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地西泮的肌松作用。与神经肌肉阻滞剂和胆碱能药物的相互作用。

Myorelaxant effect of diazepam. Interactions with neuromuscular blocking agents and cholinergic drugs.

作者信息

Wali F A

出版信息

Acta Anaesthesiol Scand. 1985 Nov;29(8):785-9. doi: 10.1111/j.1399-6576.1985.tb02301.x.

DOI:10.1111/j.1399-6576.1985.tb02301.x
PMID:4082878
Abstract

Experiments were performed, using electrophysiological techniques, to investigate the effects and interactions of diazepam with commonly-used neuromuscular blocking agents and cholinergic agonists in chick and rat isolated nerve-muscle preparations. The results showed that in low concentrations (3.4-340 mumol/l, i.e. 1-100 micrograms ml-1) diazepam increased, in a dose-dependent manner, the twitch contractions in response to motor nerve stimulation of the chick and rat. High concentrations of diazepam (greater than 340 mumol/l) decreased the twitch tension and greatly reduced the contractures produced by acetylcholine (ACh) and tetraethylammonium (TEA) in the chick skeletal muscle. However, in the concentration range studied (close to a therapeutic dose of 0.15 mg kg-1), diazepam had no significant effect on the neuromuscular blockade produced either by tubocurarine or by succinylcholine. It was concluded that diazepam may either increase or decrease the twitch tension, in rat and chick skeletal muscle, the effect being dependent on the concentrations used. The mechanism of action of diazepam may depend on an increasing intracellular calcium concentration, which is directly involved in the increase of the twitch tension by low concentrations of diazepam.

摘要

采用电生理技术进行实验,以研究地西泮与常用神经肌肉阻滞剂及胆碱能激动剂在鸡和大鼠离体神经肌肉标本中的作用及相互作用。结果表明,低浓度(3.4 - 340 μmol/l,即1 - 100 μg/ml)的地西泮以剂量依赖性方式增加鸡和大鼠对运动神经刺激的抽搐收缩。高浓度的地西泮(大于340 μmol/l)降低了抽搐张力,并极大地减少了鸡骨骼肌中乙酰胆碱(ACh)和四乙铵(TEA)产生的挛缩。然而,在所研究的浓度范围内(接近0.15 mg/kg的治疗剂量),地西泮对筒箭毒碱或琥珀酰胆碱产生的神经肌肉阻滞没有显著影响。得出的结论是,地西泮可能会增加或降低大鼠和鸡骨骼肌的抽搐张力,其效果取决于所用的浓度。地西泮的作用机制可能取决于细胞内钙浓度的增加,低浓度的地西泮通过直接增加细胞内钙浓度来增加抽搐张力。

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