Spironolactone
Spironolactone. Aldosterone receptor antagonist (mineralocorticoid receptor) — K+-sparing diuretic; also weak androgen receptor antagonist (used… Oral half-life 1.4 h.
Aldosterone receptor antagonist (mineralocorticoid receptor) — K+-sparing diuretic; also weak androgen receptor antagonist (used off-label for acne, female-pattern hair loss, PCOS). Hyperkalemia risk; gynecomastia from anti-androgen activity.
PK models the PARENT, which is a prodrug, and that is the record limitation rather than a citation defect. Half-life corrected 1.5 -> 1.4 h, the figure its own paper states. THE PARENT IS ABOUT 3% OF ACTIVE EXPOSURE: the same abstract gives day-15 areas under the curve of 231 for spironolactone against 2173 for canrenone and 2804 and 1727 for two further active metabolites, whose half-lives are 13.8 to 16.5 h. A 1.4 h curve therefore shows the effect gone in about six hours when real mineralocorticoid blockade lasts a day. ka 1.5 /h, V 80 L and F 0.9 dropped: none appears in the abstract, the V and F were a default shared with an unrelated record, and no volume or absolute bioavailability exists for spironolactone at all, since there is no intravenous formulation.
Pharmacokinetics
- Oral — t½ 1.4 h
Sources: PMID:26073023, PMID:1261153