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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 ...
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]
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]
Unlike antigonadotropic antiandrogens like cyproterone acetate and GnRH analogues, bicalutamide does not suppress production of testosterone or estradiol and instead actually increases it [citation needed], which has an important involvement in the differential side-effect profiles of the medications. [citation needed]
Cyproterone acetate was developed to overcome this problem. It is formed by adding an acetate group to cyproterone, see figure 3. Cyproterone acetate has a dual mode of action as it competes directly with DHT for binding to AR, but also inhibits gonadotropin secretion. It thereby reduces androgen, estrogen and LH levels.
The Food and Drug Administration (FDA) stated in 2015 that neither the benefits nor the safety of testosterone have been established for low testosterone levels due to aging. [17] The FDA has required that testosterone labels include warning information about the possibility of an increased risk of heart attacks and stroke. [17]
Testosterone levels with 100 to 300 mg/day oral cyproterone acetate and low-dose oral estrogen in men. [11] The estrogen used was 0.1 mg/day diethylstilbestrol (DES), [11] which has been described as an "extremely low" dosage. [12] Levels of testosterone were decreased by about 95% with the combination and by about 61% with cyproterone acetate ...
The side effects of cyproterone acetate (CPA), a steroidal antiandrogen and progestin, including its frequent and rare side effects, have been studied and characterized.It is generally well-tolerated and has a mild side-effect profile, regardless of dosage, when it used as a progestin or antiandrogen in combination with an estrogen such as ethinylestradiol or estradiol valerate in women.