Drug intelligence / Profile preview

tizanidine

Development stage
Approved
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Tizanidine is a centrally acting skeletal muscle relaxant primarily used to manage spasticity associated with conditions such as multiple sclerosis and spinal cord injury. It acts as an agonist at alpha2 adrenergic receptors (mainly the alpha2A subtype) in the central nervous system, inhibiting presynaptic motor neuron activity and reducing the release of excitatory neurotransmitters like glutamate and aspartate. This results in decreased muscle tone and relief from spasms[1][3][5][7]. Tizanidine is available in oral formulations (tablet, capsule, solution) and has a relatively short half-life (~2.5 hours). Common side effects include dry mouth, drowsiness, weakness, dizziness; serious risks include hypotension and liver dysfunction[1][6]. Developed by Novartis (originally), it is now widely available as a generic medication.

Brand names
ZanaflexSirdaludOntralfy
Other names
盐酸替扎尼定tizanidine hydrochloride4-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-8-thia-7,9-diazabicyclo[4.3.0]nona-2,4,6,9-tetraen-5-amine
02

Targets

ADRA2B (α2B)ADRA2A (α2A)ADRA1A (α1A)

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