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痉挛状态与药物治疗。

Spasticity and drug therapy.

作者信息

Wuis E W

机构信息

Department of Clinical Pharmacy, St. Radboud University Hospital, Nijmegen, The Netherlands.

出版信息

Pharm Weekbl Sci. 1987 Oct 16;9(5):249-60. doi: 10.1007/BF01953627.

Abstract

An overview is presented of pathophysiology, classification and measurement of spasticity and of its treatment, especially with dantrolene and baclofen. In spasticity, the balance between excitatory and inhibitory neurotransmitters in the central nervous system is impaired by mechanisms that are for the greater part unknown. Spasticity includes various disorders of motor control, and classification is needed for a meaningful evaluation of antispastic therapy. Cerebral palsy is a specific disorder, sometimes also called spasticity. Measurement of spasticity is complicated and should include signs characteristic of spasticity and parameters for clinical improvement. Dantrolene and baclofen have established their place in the treatment of spastic disorders, but a preference for either drug is hard to give. For tizanidine it is still too early to determine its place in therapy. Dantrolene is a direct acting muscle relaxant which should be avoided in patients with pre-existing liver damage. Its mechanism of metabolism and excretion is for the greater part unknown. The GABAB agonist baclofen is a centrally acting muscle relaxant. In patients with impaired renal function the dose should be reduced. Abrupt withdrawal carries the risk of unwanted reactions. The R(-)-enantiomer has proved to be the active isomer. This means that human trials need reappraisal, especially those relating to the pharmacokinetics of the racemate.

摘要

本文概述了痉挛的病理生理学、分类、测量方法及其治疗,尤其涉及丹曲林和巴氯芬的治疗。在痉挛状态下,中枢神经系统中兴奋性和抑制性神经递质之间的平衡因大多未知的机制而受损。痉挛包括各种运动控制障碍,为了对抗痉挛治疗进行有意义的评估,需要进行分类。脑性瘫痪是一种特殊的疾病,有时也被称为痉挛。痉挛的测量很复杂,应包括痉挛的特征性体征和临床改善的参数。丹曲林和巴氯芬在痉挛性疾病的治疗中已确立了它们的地位,但很难说更倾向于使用哪种药物。对于替扎尼定,确定其在治疗中的地位还为时过早。丹曲林是一种直接作用的肌肉松弛剂,已有肝脏损害的患者应避免使用。其代谢和排泄机制大多未知。GABAB激动剂巴氯芬是一种中枢性肌肉松弛剂。肾功能受损的患者应减少剂量。突然停药有发生不良反应的风险。已证明R(-)对映体是活性异构体。这意味着人体试验需要重新评估,尤其是那些与消旋体药代动力学有关的试验。

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