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布比卡因在儿童硬膜外麻醉期间的药代动力学。

Bupivacaine pharmacokinetics during epidural anaesthesia in children.

作者信息

Murat I, Montay G, Delleur M M, Esteve C, Saint-Maurice C

机构信息

Départment d'Anesthésie-Réanimation Chirurgicale, Hôpital Saint-Vincent-de-Paul, Paris, France.

出版信息

Eur J Anaesthesiol. 1988 Mar;5(2):113-20.

PMID:3396545
Abstract

Blood concentrations and pharmacokinetic parameters of bupivacaine were measured after epidural injection in children aged from 1 to 7 years. The children were allocated to two groups. In Group 1 (five children), pharmacokinetic parameters were measured after a single bolus injection of bupivacaine 0.25% with adrenaline 1:200,000. In Group 2 (eight children), pharmacokinetic parameters were measured after the initial injection and the second injection. The same local anaesthetic was used. The volume of the second injection was half of the initial volume. In children of Group 1, maximum mean concentration (CPmax) was 0.64 +/- 0.05 microgram ml-1, time to maximum concentration (Tmax) 19.2 +/- 3.9 min, vascular absorption (T1/2 abs) 4.3 +/- 1.5 min, terminal half-life (T1/2 beta) 227 +/- 37.7 min, volume of distribution (Vd) 3.4 +/- 0.51 kg-1, and total body clearance (Clt) 11.0 +/- 2.0 ml min-1 kg-1. When compared to an adult's pharmacokinetic parameters, both Vd and Clt were increased, so that T1/2 beta remained essentially unchanged. In children of Group 2, the first repeat injection was performed at 110 +/- 6.9 min. Mean CPmax increased significantly (20% after the second injection), whereas the values of the pharmacokinetic parameters measured did not differ significantly from those measured in children in Group 1. The results obtained in the present study demonstrate that the pharmacokinetic parameters of bupivacaine in children do not differ markedly from those reported in adults and that in the recommended dosage, the mean maximum concentrations, even after the second injection, are less than the presumed toxic levels.

摘要

对1至7岁儿童进行硬膜外注射后,测量了布比卡因的血药浓度和药代动力学参数。这些儿童被分为两组。在第1组(5名儿童)中,单次推注0.25%布比卡因与1:200,000肾上腺素后测量药代动力学参数。在第2组(8名儿童)中,在首次注射和第二次注射后测量药代动力学参数。使用的是同一种局部麻醉剂。第二次注射的体积是初始体积的一半。在第1组儿童中,最大平均浓度(CPmax)为0.64±0.05微克/毫升,达峰时间(Tmax)为19.2±3.9分钟,血管吸收(T1/2 abs)为4.3±1.5分钟,终末半衰期(T1/2 beta)为227±37.7分钟,分布容积(Vd)为3.4±0.51千克-1,全身清除率(Clt)为11.0±2.0毫升/分钟·千克-1。与成人的药代动力学参数相比,Vd和Clt均增加,因此T1/2 beta基本保持不变。在第2组儿童中,首次重复注射在110±6.9分钟时进行。平均CPmax显著增加(第二次注射后增加20%),而所测量的药代动力学参数值与第1组儿童所测量的值无显著差异。本研究获得的结果表明,儿童布比卡因的药代动力学参数与成人报道的参数无明显差异,并且在推荐剂量下,即使在第二次注射后,平均最大浓度也低于假定的中毒水平。

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