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Spironolactone has been found to increase LDL ("bad") cholesterol and decrease HDL ("good") cholesterol levels at the relatively high doses used in women with polycystic ovary syndrome (PCOS). [ 149 ] [ 150 ] As such, it may have unfavorable effects on the blood lipid profile in this context.
The AR antagonism of spironolactone mostly underlies its antiandrogenic activity and is the major mechanism responsible for its therapeutic benefits in the treatment of androgen-dependent conditions like acne, hirsutism, and pattern hair loss and its usefulness in hormone therapy for transgender women.
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 ...
Unlike spironolactone, bicalutamide has no antimineralocorticoid activity, [97] and for this reason, has no risk of hyperkalemia (which can, rarely/in severe cases, result in hospitalization or death) [112] or other antimineralocorticoid side effects such as urinary frequency, dehydration, hypotension, hyponatremia, metabolic acidosis, or ...
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. [5] [6]
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Polycystic ovary syndrome, or polycystic ovarian syndrome (PCOS), is the most common endocrine disorder in women of reproductive age. [14] The syndrome is named after cysts which form on the ovaries of some women with this condition, though this is not a universal symptom and not the underlying cause of the disorder.