Thiospas Mechanism of Action

Pharmacotherapeutic group: Muscle relaxant. ATC code: MO3BX05.
Pharmacology: Pharmacodynamics: Thiospas contains thiocolchicoside, which is a semi-synthetic sulphurated derivative of colchicoside, with myorelaxant pharmacological activity.
In-vitro, thiocolchicoside only binds to GABA-A and strychnine-sensitive glycine receptors. Thiocolchicoside acting as a GABA-A receptor antagonist, its myorelaxant effects could be exerted at the supra spinal level, via complex regulatory mechanism, although a glycinergic mechanism of action cannot be excluded. The characteristics of the interaction of thiocolchicoside with GABA-A receptors are qualitatively and quantitatively shared by its main circulating metabolite, the glucuronidated derivative.
Pharmacokinetics: Following topical administration of thiocolchicoside cream at recommended doses, the plasma levels of thiocolchicoside were below the minimum level determined.
This shows that after topical administration it has no systemic absorption and therefore also the level of tolerability is good.