DISPOSITION OF BETHANIDINE, N-BENZYL-N',N''-DIMETHYLGUANIDINE, IN RAT, DOG AND MAN

  • 1 January 1976
    • journal article
    • research article
    • Vol. 4  (3) , 269-275
Abstract
Bethanidine is metabolized in the rat and dog to a significant degree to N-benzyl-N''-methylguanidine, N-benzylguanidine, N-hydroxybenzyl-N''-methylguanidine, N-hydroxybenzyl-N'',N"-dimethylguanidine and benzoic acid, whereas in man the drug is not metabolized. It is readily absorbed in all 3 species. The elimination kinetics in man show a difference between the urinary excretion rate and the rate of decline in the blood. Whole body autoradiograms showed a high concentration of drug in rat tissues rich in adrenergic nerve terminals, but insignificant penetration, if any, of the blood-brain barrier.

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