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Spironolactone antagonizes the effects of exogenous testosterone administered to castrated animals. [30] It works by binding to the AR and displacing androgens like testosterone and DHT from the receptor, thereby reducing its activation by these hormones. [28]
Conversely, in studies of healthy men given high-dose spironolactone, gynecomastia occurred in 3 of 10 (30%) at 100 mg/day, in 5 of 8 (62.5%) at 200 mg/day, and in 6 of 9 (66.7%) at 400 mg/day, relative to none of 12 controls. [134] [135] The severity of gynecomastia with spironolactone varies considerably, but is usually mild. [110]
Spirolactones are a class of functional group in organic chemistry featuring a cyclic ester attached spiro to another ring system. The name is also used to refer to a class of synthetic steroids, called steroid-17α-spirolactones, 17α-spirolactosteroids, or simply 17α-spirolactones, which feature their spirolactone group at the C17α position.
1962: Spironolactone is first reported to produce gynecomastia in men [219] [221] 1966: Benorterone is the first known antiandrogen to be studied clinically, to treat acne and hirsutism in women [ 222 ] [ 223 ]
Aldosterone antagonists: spironolactone, which is a competitive antagonist of aldosterone. Aldosterone normally adds sodium channels in the principal cells of the collecting duct and late distal tubule of the nephron. Spironolactone prevents aldosterone from entering the principal cells, preventing sodium reabsorption.
Spironolactone (SC-9420; Aldactone) followed and had both good oral bioavailability and potency, and was the first synthetic antimineralocorticoid to be marketed. [3] It has about 46-fold higher oral potency than SC-5233.
In some cases, other medications like spironolactone may be prescribed off-label for hair loss. This is typically only used in women and not in men, because in men it can lead to gynecomastia ...
The trial was stopped early because the beneficial effect of spironolactone on all-cause death exceeded the prespecified discontinuation requirements. Spironolactone reduced the risk of death by 30% compared to placebo. Additionally, there was a 35% reduction in the risk of hospitalization for worsening heart failure in the spironolactone group.