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异戊巴比妥代谢物的独特模式。

Distinctive patterns of amobarbital metabolites.

作者信息

Kalow W, Tang B K, Kadar D, Inaba T

出版信息

Clin Pharmacol Ther. 1978 Nov;24(5):576-82. doi: 10.1002/cpt1978245576.

Abstract

This paper establishes that the relative proportion of amobarbital metabolites in urine is highly variable from person to person and that observations of plasma half-life give no indication of this variability, but it shows that a valid estimate of a given person's metabolite pattern can be obtained by studying a single urine specimen in the postdistributive phase. The two metabolites which were measured in urine accounted on the average of 9 subjects for 80% +/- 3% of the dose with a range from 66% to 94%. The two metabolites were the well known 3'-hydroxyamobarbital (COH) as a product of side chain hydroxylation and N-beta-D-glucopyranosyl amobarbital (N-glu), a glucose conjugate which at some earlier time had been mistaken for an N-hydroxylation product. Among 129 volunteer subjects, the metabolite ratio N-glu/COH showed a median value of about 0.5 with a range from 0 to 2.8. A virtual absence of N-glu was observed in one of the 129 subjects and confirmed by a second administration of amobarbital 3 mo later. Of the 14 subjects with predominant N-glu excretion 4 were of Chinese origin, while there were 6 Chinese among the 115 other subjects (p less than 0.02).

摘要

本文证实,尿液中异戊巴比妥代谢物的相对比例因人而异,血浆半衰期的观察结果无法显示这种变异性,但研究表明,在分布后阶段分析单个尿液样本,就能有效估计特定个体的代谢物模式。在9名受试者的尿液中检测到的两种代谢物,平均占给药剂量的80%±3%,范围为66%至94%。这两种代谢物分别是众所周知的3'-羟基异戊巴比妥(COH),它是侧链羟基化的产物;以及N-β-D-吡喃葡萄糖基异戊巴比妥(N-葡糖),一种葡萄糖结合物,在早些时候曾被误认为是N-羟基化产物。在129名志愿者中,代谢物N-葡糖/COH的比例中位数约为0.5,范围从0至2.8。在129名受试者中有1名几乎没有N-葡糖,3个月后再次给予异戊巴比妥得到了证实。在14名以N-葡糖排泄为主的受试者中,有4名是华裔,而在其他115名受试者中有6名华裔(p<0.02)。

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