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Baclofen
drug data and news
Baclofen drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Baclofen | ||
| Brand Names/Synonyms | Apo-Baclofen; Ba 34647; Baclofen; Baclon; C 34647ba; Kemstro; Lioresal; Lioresal Intrathecal; Novo-Baclofen; Nu-Baclofen; Pms-Baclofen | ||
| Indication | For the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Baclofen is a muscle relaxant and antispastic. Baclofen is useful for the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity. Although Baclofen is an analog of the putative inhibitory neurotransmitter gamma-aminobutyric acid (GABA), there is no conclusive evidence that actions on GABA systems are involved in the production of its clinical effects. In studies with animals, Baclofen has been shown to have general CNS depressant properties as indicated by the production of sedation with tolerance, somnolence, ataxia, and respiratory and cardiovascular depression. Baclofen is rapidly and extensively absorbed and eliminated. Absorption may be dose-dependent, being reduced with increasing doses. Baclofen is excreted primarily by the kidney in unchanged form and there is relatively large intersubject variation in absorption and/or elimination. | ||
| Mechanism Of Action | Baclofen is a direct agonist at GABAB receptors. 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. | ||
| Baclofen News (When available) |
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| Dosage Forms | TABLET; INTRATHECAL INJECTION; | ||
| Drug_Category | Muscle Relaxants; Skeletal Muscle Relaxants; GABA Agonists; ATC:M03BX01 | ||
| Absorption | Rapidly and extensively absorbed | ||
| Interactions |
-->Interactions for Baclofen: Injection There is inadequate systematic experience with the use of baclofen injection in combination with other medications to predict specific drug-drug interactions. Interactions attributed to the combined use of baclofen injection and epidural morphine include hypotension and dyspnea. SIDE EFFECTS (KEMSTRO) | ||
| Toxicity | LD50=45 mg/kg (male mice, IV0; LD50=78 mg/kg (male rat, IV) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 4-amino-3-(4-chlorophenyl)-butanoic acid | ||
| Chemical Formula | C10H12ClNO2 | ||
| Molecular Weight | 213.661 g/mol | ||
| Smiles String | C1=CC(=CC=C1C(CC(=O)O)CN)Cl | ||
| Melting Point | 206-208 °C | ||
| Water Solubility | 2090 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 1.42 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 1.51 hours | ||
| Protein Binding [%] | 30% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Baclofen.html http://www.rxlist.com/cgi/generic/baclofen.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00551 | ||
| CAS Registry Number | 1134-47-0 | ||
| KEGG Compound ID | C06841 | ||
| PubChem ID | SID:9059 | ||
| PharmGKB ID | PA448533 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2242151 |
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