• Leonard Kamen, Herbert R Henney, and Jacob D Runyan.
• Albert Einstein Medical Center, Moss Rehabilitation Outpatient Center, Philadelphia, PA, USA.
• Curr Med Res Opin. 2008 Feb 1;24(2):425-39.

ObjectiveTizanidine is an imidazoline central alpha(2)-adrenoceptor agonist widely used to manage spasticity secondary to conditions such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI). While there is widespread use of tizanidine in clinical practice, little practical information is available to assist prescribers with the effective use of tizanidine for spasticity management. The aim of this review is to provide an up-to-date overview of tizanidine and its use in the management of spasticity associated with acquired (SCI), static (stroke), and progressive neurological (MS) diseases.ScopeAn unfiltered literature search of the term 'tizanidine' was undertaken on the Medline database resulting in 311 papers. As the review focused on tizanidine clinical pharmacokinetics, efficacy, and tolerability, with comparisons limited to the oral antispastic agents baclofen, diazepam, and dantrolene, 53 articles were selected for detailed assessment.FindingsTizanidine, an alpha(2)-adrenoceptor agonist, is a short-acting drug with larger interpatient variability, and linear pharmacokinetics that is dosage form-dependent. Clinical trials have demonstrated that the efficacy of tizanidine is comparable to that of baclofen or diazepam with global tolerability data favoring tizanidine. A clinical case presentation demonstrated the effective use of tizanidine in combination with baclofen as a logical avenue for improved spasticity control.ConclusionsThere is a large body of evidence for the effective use of tizanidine monotherapy in the management of spasticity. A case study demonstrates that combination therapy can effectively control spasticity while better managing dose-dependent adverse events, although additional studies need to be performed to confirm these results.

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