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Spironolactone has been identified as an inhibitor of NRG1‐ERBB4 signaling. [142] Spironolactone has been found to act as a potent inhibitor of the pannexin 1 channel, and this action appears to be involved in its antihypertensive effects independently of MR antagonism. [143] Spironolactone has been found to block hERG channels. [144]
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 ...
[173] [174] In men, a study found that treatment with a relatively low dosage of 20 μg/day ethinylestradiol for 5 weeks increased circulating SHBG levels by 150% and, due to the accompanying decrease free testosterone levels, increased total circulating levels of testosterone by 50% (via reduced negative feedback by androgens on the HPG axis).
Eplerenone differs from spironolactone in its extensive metabolism, with a short half-life and inactive metabolites. [4] Eplerenone seems to be about 50 to 75% as potent as spironolactone as an antimineralocorticoid. [24] Hence, 25 mg/day spironolactone may be equivalent to approximately 50 mg/day eplerenone. [25]
[86] [111] For example, about 20% of women experienced menstrual irregularities with 50 to 100 mg/day spironolactone, whereas about 70% experienced menstrual irregularities at 200 mg/day. [63] Most women taking moderate doses of spironolactone develop amenorrhea, and normal menstruation usually returns within two months of discontinuation. [111]
Bicalutamide is used primarily in the treatment of early and advanced prostate cancer. [1] It is approved at a dosage of 50 mg/day as a combination therapy with a gonadotropin-releasing hormone analogue (GnRH analogue) or orchiectomy (that is, surgical or medical castration) in the treatment of stage D2 metastatic prostate cancer (mPC), [2] [3] and as a monotherapy at a dosage of 150 mg/day ...
Spironolactone – most widespread use, inexpensive; Eplerenone – more selective so reduced side-effects but more expensive and less potent; Finerenone – non-steroidal, more selective and potent than spironolactone and eplerenone; Canrenone – very limited use
This is a complete list of androgens/anabolic steroids (AAS) and formulations that are approved by the FDA Tooltip Food and Drug Administration and available in the United States.