Distinctive patterns of amobarbital metabolites

Distinctive patterns of amobarbital metabolites
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异戊巴比妥代谢物的独特模式

DOI:
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发表时间:
1978
期刊:
Clinical pharmacology and therapy
影响因子:
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通讯作者:
T. Inaba
T. Inaba
中科院分区:
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文献类型:
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作者:
W. Kalow;B. Tang;D. Kadar;T. Inaba

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本文证实了尿液中异巴比妥代谢物的相对比例因人而异,血浆半衰期的观察并没有给出这种变化的迹象,但它表明,通过研究分布后阶段的单个尿样,可以获得对特定人的代谢物模式的有效估计。尿中两种代谢物平均占受试者剂量的80%±3%,范围为66%~94%。这两种代谢物分别是众所周知的侧链羟化产物3‘-羟基异巴比妥和N-β-D-葡萄糖异巴比妥(N-Glu),N-Glu是一种葡萄糖偶联物,曾被误认为是N-羟基化产物。在129名志愿者中,N-Glu/COH代谢物比率的中位数约为0.5,范围为0至2.8。在129名受试者中有一人观察到N-Glu的实际缺失,并在3个月后再次服用异巴比妥证实。在14名以N-Glu排泄为主的受试者中,有4名来自中国,而在115名其他受试者中,有6名是中国人(p<0.02)。
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‐β‐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 < 0.02).