AGE-RELATED DIFFERENCES IN SALICYLAMIDE AND ACETAMINOPHEN CONJUGATION IN MAN

AGE-RELATED DIFFERENCES IN SALICYLAMIDE AND ACETAMINOPHEN CONJUGATION IN MAN
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DOI:
10.1016/s0022-3476(77)80787-7
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发表时间:
1977-01-01
影响因子:
5.1
通讯作者:
FISCHER, LJ
FISCHER, LJ
中科院分区:
医学2区
文献类型:
--
作者:
ALAM, SN;ROBERTS, RJ;FISCHER, LJ

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在儿童(7-10岁)和成人中同时口服水杨酰胺和对乙酰氨基酚(各 5 mg/kg)后,跟踪药物的葡萄糖醛酸和硫酸盐结合物的尿排泄情况。尿液中水杨酰胺结合物的半衰期在两个年龄组之间没有观察到显着差异。然而,观察到代谢途径中与年龄相关的变化。儿童中以水杨酰胺硫酸盐形式排泄的平均剂量百分比(78%)显着高于成人(36%)。相反,水杨酰胺葡萄糖醛酸是成人的主要排泄产物。对乙酰氨基酚缀合观察到类似的与年龄相关的差异。药代动力学分析表明,这些药物在儿童中葡萄糖醛酸结合的缺陷伴随着较高的硫酸盐形成率。
Following a concomitant oral dose of salicylamide and acetaminophen (5 mg/kg of each) the urinary excretion of glucuronide and sulfate conjugates of the drugs were followed in children (ages 7-10 yr) and adults. No significant difference was observed between the 2 age groups in the half-lives for appearance of salicylamide conjugates in urine. Age-related changes in the metabolic pathways, however, were observed. The mean percentage of dose excreted as salicylamide sulfate was significantly higher in children (78%) than in adults (36%). In contrast, salicylamide glucuronide was the major excretory product in adults. Similar age-related differences were observed for acetaminophen conjugation. Pharmacokinetic analysis indicated that the deficiency in glucuronide conjugation of these drugs in children was accompanied by a higher rate of sulfate formation.