The renin-angiotensin-aldosterone system can be blocked at specific levels by using different classes of pharmacologic agents, including
angiotensin-converting-enzyme inhibitors,
angiotensin II receptor blockers and
mineralocorticoid receptor antagonists. Broad use of the latter, such as
spironolactone, has been limited by significant incidence of
gynecomastia and other sex-related adverse effects. These problems can be overcome with use of
eplerenone, a selective
mineralocorticoid receptor antagonist.
Eplerenone has been specifically developed to bind selectively to the
mineralocorticoid receptors in order to minimize binding to the
progesterone and
androgen receptors. In the last decade, multiple scientific evidences have been accumulated showing the efficacy and safety of the
drug in multiple clinical conditions, including
heart failure and arterial
hypertension.
Eplerenone is generally well tolerated, with the most frequent adverse event being
hyperkalemia, with sexual adverse events (i.e.
gynecomastia) being more uncommon, due to the selectivity of
eplerenone. This review focuses on the pharmacodynamic and pharmacokinetic properties of
eplerenone, thus providing the scientific basis to fully understand
drug-to-drug interactions, in particular, and its efficacy and tolerability, in general. Noteworthy, the activity of
eplerenone in special conditions and different patient populations is summarized.