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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.
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]
Eplerenone differs from spironolactone in its extensive metabolism, with a short half-life and inactive metabolites. [4] Eplerenone seems to be about 50 to 75% as potent as spironolactone as an antimineralocorticoid. [24] Hence, 25 mg/day spironolactone may be equivalent to approximately 50 mg/day eplerenone. [25]
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 ] )
For most people, recommendations are to reduce blood pressure to less than or equal to somewhere between 140/90 mmHg and 160/100 mmHg. [2] In general, for people with elevated blood pressure, attempting to achieve lower levels of blood pressure than the recommended 140/90 mmHg will create more harm than benefits, [3] in particular for older people. [4]
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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.