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DB00660 - Metaxalone


Identification
Name Metaxalone
Accession Number DB00660 (APRD00514)
Type small molecule
Description Metaxalone (marketed by King Pharmaceuticals under the brand name Skelaxin(R)) is a muscle relaxant used to relax muscles and relieve pain caused by strains, sprains, and other musculoskeletal conditions. Its exact mechanism of action is not known, but it may be due to general central nervous system depression. It is considered to be a moderately strong muscle relaxant, with relatively low incidence of side effects. Skelaxin comes in an 800 mg scored tablet. It previously came in both 400 mg and 800 mg tablets. The 400 mg tablet has been discontinued. Possible side effects include nausea, vomiting, drowsiness and CNS side effects such as dizziness, headache, and irritability.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 221.2524
Groups approved
Monoisotopic Weight 221.105193351
Pharmacology
Indication For the treatment of painful peripheral musculoskeletal conditions and spasticity from upper motor neuron syndromes.
Mechanism of action The mechanism of action of metaxalone in humans has not been established, but may be due to general central nervous system depression.
Absorption The absolute bioavailability of metaxalone from Skelaxin tablets is not known.
Protein binding Not Available
Biotransformation Probably hepatic.
Route of elimination Metaxalone is metabolized by the liver and excreted in the urine as unidentified metabolites.
Toxicity LD50=775mg/kg (Rat, oral); LD50=1690 mg/kg (Mouse, oral). When determining the LD50 in rats and mice, progressive sedation, hypnosis and finally respiratoryfailure were noted as the dosage increased. In dogs, no LD50 could be determined as the higher doses produced an emetic action in 15 to 30 minutes.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Triprolidine The CNS depressants, Triprolidine and Metaxalone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Food Interactions Not Available

Predictions


Id Partner name Gene Name Score
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