The metabolism of [14C]-debrisoquine in man.
1 The synthesis of [14C]-debrisoquine hydrochloride and 4-hydroxy-debrisoquine sulphate is described. 2 The metabolic fate and excretion profile in both urine and faeces of 14C-labelled debrisoquine was studied in five healthy human subjects. 3 Investigations showed that the drug is well-absorbed after a single oral dose of 32 mg and quantitatively eliminated from the body within three days. 4 4-Hydroxy-debrisoquine is the major metabolite of debrisoquine, although significant amounts of 5-,6-, 7- and 8-hydroxy-debrisoquine are also formed. 5 Electron-capture gas chromatography is a useful method for measuring debrisoquine and its five hydroxylated metabolites in urine at the pg level.
D000328:Adult; D001711:Biotransformation; D002849:Chromatography, Gas; D003647:Debrisoquin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000378:metabolism*; D005243:Feces / Q000032:analysis; D005410:Flame Ionization; D006801:Humans; D007546:Isoquinolines / Q000378:metabolism*; D008297:Male; D013058:Mass Spectrometry; D011865:Radioisotope Dilution Technique
D007546:Isoquinolines; D003647:Debrisoquin