(es zoe PIK lone)
Insomnia: Treatment of insomnia
Hypersensitivity to eszopiclone or any component of the formulation.
Insomnia: Oral: Note: The lowest effective dose should be used.
Initial: 1 mg immediately before bedtime; dosing may be increased to 2 mg or 3 mg if clinically necessary (maximum dose: 3 mg daily)
Debilitated patients: Initial: 1 mg immediately before bedtime (maximum dose: 2 mg)
Concurrent use with strong CYP3A4 inhibitor: Initial: 1 mg immediately before bedtime (maximum dose: 2 mg)
Initial: 1 mg immediately before bedtime (maximum dose: 2 mg)
No dosage adjustment necessary.
Mild to moderate impairment: No dosage adjustment necessary.
Severe impairment: Initial: 1 mg immediately before bedtime (maximum dose: 2 mg); use with caution; systemic exposure is doubled in severe impairment.
Because of the rapid onset of action, eszopiclone should be administered immediately prior to bedtime or after the patient has gone to bed and is having difficulty falling asleep. Do not take with, or immediately following, a high-fat meal (may delay onset).
Avoid taking after a heavy meal; may delay onset.
Store at 25 ‚ °C (77 ‚ °F); excursions permitted to 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Lunesta: 1 mg [contains fd&c blue #2 (indigotine)]
Lunesta: 2 mg
Lunesta: 3 mg [contains fd&c blue #2 (indigotine)]
Generic: 1 mg, 2 mg, 3 mg
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Monitor therapy
Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). Avoid combination
Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Consider therapy modification
Bosentan: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine patches (Butrans brand) at 5 mcg/hr in adults when used with other CNS depressants. Consider therapy modification
Cannabis: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination
CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Monitor therapy
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Eszopiclone. Management: Limit the eszopiclone dose to 2 mg daily when combined with strong CYP3A4 inhibitors and monitor for increased eszopiclone effects and toxicities (eg, somnolence, drowsiness, CNS depression). Consider therapy modification
Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates. Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification
Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Dimethindene: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Monitor therapy
Dronabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Consider therapy modification
Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates. Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Consider therapy modification
Flumazenil: May diminish the sedative effect of Hypnotics (Nonbenzodiazepine). Monitor therapy
Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Consider therapy modification
Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination
HYDROcodone: CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Consider starting with a 20% to 30% lower hydrocodone dose when using together with any other CNS depressant. Dose reductions in the other CNS depressant may also be warranted. Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination
Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy
Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Consider therapy modification
MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Monitor therapy
MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates. Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Consider therapy modification
Minocycline: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Mirtazapine: CNS Depressants may enhance the CNS depressant effect of Mirtazapine. Monitor therapy
Mitotane: May decrease the serum concentration of CYP3A4 Substrates. Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification
Nabilone: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Netupitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Avoid combination
Osimertinib: May increase the serum concentration of CYP3A4 Substrates. Osimertinib may decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: When oxycodone is combined with another CNS depressant, a dose reduction of one or both agents should be considered. The extended release oxycodone starting dose should be reduced 50% to 67% when initiated in patients already receiving CNS depressants. Consider therapy modification
Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Avoid combination
Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Consider therapy modification
Piribedil [INT]: CNS Depressants may enhance the CNS depressant effect of Piribedil [INT]. Monitor therapy
Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Monitor therapy
ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Monitor therapy
Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Monitor therapy
Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Monitor therapy
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Monitor therapy
Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Sodium Oxybate: Hypnotics (Nonbenzodiazepine) may enhance the CNS depressant effect of Sodium Oxybate. Avoid combination
St Johns Wort: May decrease the serum concentration of CYP3A4 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification
Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification
Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Consider therapy modification
Tapentadol: May enhance the CNS depressant effect of CNS Depressants. Management: Start tapentadol at a dose of one-third to one-half of the normal dose if being initiated in a patient who is taking another drug with CNS depressant effects. Monitor closely for evidence of excessive CNS depression. Consider therapy modification
Tetrahydrocannabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Avoid combination
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Consider therapy modification
>10%:
Central nervous system: Headache (15% to 21%)
Gastrointestinal: Dysgeusia (8% to 34%)
1% to 10%:
Cardiovascular: Chest pain ( ≥1%), peripheral edema ( ≥1%)
Central nervous system: Drowsiness (8% to 10%), dizziness (5% to 7%), pain (4% to 5%), nervousness ( ≤5%), depression (1% to 4%), confusion ( ≤3%), neuralgia ( ≤3%), abnormal dreams (1% to 3%), anxiety (1% to 3%), hallucination (1% to 3%), migraine
Dermatologic: Skin rash (3% to 4%), pruritus (1% to 4%)
Endocrine & metabolic: Decreased libido ( ≤3%), gynecomastia ( ≤3%)
Gastrointestinal: Xerostomia (3% to 7%), dyspepsia (2% to 6%), nausea (4% to 5%), diarrhea (2% to 4%), vomiting ( ≤3%)
Genitourinary: Dysmenorrhea ( ≤3%), urinary tract infection ( ≤3%)
Infection: Infection (5% to 10%), viral infection (3%)
Miscellaneous: Accidental injury ( ≤3%)
<1% (Limited to important or life-threatening): Abnormality in thinking, alopecia, amenorrhea, anaphylaxis, anemia, angioedema, anorexia, aphthous stomatitis, asthma, ataxia, blepharoptosis, breast hypertrophy, breast neoplasm, bronchitis, bursitis, cholelithiasis, colitis, conjunctivitis, contact dermatitis, cystitis, dehydration, dysphagia, dyspnea, emotional lability, epistaxis, erythema multiforme, facial edema, gastric ulcer, gastritis, gout, halitosis, heatstroke, hematuria, hepatitis, hepatomegaly, herpes zoster, hypercholesterolemia, hypermenorrhea, hypersensitivity reaction, hypertension, hypokalemia, hyporeflexia, insomnia, laryngitis, lymphadenopathy, mastalgia, melena, memory impairment, myasthenia, mydriasis, myopathy, neck stiffness, nephrolithiasis, neuritis, neuropathy, nystagmus, oliguria, pyelonephritis, rectal hemorrhage, reflexes decreased, renal pain, skin discoloration, skin photosensitivity, sleep disorder (complex sleep-related behavior, including cooking or eating food, making phone calls, sleep driving), thrombophlebitis, tongue edema, urethritis, urinary incontinence, uterine hemorrhage, vaginal hemorrhage, vaginitis, vesiculobullous dermatitis, vestibular disturbance
Systemic exposure is doubled in severe hepatic impairment with no change in Cmax or Tmax
Subjects ≥65 years of age had a 41% increase in total exposure (AUC) and a 50% increase in elimination half-life.
