The mechanism of action of metaxalone in humans has not been established, but may be due to general central nervous system depression. Metaxalone has no direct action on the contractile mechanism of striated muscle, the motor end plate or the nerve fiber.
Metaxalone (marketed by King Pharmaceuticals under the brand name Skelaxin®) 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.
The most frequent reactions to Skelaxin include nausea, vomiting, gastrointestinal upset, drowsiness, dizziness, headache, and nervousness or "irritability." Other adverse reactions are: hypersensitivity reactions, characterized by a light rash with or without pruritus; leukopenia; hemolytic anemia; jaundice.
Deaths by deliberate or accidental overdose have occurred with metaxalone, particularly in combination with antidepressants, and have been reported with this class of drug in combination with alcohol.
When determining the LD50 in rats and mice, progressive sedation, hypnosis and finally respiratory failure 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.
Use caution when driving, operating machinery, or performing other hazardous activities. Skelaxin may cause dizziness or drowsiness. If you experience dizziness or drowsiness, avoid these activities.