METABOLISM OF [C-14]-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. 1979 The British Pharmacological Society