Baclofen is a centrally acting skeletal muscle relaxant and an antispastic agent with a spinal site of action.
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Baclofen is an effective muscle relaxant and antispastic agent with a spinal site of action. Baclofen is structurally similar to the inhibitory neurotransmitter gamma-amino-butyric acid, though its actions are different. It binds stereospecifically to GABA-B receptors. It is thought that activation of the GABA-B receptors on presynaptic terminal reduces evoked transmitter release, perhaps through reduced presynaptic Ca2+ influx. Baclofen can inhibit the function of inward calcium currents in some cells. The drug is rapidly absorbed after oral administration and is widely distributed throughout the body.