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140 - Tizanidine

Published online by Cambridge University Press:  06 October 2020

Stephen D. Silberstein
Affiliation:
Thomas Jefferson University, Philadelphia
Michael J. Marmura
Affiliation:
Thomas Jefferson University, Philadelphia
Hsiangkuo Yuan
Affiliation:
Thomas Jefferson University, Philadelphia
Stephen M. Stahl
Affiliation:
University of California, San Diego
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Summary

THERAPEUTICS

Brands

• Zanaflex, Sirdalud

Generic?

• Yes

Class

• α2-adrenergic agonist, muscle relaxant

Commonly Prescribed for

(FDA approved in bold)

Acute and intermittent management of increased muscle tone related to spasticity

• Migraine prophylaxis

• Neck pain/lower back pain

• Myofascial pain

• Trigeminal neuralgia

How the Drug Works

• Central α2-adrenergic agonist (mostly at α2A receptors) that also acts at imidazoline receptors. Both α2A and imidazoline receptors are involved in the supraspinal inhibitory effects on mono- or poly-synaptic reflexes, hence reducing spasticity, which can result from neurological conditions, such as multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS), primary lateral sclerosis, and spinal cord injury. α2A-agonist also increases presynaptic inhibition in locus coeruleus, periaqueductal gray area, and parabrachial nucleus, hence the anesthetic responses. Both receptors are involved in sympatholytic responses

How Long Until It Works

• Hours to weeks

If It Works

• Slowly titrate to most effective tolerated dose

If It Doesn't Work

• Increase to highest tolerated dose. If ineffective, gradually reduce dose and consider alternative medications

Best Augmenting Combos for Partial Response or Treatment-Resistance

• Botulinum toxin is effective, especially as an adjunct for focal spasticity, e.g., post-stroke or head injury affecting the upper limbs. For conditions with multiple areas of spasticity, i.e., cerebral palsy, this combination can be very useful

• May be used carefully in combination with baclofen, although additive sedation can be problematic

• Use other centrally acting muscle relaxants with caution due to potential additive CNS depressant effect

Tests

• Monitor liver and renal function at baseline and at 1, 2, and 3 months. Monitor hepatic enzymes at 6 months and periodically after that

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• Related to α2 and imidazoline agonist effect, causing hypotension and increased sedation

Notable AEs

• Dry mouth, weakness, and somnolence are most common. Dizziness, hypotension, and elevation of hepatic transaminases. Hallucinations (usually visual) occur in about 3% of patients

Life-Threatening or Dangerous AEs

• Bradycardia and prolongation of QTc interval with higher doses. Tizanidine withdrawal can cause rebound hypertension

Type
Chapter
Information
Essential Neuropharmacology
The Prescriber's Guide
, pp. 513 - 516
Publisher: Cambridge University Press
Print publication year: 2015

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  • Tizanidine
  • Stephen D. Silberstein, Thomas Jefferson University, Philadelphia, Michael J. Marmura, Thomas Jefferson University, Philadelphia, Hsiangkuo Yuan, Thomas Jefferson University, Philadelphia
  • Edited in consultation with Stephen M. Stahl, University of California, San Diego
  • Book: Essential Neuropharmacology
  • Online publication: 06 October 2020
  • Chapter DOI: https://doi.org/10.1017/9781316161753.141
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Save book to Dropbox

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  • Tizanidine
  • Stephen D. Silberstein, Thomas Jefferson University, Philadelphia, Michael J. Marmura, Thomas Jefferson University, Philadelphia, Hsiangkuo Yuan, Thomas Jefferson University, Philadelphia
  • Edited in consultation with Stephen M. Stahl, University of California, San Diego
  • Book: Essential Neuropharmacology
  • Online publication: 06 October 2020
  • Chapter DOI: https://doi.org/10.1017/9781316161753.141
Available formats
×

Save book to Google Drive

To save content items to your account, please confirm that you agree to abide by our usage policies. If this is the first time you use this feature, you will be asked to authorise Cambridge Core to connect with your account. Find out more about saving content to Google Drive.

  • Tizanidine
  • Stephen D. Silberstein, Thomas Jefferson University, Philadelphia, Michael J. Marmura, Thomas Jefferson University, Philadelphia, Hsiangkuo Yuan, Thomas Jefferson University, Philadelphia
  • Edited in consultation with Stephen M. Stahl, University of California, San Diego
  • Book: Essential Neuropharmacology
  • Online publication: 06 October 2020
  • Chapter DOI: https://doi.org/10.1017/9781316161753.141
Available formats
×