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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 ...
Canrenone is an active metabolite of spironolactone, canrenoic acid, and potassium canrenoate, and is considered to be partially responsible for their effects. [9] It has been found to have approximately 10 to 25% of the potassium-sparing diuretic effect of spironolactone, [ 16 ] whereas another metabolite, 7α-thiomethylspironolactone (7α-TMS ...
[9] [95] It is an analogue of other spirolactones like spironolactone, canrenone, and spirorenone. [9] [95] Drospirenone differs structurally from spironolactone only in that the C7α acetyl thio substitution of spironolactone has been removed and two methylene groups have been substituted in at the C6β–7β and C15β–16β positions. [96]
[4] [22] [23] It can also be used to block the effects of testosterone in transgender women and nonbinary people undergoing feminizing hormone replacement therapy. [24] Spironolactone usually available in tablets, taken by mouth, though topical forms are also available. [4]
A steroidal antiandrogen (SAA) is an antiandrogen with a steroidal chemical structure. [1] [2] [3] They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like testosterone and dihydrotestosterone (DHT) and by suppressing gonadal androgen production.
CPA/EE-containing birth control pills were developed by 1975 [20] [21] and were first introduced for medical use in 1978. [22] They originally contained 50 μg EE (Diane); subsequently, the EE dosage was decreased to 35 μg in a new "low-dose" preparation in 1986 (Diane-35).
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This use of the drug is off-label, however, not having been approved by the Food and Drug Administration and without data on long-term effects of this use. [needs update] [18] They are also sometimes used as alternatives to antiandrogens like spironolactone and cyproterone acetate for suppressing testosterone production in transgender women.
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