Metaxalone

— THERAPEUTIC CATEGORIES —
  • Musculoskeletal pain

Metaxalone Generic Name & Formulations

General Description

Metaxalone 400mg, 800mg+; tabs; +scored.

Pharmacological Class

Muscle relaxant (central).

How Supplied

Contact supplier

Mechanism of Action

The mechanism of action of metaxalone in humans has not been established, but may be due to general central nervous system (CNS) depression. Metaxalone has no direct action on the contractile mechanism of striated muscle, the motor end plate, or the nerve fiber.

Metaxalone Indications

Indications

As adjunct treatment for acute, painful musculoskeletal conditions.

Metaxalone Dosage and Administration

Adult

800mg 3–4 times daily.

Children

≤12yrs: not established.

Metaxalone Contraindications

Contraindications

Anemias. Significant renal or hepatic dysfunction.

Metaxalone Boxed Warnings

Not Applicable

Metaxalone Warnings/Precautions

Warnings/Precautions

Renal or hepatic impairment (monitor LFTs). Elderly. Pregnancy, nursing mothers: not recommended.

Metaxalone Pharmacokinetics

Absorption

Peak plasma concentrations: ~3 hours (after a 400 mg dose).

Distribution

Volume of distribution: ~800 L.

Metabolism

Hepatic.

Elimination

Renal. Half-life: 9.0 ± 4.8 hours.

Metaxalone Interactions

Interactions

Increased risk of sedation, respiratory depression with concomitant other CNS depressants (eg, alcohol, benzodiazepines, opioids, TCAs); monitor closely. Risk of serotonin syndrome with serotonergic drugs (eg, SSRIs, SNRIs, TCAs, triptans, 5-HT3 antagonists, opioids, mirtazapine, trazodone, tramadol, MAOIs, linezolid, IV methylene blue); monitor and discontinue if suspected. Concomitant with food may enhance CNS depression. May cause false (+) Benedict's test.

Metaxalone Adverse Reactions

Adverse Reactions

Drowsiness, dizziness, headache, nervousness, GI upset, rash, jaundice, hemolytic anemia, leukopenia; hypersensitivity reactions.

Metaxalone Clinical Trials

See Literature

Metaxalone Note

Notes

Formerly known under the brand name Skelaxin.

Metaxalone Patient Counseling

See Literature