The Sound of Evolution
Eplerenone
Mechanism of action:
Eplerenone is a selective mineralocorticoid receptor antagonist. Eplerenone competitively antagonizes aldosterone and acts primarily at the distal nephron of the kidney, especially in principal cells of the collecting duct. When aldosterone binds to the mineralocorticoid receptor, it increases the expression of the epithelial sodium channel (ENaC) and the Na⁺/K⁺-ATPase, leading to increased sodium and water reabsorption and increased potassium excretion. Eplerenone competitively blocks the mineralocorticoid receptor, thereby suppressing the expression and transport activity of sodium channels and the Na⁺/K⁺-ATPase.
Reference(s):
1. Moore TD et al. (2003). Eplerenone: a selective aldosterone receptor antagonist for hypertension and heart failure. Heart Dis.
2. Fraccarollo D et al. (2003). Additive improvement of left ventricular remodeling and neurohormonal activation by aldosterone receptor blockade with eplerenone and ACE inhibition in rats with myocardial infarction. J Am Coll Cardiol.