Brown Nancy J
Division of Clinical Pharmacology, Department of Medicine, Vanderbilt University Medical Center, Nashville, Tenn 37232-6602, USA.
Circulation. 2003 May 20;107(19):2512-8. doi: 10.1161/01.CIR.0000071081.35693.9A.
Data from animal studies and clinical trials indicate that aldosterone causes cardiovascular and renal injury through mineralocorticoid receptor-dependent mechanisms. However, although aldosterone receptor antagonism reduces mortality in patients with congestive heart failure, the progestational and antiandrogenic side effects of the nonspecific aldosterone receptor antagonist, spironolactone, have limited its usefulness in the treatment of hypertension. This review provides an overview of the pharmacology, efficacy, and safety of a new, more selective aldosterone receptor antagonist, eplerenone, in the context of emerging concepts of the role of aldosterone in cardiovascular toxicity.
来自动物研究和临床试验的数据表明，醛固酮通过盐皮质激素受体依赖性机制导致心血管和肾脏损伤。然而，尽管醛固酮受体拮抗剂可降低充血性心力衰竭患者的死亡率，但非特异性醛固酮受体拮抗剂螺内酯的孕激素样和抗雄激素副作用限制了其在高血压治疗中的应用。在醛固酮在心血管毒性中作用的新观念背景下，本综述概述了一种新型、更具选择性的醛固酮受体拮抗剂依普利酮的药理学、疗效和安全性。
