Drug Guide
Metaxalone
Classification
Therapeutic: Muscle Relaxant
Pharmacological: Centrally Acting Skeletal Muscle Relaxant
FDA Approved Indications
- Relief of discomfort associated with acute, painful musculoskeletal conditions
Mechanism of Action
Metaxalone acts centrally in the CNS to produce sedation and muscle relaxation; the precise mechanism is unknown but may involve sedative and analgesic effects that reduce muscle spasm and associated discomfort.
Dosage and Administration
Adult: Typically 800 mg three to four times daily as needed. Dose should be individualized based on response.
Pediatric: Not recommended for use in patients under 16 years due to lack of safety and efficacy data.
Geriatric: Caution advised; start at lower doses and monitor closely due to increased sensitivity and potential for adverse effects.
Renal Impairment: Use with caution; dosage adjustment may be necessary.
Hepatic Impairment: Use with caution; no specific dosage recommendations established.
Pharmacokinetics
Absorption: Well absorbed after oral administration
Distribution: Widely distributed in body tissues
Metabolism: Metabolized in the liver, specifics not well characterized
Excretion: Excreted primarily in urine as metabolites
Half Life: Approximately 1-2 hours
Contraindications
- Hypersensitivity to metaxalone or any component of the formulation
Precautions
- Use cautiously in patients with a history of hepatic impairment, hypersensitivity, or those taking other CNS depressants.
- Pregnancy Category C; use only if clearly needed, weighing potential benefits and risks.
Adverse Reactions - Common
- Drowsiness (Common)
- Dizziness (Common)
- Headache (Common)
- GI upset (Common)
Adverse Reactions - Serious
- Hepatotoxicity (Rare)
- Allergic reactions including rash, urticaria (Rare)
- Severe CNS depression (Rare)
Drug-Drug Interactions
- CNS depressants (additive sedative effect)
- Antidepressants (risk of serotonin syndrome)
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor hepatic function if therapy is prolonged or if pre-existing liver disease.
Diagnoses:
- Risk for injury related to sedation or dizziness
Implementation: Administer with food to decrease GI upset; monitor for adverse reactions; instruct patient on safety precautions.
Evaluation: Assess for effectiveness in reducing muscle spasm and pain; monitor for adverse effects such as excessive sedation or liver dysfunction.
Patient/Family Teaching
- Do not operate heavy machinery or drive until response is known.
- Avoid alcohol and other CNS depressants during therapy.
- Report any signs of allergic reactions or unusual symptoms to healthcare provider.
Special Considerations
Black Box Warnings:
- None currently
Genetic Factors: None identified as significant influencing pharmacokinetics or effects.
Lab Test Interference: None known.
Overdose Management
Signs/Symptoms: Drowsiness, dizziness, vomiting, lethargy,
Treatment: Supportive care; gastric lavage if ingestion was recent; activated charcoal may be administered; hemodialysis is generally not effective.
Storage and Handling
Storage: Store at room temperature, away from moisture and heat.
Stability: Stable under recommended storage conditions.