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[30] [70] [71] [72] Although spironolactone is said to be a relatively weak inhibitor of 17α-hydroxylase and 17,20-lyase, [73] [30] at least compared to more potent steroidogenesis inhibitors like ketoconazole and abiraterone acetate (which can reduce testosterone concentrations to castrate levels), this action may contribute to a significant ...
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 ...
[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]
A nonsteroidal antiandrogen (NSAA) is an antiandrogen with a nonsteroidal chemical structure. [1] [2] [3] They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the effects of androgens like testosterone and dihydrotestosterone (DHT).
Eplerenone may have a lower incidence than spironolactone of sexual side effects such as feminization, gynecomastia, impotence, low sex drive and reduction of size of male genitalia. [18] This is because other antimineralocorticoids have structural elements of the progesterone molecule, causing progestogenic and antiandrogenic outcomes. [ 4 ]
For this observational study, researchers analyzed data from the U.K. Biobank and Whitehall II study of more than 20,000 adults in the U.K. 70 years and older with or without previous ...
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]
The RALES trial [30] showed that the addition of spironolactone can improve mortality, particularly in severe cardiomyopathy (ejection fraction less than 25%.) The related medication eplerenone was shown in the EPHESUS trial [ 31 ] to have a similar effect, and it is specifically labelled for use in decompensated heart failure complicating ...