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The metabolism of [14C]‐debrisoquine in man.
Author(s) -
Idle JR,
Mahgoub A,
Angelo MM,
Dring LG,
Lancaster R,
Smith RL
Publication year - 1979
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1979.tb00930.x
Subject(s) - debrisoquine , urine , metabolite , excretion , metabolism , chemistry , feces , pharmacokinetics , pharmacology , biology , biochemistry , cyp2d6 , cytochrome p450 , paleontology
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.