Summary
During 5 days following a single oral dose of 3H-11-bromovincamine (40 mg) to two human subjects, means of 55% and 27% of the3H dose were excreted in the urine and faeces respectively, mainly within 24 and 48 h.
Mean plasma concentrations of3H reached a peak (1900 ng equiv./ml) at 1 h after dosing and declined biphasically with half-lives of 5 h and 11 h which were similar to half-lives for urinary excretion of3H. Parent drug and 11 -bromovincaminic acid were the major dose-related components in plasma at 1.5 and 3 h. Mean plasma concentrations of 11-bromovincamine reached a peak (620 ng/ml) at 0.75 h and declined biphasically with half-lives of about 1 h and 5 h.
The major urinary metabolite was 11-bromovincaminic acid (31% dose). Also present in urine were 11-bromovincamine (3%), 11-bromoapovincamine (1%) and 2 unknown metabolites (9% and 6%). Similar metabolites were detected in faecal extracts.
If inadequately stored in biological samples, 11-bromovincamine could be hydrolysed to 11-bromovincaminic acid and be epimerised to 11-bromo-epivincamine.
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Mayo, B.C., Biggs, S.R., Hawkins, D.R. et al. The metabolic fate of 11-bromo[15-3H]vincamine in man. European Journal of Drug Metabolism and Pharmacokinetics 10, 189–196 (1985). https://doi.org/10.1007/BF03189741
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DOI: https://doi.org/10.1007/BF03189741