Alternative (1)metaxalone and olopatadine intranasal both increase sedation. Avoid or Use Alternate Drug. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment. opium tinctureMonitor Closely (1)metaxalone and opium tincture both increase sedation. Use Caution/Monitor.orphenadrineMonitor Closely (1)metaxalone and orphenadrine both increase sedation. Use Caution/Monitor.oxazepamMonitor Closely (1)oxazepam and metaxalone both increase sedation. Use Caution/Monitor.oxycodoneMonitor Closely (1)metaxalone and oxycodone both increase sedation. Use Caution/Monitor.oxymorphoneMonitor Closely (1)metaxalone and oxymorphone both increase sedation. Use Caution/Monitor.paliperidoneMonitor Closely (1)metaxalone and paliperidone both increase sedation. Use Caution/Monitor.papaveretumMonitor Closely (1)metaxalone and papaveretum both increase sedation. Use Caution/Monitor.papaverineMonitor Closely (1)metaxalone and papaverine both increase sedation. Use Caution/Monitor.pentazocineMonitor Closely (1)metaxalone and pentazocine both increase sedation. Use Caution/Monitor.pentobarbitalMonitor Closely (1)pentobarbital and metaxalone both increase sedation. Use Caution/Monitor.perphenazineMonitor Closely (1)metaxalone and perphenazine both increase sedation. Use Caution/Monitor.phenobarbitalMonitor Closely (1)phenobarbital and metaxalone both increase sedation. Use Caution/Monitor.phenylephrine POMonitor Closely (1)metaxalone increases and phenylephrine PO decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor. .pholcodineMonitor Closely (1)metaxalone and pholcodine both increase sedation. Use Caution/Monitor.pimozideMonitor Closely (1)metaxalone and pimozide both increase sedation. Use Caution/Monitor.prabotulinumtoxinAMonitor Closely (1)metaxalone increases effects of prabotulinumtoxinA by pharmacodynamic synergism. Use Caution/Monitor. Muscle relaxants may enhance botulinum toxin effects. Closely monitor for increased neuromuscular blockade.primidoneMonitor Closely (1)primidone and metaxalone both increase sedation. Use Caution/Monitor.prochlorperazineMonitor Closely (1)metaxalone and prochlorperazine both increase sedation. Use Caution/Monitor.promethazineMonitor Closely (1)promethazine and metaxalone both increase sedation. Use Caution/Monitor.propofolMonitor Closely (1)propofol and metaxalone both increase sedation. Use Caution/Monitor.propylhexedrineMonitor Closely (1)metaxalone increases and propylhexedrine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.protriptylineMonitor Closely (1)metaxalone and protriptyline both increase sedation. Use Caution/Monitor.quazepamMonitor Closely (1)quazepam and metaxalone both increase sedation. Use Caution/Monitor.quetiapineMonitor Closely (1)metaxalone and quetiapine both increase sedation. Use Caution/Monitor.ramelteonMonitor Closely (1)metaxalone and ramelteon both increase sedation. Use Caution/Monitor.remifentanilMonitor Closely (1)metaxalone increases effects of remifentanil by pharmacodynamic synergism. Modify Therapy/Monitor Closely. CNS depressant effect increased.remimazolamMonitor Closely (1)remimazolam, metaxalone. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely. Coadministration may result in profound sedation, respiratory depression, coma, and/or death. Continuously monitor vital signs during sedation and recovery period if coadministered. Carefully titrate remimazolam dose if administered with opioid analgesics and/or sedative/hypnotics.ribociclibMinor (1)ribociclib will increase the level or effect of metaxalone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.risperidoneMonitor Closely (1)metaxalone and risperidone both increase sedation. Use Caution/Monitor.rucaparibMonitor Closely (1)rucaparib will increase the level or effect of metaxalone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.sageMinor (1)metaxalone and sage both increase sedation. Minor/Significance Unknown.scullcapMonitor Closely (1)metaxalone and scullcap both increase sedation. Use Caution/Monitor.secobarbitalMonitor Closely (1)secobarbital and metaxalone both increase sedation. Use Caution/Monitor.shepherd's purseMonitor Closely (1)metaxalone and shepherd's purse both increase sedation. Use Caution/Monitor.sodium oxybateSerious - Use Alternative (1)metaxalone, sodium oxybate. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.stiripentolMonitor Closely (2)stiripentol, metaxalone. Either increases effects of the other by sedation. Use Caution/Monitor. Concomitant use stiripentol with other CNS depressants, including alcohol, may increase the risk of sedation and somnolence. stiripentol, metaxalone. