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替考拉宁在儿科患者中的药代动力学。

Pharmacokinetics of teicoplanin in pediatric patients.

作者信息

Terragna A, Ferrea G, Loy A, Danese A, Bernareggi A, Cavenaghi L, Rosina R

机构信息

First Infectious Diseases Clinic, University of Genova, G. Gaslini Institute, Italy.

出版信息

Antimicrob Agents Chemother. 1988 Aug;32(8):1223-6. doi: 10.1128/AAC.32.8.1223.

Abstract

The pharmacokinetics of teicoplanin have been studied in 13 pediatric male patients from 2 to 12 years of age. Patients were given a single 3-mg/kg intravenous dose of teicoplanin for prophylaxis. Blood and urine samples were collected for 8 days after administration, and teicoplanin levels were determined by microbiological assay. Pharmacokinetic parameters were estimated from a three-compartment open pharmacokinetic model and from a noncompartmental analysis. Levels in plasma 1 h after the administration averaged 14.8 mg/liter. The half-lives of the two distribution phases were 1.3 and 9.7 h. The half-life of the terminal phase averaged 57.9 h, with similar estimates obtained from the noncompartmental analysis and from data from urine. The volume of distribution of the central compartment was 0.15 liter/kg, whereas the volume of distribution at steady state and during the elimination phase were 0.80 and 1.25 liters/kg. The total teicoplanin clearance averaged 14.8 ml/h per kg, with renal clearance accounting for about 60% of the total. The average cumulative recovery of teicoplanin in urine over 8 days was 59% of the dose, similar to the value obtained in adult volunteers. There was no significant linear correlation between elimination half-life and age. Preliminary data after repeated administration support the reliability of the model used and the validity of the mean estimated parameters. There were no local or systemic adverse reactions to teicoplanin.

摘要

已对13名2至12岁的儿科男性患者进行了替考拉宁的药代动力学研究。患者接受单次3毫克/千克静脉注射替考拉宁进行预防。给药后8天采集血液和尿液样本,并用微生物学测定法测定替考拉宁水平。药代动力学参数通过三室开放药代动力学模型和非房室分析进行估算。给药后1小时血浆水平平均为14.8毫克/升。两个分布相的半衰期分别为1.3小时和9.7小时。终末相的半衰期平均为57.9小时,通过非房室分析和尿液数据获得的估算值相似。中央室的分布容积为0.15升/千克,而稳态和消除期的分布容积分别为0.80升/千克和1.25升/千克。替考拉宁的总清除率平均为每千克14.8毫升/小时,其中肾清除率约占总清除率的60%。8天内尿液中替考拉宁的平均累积回收率为剂量的59%,与成年志愿者获得的值相似。消除半衰期与年龄之间无显著线性相关性。重复给药后的初步数据支持所用模型的可靠性和平均估算参数的有效性。未观察到对替考拉宁的局部或全身不良反应。

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