Metaxalone


Full Generic Medicine Info
Dosage/Direction for Use

Oral
Acute musculoskeletal disorders
Adult: As a treatment adjunct: 800 mg 3-4 times daily.
Child: >12 years Same as adult dose.
Contraindications
Drug-induced, haemolytic anaemia, or other anaemias. Significantly impaired hepatic or renal function.
Special Precautions
Concomitant use with serotonergic agents (e.g. SSRIs, SNRIs, TCAs, triptans, 5-HT3 receptor antagonists, MAOIs). Hepatic and renal impairment. Pregnancy and lactation. Patient Counselling This medicine may cause drowsiness or dizziness, if affected, do not drive or operate machinery.
Adverse Reactions
Significant: CNS depression. Blood and lymphatic system disorders: Haemolytic anaemia, leucopenia. Gastrointestinal disorders: Nausea, vomiting, gastrointestinal distress. Immune system disorders: Hypersensitivity reaction, anaphylaxis. Rarely, anaphylactoid reaction. Nervous system disorders: Dizziness, headache, drowsiness, nervousness, irritability. Skin and subcutaneous tissue disorders: Rash (with or without pruritus), jaundice.
Potentially Fatal: Serotonin syndrome when used with serotonergic agents (e.g. SSRIs, SNRIs, TCAs, triptans, 5-HT3 receptor antagonists, MAOIs).
Overdosage
Symptoms: Serotonin syndrome, death. Management: Supportive therapy. Perform gastric lavage.
Drug Interactions
Increased risk of serotonin syndrome with other serotonergic agents (e.g. SSRIs, SNRIs, TCAs, triptans, 5-HT3 receptor antagonists, MAOIs). Enhanced sedative effects with benzodiazepines.
Food Interaction
Enhanced CNS depressant effect with alcohol.
Lab Interference
May cause false-positive results for glucose determinations using cupric sulfate (e.g. Benedict's solution, Fehling's solution).
Action
Metaxalone is a centrally acting muscle relaxant. The precise mechanism of action has not been established. Its effect may be associated with CNS depression. It has no direct effect on the contractile mechanism of striated muscle, the motor end plate or the nerve fibre.
Onset: Within 1 hour.
Duration: 4-6 hours.
Absorption: Absorbed from the gastrointestinal tract. Bioavailability: May be increased with food. Time to peak plasma concentration: Approx 3 hours.
Distribution: Extensively distributed in the tissues. Volume of distribution: Approx 800 L.
Metabolism: Metabolised in the liver by CYP1A2, CYP2D6, CYP2E1, CYP3A4 and to a lesser extent by CYP2C8, CYP2C9, and CYP2C19.
Excretion: Via urine (as metabolites). Elimination half-life: 9±4.8 hours.
Storage
Oral: Store between 15-30°C.
CIMS Class
Muscle Relaxants
Disclaimer: This information is independently developed by CIMS based on metaxalone from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2022 CIMS. All rights reserved. Powered by CIMSAsia.com
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