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Eplerenone lowers blood pressure in patients with primary hypertension. [9] Eplerenone also reduces arterial stiffness and vascular endothelial dysfunction. [10] For persons with resistant hypertension, eplerenone is safe and effective for reducing blood pressure, [11] particularly in persons with resistant hypertension due to ...
Eplerenone is a newer drug that was developed as a spironolactone analog with reduced adverse effects. In addition to the y-lactone ring and the substituent on C-7, eplerenone has a 9α,11α-epoxy group. This group is believed to be the reason why eplerenone has a 20-40-fold lower affinity for the mineralocorticoid receptor than spironolactone. [7]
They are typically used as an adjunct in management of hypertension, cirrhosis, and congestive heart failure. [3] The steroidal aldosterone antagonists can also be used for treatment of primary hyperaldosteronism. Spironolactone, a steroidal aldosterone antagonist, is also used in management of female hirsutism and acne from PCOS or other ...
eplerenone; spironolactone; Aldosterone receptor antagonists are not recommended as first-line agents for blood pressure, [47] but spironolactone and eplerenone are both used in the treatment of heart failure and resistant hypertension.
Spironolactone is used in the treatment of hyperaldosteronism (high aldosterone levels or mineralocorticoid excess), for instance primary aldosteronism (Conn's syndrome). [47] Antimineralocorticoids like spironolactone and eplerenone are first-line treatments for hyperaldosteronism. [47]
Guidelines on the choice of agents and how best to step up treatment for various subgroups in hypertension (high blood pressure) have changed over time and differ between countries. A Comparison of International Guidelines on Goal Blood Pressure and Initial Therapy for Adults With Hypertension (adapted from JNC 8 guidelines [ 1 ] )
The AR antagonism of spironolactone mostly underlies its antiandrogenic activity and is the major mechanism responsible for its therapeutic benefits in the treatment of androgen-dependent conditions like acne, hirsutism, and pattern hair loss and its usefulness in hormone therapy for transgender women.
Eplerenone is also contraindicated for the treatment of hypertension in patients with type 2 diabetes with microalbuminuria, serum creatinine greater than 2.0 mg/dL in males or greater than 1.8 mg ...