Krum Henry, Liew Danny
Department of Epidemiology and Preventive Medicine, Monash University Central and Eastern Clinical School, Alfred Hospital, Melbourne, Victoria 3004, Australia.
Expert Rev Cardiovasc Ther. 2004 May;2(3):315-20. doi: 10.1586/14779072.2.3.315.
There has been a recent revival of interest in aldosterone receptor antagonists for the treatment of chronic heart failure. This was largely triggered by fresh insights into the role of aldosterone in a number of key pathophysiological processes, including fibrosis and remodeling, inflammation, and the potentiation of catecholamine effects. The therapeutic efficacy of spironolactone (Aldactone), Pfizer) in severe chronic heart failure was established by the Randomized Aldactone Evaluation Study, but hormonal side effects (gynecomastia) associated with the drug posed a problem. More recently, the Eplerenone Post-Acute Myocardial Infarction Heart Failure Efficacy and Survival Study has provided firm support for the use of eplerenone (Inspra, Pfizer) in heart failure following acute myocardial infarction in addition to neurohormonal blockade with angiotensin-converting enzyme inhibitors or angiotensin II receptor blockers and beta-blockers. This strategy can be expected to benefit both mortality and morbidity. Due to the fact that eplerenone is a selective aldosterone receptor antagonist, it does not cause troublesome hormonal side effects. This is an important feature of the drug that is likely to help maintain compliance.
近期,醛固酮受体拮抗剂在慢性心力衰竭治疗中的应用再度引发关注。这主要是由于对醛固酮在包括纤维化和重塑、炎症以及儿茶酚胺作用增强等多个关键病理生理过程中的作用有了新的认识。随机螺内酯评估研究证实了辉瑞公司的螺内酯(安体舒通)在重度慢性心力衰竭治疗中的疗效,但该药物相关的激素副作用(男性乳房发育)成为一个问题。最近,依普利酮急性心肌梗死后心力衰竭疗效和生存研究为依普利酮(辉瑞公司的 Inspra)除与血管紧张素转换酶抑制剂或血管紧张素 II 受体阻滞剂及β受体阻滞剂联合进行神经激素阻断外,在急性心肌梗死后心力衰竭治疗中的应用提供了有力支持。这种策略有望对死亡率和发病率都产生益处。由于依普利酮是一种选择性醛固酮受体拮抗剂,它不会引起麻烦的激素副作用。这是该药物的一个重要特性,可能有助于维持患者的依从性。