hypotension, profound sedation, respiratory depression, or comaphenobarbitalSerious - Use Alternative (1)phenobarbital will decrease the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.phenytoinMonitor Closely (1)phenytoin will decrease the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.posaconazoleSerious - Use Alternative (1)posaconazole will increase the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.pregabalinMonitor Closely (1)pregabalin, eszopiclone. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.primidoneSerious - Use Alternative (1)primidone will decrease the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.remimazolamMonitor Closely (1)remimazolam, eszopiclone. 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.ribociclibMonitor Closely (1)ribociclib will increase the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.rifabutinMonitor Closely (1)rifabutin will decrease the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.rifampinMonitor Closely (1)rifampin will decrease the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. According to prescribing information, zopiclone AUC was decreased 80% by concomitant use of rifampin. A similar effect would be expected with eszopiclone (S-enantiomer of zopiclone).rifapentineMonitor Closely (1)rifapentine will decrease the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.ritonavirMonitor Closely (1)ritonavir increases levels of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce eszopiclone starting dose to 1 mg/day.rucaparibMonitor Closely (1)rucaparib will increase the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.saquinavirMonitor Closely (1)saquinavir increases levels of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce eszopiclone starting dose to 1 mg/day.secobarbitalSerious - Use Alternative (1)secobarbital will decrease the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. May also enhance CNS depressant effect of eszopicloneselinexorSerious - Use Alternative (1)selinexor, eszopiclone. unspecified interaction mechanism. Avoid or Use Alternate Drug. Patients treated with selinexor may experience neurological toxicities. Avoid taking selinexor with other medications that may cause dizziness or confusion.sodium oxybateContraindicated (1)eszopiclone, sodium oxybate. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Coadministration with alcohol or sedative hypnotics are contraindicated because of additive CNS depression.stiripentolMonitor Closely (2)stiripentol, eszopiclone. 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, eszopiclone. 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.sufentanil SLSerious - Use Alternative (1)sufentanil SL, eszopiclone. 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.tazemetostatMonitor Closely (1)tazemetostat will decrease the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.tecovirimatMonitor Closely (1)tecovirimat will decrease the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.tipranavirMonitor Closely (1)tipranavir increases levels of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce eszopiclone starting dose to 1 mg/day.tucatinibSerious - Use Alternative (1)tucatinib will increase the level or effect of eszopiclone 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.valerianSerious - Use Alternative (1)valerian and eszopiclone both increase sedation. Avoid or Use Alternate Drug.voriconazoleMonitor Closely (1)voriconazole increases levels of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce eszopiclone starting dose to 1 mg/day.voxelotorSerious - Use Alternative (1)voxelotor will increase the level or effect of eszopiclone 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. >10% Headache (13-21%) Unpleasant taste (17-34% in non-elderly) 1-10% Abnormal dreams (elderly) Accidental injury (elderly) Diarrhea Dizziness Dry mouth Dyspepsia Nervousness Neuralgia Pain Pruritus Rash (in non-elderly) Somnolence Unpleasant taste (elderly) UTI <1% Agitation Alopecia Angioedema Asthma Anorexia Cystitis Dysphagia Fever Epistaxis Hypertension Hostility Hypercholesterolemia Hypokalemia Postmarketing Reports Dysosmia Complex sleep behaviors Black Box Warnings Complex sleep behaviors including sleep-walking, sleep-driving, and engaging in other activities while not fully awake may occur with therapy; some of these events may result in serious injuries, including death; discontinue therapy immediately if patient experiences a complex sleep behaviorContraindications Documented hypersensitivity Patients who have experienced complex sleep behaviors after receiving therapy Cautions Take immediately before going to bed - taking earlier may cause memory loss, hallucinations, dizziness, lightheadedness Can impair daytime function in some patients at the higher doses (2 mg or 3 mg), even when used as prescribed; monitor for next day next-day psychomotor impairment Take only when able to have a full night of sleep (7-8 hr); coadministration with other sedative-hypnotics at bedtime or taking eszopiclone the middle of the night is not recommended because of risk for next-day psychomotor impairment May cause CNS depression and impair physical and mental abilities May worsen clinical depression Use minimum dose that will effectively treat patient; write prescription for smallest quantity consistent with good patient care May cause abnormal thinking & bizarre behavior May impair ability to drive or operate heavy machinery Caution in history of drug or substance abuse, respiratory diseases, hepatic impairment Amnesia may occur Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric and/or medical illness