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Due to its progestogenic (and by extension antigonadotropic) activity, CPA is able to suppress circulating testosterone levels by 70 to 80% in men at high dosages. [ 25 ] [ 94 ] In contrast, NSAAs increase testosterone levels by up to 2-fold via blockade of the AR , a difference that is due to their lack of concomitant antigonadotropic action ...
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]
[10] [96] It is an analogue of other spirolactones like spironolactone, canrenone, and spirorenone. [10] [96] 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. [97]
1957: The steroidal antiandrogen spironolactone is first synthesized [219] 1960: Spironolactone is first introduced for medical use, as an antimineralocorticoid [219] 1961: The steroidal antiandrogen cyproterone acetate is first synthesized [220] 1962: Spironolactone is first reported to produce gynecomastia in men [219] [221]
Spironolactone is used for the treatment of hirsutism in the United States. [40] High doses of spironolactone, which are needed for considerable antiandrogenic effects, are not recommended for men due to the high risk of feminization and other side effects.
[28] [16] In addition, the AR antagonism of spironolactone is involved in its feminizing side effects, such as gynecomastia in men. [28] Spironolactone has been found to produce gynecomastia without changes in testosterone or estradiol levels, implicating AR antagonism in this side effect. [30] Gynecomastia is a major known side effect of AR ...
Upon analysis, scientists found that participants who stayed on standard statin treatment for their lifetime increased their quality-adjusted life years by 0.24-0.70, and those on higher-intensity ...
[152] [148] [161] For these reasons, bicalutamide has replaced spironolactone in the treatment of the condition. [100]: 2139 For comparison to bicalutamide, a higher dosage of spironolactone of 5 mg/kg (or about 100 to 150 mg in boys that are 20 to 30 kg or 45 to 65 lbs) once daily is recommended for use in male peripheral precocious puberty.