Metaxalone (Skelaxin®)
Metaxalone
Brand name: Skelaxin®
Classification:
» Musculoskeletal Agents
» Skeletal Muscle Relaxants
Description: Metaxalone is an oral CNS depressant used as adjunct therapy for acute, painful musculoskeletal conditions. Although the drug is classified as a skeletal muscle relaxant, it does not directly relax skeletal muscle. Most of the beneficial effects of metaxalone are thought to be due to its sedative properties. Metaxalone does not effectively treat skeletal muscle hyperactivity secondary to chronic neurologic disorders (e.g., cerebral palsy). This drug was approved by the FDA in 1962.
Mechanism of Action: The mechanism of action of metaxalone has not been established. Metaxalone has no direct effect on the contractile mechanism of striated muscle, the motor end plate, or the nerve fiber. Its mode of action may be related to its sedative properties.
 Skelaxin Tablets (Tablet 400 mg)
Pharmacokinetics: Metaxalone is administered orally. Mean peak plasma concentrations occur about 3 hours after a single 400 mg dose given on an empty stomach and about 4 hours after a single 400 mg dose given with food. The onset of action is usually within 1 hour, and the duration of effect is about 4 - 6 hours. Administering metaxalone with a high-fat meal increases the mean Cmax and AUC to 177.5% and 123.5%, respectively. The terminal half-life is approximately 9 hours, decreasing to 2.5 hours when given with a high-fat meal. It is not known if metaxalone crosses the placenta or if it is distributed into milk. Metaxalone is metabolized by the liver and excreted in urine as unidentified metabolites.
Special Populations: The impact of age, gender, hepatic impairment or renal impairment on the pharmacokinetics of metaxalone tablets has not been determined.
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[ Revised 12/8/2005 1:08:00 PM ]
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