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Published Online, 8 December 2004, www.theannals.com, DOI 10.1345/aph.1E306.
The Annals of Pharmacotherapy: Vol. 39, No. 1, pp. 68-76. DOI 10.1345/aph.1E306
© 2005 Harvey Whitney Books Company.
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FORMULARY FORUM

Eplerenone: A Selective Aldosterone Receptor Antagonist for Patients with Heart Failure

Brian J Barnes, PharmD

Assistant Professor, Department of Pharmacy Practice; Clinical Pharmacist, Department of Cardiothoracic Surgery, University of Kansas Medical Center, Kansas City, KS

Patricia A Howard, PharmD FCCP BCPS (AQ CV)

Professor and Vice Chair, Department of Pharmacy Practice, University of Kansas Medical Center

Reprints: Dr. Barnes, Department of Pharmacy Practice, University of Kansas Medical Center, Mail Stop 4047, 3901 Rainbow Blvd., Kansas City, KS 66160-7231, fax 913/588-2355, bbarnes{at}kumc.edu

OBJECTIVE: To evaluate the pharmacology, pharmacokinetics, safety, and clinical use of eplerenone in heart failure (HF).

DATA SOURCES: English-language MEDLINE searches were performed from 1966 to May 2004. Key words included eplerenone, aldosterone receptor antagonist, heart failure, myocardial infarction, left-ventricular dysfunction, and cost-effectiveness. Additional references were identified from bibliographies of selected articles.

STUDY SELECTION AND DATA EXTRACTION: Human trials evaluating the efficacy, safety, and cost-effectiveness of aldosterone receptor antagonists in HF were evaluated.

DATA SYNTHESIS: Eplerenone is the first selective aldosterone receptor antagonist. The drug is indicated to improve the survival of stable patients with left-ventricular systolic dysfunction (ejection fraction <40%) and clinical evidence of HF following acute myocardial infarction. Efficacy and safety in this population have been demonstrated in a large, randomized clinical trial. Eplerenone is associated with severe and sometimes life-threatening hyperkalemia. Patients with reduced renal function and diabetes, as well as those on other drugs that increase potassium levels, are at highest risk. Eplerenone is metabolized by the cytochrome P450 system and may interact with drugs that interfere with this system. A major advantage of eplerenone over the nonselective aldosterone receptor antagonist spironolactone is lack of binding to progesterone and androgen receptors, which is associated with drug-induced gynecomastia, breast pain, and impotence.

CONCLUSIONS: The addition of eplerenone to traditional HF therapy has been shown to reduce morbidity and mortality in patients who develop left-ventricular dysfunction after acute myocardial infarction. Eplerenone's selectivity reduces sex hormone–related adverse effects. Despite these benefits, the overall cost-effectiveness has yet to be determined.

Key Words: aldosterone receptor antagonist, eplerenone, heart failure, left-ventricular dysfunction

Published Online, December 8, 2004. www.theannals.com, DOI 10.1345/aph.1E306

THIS ARTICLE IS APPROVED FOR CONTINUING EDUCATION CREDIT
ACPE UNIVERSAL PROGRAM NUMBER:
407-000-05-001-H01


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