Objective: Tizanidine 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.
Scope: An 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.
Findings: Tizanidine, 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.
Conclusions: There 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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http://dx.doi.org/10.1185/030079908x261113 | DOI Listing |
Can J Neurol Sci
November 2024
Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Alberta, Canada.
JAMA Netw Open
September 2024
Challenges in Managing and Preventing Pain Clinical Research Center, University of Pittsburgh, Pittsburgh, Pennsylvania.
Importance: Stricter opioid prescribing guidelines have increased prescriptions of skeletal muscle relaxants (SMRs) for chronic pain, but the efficacy of long-term use of SMRs for chronic pain is unknown.
Objective: To systematically review the effectiveness or efficacy of long-term use of SMRs for chronic pain.
Evidence Review: Two reviewers systematically searched Ovid MEDLINE, Embase (Ovid), Web of Science, CINAHL, and Cochrane through December 4, 2023.
Temperature (Austin)
April 2024
Center for Clinical Pharmaceutical Sciences, Department of Pharmacy and Therapeutics, University of Pittsburgh School of Pharmacy, Pittsburgh, PA, USA.
Intravenous alpha-2-adrenergic receptor agonists reduce energy expenditure and lower the temperature when shivering begins in humans, allowing a decrease in core body temperature. Because there are few data about similar effects from oral drugs, we tested whether single oral doses of the sedative dexmedetomidine (1 µg/kg sublingual or 4 µg/kg swallowed) or the muscle relaxant tizanidine (8 mg or 16 mg), combined with surface cooling, reduce energy expenditure and core body temperature in humans. A total of 26 healthy participants completed 41 one-day laboratory studies measuring core body temperature using an ingested telemetry capsule and measuring energy expenditure using indirect calorimetry for up to 6 hours after drug ingestion.
View Article and Find Full Text PDFMult Scler Relat Disord
September 2024
Jazz Pharmaceuticals Inc., Carlsbad, CA, USA.
Background: Spasticity is a common and potentially debilitating symptom of multiple sclerosis (MS) with a highly variable presentation. Understanding, quantifying, and managing MS-associated spasticity (MSS) is a challenge for research and in clinical practice. The tetrahydrocannabinol:cannabidiol oromucosal spray nabiximols has demonstrated beneficial effects in the treatment of MSS in clinical studies as well as real-world observational studies, and is approved for the treatment of MSS in 29 countries globally.
View Article and Find Full Text PDFExpert Rev Neurother
August 2024
Paolo Procacci Foundation, Rome, Italy.
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