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A comparison of the aldosterone-blocking agents eplerenone and spironolactone.

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  • 1. Division of Medicine and Therapeutics, Ninewells Hospital and Medical School, Dundee, UK.
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    • Struthers A 1
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Clinical Cardiology, 01 Apr 2008, 31(4):153-158
https://doi.org/10.1002/clc.20324 PMID: 18404673 PMCID: PMC6652937

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A comment on this article appears in "A comparison of the aldosterone-blocking agents eplerenone and spironolactone." Clin Cardiol. 2009 Apr;32(4):230.

Abstract 

Improved understanding of the adverse pharmacological properties of aldosterone has prompted investigation of the clinical benefits of blocking aldosterone at the receptor level. This article reviews the pharmacology, clinical efficacy, and tolerability of the two available blocking agents, spironolactone and eplerenone. A Medline search identified clinical studies assessing spironolactone and eplerenone. Priority was given to large, well-controlled, clinical trials and comparative studies. Pharmacological differences between spironolactone and eplerenone include lower affinity of eplerenone for progesterone, androgen, and glucocorticoid receptors; more consistently demonstrated nongenomic properties for eplerenone; and the presence of long-acting metabolites for spironolactone. Both agents effectively treat hypertension and heart failure but comparisons are complicated by the deficiency of head-to-head trials and differences between patient populations. There are differences in the tolerability profiles; spironolactone is associated with dose-dependent sexual side effects. Both agents produce dose-dependent increases in potassium concentrations, although the effect with spironolactone appears to be greater when both agents are administered at recommended doses. Choice of a specific agent should be based on individual patient issues, such as the nature of heart failure and patient concerns about adverse events.

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Logo of clincardiolLink to Publisher's site
Clin Cardiol. 2008 Apr; 31(4): 153–158.
Published online 2008 Apr 10. https://doi.org/10.1002/clc.20324
PMCID: PMC6652937
PMID: 18404673

A Comparison of the Aldosterone‐blocking Agents Eplerenone and Spironolactone

Allan Struthers, MD,corresponding author 1 Henry Krum, MD, PhD, 2 and Gordon H. Williams, MD 3
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Abstract

Improved understanding of the adverse pharmacological properties of aldosterone has prompted investigation of the clinical benefits of blocking aldosterone at the receptor level. This article reviews the pharmacology, clinical efficacy, and tolerability of the two available blocking agents, spironolactone and eplerenone. A Medline search identified clinical studies assessing spironolactone and eplerenone. Priority was given to large, well‐controlled, clinical trials and comparative studies. Pharmacological differences between spironolactone and eplerenone include lower affinity of eplerenone for progesterone, androgen, and glucocorticoid receptors; more consistently demonstrated nongenomic properties for eplerenone; and the presence of long‐acting metabolites for spironolactone. Both agents effectively treat hypertension and heart failure but comparisons are complicated by the deficiency of head‐to‐head trials and differences between patient populations. There are differences in the tolerability profiles; spironolactone is associated with dose‐dependent sexual side effects. Both agents produce dose‐dependent increases in potassium concentrations, although the effect with spironolactone appears to be greater when both agents are administered at recommended doses. Choice of a specific agent should be based on individual patient issues, such as the nature of heart failure and patient concerns about adverse events. Copyright © 2008 Wiley Periodicals, Inc.

Keywords: eplerenone, spironolactone, aldosterone blockade, hypertension, heart failure

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Selected References

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