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Baclofen is an effective muscle relaxant and antispastic agent with a spinal site of action.

It inhibits both monosynaptic and polysynaptic reflexes at the spinal level by stimulating the GABAB receptors, which inhibits the release of Glutamate and Aspartate. It may also act at intra spinal sites producing CNS depression. Neuromuscular transmission is not affected by Baclofen. Baclofen also exerts an antinociceptic effect.