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儿科人群与成人之间药代动力学差异的因素和机制。

Factors and Mechanisms for Pharmacokinetic Differences between Pediatric Population and Adults.

机构信息

Department of Pharmacy, Getafe University Hospital, Carretera Toledo Km 12,5 Getafe, Madrid, Spain.

出版信息

Pharmaceutics. 2011 Feb 7;3(1):53-72. doi: 10.3390/pharmaceutics3010053.

Abstract

Many physiologic differences between children and adults may result in age-related changes in pharmacokinetics and pharmacodynamics. Factors such as gastric pH and emptying time, intestinal transit time, immaturity of secretion and activity of bile and pancreatic fluid among other factors determine the oral bioavailability of pediatric and adult populations. Anatomical, physiological and biochemical characteristics in children also affect the bioavailability of other routes of administration. Key factors explaining differences in drug distribution between the pediatric population and adults are membrane permeability, plasma protein binding and total body water. As far as drug metabolism is concerned, important differences have been found in the pediatric population compared with adults both for phase I and phase II metabolic enzymes. Immaturity of glomerular filtration, renal tubular secretion and tubular reabsorption at birth and their maturation determine the different excretion of drugs in the pediatric population compared to adults.

摘要

许多生理差异在儿童和成人之间可能导致与年龄相关的药代动力学和药效学变化。胃 pH 值和排空时间、肠转运时间、胆汁和胰腺液分泌和活性的不成熟等因素决定了儿科和成人人群的口服生物利用度。儿童的解剖、生理和生化特征也会影响其他给药途径的生物利用度。解释儿科人群与成人之间药物分布差异的关键因素是膜通透性、血浆蛋白结合和总体水。就药物代谢而言,与成人相比,儿科人群中发现了重要的差异,无论是在 I 相和 II 相代谢酶方面。出生时肾小球滤过、肾小管分泌和重吸收的不成熟及其成熟决定了与成人相比,儿科人群中药物的不同排泄。

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