which occurs with ACE inhibitors.
出处
《医学研究生学报》
CAS
1999年第4期268-271,共4页
Journal of Medical Postgraduates
