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罗库溴铵在人体声带和拇内收肌处的药代动力学与药效学

Pharmacokinetics and pharmacodynamics of rocuronium at the vocal cords and the adductor pollicis in humans.

作者信息

Plaud B, Proost J H, Wierda J M, Barre J, Debaene B, Meistelman C

机构信息

Department of Anesthesiology, Institut Gustave Roussy, Villejuif, France.

出版信息

Clin Pharmacol Ther. 1995 Aug;58(2):185-91. doi: 10.1016/0009-9236(95)90196-5.

Abstract

The pharmacokinetic-pharmacodynamic relationship of rocuronium at the laryngeal adductor muscles and the adductor pollicis was determined in eight patients during general anesthesia. Rocuronium was administered as an infusion at a rate of 100 micrograms.kg-1.min-1 over 5 minutes. The half-life of transport between plasma and biophase (effect compartment) was significantly shorter at the adductor laryngeal muscles (2.7 +/- 0.6 minutes, mean +/- SD) than at the adductor pollicis (4.4 +/- 1.5 minutes, p = 0.003). The concentration in the effect compartment producing 50% of the maximum effect was significantly greater at the adductor laryngeal muscles (1424 +/- 148 micrograms.L-1) than at the adductor pollicis (823 +/- 157 micrograms.L-1, p = 0.0001). The shorter onset of neuromuscular blockade at the laryngeal muscles than at the adductor pollicis may be explained by a faster transfer rate at the laryngeal adductor muscles neuromuscular junction than at the adductor pollicis neuromuscular junction.

摘要

在全身麻醉期间,对8例患者测定了罗库溴铵在喉内收肌和拇内收肌处的药代动力学-药效学关系。罗库溴铵以100微克·千克⁻¹·分钟⁻¹的速率静脉输注5分钟。血浆与生物相(效应室)之间转运的半衰期在喉内收肌处(2.7±0.6分钟,均值±标准差)显著短于拇内收肌处(4.4±1.5分钟,p = 0.003)。产生最大效应50%时效应室内的浓度在喉内收肌处(1424±148微克·升⁻¹)显著高于拇内收肌处(823±157微克·升⁻¹,p = 0.0001)。喉肌处神经肌肉阻滞起效比拇内收肌处更快,这可能是由于喉内收肌神经肌肉接头处的转运速率比拇内收肌神经肌肉接头处更快。

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