Version May 2024
Complex sleep behaviors, including sleep-walking, sleep-driving, and engaging in other activities while not fully awake, may occur following use of eszopiclone. Some of these events may result in serious injuries, including death. Discontinue eszopiclone immediately if a patient experiences a complex sleep behavior.
Insomnia, sleep onset or sleep maintenance:
Note: Limit long-term use (>4 weeks) to cases for which nonpharmacologic treatments are not available or not effective and benefits are felt to outweigh risks (Ref).
Oral: Initial: 1 mg once daily immediately before bedtime, as needed; may increase to 2 or 3 mg based on response and tolerability (maximum dose: 3 mg/day).
Discontinuation of therapy: Reduce by ~25% of the original dose each week or every other week (eszopiclone can be reduced by 1 mg each week or every other week). For patients taking higher doses of eszopiclone (eg, 3 mg/day) for an extended period, tapering eszopiclone even more slowly in conjunction with cognitive behavioral therapy for insomnia is encouraged (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
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.
Avoid use (Ref).
Insomnia, sleep onset or sleep maintenance: Oral: Initial: 1 mg once daily immediately before bedtime, as needed; may increase to 2 mg based on response and tolerability (maximum dose: 2 mg/day).
Discontinuation of therapy: Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>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%, postmarketing, and/or case reports: Abnormal gait, abnormality in thinking, agitation, alopecia, altered sense of smell, amenorrhea, anaphylaxis, anemia, angioedema, anorexia, apathy, aphthous stomatitis, arthritis, asthma, ataxia, blepharoptosis, breast hypertrophy, breast neoplasm, bronchitis, bursitis, cholelithiasis, colitis, complex sleep-related disorder, conjunctivitis, contact dermatitis, cystitis, dehydration, diaphoresis, dry eye syndrome, dysphagia, dyspnea, dysuria, eczema, emotional lability, epistaxis, erythema multiforme, euphoria, facial edema, fever, gastric ulcer, gastritis, gout, halitosis, heatstroke, heavy menstrual bleeding, hematuria, hepatic disease, hepatitis, hepatomegaly, herpes zoster infection, hirsutism, hostility, hypercholesterolemia, hypersensitivity reaction, hypertension, hypokalemia, hyporeflexia, increased appetite, increased thirst, insomnia, laryngitis, lymphadenopathy, maculopapular rash, malaise, mastalgia, mastitis, melena, memory impairment, myasthenia, mydriasis, myopathy, neck stiffness, nephrolithiasis, neuritis, neuropathy, neurosis, nystagmus disorder, oliguria, paresthesia, photophobia, pyelonephritis, rectal hemorrhage, renal pain, skin discoloration, skin photosensitivity, swelling, thrombophlebitis, tinnitus, tongue edema, tremor, twitching, urethritis, urinary frequency, urinary incontinence, urticaria, uterine hemorrhage, vaginal hemorrhage, vaginitis, vertigo, vesiculobullous dermatitis, vestibular disturbance
Hypersensitivity to eszopiclone or any component of the formulation; patients who have experienced complex sleep behaviors after taking eszopiclone.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to zopiclone; myasthenia gravis; severe respiratory impairment (eg, significant sleep apnea syndrome); older adults with severe hepatic impairment or receiving concomitant potent CYP3A4 inhibitors.
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
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. Amnesia and other neuropsychiatric symptoms 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 or 3 mg), even if used as prescribed; caution patients taking 3 mg about performing tasks that require mental alertness (eg, operating machinery, driving) the day after use. The risk of next-day psychomotor impairment is increased if taken with less than a full night of sleep (7 to 8 hours); if a higher than recommended dose is taken; or if coadministered 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.
• Complex sleep behaviors: [US Boxed Warning]: Complex sleep behaviors, including sleep-walking, sleep-driving, and engaging in other activities while not fully awake, may occur following the use of eszopiclone. Some of these events may result in serious injuries, including death. Other complex sleep behaviors (eg, preparing and eating food, making phone calls, having sex) while asleep have also been reported. Patients usually do not remember these events. May occur with first use and at recommended dosages with or without the use of alcohol or other CNS depressants. Discontinue immediately if a patient experiences a complex sleep behavior; use is contraindicated in patients who have experienced these events.
• 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.
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.
Special populations:
• Debilitated: Use with caution in debilitated patients; increased risk of impaired cognitive and/or motor performance. Dose adjustment recommended; monitor closely.
• Older adult: Increased risk of impaired cognitive and/or motor performance and falls; monitor closely.
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.
• Rebound insomnia: Following withdrawal of therapy, transient insomnia may recur accompanied by other reactions, including restlessness, anxiety, and mood changes.
