Nahata M C, Fan-Havard P, Barson W J, Bartkowski H M, Kosnik E J
College of Pharmacy, Ohio State University, Department of Pediatrics, Columbus.
Eur J Clin Pharmacol. 1990;38(5):515-7. doi: 10.1007/BF02336694.
The objectives of this study were to characterize the pharmacokinetics and determine the cerebrospinal fluid concentrations and safety of intravenous rifampin in pediatric patients undergoing shunt placement. Nine patients (mean age 5.6 y) received a single dose of rifampin, 20 mg.kg-1, administered intravenously 1 h prior to surgery. The peak serum concentrations ranged from 13.5-26.7 micrograms.ml-1; cerebrospinal fluid concentrations ranged from 0.12-3.0 (mean: 1.4) micrograms.ml-1. The mean total clearance, apparent distribution volume, and elimination half-life were 0.29 l.kg-1.h-1, 1.11.kg-1, and 2.8 h. The concentrations of rifampin achieved in the cerebrospinal fluid exceeded the minimum inhibitory concentrations by 100- to 1000-fold against Staphylococcus epidermidis. However, 5 of 9 patients developed cutaneous reactions during intravenous rifampin prophylactic therapy. Because of the high frequency of adverse effects and more than adequate rifampin concentrations achieved in the cerebrospinal fluid, rifampin doses lower than that used in this study may be evaluated in future studies.
本研究的目的是描述静脉注射利福平在接受分流管置入术的儿科患者中的药代动力学特征,测定其脑脊液浓度及安全性。9例患者(平均年龄5.6岁)在手术前1小时静脉注射单剂量利福平,剂量为20mg/kg。血清峰浓度范围为13.5 - 26.7μg/ml;脑脊液浓度范围为0.12 - 3.0(平均:1.4)μg/ml。平均总清除率、表观分布容积和消除半衰期分别为0.29L/kg·h、1.11L/kg和2.8小时。脑脊液中利福平的浓度超过针对表皮葡萄球菌的最低抑菌浓度100至1000倍。然而,9例患者中有5例在静脉注射利福平预防性治疗期间出现皮肤反应。由于不良反应发生率高且脑脊液中利福平浓度已足够,未来研究可能会评估低于本研究使用剂量的利福平。