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Chlormadinone acetate (CMA), sold under the brand names Belara, Gynorelle, Lutéran, and Prostal among others, is a progestin and antiandrogen medication which is used in birth control pills to prevent pregnancy, as a component of menopausal hormone therapy, in the treatment of gynecological disorders, and in the treatment of androgen-dependent conditions like enlarged prostate and prostate ...
Medroxyprogesterone acetate (Amen, Curretab, Cycrin, Provera) – 2.5 mg, 5 mg, 10 mg; Megestrol acetate (Megace) – 20 mg, 40 mg – approved specifically for the treatment of breast and endometrial cancer [46] and for the treatment of anorexia, cachexia, and weight loss in patients with AIDS Tooltip acquired immunodeficiency syndrome [47]
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 ...
Cyproterone is a potent antiandrogen, similarly to CPA. [5] [6] However, it has approximately three-fold lower potency as an antagonist of the androgen receptor (AR) relative to CPA. [6] Like CPA, cyproterone is actually a weak partial agonist of the AR, and hence has the potential for both antiandrogenic and androgenic activity in some ...
[159] [193] Based on ovulation inhibition, a dosage of 50 mg/day cyproterone acetate has on the order of 200 times the progestogenic potency of 2.5 mg/day medroxyprogesterone acetate. [159] [193] In addition to its progestogenic activity, CPA produces androgen and estrogen deficiency when used as a monotherapy, [194] and this influences health ...
Testosterone levels with 100 to 300 mg/day oral cyproterone acetate and low-dose oral estrogen in men. [160] The estrogen used was 0.1 mg/day diethylstilbestrol (DES), [160] which has been described as an "extremely low" dosage. [87] Levels of testosterone were decreased by about 95% with the combination and by about 61% with cyproterone ...
[125] [126] [127] Combined birth control pills containing different progestins result in SHBG levels that are increased 1.5- to 2-fold with levonorgestrel, 2.5- to 4-fold with desogestrel and gestodene, 3.5- to 4-fold with drospirenone and dienogest, and 4- to 5-fold with cyproterone acetate. [125]
[84] [85] [7] [8] Aside from cyproterone acetate and chlormadinone acetate, a few other progestins used in oral contraceptives and/or in menopausal HRT including dienogest, drospirenone, medrogestone, nomegestrol acetate, promegestone, and trimegestone also have varying degrees of AR antagonistic activity. [86] [87] [88]