Concerns related to adverse effects:
- Abnormal thinking/behavioral changes: Hypnotics/sedatives have been associated with abnormal thinking and behavior changes including decreased inhibition, aggression, bizarre behavior, agitation, hallucinations, and depersonalization. These changes may occur unpredictably and may indicate previously unrecognized psychiatric disorders; evaluate appropriately.
- CNS depression: Daytime function may be impaired in patients taking higher doses (2 mg or 3 mg) even if used as prescribed; patients taking 3 mg must be cautioned about performing tasks which require mental alertness (operating machinery or driving) the day after use. An increased risk of next-day psychomotor impairment may occur if taken with less than a full night of sleep (7 to 8 hours); if a higher than recommended dose is taken; if co-administered with other CNS depressants or other drugs that increase blood concentrations of eszopiclone. Dose adjustment may be necessary if taking concomitant CNS depressants; the use of concomitant sedative-hypnotics at bedtime or in the middle of the night is not recommended.
- Hypersensitivity reactions: Hypersensitivity reactions including anaphylaxis as well as angioedema have been reported, in some cases following initial dosing. Patients who develop severe reactions should not be rechallenged.
- Sleep-related activities: An increased risk for hazardous sleep-related activities such as sleep-driving, cooking and eating food, and making phone calls while asleep has also been noted; amnesia may also occur. The use of alcohol, other CNS depressants, and exceeding the recommended maximum dose may increase the risk of these activities. Discontinue treatment in patients who report any sleep-related episodes.
Disease-related concerns:
- Depression: Use with caution in patients with depression; worsening of depression, including suicidal ideation has been reported with the use of hypnotics. Intentional overdose may be an issue in this population. The minimum dose that will effectively treat the individual patient should be used. Prescriptions should be written for the smallest quantity consistent with good patient care.
- Drug abuse: Use with caution in patients with a history of drug dependence.
- Hepatic impairment: Use with caution in patients with hepatic impairment; dosage adjustment required with severe impairment.
- Respiratory disease: Use with caution in patients with respiratory compromise, COPD or sleep apnea.
Concurrent drug therapy issues:
- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Special populations:
- Debilitated/Elderly: Use with caution in debilitated and elderly patients; dose adjustment recommended. Closely monitor for impaired cognitive and/or motor performance, confusion, and potential for falling.
Other warnings/precautions:
- Appropriate use: Symptomatic treatment of insomnia should be initiated only after careful evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric and/or medical illness.
- Duration of therapy: Tolerance, as assessed by sleep measurement, did not develop over 6 months of use.
- Rapid onset: Because of the rapid onset of action, administer immediately prior to bedtime or after the patient has gone to bed and is having difficulty falling asleep.
- Withdrawal: Abrupt discontinuance or rapid dose decreases may lead to withdrawal symptoms.
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Adverse effects were observed in animal reproduction studies. Eszopiclone is the S-isomer of the racemic derivative zopiclone. Available data related to zopiclone (not available in the United States) and similar medications note the potential for preterm birth, low birth weight, and/or small for gestational age infants following maternal use. Long-term use of medications in this class is not recommended during pregnancy and a planned discontinuation should be done to prevent rebound insomnia (Okun 2015).
May interact with GABA-receptor complexes at binding domains located close to or allosterically coupled to benzodiazepine receptors.
Rapid; high-fat/heavy meal may delay absorption
Hepatic via oxidation and demethylation (CYP2E1, 3A4); (S)-N-desmethyl zopiclone metabolite has less activity than parent compound
Urine (up to 75%, primarily as metabolites; <10% as parent drug)
~1 hour
~6 hours; Elderly ( ≥65 years): ~9 hours
52% to 59%
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience bad taste, dry mouth, headache, common cold symptoms, or fatigue. Have patient report immediately to prescriber signs of depression (suicidal ideation, anxiety, emotional instability, or illogical thinking), behavioral changes, hallucinations, memory impairment, severe dizziness, change in balance, confusion, severe loss of strength and energy, severe vomiting, or severe nausea (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.