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Spironolactone also commonly and dose-dependently produces gynecomastia (breast development) as a side effect in men. [ 110 ] [ 129 ] [ 131 ] [ 132 ] At low doses, the rate is only 5 to 10%, [ 132 ] but at high doses, up to or exceeding 50% of men may develop gynecomastia.
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. [35] [36]
Structural formula of the potassium-sparing diuretics. Click to enlarge. Potassium-sparing diuretics or antikaliuretics [1] refer to drugs that cause diuresis without causing potassium loss in the urine. [2] They are typically used as an adjunct in management of hypertension, cirrhosis, and congestive heart failure. [3]
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Pharmacokinetics of 100 mg/day spironolactone and its metabolites Compound C max Tooltip Peak concentrations (day 1) C max Tooltip Peak concentrations (day 15) AUC Tooltip Area-under-the-curve concentrations (day 15) t 1/2 Tooltip Elimination half-life; Spironolactone: 72 ng/mL (173 nmol/L) 80 ng/mL (192 nmol/L) 231 ng•hour/mL (555 nmol ...
Consideration has to be given to what is known as "drug loading" - the ratio of the active drug to the total contents of the dose. A low drug load may cause homogeneity problems. A high drug load may pose flow problems or require large capsules if the compound has a low bulk density.
They are also sometimes used as alternatives to antiandrogens like spironolactone and cyproterone acetate for suppressing testosterone production in transgender women. [19] [20] [21] It also is used for suppressing estrogen production in transgender men. [22] It is considered a possible treatment for paraphilias. [23]