ATC Group: M03BX Other centrally acting agents

Baclofen depresses monosynaptic and polysynaptic reflex transmission, probably by stimulating the GABA_B-receptors. This stimulation in turn inhibits the release of the excitatory amino acids glutamate and aspartate. Neuromuscular transmission is unaffected by baclofen. Baclofen also exerts an antinociceptive effect.

Cyclobenzaprine relieves skeletal muscle spasm of local origin without interfering with muscle function. Cyclobenzaprine has not been shown to be effective in muscle spasm due to central nervous system disease.

Eperisone is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain.

Pridinol is a piperidin- polyalcohol derivative with the chemical formula 1,1-Diphenyl-1-ol-3-piperidin-propan-methanesulfonate. Its pharmacological effect develops via an atropine-like mechanism that acts on both smooth and the striated muscles. This effect is used for the treatment of skeletal muscle tension of both central and peripheral origin.

Thiocolchicoside is a semisynthetic sulphide derivative of colchicoside, showing muscle relaxant pharmacological activity. In vitro thiocolchicoside binds solely with gaba receptors and glycinergic stricnine sensitive.Tivozanib

Tizanidine is a centrally acting skeletal muscle relaxant. Polysynaptic signal transmission at spinal interneuron level, which is responsible for excessive muscle tone, is inhibited and muscle tone reduced.

As a skeletal muscle relaxant whose prototype is mephenesine, tolperisone induces ataxia and muscle weakness in animal models by acting on the central nervous system at the spinal level. In fact it inhibits polysynaptic and monosynaptic reflexes with little action on non-reflex muscle response and without potentiating the phenobarbital sleep.