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.sufentanilMonitor Closely (1)metaxalone and sufentanil both increase sedation. Use Caution/Monitor.sufentanil SLSerious - Use Alternative (1)sufentanil SL, metaxalone. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may result in hypotension, profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.tapentadolMonitor Closely (1)metaxalone and tapentadol both increase sedation. Use Caution/Monitor.tazemetostatMonitor Closely (1)tazemetostat will decrease the level or effect of metaxalone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.tecovirimatMonitor Closely (1)tecovirimat will decrease the level or effect of metaxalone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.temazepamMonitor Closely (1)temazepam and metaxalone both increase sedation. Use Caution/Monitor.teriflunomideMonitor Closely (2)teriflunomide increases levels of metaxalone by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates. teriflunomide decreases levels of metaxalone by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.thioridazineMonitor Closely (1)metaxalone and thioridazine both increase sedation. Use Caution/Monitor.thiothixeneMonitor Closely (1)metaxalone and thiothixene both increase sedation. Use Caution/Monitor.topiramateMonitor Closely (1)metaxalone and topiramate both increase sedation. Modify Therapy/Monitor Closely.tramadolMonitor Closely (1)metaxalone and tramadol both increase sedation. Use Caution/Monitor.trazodoneMonitor Closely (1)metaxalone and trazodone both increase sedation. Use Caution/Monitor.triazolamMonitor Closely (1)triazolam and metaxalone both increase sedation. Use Caution/Monitor.triclofosMonitor Closely (1)triclofos and metaxalone both increase sedation. Use Caution/Monitor.trifluoperazineMonitor Closely (1)metaxalone and trifluoperazine both increase sedation. Use Caution/Monitor.trimipramineMonitor Closely (1)metaxalone and trimipramine both increase sedation. Use Caution/Monitor.tucatinibSerious - Use Alternative (1)tucatinib will increase the level or effect of metaxalone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.voxelotorSerious - Use Alternative (1)voxelotor will increase the level or effect of metaxalone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.xylometazolineMonitor Closely (1)metaxalone increases and xylometazoline decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.ziconotideMonitor Closely (1)metaxalone and ziconotide both increase sedation. Use Caution/Monitor.ziprasidoneMonitor Closely (1)metaxalone and ziprasidone both increase sedation. Use Caution/Monitor.zotepineMonitor Closely (1)metaxalone and zotepine both increase sedation. Use Caution/Monitor. Frequency Not Defined Drug-induced gastrointestinal disturbance Nausea Vomiting Dizziness Headache Somnolence Nervousness Hemolytic anemia (rare) Leukopenia (rare) Jaundice (rare) Immune hypersensitivity reaction (rare) Postmarketing Report Serotonin syndrome (when used concomitantly with serotonergic drugs or doses higher than recommended) Contraindications Hypersensitivity History of drug-induced hemolytic anemia Significant renal/hepatic impairment Cautions CNS depression may occur Sedative effects may be potentiated when used with other sedatives Medication is poorly tolerated by the elderly Bioavailability may increase in female patients Use caution in renal and hepatic impairment Safety and efficacy not established in children <12 years May impair physical or mental abilities; caution patient against operating heavy machinery or performing tasks requiring mental alertness Serotonin syndrome Cases of serotonin syndrome, a potentially life-threatening condition, reported during concomitant use of serotonergic drugs with this drug when used within recommended dosage range and with metaxalone as a single agent taken at doses higher than recommended dose (see drug interaction overview) Serotonin syndrome symptoms may include mental status changes (eg, agitation, hallucinations, coma), autonomic instability (eg, tachycardia, labile blood pressure, hyperthermia), neuromuscular aberrations (eg, hyperreflexia, incoordination, rigidity), and/or gastrointestinal symptoms (eg, nausea, vomiting, diarrhea); the onset of symptoms generally occurs within several hours to a few days, but may occur later than that Discontinue therapy if serotonin syndrome suspected Drug interaction overview Sedative effects of this drug and other CNS depressants (e.g., alcohol, benzodiazepines, opioids, tricyclic