Cone E J, Darwin W D, Gorodetzky C W, Tan T
Drug Metab Dispos. 1978 Jul-Aug;6(4):488-93.
The metabolism of hydrocodone was studied in man, rat, guinea pig, rabbit, and dog. Routes of metabolism included O-demethylation, N-dealkylation, and 6-keto-reduction to the corresponding 6-alpha- and 6-beta-hydroxy metabolites, where each metabolic pathway produces an active metabolite. Mean total recovery of drug and metabolites as percentage of administered dose ranged from a low of 10.6% for the rabbit to a high of 46.8% for the guinea pig; man was intermediate at 25.7%. For man, approximately 70% of the total drug recovered was excreted in the first 24 hr, and the remainder by 72 hr. Considerable species differences were observed in the patterns of metabolism of hydrocodone. Also, stereoselectivity of 6-keto reduction to the beta-form was observed for all species in the reduction of hydrocodone and hydromorphone with the exception of the reduction of hydrocodone by man.
在人、大鼠、豚鼠、兔子和狗身上研究了氢可酮的代谢情况。代谢途径包括O-去甲基化、N-脱烷基化以及6-酮还原为相应的6-α-和6-β-羟基代谢物，其中每条代谢途径都会产生一种活性代谢物。药物和代谢物的平均总回收率（占给药剂量的百分比）范围从兔子的低至10.6%到豚鼠的高至46.8%；人的回收率处于中间水平，为25.7%。对于人来说，回收的总药物中约70%在最初24小时内排出，其余在72小时内排出。在氢可酮的代谢模式中观察到了显著的种属差异。此外，除人对氢可酮的还原外，在所有物种中，氢可酮和氢吗啡酮的6-酮还原为β-形式时均观察到立体选择性。
