@article {KARIM467, author = {A. KARIM and J. HRIBAR and W. AKSAMIT and M. DOHERTY and L. J. CHINN}, title = {SPIRONOLACTONE METABOLISM IN MAN STUDIED BY GAS CHROMATOGRAPHY-MASS SPECTROMETRY}, volume = {3}, number = {6}, pages = {467--478}, year = {1975}, publisher = {American Society for Pharmacology and Experimental Therapeutics}, abstract = {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 {\textmu}Ci). 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 6β-hydroxy-sulfoxide (X; 1.8\% of the dose). The remaining were the new metabolites, 15α-hydroxycanrenone (XI; 0.8\% of dose) and the 6β-hydroxy-thiomethyl derivative (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 Xl were present at extremely low levels. Copyright {\textcopyright} 1975 by The American Society for Pharmacology and Experimental Therapeutics}, issn = {0090-9556}, URL = {https://dmd.aspetjournals.org/content/3/6/467}, eprint = {https://dmd.aspetjournals.org/content/3/6/467.full.pdf}, journal = {Drug Metabolism and Disposition} }