How it works

Tolperisone, a centrally acting muscle relaxant agent, has been in therapeutic use for more than three decades & has been widely used as spasmolytics of choice. Tolperisone is an aryl alkyl β-aminoketone having an asymmetric carbon atom α to the carbonyl group. It has higher muscle relaxant activity than the dextrorotatory enantiomer. It exhibits membrane stabilizing potency, which is characteristic of anti arrythmic and local anesthetic agents. Tolperisone acts at the level of spinal cord by blocking sodium channels and calcium channels. It exerts its spinal reflex inhibitory action predominantly via a pre synaptic inhibition of the transmitter release from the primary afferent endings via a combined action on voltage-gated sodium and calcium channels. Tolperisone causes muscle relaxation by its action on central nervous system. It also leads to membrane stabilization & has analgesic activity. This muscle relaxation is dose dependant.