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地西泮和去甲基地西泮对痉挛和强直的影响。反射和血浆浓度的定量研究。

Effect of diazepam and desmethyldiazepam in spasticity and rigidity. A quantitative study of reflexes and plasma concentrations.

作者信息

Lossius R, Dietrichson P, Lunde P K

出版信息

Acta Neurol Scand. 1980 Jun;61(6):378-83. doi: 10.1111/j.1600-0404.1980.tb01507.x.

Abstract

Benzodiazepines are known to reduce increased muscle stretch reflexes. To investigate the relationship between the necessary plasma concentrations of diazepam and its major metabolite desmethyldiazepam on the one hand and the phasic and tonic ankle reflex activity on the other, 10 mg diazepam was given intravenously to nine patients, seven with spasticity due to multiple sclerosis and two with parkinsonian rigidity. Diazepam and desmethyldiazepam both had a normalizing effect on the increased phasic ankle reflex seen in spasticity. No effect was observed on the increased tonic reflexes in rigidity. The concentrations of diazepam necessary to reduce spasticity ranged between 300-2,200 mg/l and were so high that drowsiness did occur. However, the study may indicate that desmethyldiazepam has a higher potency and a more long lasting effect on the increased phasic reflexes than diazepam.

摘要

已知苯二氮䓬类药物可降低增强的肌肉牵张反射。为了研究一方面地西泮及其主要代谢产物去甲基地西泮的血浆浓度与另一方面相性和紧张性踝关节反射活动之间的关系,对9例患者静脉注射10mg地西泮,其中7例因多发性硬化导致痉挛,2例因帕金森病导致僵硬。地西泮和去甲基地西泮对痉挛时出现的增强相性踝关节反射均有正常化作用。对僵硬时增强的紧张性反射未观察到作用。减轻痉挛所需的地西泮浓度在300 - 2200mg/L之间,且浓度如此之高以至于确实出现了嗜睡。然而,该研究可能表明,去甲基地西泮对增强的相性反射的效力比地西泮更高,且作用更持久。

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