(1) Baclofen (brand names Kemstro, Lioresal, Liofen, Gablofen, Lyflex, Beklo and Baclosan) is a derivative of gamma-aminobutyric acid (GABA). It is primarily used to treat spasticity and is in the early research stages for use for the treatment of alcoholism. It is also used by compounding pharmacies in topical pain creams as a muscle relaxant.
(2) It is an agonist for the GABAB receptors. Its beneficial effects in spasticity result from actions at spinal and supraspinal sites. Baclofen can also be used to treat hiccups.
(3)A beneficial property of baclofen is that tolerance does not seem to occur to a significant degree - baclofen retains its therapeutic anti-spasmodic effects even after many years of continued use. Newer studies, however, indicate that tolerance may develop in some patients receiving intrathecal baclofen treatment. 3. Medical uses: Baclofen is primarily used for the treatment of spastic movement disorders, especially in instances of spinal cord injury, cerebral palsy, and multiple sclerosis. Its use in people with stroke or Parkinson's disease is not recommende. 4. Mechanism of action: Baclofen produces its effects by activating the GABAB receptor, similar to the drug which also activates this receptor and shares some of its effects. However, baclofen does not have significant affinity for the receptor, and has no known abuse potential. The modulation of the GABAB receptor is what produces baclofen's range of therapeutic properties.
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