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Metaxalone
- indication:For the treatment of painful musculoskeletal conditions
- pharmacologypharmacology:
- mechanism: The mechanism of action of metaxalone in humans has not been established, but may be due to general central nervous system depression.
- toxicity: LD<sub>50</sub>=775mg/kg (Rat, oral); LD<sub>50</sub>=1690 mg/kg (Mouse, oral). When determining the LD<sub>50</sub> in rats and mice, progressive sedation, hypnosis and finally respiratoryfailure were noted as the dosage increased. In dogs, no LD<sub>50</sub> could be determined as the higher doses produced an emetic action in 15 to 30 minutes.
- absorprion: The absolute bioavailability of metaxalone from Skelaxin tablets is not known.
- halflife: 9.2 (+/- 4.8) hours
- roouteelimination: Metaxalone is metabolized by the liver and excreted in the urine as unidentified metabolites.
- volumedistribution: * 800 L
- clearance: * 68 +/- 50 L/h [Subjects received 1×400mg tablet under fasted conditions] * 66 +/- 51 L/h [Subjects received 2×400 mg tablets under fasted conditions]