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A study found that oral spironolactone had "about 10 to 20% of the feminizing effect of cyproterone acetate" on sexual differentiation in male rat fetuses, with a dose of 40 mg/day spironolactone having an effect equal to 1–3 mg/day cyproterone acetate.
A study found that spironolactone was not associated with teratogenicity in the offspring of rats. [161] [162] [163] Because it is an antiandrogen, however, spironolactone could theoretically have the potential to cause feminization of male fetuses at sufficient doses.
Spironolactone is a prodrug with a short terminal half-life of 1.4 hours. [ 5 ] [ 6 ] [ 7 ] The active metabolites of spironolactone have extended terminal half-lives of 13.8 hours for 7α-TMS, 15.0 hours for 6β-OH-7α-TMS, and 16.5 hours for canrenone, and accordingly, these metabolites are responsible for the therapeutic effects of the drug.
However, spironolactone is metabolized to three active metabolites, which give it prolonged activity (13.8 – 16. 5 hours). Spironolactone has a long half-life and is excreted 47-51% through kidneys. Patients with chronic kidney disease therefore require close monitoring when taking the drug. Spironolactone is also eliminated through feces (35-41%
Spironolactone is a prodrug with a short terminal half-life of 1.4 hours. [ 5 ] [ 6 ] [ 7 ] The active metabolites of spironolactone have extended terminal half-lives of 13.8 hours for 7α-TMS, 15.0 hours for 6β-OH-7α-TMS, and 16.5 hours for canrenone, and accordingly, these metabolites are responsible for the therapeutic effects of the drug.
The Randomized Aldactone Evaluation Study (RALES) trial is a landmark clinical study that assessed the impact of spironolactone, an aldosterone antagonist, on morbidity and mortality in patients with severe heart failure due to systolic dysfunction. [1] The findings from this trial significantly influenced the treatment guidelines for heart ...
Spironolactone is a prodrug with a short terminal half-life of 1.4 hours. [ 5 ] [ 6 ] [ 7 ] The active metabolites of spironolactone have extended terminal half-lives of 13.8 hours for 7α-TMS, 15.0 hours for 6β-OH-7α-TMS, and 16.5 hours for canrenone, and accordingly, these metabolites are responsible for the therapeutic effects of the drug.
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.
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