Eplerenone Pharmacology

Eplerenone is an antimineralocorticoid, or an adversary of the mineralocorticoid receptor (MR). Eplerenone is aswell accepted chemically as 9,11α-epoxy-7α-methoxycarbonyl-3-oxo-17α-pregn-4-ene-21,17-carbolactone and "was acquired from spironolactone by the addition of a 9α,11α-epoxy arch and by barter of the 17α-thoacetyl accumulation of spironolactone with a carbomethoxy group". The biologic controls top claret burden by bounden the aldosterone hormone to the mineralocorticoid receptor (MR) in epithelial tissues, such as the kidney.

This helps to access claret aggregate and adapt claret pressure.It has 10- to 20-fold lower affection for the MR about to spironolactone, and is beneath almighty in vivo as an antimineralocorticoid.However, in adverse to spironolactone, eplerenone has little affection for the androgen, progesterone, and glucocorticoid receptors. It aswell has added consistently empiric non-genomic antimineralocorticoid furnishings about to spironolactone (see film mineralocorticoid receptor). Eplerenone differs from spironolactone in its all-encompassing metabolism, with a abbreviate half-life and abeyant metabolites.