Drug intelligence / Profile preview

tolperisone

Development stage
Phase 3
Lead developer
Gedeon Richter
Modality
Small Molecules
Administration
Oral
01

Overview

Tolperisone is a centrally acting muscle relaxant primarily used to relieve spasticity and increased muscle tone associated with neurological diseases, such as post-stroke spasticity, multiple sclerosis, myelopathy, and encephalomyelitis. It is also used for musculoskeletal pain and spasms due to various causes. The precise mechanism of action is not fully understood but involves blockade of voltage-gated sodium channels and inhibition of calcium ion influx in neurons, leading to reduced nerve impulse transmission in the brainstem and spinal cord. This results in decreased muscle contraction without significant sedation or reduction in muscle strength. Tolperisone also exhibits membrane-stabilizing properties with mild local anesthetic effects and may improve peripheral circulation through antispasmodic and antiadrenergic actions[1][2][5].

Brand names
MydocalmBiocalmMiderizoneMydetonMydoflexMyolaxMyoxanTolsonTopeeViveoAbbsaAtmosgenArantoickBesnolineIsocalmKineorlMenopatolMetosominMinacalmMiodomMuscalmMusclexMusocalmMusolaxMyderisonNaismeritinTolisartineTopxolTolfreeUserm
Other names
tolperisone hydrochloride
02

Targets

NaV (Voltage-gated sodium channels)CACNA1B (Voltage-dependent N-type calcium channel subunit alpha-1B)Kir (Inward-rectifier potassium channels)

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