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Antiandrogens alter the androgen pathway by blocking the appropriate receptors, competing for binding sites on the cell's surface, or affecting androgen production.

There are steroidal and nonsteroidal compounds.

  • The nonsteroidal include: Flutamide and Nilutamide.
  • The steroidal include Cyproterone, a more hepatotoxic and less effective drug.

[edit] Indications

  • Prostate cancer: antiandrogens are mainly used for prostate cancer, the androgen-dependent one.
  • Benign prostatic hyperplasia (Dutasteride (Avodart), Finasteride (Proscar))
  • Androgenic alopecia (Finasteride)
  • Acne, amenorrhea, seborrhea and hirsutism (Women)
  • Antiandrogens are sometimes used with analogues or agonists of GnRH used for the treatment of advanced Prostate Cancer. GnRH analogues or agonists, by binding to the gonadotropin releasing hormone receptor lead to an initial stimulation of gonadotropins release that temporary rise serum testosterone before downregulating the secretion of gonadotropins leading to a dramatic reduction in testosterone.
    Antiandrogens like Bicalutamide (Casodex) are strongly recommended as adjunctive therapy before starting and during the first weeks of GnRH agonist therapy in order to prevent the initial and temporary rise in serum testosterone (flare up effect)

Agonists Androstanolone   Dihydrotestosterone   Fluoxymesterone   Mesterolone   Methyltestosterone   Testosterone
Antiandrogens Androgen antagonists Bicalutamide   Chlormadinone acetate   Cyproterone acetate   Dienogest   Drospirenone   Flutamide   Nilutamide   Spironolactone
5α reductase inhibitors Dutasteride (Avodart)   Finasteride (Proscar)