Baclofen is a gamma-amino-butyric acid (GABA) derivative. It is a direct agonist at GABAB receptors and by stimulating these receptors it leads to decreased frequency and amplitude of muscle spasms. It is especially useful in treating muscle spasticity associated with spinal cord injury.
Although the precise mechanism of action of Baclofen is not fully known, it is capable of inhibiting both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect. So, Baclofen is postulated to block mono-and-polysynaptic reflexes by acting as an inhibitory neurotransmitter, blocking the release of excitatory transmitters.
At the presynaptic site, baclofen decreases calcium conductance with resultant decreased neurotransmitter and excitatory amino acid uptake. At the postsynaptic site, baclofen increases potassium conductance with resultant neuronal hyperpolarization and may also inhibit the release of substance P.
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