Metaxalone

Pronunciation

(me TAKS a lone)

U.S. Brand Names

Skelaxin®

Generic Available

Canadian Brand Names

Skelaxin®

Use

Relief of discomfort associated with acute, painful musculoskeletal conditions

Pregnancy Risk Factor

Contraindications

Hypersensitivity to metaxalone or any component of the formulation; impaired hepatic or renal function, history of drug-induced hemolytic anemias or other anemias

Warnings/Precautions

Use with caution in patients with impaired hepatic function

Adverse Reactions

Frequency not defined.

Central nervous system: Paradoxical stimulation, headache, drowsiness, dizziness, irritability

Dermatologic: Allergic dermatitis

Gastrointestinal: Nausea, vomiting, stomach cramps

Hematologic: Leukopenia, hemolytic anemia

Hepatic: Hepatotoxicity

Miscellaneous: Anaphylaxis

Overdosage/Toxicology

Signs and symptoms: No major toxicities have been reported

Drug Interactions

Increased effect of alcohol, CNS depressants

Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may increase CNS depression).

Mechanism of Action

Does not have a direct effect on skeletal muscle; most of its therapeutic effect comes from actions on the central nervous system

Pharmacodynamics/Kinetics

Onset of action: ~1 hour

Duration: ~4-6 hours

Metabolism: Hepatic

Bioavailability: Not established; food may increase

Half-life elimination: 9 hours

Time to peak: Tmax: 3 hours

Excretion: Urine (as metabolites)

Dosage

Children >12 years and Adults: Oral: 800 mg 3-4 times/day

Administration

May be administered with or without food. However, serum concentrations may be increased when administered with food; clinical significance has not been established. Patients should be monitored.

Test Interactions

False-positive Benedict's test

Dietary Considerations

Administration with food may increase serum concentrations.

Patient Education

Avoid alcohol and other CNS depressants; may cause drowsiness, impairment of judgment, or coordination; notify physician of dark urine, pale stools, yellowing of eyes, severe nausea, vomiting, or abdominal pain

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

Drowsiness and dizziness are common; may cause paradoxical stimulation

Mental Health: Effects on Psychiatric Treatment

May cause leukopenia; use caution with clozapine and carbamazepine; concurrent use with psychotropics may produce additive sedation

Dosage Forms

[DSC] = Discontinued product

Tablet: 400 mg [DSC], 800 mg

International Brand Names

Skelaxin® (CA)

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