Current Update of Antispastic Drug

Article information

J Korean Med Assoc. 2007;50(2):161-169
Publication date (electronic) : 2007 January 20
doi : https://doi.org/10.5124/jkma.2007.50.2.161
Department of Rehabilitation Medicine and Research Institute, Yonsei University College of Medicine E-mail: kimdy@yumc.yonsei.ac.kr

Abstract

Abstract

Spasticity is a velocity-dependent increase in tonic stretch reflexes (muscle tone) with exaggerated tendon jerks, resulting from hyperexcitability of the stretch reflex. As one component of the upper motor neuron syndrome, spasticity remains a vexing problem for both clinicians and patients. Although several medications have been approved for clinical use in patients with spasticity, the literature has yielded no clear standard of care. The aims of this article are to review the mechanisms of spasticity, factors to consider when choosing and starting antispastic drugs in clinical settings, and the typical characteristics and effects of commonly used agents. This review will focus only on enteral medications, not neurolytic or intrathecal therapy.

Considering factors for antispasticity drug selection

Comparison of Mechanism, Half life, Dose, Excretion

Comparison of side effect, withdrawal symptoms, cautions

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Article information Continued

TABLE.1

Considering factors for antispasticity drug selection

Expected benefits & detriments
Component of hypertonia
Distribution
Etiology of spasticity
Time since onset & recovery
Cognitive status
Adverse effects
Concurrent medical problem
Others

TABLE.2

Comparison of Mechanism, Half life, Dose, Excretion

  Mechanism Half life Peak time Starting Dose Excretion
Baclofen Activate GABA B receptor 3.5hrs 2~3hr 15mg#3 15~80mg Kidney
Dantrolene sodium Interferewith ca++ release from SR 8.7hrs 4hr 50mg#2 25~400mg Kidney & Liver
Diazepam Facilitate postsynaptic effect of GABA 27~37hrs 1hr 4mg#2, 5mg#1 4~60mg Liver
Clonidine Alpha-2 adrenergic antagonist 12~16hrs 3~5hrs 0.075mg#1 0.2~0.6mg Kidney
Tizanidine Central selective alpha-2 antagonist 2.5hrs 1~2hr 2~4mg qhs 4~36mg Kidney

TABLE.3

Comparison of side effect, withdrawal symptoms, cautions

  Side effect Withdrawal symptoms Comments
Baclofen Drowsiness, nausea, paresthesia, confusion, sedation, hypotonia, ataxia rebound spasticity, hallucination and seizure Adjusted with renal disease spinal origin: drug of choice
Dantrolene sodium Malaise, nausea, vomiting, dizziness, diarrhea, hepatotoxicity(1%), fetal hepatitis(0.1∼0.2%)   LFT is needed preferred for cerebral form
Diazepam Sedation, memory impairment, reduced coordination, addiction, respiratory depression Tremor, irritability, insomnia, headache Very long half life
Clonidine Syncope, postural hypotension, nausea, vomiting, sedation, depression   Primarily in SCI
Tizanidine Hypotension, daytime sleepness, dry mouth, abnormal liver function(50%)   LFT is needed