Document Detail


Eplerenone: a selective aldosterone blocker.
MedLine Citation:
PMID:  12931252     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Recent studies suggest that aldosterone may play a larger role than once appreciated in normal physiologic function and cardiovascular disease. Some of the adverse cardiovascular effects that have been described include cardiac and vascular fibrosis, vascular necrosis and inflammation, impaired endothelial function, reduced fibrinolysis, hypertension, left ventricular hypertrophy (LVH), congestive heart failure, and cardiac arrhythmias. In light of these findings, the ability to block the actions of aldosterone has gained increased therapeutic importance. Eplerenone is a selective aldosterone receptor blocker that displays little interaction with androgen and progesterone receptors. Eplerenone has already been approved for the treatment of systemic hypertension and has been evaluated in numerous hypertension subgroups, including patients with low plasma renin activity; diabetes; LVH; uncontrolled blood pressure while receiving monotherapy with angiotensin-converting enzyme inhibitors, angiotensin-receptor blockers, calcium channel blockers, or beta-blockers; and in black patients. Results of these trials indicate that eplerenone lowers blood pressure and reduces end-organ damage. Further proof of the therapeutic importance of mineralocorticoid receptor blockade comes from the eplerenone post acute myocardial infarction survival and efficacy study (EPHESUS). In this large-scale clinical outcome trial, eplerenone was shown to reduce total mortality by 15% as well as the combined endpoint of cardiovascular mortality/cardiovascular hospitalization by 13% when administered at a mean of 7.3 days post myocardial infarction to patients with evidence of systolic left ventricular dysfunction and symptoms of heart failure. Eplerenone is well tolerated, with an adverse effect profile comparable to placebo. The advent of selective aldosterone blockers, such as eplerenone, should prove to be of great therapeutic value in hypertension control and prevention of cardiovascular disease and associated end-organ damage.
Authors:
Charles T Stier
Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.; Review    
Journal Detail:
Title:  Cardiovascular drug reviews     Volume:  21     ISSN:  0897-5957     ISO Abbreviation:  Cardiovasc Drug Rev     Publication Date:  2003  
Date Detail:
Created Date:  2003-08-21     Completed Date:  2004-02-20     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  9006912     Medline TA:  Cardiovasc Drug Rev     Country:  United States    
Other Details:
Languages:  eng     Pagination:  169-84     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, New York Medical College, Valhalla, NY 10595, USA. Charles_Stier@nymc.edu.
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MeSH Terms
Descriptor/Qualifier:
Aldosterone Antagonists / pharmacokinetics,  pharmacology*,  therapeutic use*
Animals
Clinical Trials as Topic
Heart Failure / drug therapy,  etiology
Humans
Hypertension / complications,  drug therapy
Hypertrophy, Left Ventricular / drug therapy,  etiology
Spironolactone / analogs & derivatives*,  pharmacokinetics,  pharmacology*,  therapeutic use*
Grant Support
ID/Acronym/Agency:
HL-35522/HL/NHLBI NIH HHS
Chemical
Reg. No./Substance:
0/Aldosterone Antagonists; 0/eplerenone; 52-01-7/Spironolactone

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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