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Tizanidine

替扎尼定

Mechanism of action:

Tizanidine 是一種中樞作用型 α₂-腎上腺素受體促效劑（central α₂-adrenergic agonist）。Tizanidine 會刺激脊髓與腦幹中的 α₂ 受體（主要為突觸前受體），抑制正腎上腺素（norepinephrine）的釋放，進而間接抑制 glutamate、aspartate 等興奮性胺基酸的釋放。這會導致脊髓反射弧興奮性下降，肌梭相關的張力反射被抑制，使肌肉不正常收縮與僵硬程度降低。

​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.

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