人体内多态性乙酰化的氨鲁米特
Polymorphically acetylated aminoglutethimide in humans.
作者信息
Coombes R C, Foster A B, Harland S J, Jarman M, Nice E C
出版信息
Br J Cancer. 1982 Sep;46(3):340-5. doi: 10.1038/bjc.1982.209.
The urinary excretion during 24 h of aminoglutethimide (AG) its major metabolite (N-acetylAG) and two minor metabolites (N-formylAG and nitroG) were measured in 10 volunteers given AG who had been typed for acetylator phenotype using sulphadimidine. The slow acetylators of sulphadimidine excreted more AG (mean 28% of the administered dose) than did the fast acetylators (12%), but the latter excreted more of the dose as N-acetylAG (8.8%) than did the former (3.9%). NitroG and N-formylAG were minor urinary metabolites of AG in humans. The former was more abundant in the urine of slow acetylators (0.10% of the dose) than in that of fast acetylators (0.047%), whereas the respective proportions of doses excreted as the N-formyl derivative (0.475 and 0.465%) were not significantly different for the two acetylator phenotypes. These results show that AG is among those drugs that are polymorphically acetylated in humans.
在10名服用氨鲁米特（AG）的志愿者中，测定了24小时内AG及其主要代谢产物（N - 乙酰AG）和两种次要代谢产物（N - 甲酰AG和硝基AG）的尿排泄量。这些志愿者已通过磺胺二甲嘧啶确定了乙酰化表型。磺胺二甲嘧啶的慢乙酰化者排泄的AG（平均占给药剂量的28%）比快乙酰化者（12%）多，但快乙酰化者排泄的剂量中以N - 乙酰AG形式存在的比例（8.8%）比慢乙酰化者（3.9%）高。硝基AG和N - 甲酰AG是AG在人体中的次要尿代谢产物。前者在慢乙酰化者尿液中的含量（占剂量的0.10%）比快乙酰化者尿液中的含量（0.047%）高，而两种乙酰化表型以N - 甲酰衍生物形式排泄的剂量比例（分别为0.475%和0.465%）没有显著差异。这些结果表明，AG是人类中存在多态性乙酰化的药物之一。
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