Turnbull L B, Teng L, Newman J, Chremos A N, Bruce R B
Drug Metab Dispos. 1976 May-Jun;4(3):269-75.
Bethanidine is metabolized in the rat and dog to a significant degree to N-benzyl-N'-methylguanidine, N-benzylguanidine, N-hydroxybenzyl-N'-methylguanidine, N-methylguanidine, N-hydroxybenzyl-N',N''-di-methylguanidine, and benzoic acid, whereas in man the drug is not metabolized. It is readily absorbed in all three 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.
苄胍在大鼠和狗体内会大量代谢为N-苄基-N'-甲基胍、N-苄基胍、N-羟基苄基-N'-甲基胍、N-甲基胍、N-羟基苄基-N',N''-二甲基胍和苯甲酸，而在人体内该药物不发生代谢。它在这三种物种中均易于吸收。人体的消除动力学显示尿排泄率和血液中药物下降速率之间存在差异。全身放射自显影显示，在富含肾上腺素能神经末梢的大鼠组织中药物浓度很高，但血脑屏障的穿透（若有）不明显。
