tizanidine

Class




  • Skeletal muscle relaxant, centrally acting; alpha-2 agonist




Tizanidine


Commonly Prescribed for


(FDA approved in bold)



  • Acute and intermittent management of increased muscle tone related to spasticity
  • Spasticity can result from neurological conditions, such as multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS), primary lateral sclerosis, and spinal cord injury
  • Migraine prophylaxis
  • Neck pain/lower back pain
  • Myofascial pain



Tizanidine


How the Drug Works



  • Alpha-2 adrenergic agonist (mostly at alpha-2A receptors) which also acts at imidazoline receptors. Reduces spasticity by increasing presynaptic inhibition of motor neurons



Tizanidine


How Long Until It Works



  • Pain – hours-weeks



Tizanidine


If It Works



  • Slowly titrate to most effective tolerated dose



Tizanidine


If It Doesn’t Work



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



Tizanidine


Best Augmenting Combos for Partial Response or Treatment-Resistance



  • Botulinum toxin is effective, especially as an adjunct for focal spasticity, i.e., 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



Tizanidine


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)




Tizanidine


How Drug Causes AEs



  • Related to alpha-2 adrenergic agonist effect causing hypotension. Increased sedation may be due to actions at the imidazoline receptors



Tizanidine


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



Tizanidine


Life-Threatening or Dangerous AEs



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



Tizanidine


Weight Gain



  • Not unusual



Tizanidine


Sedation



  • Common



Tizanidine


What to Do About AEs

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Feb 16, 2017 | Posted by in PHARMACY | Comments Off on tizanidine

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