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The Pharmacokinetics of Esmolol in Pediatric Subjects with Supraventricular Arrhythmias

机译:艾司洛尔在小儿室上性心律失常中的药代动力学

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摘要

Esmolol is often used in the acute management of children with arrhythmias and/or hypertension; however, pharmacokinetic studies of the drug in children have been limited. The objective of this study was to determine the pharmacokinetics of esmolol in children with a history of supraventricular arrhythmias (SVT) who were scheduled for diagnostic electrophysiology study or a catheter ablation procedure. Subjects were stratified into two age groups: 2–11 and 12–16 years. After an episode of stimulated or spontaneous SVT, esmolol was administered intravenously as a 1,000 μg/kg bolus followed by continuous infusion at 300 μg/kg/min. Blood samples were collected before, at 5, 10 and 15 min after the loading dose, and 3, 6, 9, 12, 15 and 20 min after the end of the infusion. Plasma concentration of esmolol was quantitated by a specific LC/MS assay. Pharmacokinetic data were available for 25 subjects. Arterial esmolol concentrations were approximately five times greater than venous concentrations. Esmolol had an extremely short distribution half-life (0.6 min), a rapid terminal elimination half-life (6.9 min), and a rapid clearance (119 ± 51 mL/min/kg) which was not related to subject age or weight. Seventeen of the subjects (63%) converted to normal sinus rhythm in an average of 2 min (range 0–5 min). The pharmacokinetics of esmolol and its efficacy in terminating SVT in children is similar to that observed in adults.
机译:艾司洛尔通常用于心律不齐和/或高血压儿童的急性治疗;但是,该药物在儿童中的药代动力学研究受到限制。这项研究的目的是确定艾司洛尔对计划用于诊断性电生理研究或导管消融术的室上性心律失常(SVT)病史的儿童的药代动力学。受试者分为两个年龄段:2-11岁和12-16岁。在发生刺激性或自发性SVT后,艾司洛尔以1,000μg/ kg推注静脉内给药,然后以300μg/ kg / min的速度连续输注。在加载剂量之前,之后的5、10和15分钟以及输注结束后的3、6、9、12、15和20分钟时收集血液样本。艾司洛尔的血浆浓度通过特定的LC / MS测定进行定量。有25位受试者的药代动力学数据。动脉艾司洛尔浓度约为静脉浓度的五倍。艾司洛尔具有极短的分布半衰期(0.6分钟),快速的末端消除半衰期(6.9分钟)和快速清除(119±51 mL / min / kg),与受试者的年龄或体重无关。 17名受试者(63%)平均2分钟(0-5分钟)即可恢复正常窦性心律。艾司洛尔的药代动力学及其终止儿童SVT的功效与在成人中观察到的相似。

著录项

  • 来源
    《Pediatric Cardiology》 |2006年第4期|420-427|共8页
  • 作者单位

    Division of Clinical Pharmacology and Therapeutics The Children’s Hospital of Philadelphia ARC 916;

    Division of Cardiology The Children’s Hospital of Philadelphia;

    Division of Pediatric Cardiology Medical University of South Carolina;

    Division of Pediatric Cardiology The University of Michigan;

    Division of Cardiology Cincinnati Children’s Hospital;

    School of Veterinary Medicine University of Pennsylvania;

    School of Veterinary Medicine University of Pennsylvania;

    Children’s Clinical Research Institute The Children’s Hospital of Philadelphia;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

    Esmolol; SVT; Pharmacokinetics;

    机译:艾司洛尔;SVT;药代动力学;

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