Eplerenone--a novel selective aldosterone blocker

Ann Pharmacother. 2002 Oct;36(10):1567-76. doi: 10.1345/aph.1C027.


Objective: To review the pharmacology, pharmacokinetics, clinical efficacy, and safety of eplerenone, a new selective aldosterone blocker.

Data sources: Primary literature and review articles were obtained via MEDLINE search (1966-April 2002). Additional studies and abstracts were identified from the bibliographies of reviewed literature.

Study selection and data extraction: Studies and review articles related to eplerenone, aldosterone, aldosterone antagonist, and spironolactone were reviewed. Data pertinent to this article were included.

Data synthesis: Eplerenone is a selective aldosterone blocker. Recent data have demonstrated the deleterious effects of aldosterone in several chronic disease states including hypertension and heart failure. Animal studies using eplerenone have shown a positive role for aldosterone antagonism in the treatment of hypertension, heart failure, myocardial infarction, renal disease, and atherosclerosis. In humans, eplerenone appears to be effective for the treatment of hypertension. An ongoing study will examine the effect of eplerenone for heart failure. To date, the incidence of adverse effects with eplerenone has been slightly lower than with spironolactone.

Conclusions: Eplerenone appears to be a promising drug in a new class of agents called selective aldosterone blockers. The drug may be approved for treatment of hypertension in 2002. Additional studies are ongoing that may provide information on other clinical uses for this medication.

Publication types

  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic
  • Eplerenone
  • Heart Failure / drug therapy
  • Humans
  • Hypertension / drug therapy
  • Mineralocorticoid Receptor Antagonists / adverse effects
  • Mineralocorticoid Receptor Antagonists / pharmacokinetics
  • Mineralocorticoid Receptor Antagonists / pharmacology*
  • Mineralocorticoid Receptor Antagonists / therapeutic use
  • Spironolactone / adverse effects
  • Spironolactone / analogs & derivatives*
  • Spironolactone / pharmacokinetics
  • Spironolactone / pharmacology*
  • Spironolactone / therapeutic use


  • Mineralocorticoid Receptor Antagonists
  • Spironolactone
  • Eplerenone