Eplerenone: A Review of Its Use in Patients with Chronic Systolic Heart Failure and Mild Symptoms

被引:15
作者
Dhillon, Sohita [1 ]
机构
[1] Adis Int Ltd, Auckland 0754, New Zealand
关键词
LEFT-VENTRICULAR DYSFUNCTION; ALDOSTERONE-RECEPTOR ANTAGONISM; LONG-TERM MONOTHERAPY; ATRIAL-FIBRILLATION; MYOCARDIAL-INFARCTION; PATIENTS HOSPITALIZATION; ACE-INHIBITION; EMPHASIS-HF; ESSENTIAL-HYPERTENSION; ENDOTHELIAL FUNCTION;
D O I
10.1007/s40265-013-0098-z
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Eplerenone (Inspra(A (R))) is a selective mineralocorticoid receptor antagonist (MRA). In the EU, it is approved for use (in addition to standard optimal therapy) to reduce the risk of cardiovascular (CV) mortality and morbidity in adult patients with chronic systolic heart failure (HF) and mild symptoms. This article reviews the efficacy and tolerability of eplerenone in this indication and briefly summarizes its pharmacology. In the EMPHASIS-HF study, relative to placebo, the addition of eplerenone to optimal background therapy significantly reduced the risk of death from CV causes or hospitalization for HF in patients with chronic systolic HF and mild symptoms. Benefits of eplerenone therapy over placebo were also observed in several secondary outcomes, including: death from any cause or hospitalization for HF; death from any cause; hospitalization for any reason; or hospitalization for HF. Eplerenone was generally well tolerated in this study, with the most frequent adverse event being hyperkalaemia, which is a known adverse event of the drug class. Sexual adverse events (e.g. gynecomastia) occurred in < 1 % of eplerenone recipients, reflecting the selectivity of eplerenone for mineralocorticoid receptors. Based on these results, European guidelines have been updated and recommend the use of an MRA to reduce the risk of HF hospitalization and premature death in all patients with persisting symptoms (New York Heart Association class II-IV) and a left-ventricular ejection fraction of a parts per thousand currency sign35 %, despite treatment with ACE inhibitor (or an angiotensin receptor blocker if an ACE inhibitor is not tolerated) and a beta-blocker.
引用
收藏
页码:1451 / 1462
页数:12
相关论文
共 72 条
  • [1] Aldosterone Antagonists - Last Man Standing?
    Armstrong, Paul W.
    [J]. NEW ENGLAND JOURNAL OF MEDICINE, 2011, 364 (01) : 79 - 80
  • [2] High plasma aldosterone levels on admission are associated with death in patients presenting with acute ST-elevation myocardial infarction
    Beygui, Farzin
    Collet, Jean-Philippe
    Benoliel, Jean-Jacques
    Vignolles, Nicolas
    Dumaine, Raphaelle
    Barthelemy, Olivier
    Montalescot, Gilles
    [J]. CIRCULATION, 2006, 114 (24) : 2604 - 2610
  • [3] Blacher J, 1997, AM J HYPERTENS, V10, P1326, DOI 10.1016/S0895-7061(97)00301-4
  • [4] Eplerenone - Cardiovascular protection
    Brown, NJ
    [J]. CIRCULATION, 2003, 107 (19) : 2512 - 2518
  • [5] Aldosterone and cardiovascular disease - Smoke and fire
    Calhoun, David A.
    [J]. CIRCULATION, 2006, 114 (24) : 2572 - 2574
  • [6] Center for Drug Evaluation and Research, 2003, 21437 NDA CTR DRUG E
  • [7] Center for Drug Evaluation and Research, 2003, 21437S002 CTR DRUG E
  • [8] CLELAND JGF, 1987, BRIT HEART J, V58, P572
  • [9] Pharmacokinetics and metabolism of [14C]eplerenone after oral administration to humans
    Cook, CS
    Berry, LM
    Bible, RH
    Hribar, JD
    Hajdu, E
    Liu, NW
    [J]. DRUG METABOLISM AND DISPOSITION, 2003, 31 (11) : 1448 - 1455
  • [10] Spironolactone impairs endothelial function and heart rate variability in patients with Type 2 diabetes
    Davies, JI
    Band, M
    Morris, A
    Struthers, AD
    [J]. DIABETOLOGIA, 2004, 47 (10) : 1687 - 1694