Updated: 12/3/2021

Antiandrogens

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  • Snapshot
    • A 52-year-old man presents to his primary care physician for a routine visit. On further questioning, the patient reports increased daytime urinary frequency, nocturia, slow urinary stream, and terminal dribbling. On digital rectal exam there is an enlarged prostate. The patient was started on finasteride. (Benign prostatic hyperplasia)
  • Finasteride
    • Mechanism of action
      • 5α-reductase inhibitor resulting in
        • ↓ conversion of testosterone to dihydrotestosterone
    • Clinical use
      • benign prostatic hyperplasia (BPH)
      • androgenetic alopecia (in men only)
        • also known as male pattern baldness
    • Toxicity
      • dizziness
  • Flutamide
    • Mechanism of action
      • testosterone receptor blocker
    • Clinical use
      • prostate cancer
    • Toxicity
      • hot flashes
      • decreased libido
  • Ketoconazole
    • Mechanism of action
      • multiple mechanisms
        • inhibits cytochrome P450 (14α-demethylase)
          • results in increased fungal cellular permeability
        • inhibits fungal biosynthesis of triglycerides and phospholipids
        • impairs androgen synthesis
          • by inhibiting 17,20-desmolase/17α-hydroxylase
    • Clinical use
      • prostate cancer
    • Toxicity
      • gynecomastia
      • amenorrhea
  • Spironolactone
    • Mechanism of action
      • potassium sparing diuretic
        • competitive aldosterone receptor inhibitor in the cortical collecting tubule
          • inhibits 17,20-desmolase/17α-hydroxylase
    • Clinical use
      • hirsutism
      • acne vulgaris (in women)
    • Toxicity
      • gynecomastia
      • amenorrhea
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