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阿米卡星在研发过程中的药代动力学变化。

Modification in the pharmacokinetics of amikacin during development.

作者信息

Lanao J M, Dominguez-Gil A, Dominguez-Gil A A, Málaga S, Crespo M, Nuño F

出版信息

Eur J Clin Pharmacol. 1982;23(2):155-60. doi: 10.1007/BF00545971.

Abstract

The disposition kinetics of a single i.v. dose of amikacin was studied in 6 neonates (6-25 days old), 10 infants (4-18 months) and 8 young children (3-11 years). There was a progressive change in the distribution and elimination kinetics during development. The distribution coefficient of the antibiotic averaged of 0.429, 0.320 and 0.210 l/kg in the newborns, infants and young children, respectively and serum half-life (t1/2 beta) in these three groups averaged 2.812, 1.803 and 1.196 h, respectively. Significant differences in certain pharmacokinetic parameters were found between the values in paediatric patients and in adults receiving the same dose. A linear relationship was established between the distribution volume of the antibiotic and the weight of the patients, as defined by the following equation: Vdss (1) = 0.976 + 0.140 . TBW (kg); r = 0.954. The results suggest that a regimen of very frequent administrations should be employed in infants and young children in order to maintain a therapeutic level throughout treatment.

摘要

对6名新生儿(6 - 25日龄)、10名婴儿(4 - 18个月)和8名幼儿(3 - 11岁)进行了单次静脉注射阿米卡星的处置动力学研究。在发育过程中,分布和消除动力学存在渐进性变化。抗生素的分布系数在新生儿、婴儿和幼儿中分别平均为0.429、0.320和0.210升/千克,这三组的血清半衰期(t1/2β)分别平均为2.812、1.803和1.196小时。在接受相同剂量的儿科患者和成人的值之间,某些药代动力学参数存在显著差异。抗生素的分布容积与患者体重之间建立了线性关系,由以下方程定义:Vdss(1)=0.976 + 0.140·TBW(kg);r = 0.954。结果表明,为了在整个治疗过程中维持治疗水平,应采用非常频繁给药的方案用于婴儿和幼儿。

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