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人体中水杨酰胺和对乙酰氨基酚结合反应的年龄相关差异。

Age-related differences in salicylamide and acetaminophen conjugation in man.

作者信息

Alam S N, Roberts R J, Fischer L J

出版信息

J Pediatr. 1977 Jan;90(1):130-5. doi: 10.1016/s0022-3476(77)80787-7.

DOI:10.1016/s0022-3476(77)80787-7
PMID:830879
Abstract

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 seven to ten years) and adults. No significant difference were observed between the two 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 is accompanied by a higher rate of sulfate formation.

摘要

给儿童(7至10岁)和成人同时口服水杨酰胺和对乙酰氨基酚(各5毫克/千克)后,对药物的葡萄糖醛酸苷和硫酸酯结合物的尿排泄情况进行了跟踪。两个年龄组之间尿中水杨酰胺结合物出现的半衰期无显著差异。然而,观察到了代谢途径中与年龄相关的变化。儿童中以硫酸水杨酰胺形式排泄的剂量平均百分比(78%)显著高于成人(36%)。相比之下,水杨酰胺葡萄糖醛酸苷是成人的主要排泄产物。对乙酰氨基酚结合也观察到了类似的与年龄相关的差异。药代动力学分析表明,儿童中这些药物葡萄糖醛酸结合的缺乏伴随着较高的硫酸酯形成速率。

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Age-related differences in salicylamide and acetaminophen conjugation in man.人体中水杨酰胺和对乙酰氨基酚结合反应的年龄相关差异。
J Pediatr. 1977 Jan;90(1):130-5. doi: 10.1016/s0022-3476(77)80787-7.
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Effect of route of administration on competitive drug biotransformation interaction: salicylamide-ascorbic acid interaction in rats.给药途径对竞争性药物生物转化相互作用的影响:大鼠体内水杨酰胺 - 抗坏血酸的相互作用
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