• Withdrawal: A longer sleep-onset latency and increased awakenings during sleep may occur for 1 to 2 days following the discontinuation of GABA-mediated (GABAergic) medications. A more severe withdrawal syndrome may rarely occur following abrupt discontinuation or large decreases in dose after sustained use, and is characterized by abdominal pain, anxiety, confusion, delirium, disorientation, euphoria, hypertension, insomnia, irritability, restlessness, speech difficulties, seizures, and tremor. This withdrawal syndrome is generally mild and infrequent and resolves within weeks or upon re-initiation of the GABAergic medication. Intermittent dosing may reduce the risk of withdrawal symptoms (BAP [Wilson 2019]; Schifano 2019).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Lunesta: 1 mg [contains fd&c blue #2 (indigotine,indigo carmine)]
Lunesta: 2 mg
Lunesta: 3 mg [contains fd&c blue #2 (indigotine,indigo carmine)]
Generic: 1 mg, 2 mg, 3 mg
Yes
Tablets (Eszopiclone Oral)
1 mg (per each): $11.66 - $12.16
2 mg (per each): $11.66 - $12.16
3 mg (per each): $11.66 - $12.16
Tablets (Lunesta Oral)
1 mg (per each): $36.58
2 mg (per each): $36.58
3 mg (per each): $36.58
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Lunesta: 1 mg [contains fd&c blue #2 (indigotine,indigo carmine)]
Lunesta: 2 mg
Lunesta: 3 mg [contains fd&c blue #2 (indigotine,indigo carmine)]
C-IV
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).
An FDA-approved patient medication guide, which is available with the product information and at https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021476s038lbl.pdf#page=26, must be dispensed with this medication.
Insomnia, sleep onset or sleep maintenance: Treatment of insomnia.
Lunesta may be confused with Neulasta
Beers Criteria: Eszopiclone, a nonbenzodiazepine benzodiazepine-receptor agonist hypnotic, is identified in the Beers Criteria as a potentially inappropriate medication to be avoided in patients 65 years and older (independent of diagnosis or condition) due to adverse events similar to benzodiazepines in older adults (eg, delirium, falls, fractures) and an increase in emergency room visits, hospitalizations, and motor vehicle crashes. In addition, improvement in sleep latency and duration is minimal (Beers Criteria [AGS 2023]).
Substrate of CYP2E1 (minor), CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider therapy modification
Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Risk C: Monitor therapy
Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Bromopride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
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 at lower doses in patients already receiving CNS depressants. Risk D: Consider therapy modification
Cannabinoid-Containing Products: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products. Risk C: Monitor therapy
Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider therapy modification
Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of Eszopiclone. Risk C: Monitor therapy
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Eszopiclone. Risk C: 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). Risk D: Consider therapy modification
Daridorexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification
DexmedeTOMIDine: CNS Depressants may enhance the CNS depressant effect of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider therapy modification
Difelikefalin: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Doxylamine: CNS Depressants may enhance the CNS depressant effect of Doxylamine. Risk C: Monitor therapy
DroPERidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
Esketamine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. Risk X: Avoid combination
Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider therapy modification
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider therapy modification
Ixabepilone: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Kava Kava: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Kratom: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider therapy modification
Lisuride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Melatonin: May enhance the sedative effect of Hypnotics (Nonbenzodiazepine). Risk C: 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 the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider therapy modification
Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy
Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Olopatadine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification
Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination
Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Oxybate Salt Products: Hypnotics (Nonbenzodiazepine) may enhance the CNS depressant effect of Oxybate Salt Products. Risk X: Avoid combination
OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification
Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination
Perampanel: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy
Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy
Procarbazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Ropeginterferon Alfa-2b: CNS Depressants may enhance the adverse/toxic effect of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider therapy modification
ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy
Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy
Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy
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. Risk D: Consider therapy modification
Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination
Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Valerian: May enhance the CNS depressant effect of CNS Depressants. Risk C: 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. Risk D: Consider therapy modification
Zuranolone: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider therapy modification
Onset of action may be reduced if taken with or immediately after a heavy meal. Management: Take immediately prior to bedtime, not with or immediately after a heavy or high-fat meal.
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).
It is not known if eszopiclone is present in breast milk.
Eszopiclone is the S-isomer of the racemic derivative zopiclone. Zopiclone is excreted in human milk (Matheson 1990).
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.
Avoid taking after a heavy meal; may delay onset.
May interact with GABA-receptor complexes at binding domains located close to or allosterically coupled to benzodiazepine receptors.
Absorption: Rapid; high-fat/heavy meal may delay absorption
Protein binding: 52% to 59%
Metabolism: Hepatic via oxidation and demethylation (CYP2E1, 3A4); (S)-N-desmethyl zopiclone metabolite has less activity than parent compound
Half-life elimination: ~6 hours; Elderly (≥65 years): ~9 hours
Time to peak, plasma: ~1 hour
Excretion: Urine (up to 75%, primarily as metabolites; <10% as parent drug)
Hepatic function impairment: Systemic exposure is doubled in severe hepatic impairment with no change in Cmax or Tmax.
Older adult: Subjects ≥65 years of age had a 41% increase in total exposure (AUC) and a 50% increase in elimination half-life.
آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟
