Pharmacology · Corticosteroids and Sex Hormones (OCPs, Androgens)

A woman presents with hirsutism and acne. She is started on spironolactone. The rationale for this use is:

  • A Spironolactone is a progesterone receptor agonist that reduces LH and FSH secretion
  • B Spironolactone is an aldosterone antagonist that also blocks androgen receptors and inhibits 5-alpha reductase, reducing androgenic effects on hair follicles and sebaceous glands
  • C Spironolactone inhibits CYP17 (17-alpha hydroxylase), blocking adrenal androgen synthesis
  • D Spironolactone is a GnRH antagonist that reduces ovarian androgen secretion
Correct answer: B. Spironolactone is an aldosterone antagonist that also blocks androgen receptors and inhibits 5-alpha reductase, reducing androgenic effects on hair follicles and sebaceous glands

Explanation

Spironolactone competitively antagonises the mineralocorticoid (aldosterone) receptor but also has anti-androgen properties: it competitively blocks androgen (dihydrotestosterone) receptors in hair follicles and sebaceous glands and weakly inhibits 5-alpha reductase (the enzyme converting testosterone to DHT). These combined actions reduce androgen-driven hirsutism and acne. CYP17 inhibition is the mechanism of abiraterone (used in prostate cancer). GnRH antagonists (like cetrorelix) are used in fertility treatment.

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

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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