Metaxalone

Indications
 Oral
Painful muscle spasm associated with musculoskeletal conditions
Adult: As an adjunct to rest, physical therapy, and analgesics to relieve discomfort: 800 mg 3-4 times daily.
Child: >12 yr: 800 mg 3-4 times daily.
Contraindications
 Patient with history of drug-induced, haemolytic or other anaemias; significantly impaired renal or hepatic function.
Warnings / Precautions
 Pregnancy; lactation; mild to moderate renal and hepatic impairment. Monitor liver function periodically during treatment. May cause CNS depression and impair mental and/or physical ability; caution when driving or operating machinery. Metaxalone is poorly tolerated by geriatric patient. Safety and efficacy have not been established in children 12 yr of age and below.
Adverse Reactions
 Headache, dizziness, drowsiness, nausea, vomiting, GI upset, rash with/without pruritus, hypersensitivity reaction, nervousness/irritability, leukopenia, haemolytic anaemia, and jaundice.
Potentially Fatal: Anaphylactoid reactions.
Overdose Reactions
 Symptoms: Drowsiness, dizziness, nausea, vertigo, lethargy, agitation, slurred speech, tremor and tachycardia may occur. Treatment: Gastric lavage and supportive therapy.
Drug Interactions
 Concurrent use of Metaxalone with alcohol and other CNS depressants e.g. benzodiazepines, opioids, and tricyclic antidepressants may enhance sedative effects of both drugs.
See Below for More metaxalone Drug Interactions
Lab Interactions
 May cause false-positive Benedict's test.
Food Interactions
 Avoid alcohol and St. John's wort. Administration with high-fat meal may delay absorption, increase serum concentrations, and increase exposure of Metaxalone; which may enhance general CNS depression.
Mechanism of Actions
 Metaxalone is a centrally acting skeletal muscle relaxant. The precise mechanism of action in humans is not known. Its effect may be associated with general CNS depression. Unlike neuromuscular blocking agents, Metaxalone does not have direct effect on the contractile mechanism of striated muscle, the motor end plate or the nerve fiber.
Onset: Usually within 1 hr.
Duration: Approx 4-6 hr.
Distribution: Extensively distributed; apparent Vd: About 800 L.
Metabolism: Undergoes hepatic metabolism.
Excretion: Excreted in urine (as unidentified metabolites). Terminal half-life: About 4-14 hr. Apparent oral clearance: About 59-68 L/hr.
Storage Conditions
 Oral: Store at 15-30°C (68-77°F).
Storage
 Oral: Store at 15-30°C (68-77°F).
Available As
  • Metaxalone 400 mg

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