Wiest D B, Trippel D L, Gillette P C, Garner S S
Department of Clinical Pharmacy, Medical University of South Carolina, Charleston 29425.
Clin Pharmacol Ther. 1991 Jun;49(6):618-23. doi: 10.1038/clpt.1991.78.
The pharmacokinetics and concentration-response relationships of intravenous esmolol were investigated in 20 children undergoing indicated cardiac electrophysiologic testing. A loading dose of 600 micrograms/kg was infused for 2 minutes. An infusion of esmolol was initiated and dosage was titrated until beta-blockade occurred. Serial esmolol blood samples were obtained for pharmacokinetic analysis. Non-compartmental pharmacokinetic analysis of the data revealed the following parameter estimates (mean +/- SD): volume of distribution at steady state, 2.0 +/- 1.4 L/kg; total body clearance, 321.2 +/- 238.8 ml/kg/min; and terminal elimination half-life, 4.5 +/- 2.1 minutes. There was a significant correlation between mean esmolol concentrations and mean percentage of reductions of mean arterial pressures and heart rates at each sample time (p less than 0.001). The doses of esmolol required for beta-blockade (mean +/- SD, 535 +/- 180 micrograms/kg/min) in children were considerably higher than those typically used in adults. Esmolol should prove useful in children in the acute management of cardiac arrhythmias and hypertension.
在20名接受心脏电生理检查的儿童中研究了静脉注射艾司洛尔的药代动力学和浓度-反应关系。给予600微克/千克的负荷剂量，静脉输注2分钟。开始输注艾司洛尔并滴定剂量，直至出现β受体阻滞。采集系列艾司洛尔血样进行药代动力学分析。对数据进行的非房室药代动力学分析得出以下参数估计值（均值±标准差）：稳态分布容积，2.0±1.4升/千克；全身清除率，321.2±238.8毫升/千克/分钟；终末消除半衰期，4.5±2.1分钟。在每个采样时间，艾司洛尔平均浓度与平均动脉压和心率降低的平均百分比之间存在显著相关性（p<0.001）。儿童达到β受体阻滞所需的艾司洛尔剂量（均值±标准差，535±180微克/千克/分钟）明显高于成人常用剂量。艾司洛尔在儿童心律失常和高血压的急性处理中应是有用的。
