USMLE

Danazol

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Reproductive Pharm
  1. Leuprolide
  2. Anastrozole
  3. Estrogens
  4. Clomiphene
  5. Progestins
  6. Mifepristone
  7. Copper IUDs
  8. Danazol
  9. Terbutaline, Ritodrine
  10. Minoxidil
  11. Androgens (Testosterone, Methyltestosterone)
  12. Flutamide
  13. PDE-5 Inhibitors (Sildenafil, Vardenafil, Tadalafil)
  14. Finasteride

Summary

Danazol is a partial agonist at the androgen receptor. It increases androgenic activity, which then suppresses estrogen production by way of negative feedback at the pituitary gland.  Danazol is indicated for the treatment of endometriosis. Side effects of danazol use include the development of masculine symptoms in women, such as muscle development, increased acne, and facial hair.

Key Points

  • Danazol
    • Mechanism 
      • Complex with multiple proposed mechanisms
      • Synthetic partial agonist at androgen receptors
        • Also modulates estrogen, progesterone, and gonadotropin receptors
        • May modulate LH/FSH levels and inhibit steroid hormone synthesis
    • Indications
      • Endometriosis
        • Decreased estrogen production may reduce excess endometrial tissue causing pain and other symptoms
      • Hereditary angioedema
        • May reduce the number of swelling attacks in hereditary angioedema
        • Decreased LH and FSH → increased C1 esterase→ inhibits  kallikrein→ lower levels of bradykinin
    • Adverse Effects
      • Masculinization (androgenic)
        • Due to agonist activity at androgen receptors
          • Enlarged clitoris (clitoromegaly), Excessive hair growth (hirsutism), Deepening of the voice, Acne, Breast atrophy
      • Pseudotumor Cerebri (Idiopathic Intracranial Hypertension)
      • Hepatotoxicity
      • Weight gain
        • Due to fluid retention (edema)