The Sound of Evolution
Tizanidine
Mechanism of action:
Tizanidine is a central alpha2-adrenergic agonist. Tizanidine stimulates alpha2 receptors in the spinal cord and brainstem, mainly presynaptic receptors, suppressing norepinephrine release and thereby indirectly reducing the release of excitatory amino acids such as glutamate and aspartate. This lowers the excitability of spinal reflex pathways, suppresses muscle spindle-related stretch reflexes, and reduces abnormal muscle contraction and rigidity.
Reference(s):
1. Henney HR 3rd et al. (2008). A clinically relevant review of tizanidine hydrochloride dose relationships to pharmacokinetics, drug safety and effectiveness in healthy subjects and patients. Int J Clin Pract.
2. Malanga G et al. (2008). Update on tizanidine for muscle spasticity and emerging indications. Expert Opin Pharmacother.
3. Wagstaff AJ et al. (1997). Tizanidine. A review of its pharmacology, clinical efficacy and tolerability in the management of spasticity associated with cerebral and spinal disorders. Drugs.