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在心力衰竭的药物疗法中,主要使用抑制肾素-血管紧张素系统(RAS)药物——血管紧张素转换酶(ACE)抑制剂和血管紧张素Ⅱ的1型(AT1)受体拮抗剂(ARB)。另外,除降压效果外,ACE抑制剂和ARB还具有多种作用,而多数情况是希望应用其脏器保护作用。ARB不仅没有ACE抑制剂的干咳副作用、耐受性好,而且还与ACE抑制剂药理作用不同,因而受到关注。近期作者等报道了ARB新的药理作用,即针对AT1受体的反激动作用(inverse agonism)进行讨论。虽然关于ARB的反激动作用仍有许多不明之处,但有无反激动作用在临床的长期效果上有何不同及对ARB的多方面脏器保护作用有何影响等问题,今后将逐渐阐明。
In heart failure drug therapy, predominantly the type 1 (AT1) receptor antagonist (AT1) receptor antagonist that inhibits the renin-angiotensin system (RAS) drug-angiotensin converting enzyme (ACE) inhibitor and angiotensin II ARB). In addition, in addition to antihypertensive effect, ACE inhibitors and ARB also has a variety of effects, but in most cases is the hope that the application of its organ protective effect. ARB not only does not have the dry cough side effects of ACE inhibitors, tolerance, but also pharmacological effects with different ACE inhibitors, which attracted attention. Recently, the authors reported new pharmacological effects of ARB, namely, the discussion of the inverse agonism of the AT1 receptor. Although there are still many uncertainties about the anti-motility of ARB, the question of whether there is any difference in the long-term clinical efficacy of anti-rifampicin and how it affects the multi-organ protective effect of ARB will gradually be clarified in the future.