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Testosterone, the major endogenous androgen and the target mediator of antiandrogens.. This is a list of antiandrogens, [1] or drugs that prevent the effects of androgens like testosterone and dihydrotestosterone (DHT). [2]
Relative to steroidal antiandrogens like cyproterone acetate and spironolactone, bicalutamide has better selectivity in its action, superior efficacy as an antagonist of the androgen receptor, and better tolerability. Bicalutamide also shows a better safety profile than cyproterone acetate.
A study found that oral spironolactone had "about 10 to 20% of the feminizing effect of cyproterone acetate" on sexual differentiation in male rat fetuses, with a dose of 40 mg/day spironolactone having an effect equal to 1–3 mg/day cyproterone acetate. [35] [36]
1967: Cyproterone acetate was first studied clinically, to treat sexual deviance in men [225] 1969: Cyproterone acetate was first studied in the treatment of acne, hirsutism, seborrhea, and scalp hair loss in women [226] 1969: The antiandrogenic activity of spironolactone is discovered [227]
Testosterone levels with 300 mg/week cyproterone acetate or 100 mg/month estradiol undecylate both by intramuscular injection in men. [139] Solid lines are average and dashed lines highest and lowest levels. Levels of testosterone decreased by 75% with cyproterone acetate and by 91% with estradiol undecylate. [139]
Spironolactone is considered to be a first-line treatment for hirsutism, finasteride and the steroidal antiandrogen cyproterone acetate are considered to be second-line treatments, and flutamide is no longer recommended for hirsutism due to liver toxicity concerns. [68]
Cyproterone acetate (CPA), sold alone under the brand name Androcur or with ethinylestradiol under the brand names Diane or Diane-35 among others, is an antiandrogen and progestin medication used in the treatment of androgen-dependent conditions such as acne, excessive body hair growth, early puberty, and prostate cancer, as a component of feminizing hormone therapy for transgender individuals ...
5–20 mg every 2 wks Estradiol dipropionate: Agofollin: Estrogen: IM, SC: 2–10 mg/wk or 5–20 mg every 2 wks Estradiol benzoate: Progynon-B: Estrogen: IM, SC: 0.5–1.5 mg every 2–3 days Estriol: Ovestin [c] Estrogen: Oral: 4–6 mg/day Spironolactone: Aldactone: Antiandrogen: Oral: 100–400 mg/day Cyproterone acetate: Androcur ...
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