Isolation and identification of the N-oxide metabolite of picobenzide in human urine

The possible presence of metabolites was investigated in the urine of 14 patients treated with N-(4-picolyl) 3,5 dimethyl benzamide (picobenzide) after an i.v. dose of 10 mg/Kg. The metabolites formed were isolated by liquid-liquid extraction processes and chromatographic techniques. The main metabo...

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Bibliographic Details
Published in:European journal of drug metabolism and pharmacokinetics 1986, Vol.11 (1), p.23-27
Main Authors: NIETO, M. J, HDEZ HDEZ, J. M, LANAO, J. M, FERNANDEZ, C, DOMINGUEZ-GIL, A
Format: Article
Language:English
Subjects:
Adult
Benzamides - isolation & purification
Benzamides - metabolism
Benzamides - urine
Biological and medical sciences
Biotransformation
Chromatography, Thin Layer
Humans
Magnetic Resonance Spectroscopy
Mass Spectrometry
Medical sciences
Middle Aged
Neuropharmacology
Pharmacology. Drug treatments
Psycholeptics: tranquillizer, neuroleptic
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Spectrophotometry, Infrared
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Summary:The possible presence of metabolites was investigated in the urine of 14 patients treated with N-(4-picolyl) 3,5 dimethyl benzamide (picobenzide) after an i.v. dose of 10 mg/Kg. The metabolites formed were isolated by liquid-liquid extraction processes and chromatographic techniques. The main metabolite of this neuroleptic agent is the N-oxide derivative, which appears in urine together with the unaltered drug. Identification of the metabolite was made by I.R. spectroscopy, nuclear magnetic resonance (NMR) and mass spectroscopy. Its structure was confirmed by comparison with the metabolite obtained by synthesis.
ISSN:0378-7966
2107-0180
DOI:10.1007/BF03189771