Abrupt discontinuation or rapid dose decreases may lead to withdrawal symptoms Therapy can cause drowsiness and a decreased level of consciousness; patients, particularly the elderly, are at higher risk of falls Complex sleep behavior Behaviors including sleep-walking, sleep-driving, and engaging in other activities while not fully awake may occur following first or any subsequent use of drug Other complex sleep behaviors (e.g., preparing and eating food, making phone calls, or having sex) also reported Patients can be seriously injured or injure others during complex sleep behaviors Patients usually do not remember events Post-marketing reports have shown that complex sleep behaviors may occur with drug alone at recommended dosages, with or without the concomitant use of alcohol or other CNS depressants Concomitant administration with other CNS depressants, may increase risk of sleep-related episodes Discontinue treatment in patients reporting any sleep-related activities Pregnancy Available pharmacovigilance data with use in pregnant women are insufficient to identify drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes Animal data In animal reproduction studies conducted in pregnant rats and rabbits throughout organogenesis, there was no evidence of teratogenicity; administration to rats throughout pregnancy and lactation resulted in offspring toxicities at all doses tested; lowest dose was approximately 200 times maximum recommended human dose (MRHD) of 3 mg/day based on mg/ m² body surface area Lactation There are no data on prescence in either human or animal milk, effects on breastfed infant, or on milk production; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from therapy or underlying maternal conditionPregnancy 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 Unknown, may interact with GABA receptor complexes at binding domains allosterically couppled to benzodiazepine receptors Pharmacokinetics Absorption: Rapid (attenuated by high-fat meal) Protein Bound: 52-59% Peak Plasma Time: 1 hr Half-life, elimination: 6 hr (<65 years old); 9 hr (≥65 years) Metabolism: Primarily by CYP3A4 & CYP2E1 via oxidation & demethylation Metabolites: (S)-zopiclone-N-oxide & (S)-N-desmethylzopiclone Excretion: Urine (85%) BRAND FORM. UNIT PRICE PILL IMAGE eszopiclone oral- 2 mg tableteszopiclone oral- 2 mg tableteszopiclone oral- 1 mg tableteszopiclone oral- 2 mg tableteszopiclone oral- 3 mg tableteszopiclone oral- 3 mg tableteszopiclone oral- 3 mg tableteszopiclone oral- 2 mg tableteszopiclone oral- 1 mg tableteszopiclone oral- 3 mg tableteszopiclone oral- 1 mg tableteszopiclone oral- 1 mg tableteszopiclone oral- 2 mg tableteszopiclone oral- 3 mg tableteszopiclone oral- 2 mg tableteszopiclone oral- 1 mg tableteszopiclone oral- 2 mg tableteszopiclone oral- 1 mg tableteszopiclone oral- 1 mg tableteszopiclone oral- 3 mg tableteszopiclone oral- 1 mg tableteszopiclone oral- 3 mg tableteszopiclone oral- 2 mg tableteszopiclone oral- 3 mg tableteszopiclone oral- 3 mg tableteszopiclone oral- 2 mg tableteszopiclone oral- 1 mg tabletLunesta oral- 3 mg tabletLunesta oral- 2 mg tabletLunesta oral- 1 mg tabletCopyright © 2010 First DataBank, Inc.Print Patient Educationeszopiclone oral ESZOPICLONE - ORAL (es-zoe-PIK-lone) COMMON BRAND NAME(S): Lunesta WARNING: Rarely, after taking this drug, people have gotten out of bed and driven vehicles while not fully awake ("sleep-driving"). People have also sleepwalked, prepared/eaten food, made phone calls, or had sex while not fully awake. Often, these people do not remember these events. This problem can be dangerous (possibly fatal) to you or to others. If you find out that you have done any of these activities after taking this medication, tell your doctor right away. You should not take this medication or similar medications (such as zaleplon, zolpidem) if you have this reaction to the medication. USES: This medication is used to treat a certain sleep problem (insomnia). It may help you fall asleep faster, stay asleep longer, and lessen how often you wake up during the night, so you can get a better night's rest. Eszopiclone belongs to a class of drugs called sedative-hypnotics. It acts on your brain to produce a calming effect.Use of this medication is usually limited to short treatment periods of 1 to 2 weeks or less. If your insomnia continues for a longer time, talk to your doctor to see if you need other treatment. HOW TO USE: Read the Medication Guide provided by your pharmacist before you start using eszopiclone and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth as directed by your doctor, usually just before you get into bed. Do not take it with or right after a high-fat or heavy meal since it may not work as well. The dosage is based on your medical condition, age, liver function, other medications you may be taking, and response to treatment. Do not take more of this medication than prescribed because your risk of side effects will increase. The starting dose is 1 milligram at bedtime as directed. That dosage lessens the risk of having trouble safely doing activities requiring alertness the next day (such as driving or operating machinery). Also, you may not be fully alert the next day, yet you think you are fully alert. If you are prescribed the 3 milligram dosage of eszopiclone, you should not do activities the next day that require alertness. Ask your doctor or pharmacist for more details.If you are an older adult or you have liver disease, a low dose will usually be prescribed to lessen the risk of being impaired the next day. Do not stop your medication without talking to your doctor or pharmacist.Do not take