Eplerenone is metabolised by CYP3A4 but does not inhibit or induce CYP 3A4 or 2C9. It is a selective aldosterone antagonist, with less than 1 % affinity for glucocorticoid, progesterone and androgen receptors.

Eplerenone is competitive mineralocorticoid (aldosterone) receptor antagonist.

Eplerenone is given orally in the management of hypertension and heart failure. It is an aldosterone antagonist with properties similar to those of spironolactone, but with a higher selectivity for the aldosterone receptor. Eplerenone binds selectively to mineralocorticoid receptors and has low (less than 1%) affinity for glucocorticoid, progesterone, and androgen receptors. The steroid-related adverse effects (e.g., gynecomastia, impotence, menstrual abnormalities) occur less frequently with eplerenone than with spironolactone. Common adverse reactions of eplerenone that can be confused with an acute porphyric attack are diarrhoea, abdominal pain and nausea.

Eplerenone metabolism is primarily mediated via CYP3A4. Eplerenone is not an inhibitor or inducer of the (CYP) isoenzymes 1A2, 3A4, 2C19, 2C9, or 2D6 (Cook, 2002; Muldowney III, 2009; Tolbert, 2002).