The clinical pharmacology of eplerenone.
Eplerenone is an aldosterone receptor antagonist indicated for the treatment of hypertension and congestive heart failure. Eplerenone contains an epoxy group, which offers greater mineralocorticoid receptor specificity. It is an effective antihypertensive that has been shown to reduce morbidity and mortality in individuals with left ventricular dysfunction post myocardial infarction. Studies are continuing to determine whether the benefit of mineralocorticoid receptor blockade in advanced congestive heart failure is also observed when eplerenone treatment is initiated in earlier stages of the disease. The most common side effect is hyperkalemia necessitating close monitoring in individuals with diabetes and proteinuria, heart failure or in those who are taking moderate CYP450 3A4 inhibitors. It is category B in pregnancy.
Muldowney
James A
JA
Vanderbilt University Medical Center, Division of Cardiovascular Medicine, Department of Internal Medicine, 383 Preston Research Building, Nashville, Tennessee 37232-6300, USA. james.muldowney@vanderbilt.edu
Schoenhard
John A
JA
Benge
Cassandra D
CD
D000818:Animals; D018849:Controlled Clinical Trials as Topic / Q000379:methods; D000077545:Eplerenone; D006333:Heart Failure / Q000188:drug therapy / Q000378:metabolism; D006801:Humans; D006947:Hyperkalemia / Q000139:chemically induced / Q000378:metabolism; D000451:Mineralocorticoid Receptor Antagonists / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D013148:Spironolactone / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use
D000451:Mineralocorticoid Receptor Antagonists; D013148:Spironolactone; D000077545:Eplerenone