Baclofen
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| Trade names | Lioresal, Liofen, Gablofen |
| AHFS/Drugs.com | Monograph |
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| Routes of administration |
Oral, intrathecal |
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| Pharmacokinetic data | |
| Bioavailability | well absorbed |
| Protein binding | 30% |
| Metabolism | 85% excreted in urine/faeces unchanged. 15% metabolised by deamination |
| Biological half-life | 1.5 to 4 hours |
| Excretion | renal (70-80%) |
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| Synonyms | β-(4-chlorophenyl)-γ-aminobutyric acid (β-(4-chlorophenyl)-GABA) |
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| ECHA InfoCard | 100.013.170 |
| Chemical and physical data | |
| Formula | C10H12ClNO2 |
| Molar mass | 213.661 g/mol |
| 3D model (Jmol) | |
| Chirality | Racemic mixture |
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Baclofen, sold under the brand name Lioresal among others, is a central nervous system depressant used as a skeletal muscle relaxant. It is primarily used to treat spasticity. It is also used in topical creams to help with pain.
It is a GABA receptor agonist, specifically of the GABAB receptors. Its beneficial effects in spasticity result from actions at spinal and supraspinal sites. It is a derivative of γ-aminobutyric acid (GABA).
A beneficial property of baclofen is that tolerance to its muscle-related therapeutic benefits 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 people receiving intrathecal baclofen treatment. As of 2015 the cost for a typical course of treatment in the United States is less than 25 USD.
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 recommended.
Baclofen is being studied for the treatment of alcoholism. While evidence is promising that it may help with alcohol withdrawal syndrome, as of 2015 it is not strong enough to recommend its use for this purpose.
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Wikipedia