Tizanidine is an alpha-2 adrenergic agonist used for the short-term treatment of muscle spasticity. Tizanidine is a fast-acting drug used for the management of muscle spasm, which may result from the effects of multiple sclerosis, stroke, an acquired brain injury, or a spinal cord injury.
- Mechanism
- Curator reviewed · 1 reference
Tizanidine reduces spasticity by causing presynaptic inhibition of motor neurons via agonist actions at Alpha-2 adrenergic receptor sites. This drug is centrally acting and leads to a reduction in the release of excitatory amino acids like glutamate and aspartate, which cause neuronal firing that leads to muscle spasm. The above reduction and excitatory neurotransmitter release results in presynaptic inhibition of motor neurons. The strongest effect of tizanidine has been shown to occur on spinal polysynaptic pathways. The anti-nociceptive and anticonvulsant activities of tizanidine may also be attributed to agonist action on Alpha-2 receptors. Tizanidine also binds with weaker affinity to the Alpha-1 receptors, explaining its slight and temporary effect on the cardiovascular system.
- Primary indication
- Tizanidine is indicated for the relief of muscle spasticity, which can interfere with daily activities.Curator reviewed · 10 structured indications
- Formula / weight
- C9H8ClN5S · 253.711 g/mol (avg)
- First approval
- Canada, 2009 · United States, 1997
- Code names
- AN 021 · DS 103-282
- Brand names
Resolves to
XFYDIVBRZNQMJC-UHFFFAOYSA-NSMILESClC1=C(NC2=NCCN2)C2=NSN=C2C=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Tizanidine, and which of those have an active Phase 3 trial?
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