antidepressants) may be additive; caution should be exercised with patients who take more than one of these CNS depressants simultaneously Serotonin syndrome have occurred with concomitant use of serotonergic drugs, including selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), triptans, 5-HT3 receptor antagonists, opioids (particularly fentanyl, meperidine, and methadone), drugs that affect the serotonergic neurotransmitter system (eg, mirtazapine, trazodone, tramadol), and drugs that impair metabolism of serotonin (including monoamine oxidase (MAO) inhibitors, both those intended to treat psychiatric disorders and also others, such as linezolid and intravenous methylene blue) Pregnancy category: C Lactation: Unknown if excreted in breast milk; not recommendedPregnancy Categories A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk. B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available. Mechanism of Action General CNS depression; no direct effect on skeletal muscle; may disrupt the spasm-pain-spasm cycle; does not havae direct effect on skeletal muscle Absorption Onset: Within 1 hr Duration: 4-6 hr Peak plasma time: 3 hr Peak plasma concentration: 296 mcg/mL Distribution Vd: 800 L Metabolism Liver Metabolites: Unidentified Elimination Half-life elimination: 4-14 hr Excretion: Urine BRAND FORM. UNIT PRICE PILL IMAGE metaxalone oral- 800 mg tabletmetaxalone oral- 800 mg tabletmetaxalone oral- 800 mg tabletmetaxalone oral- 400 mg tabletmetaxalone oral- 800 mg tabletmetaxalone oral- 800 mg tabletmetaxalone oral- 400 mg tabletCopyright © 2010 First DataBank, Inc.Print Patient Educationmetaxalone oral METAXALONE - ORAL (me-TAX-a-lone) COMMON BRAND NAME(S): Skelaxin USES: Metaxalone is used to treat muscle spasms/pain. It is usually used along with rest, physical therapy, and other treatment. HOW TO USE: Take this medication by mouth with or without food as directed by your doctor. Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of side effects will increase. If you take this medication after a high-fat meal and experience side effects, it may be best to take this drug on an empty stomach or after a light meal.The dosage is based on your medical condition and response to treatment.To prevent a very serious high blood pressure reaction, it is very important that you follow a special diet recommended by your doctor or dietician to limit your intake of tyramine while you are taking this medicine. Avoid foods and beverages that are high in tyramine, including aged cheeses, dried/aged meats and sausages (such as salami, liverwurst), preserved fish (such as pickled herring), products that contain large amounts of yeast (such as bouillon cubes, powdered soup/gravy, homemade or sourdough bread), fermented foods (such as sauerkraut, kim chee), most soybean products (such as soy sauce, tofu), broad/fava beans, red wine, sherry, tap beers, and vermouth. Consult your doctor or dietician for more details and a complete list of other foods that contain tyramine which you should limit or avoid.Tell your doctor if your condition does not improve or if it worsens. SIDE EFFECTS: Drowsiness, dizziness, nausea, vomiting, and upset stomach may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as nervousness, irritability, confusion), signs of infection (such as sore throat that doesn't go away, fever), yellowing eyes/skin, unusual tiredness, dark urine.This medication may increase serotonin and rarely cause a very serious condition called serotonin syndrome/toxicity. The risk increases if you are also taking other drugs that increase serotonin, so tell your doctor or pharmacist of all the drugs you take (see Drug Interactions section). Get medical help right away if you develop some of the following symptoms: fast heartbeat, hallucinations, loss of coordination, severe dizziness, severe nausea/vomiting/diarrhea, twitching muscles, unexplained fever, unusual agitation/restlessness.This drug may rarely cause an attack of extremely high blood pressure (hypertensive crisis), which may be fatal. Many drug and food interactions can increase this risk (see How to Use and Drug Interactions sections). Get medical help right away if any of these serious side effects occur: severe headache, fast/slow/irregular/pounding heartbeat, chest pain, neck stiffness/soreness, severe nausea/vomiting, sweating/clammy skin (sometimes with fever), widened pupils, vision changes (such as double/blurred vision), sudden sensitivity to light (photophobia).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic