Spironolactone metabolism in man studied by gas chromatography-mass spectrometry.

TitleSpironolactone metabolism in man studied by gas chromatography-mass spectrometry.
Publication TypeJournal Article
Year of Publication1975
AuthorsKarim A, Hribar J, Aksamit W, Doherty M, Chinn LJ
JournalDrug Metab Dispos
Date Published1975 Nov-Dec
KeywordsCanrenone, Chromatography, Gas, Chromatography, Thin Layer, Humans, Male, Mass Spectrometry, Spectrophotometry, Infrared, Spironolactone, Sulfhydryl Compounds, Sulfoxides

Gas chromatography-mass spectrometry was used to identify metabolites of spironolactone in human blood and urine. In three healthy men about 20% of the radioactivity was excreted in the urine within 24 hr after an oral dose of [20-3H]spironolactone (200 mg + 200 muCi). About half of this radioactivity was extracted with chloroform at pH 3 and from this extract four stable metabolites were isolated by use of column and thin-layer chromatography. Two of these were the previously identified metabolites, canrenone (VII; 2.9% of dose) and the 6beta-hydroxy-sulfoxide (X; 1.8% of the dose). The remaining were the new metabolites, 15alpha-hydroxycanrenone (XI; 0.8% of dose) and the 6beta-hydroxy-thiomethyl derivatives (VI; 0.5% of dose). The principal water-soluble urinary metabolite was canrenoate ester glucuronide (XII; 4.5% of dose). In the 24- to 32-hr pooled serum, canrenone (VII) was the principal metabolite in the organic-extractable fraction; VI was present in appreciable amounts but X and XI were present at extremely low levels.

Alternate JournalDrug Metab Dispos
PubMed ID1221

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