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阿曲库铵的异构体51W89在氟烷麻醉期间对儿童的药效学作用。

Pharmacodynamic effects of 51W89, an isomer of atracurium, in children during halothane anaesthesia.

作者信息

Meretoja O A, Taivainen T, Wirtavuori K

机构信息

Department of Anaesthesiology, Children's Hospital University of Helsinki, Finland.

出版信息

Br J Anaesth. 1995 Jan;74(1):6-11. doi: 10.1093/bja/74.1.6.

Abstract

51W89 is one of the 10 stereoisomers of atracurium with less propensity to release histamine than atracurium. We evaluated dose-response data and neuromuscular effects of 2 x ED95 dose and maintenance doses of 51W89 during halothane anaesthesia in 68 children, 2-12 yr old. Neuromuscular function was monitored by evoked adductor pollicis EMG. Log-probit, single-dose, dose-response data gave ED50 and ED95 values of 23 and 41 micrograms kg-1, respectively, for 51W89. Twice the ED95 dose (80 micrograms kg-1) had an onset time (time from administration to maximum effect) of 2.5 (SD 0.8) min, a clinical duration (time to 25% EMG recovery) of 31 (7) min and a recovery index (time from 25 to 75% EMG recovery) of 11.1 (1.7) min. Seventy-nine incremental doses of 51W89 of 94 (19) micrograms kg-1. Duration of effect of incremental doses remained constant within individuals reflecting non-cumulative properties. There were insignificant changes in arterial pressure and heart rate after 51W89 and no side effects were observed. We regard 51W89 as a promising, non-cumulative, intermediate-acting neuromuscular blocking agent the effects of which can be antagonized easily by neostigmine.

摘要

51W89是阿曲库铵10种立体异构体之一,其释放组胺的倾向低于阿曲库铵。我们评估了68名2至12岁儿童在氟烷麻醉期间2倍ED95剂量和51W89维持剂量的剂量反应数据及神经肌肉效应。通过诱发的拇内收肌肌电图监测神经肌肉功能。51W89的对数概率单剂量剂量反应数据得出ED50和ED95值分别为23和41微克/千克。2倍ED95剂量(80微克/千克)的起效时间(从给药到最大效应的时间)为2.5(标准差0.8)分钟,临床持续时间(至肌电图恢复25%的时间)为31(7)分钟,恢复指数(从肌电图恢复25%至75%的时间)为11.1(1.7)分钟。51W89的79次递增剂量为94(19)微克/千克。递增剂量的效应持续时间在个体内保持恒定,反映出非累积特性。51W89给药后动脉压和心率无显著变化,未观察到副作用。我们认为51W89是一种有前景的、非累积性的中效神经肌肉阻滞剂,其效应可被新斯的明轻易拮抗。

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