The cardiovascular effects of eplerenone, a selective aldosterone-receptor antagonist
The cardiovascular effects of eplerenone, a selective aldosterone-receptor antagonist
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DOI：
10.1016/s0149-2918(03)80326-0
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发表时间：
2003-11-01
影响因子：
3.2
通讯作者：
Nappi, JM
中科院分区：
文献类型：
--
作者：
Davis, KL;Nappi, JM
背景资料：肾素-血管紧张素-醛固酮系统在高血压和心力衰竭的病理生理学和治疗中的作用已被广泛研究。血管紧张素转换酶抑制剂和血管紧张素II受体阻滞剂已被证明可有效降低血压，保护肾脏，降低心力衰竭患者的发病率和死亡率。因此，在心血管疾病的治疗中，对醛固酮的作用和醛固酮受体拮抗剂的使用越来越感兴趣。依普利酮是第一个被批准用于治疗高血压和急性心肌梗死（AMI）后左室功能不全的选择性醛固酮受体拮抗剂。目的：本文旨在综述依普利酮治疗高血压、左室功能不全和蛋白尿的药理学特性、临床疗效和耐受性。方法：通过检索MEDLINE确定相关英文文献（1966- 2003年5月），最新目录和国际药学文摘（1970- 2003年5月）使用术语高血压、心力衰竭、依普利酮、醛固酮和醛固酮拮抗剂。从已识别文章的参考文献列表中识别出其他相关出版物。信息也获得了在全国会议上提出的摘要和存档的数据与manufacturer.Results：在临床试验中，依普利酮单独和与肾素-血管紧张素阻滞剂相结合显着降低收缩压和舒张压与安慰剂相比（P < 0.05至P < 0.001）。在EPHESUS（依普利酮对急性心肌梗死后心力衰竭疗效和生存率的研究）中，在最佳药物治疗中加入依普利酮降低了AMI和LV功能障碍患者的发病率和死亡率，尽管严重高钾血症的发生率也显著增加。与螺内酯相比，依普利酮与男性乳房发育症和其他性高潮相关的不良反应的发生率较低。结论：无论是弥补或与其他抗高血压药物相结合，依普利酮似乎是有效的治疗高血压。当依普利酮加入标准治疗AMI并发左室功能障碍时，发病率和死亡率降低。依普利酮用于高血压或心力衰竭的用途可能限制在具有高钾血症风险的患者中（Clin Ther. 2003 25：2647-2668）版权所有（C）2003 Excerpta Medica，Inc.
Background: The role of the renin-angiotensin-aldosterone system in the pathophysiology and treatment of hypertension and heart failure has been extensively studied. Angiotensin-converting enzyme inhibitors and angiotensin II-receptor blockers have been shown to effectively reduce blood pressure, protect the kidney, and reduce morbidity and mortality in patients with heart failure. Therefore, there is increased interest in the effects of aldosterone and the use of aldosterone-receptor antagonists in the treatment of cardiovascular disease. Eplerenone is the first selective aldosterone-receptor antagonist approved for the treatment of hypertension and left ventricular (LV) dysfunction after acute myocardial infarction (AMI).Objective: The goal of this article was to review the pharmacologic properties, clinical efficacy, and tolerability of eplerenone in the treatment of hypertension, LV dysfunction, and proteinuria.Methods: Relevant English-language articles were identified through searches of MEDLINE (1966-May 2003), Current Contents, and International Pharmaceutical Abstracts (1970-May 2003) using the terms hypertension, heart failure, eplerenone, aldosterone, and aldosterone antagonist. Other pertinent publications were identified from the reference lists of the identified articles. Information was also obtained from abstracts presented at national meetings and data on file with the manufacturer.Results: In clinical trials, eplerenone alone and in combination with renin-angiotensin blockade significantly reduced both systolic and diastolic blood pressure compared with placebo (P < 0.05 to P < 0.001). In EPHESUS (Eplerenone Post-Acute Myocardial Infarction Heart Failure Efficacy and Survival Study), the addition of epterenone to optimal medical therapy reduced morbidity and mortality in patients with AMI and LV dysfunction, although the incidence of serious hyper-kalemia was also significantly greater. In comparisons with spironolactone, eplerenone was associated with a lower incidence of gynecomastia and other sex hormone-related adverse effects.Conclusions: Either atone or in combination with other antihypertensive agents, eplerenone appears to be effective for the treatment of hypertension. Morbidity and mortality were reduced when eplerenone was added to standard therapy for LV dysfunction complicating AMI. The use of eplerenone for hypertension or heart failure may be limited in patients at risk for hyperkalemia, (Clin Ther. 2003 25:2647-2668) Copyright (C) 2003 Excerpta Medica, Inc.