Pharmacology Of Tizanidine

Indication For the management of increased muscle tone associated with spasticity
Pharmacodynamics Tizanidine is a short-acting drug for the management of spasticity. Tizanidine is an agonist at a2-adrenergic receptor sites and presumably reduces spasticity by increasing presynaptic inhibition of motor neurons. In animal models, tizanidine has no direct effect on skeletal muscle fibers or the neuromuscular junction, and no major effect on monosynaptic spinal reflexes. The effects of tizanidine are greatest on polysynaptic pathways. The overall effect of these actions is thought to reduce facilitation of spinal motor neurons.
Mechanism of action Tizanidine reduces spasticity by increasing presynaptic inhibition of motor neurons through agonist action at a2-adrenergic receptor sites.
Absorption Not Available
Volume of distribution
  • 2.4 L/kg
Protein binding 30%
Metabolism Not Available
Route of elimination Approximately 95% of an administered dose is metabolized.
Half life 2.5 hours
Clearance Not Available
Toxicity Not Available