Thiocolchicoside is a potent competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist with muscle relaxant, anti-inflammatory, and analgesic activity. Thiocolchicoside has also been found to suppress nuclear factor kappa B ligand (RANKL) activation of NF-KB resulting in suppression of osteoclastogenesis.
Thiocolchicoside acts as a muscle relaxant. In experimental animals, thiocolchicoside results in malfunctions (teratogenic) and impairs chromosomes. It is advised to be used as an analgesic for patients with muscle pain, starting with paracetamol. Thiocolchicoside can be used in irrigation solution at the time of endoscopic treatment of ureteral calculus to reduce the movement of stones.