Pharmacology · Cardiovascular Drugs (Antihypertensives, Anti-Anginals, Heart Failure, Anti-Arrhythmics)

Eplerenone is preferred over spironolactone in post-MI patients with left ventricular dysfunction (EPHESUS trial) for long-term treatment because:

  • A Eplerenone has greater aldosterone receptor affinity and provides superior cardiac remodeling prevention
  • B Eplerenone is more selective for the mineralocorticoid receptor with minimal sex hormone receptor activity, avoiding gynecomastia and impotence
  • C Eplerenone is metabolized to an active form that additionally inhibits cortisol synthesis
  • D Eplerenone provides superior renal protection compared to spironolactone in post-MI CKD
Correct answer: B. Eplerenone is more selective for the mineralocorticoid receptor with minimal sex hormone receptor activity, avoiding gynecomastia and impotence

Explanation

Spironolactone binds not only the mineralocorticoid receptor (MR) but also androgen receptors and progesterone receptors, causing dose-dependent gynecomastia, breast pain, and sexual dysfunction in men, and menstrual irregularities in women. Eplerenone is a more selective MR antagonist with negligible binding to androgen or progesterone receptors, thus lacking these sex hormone-related adverse effects. Both drugs reduce post-MI mortality in EF <40% patients, but eplerenone has better tolerability for long-term adherence.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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