Eszopiclone

The mechanism of action of eszopiclone as a hypnotic is unclear; however, its effect could be related to its interaction with GABA-receptor complexes at binding domains located close to or allosterically coupled to benzodiazepine receptors.

• & USAGE Eszopiclone tablets are indicated for the treatment of insomnia. In controlled outpatient and sleep laboratory studies, eszopiclone tablets administered at bedtime decreased sleep latency and improved sleep maintenance.ICD-10: G47.00

• • Eszopiclonetablet is contraindicated in patients who have experienced complex sleep behaviors after taking eszopiclone tablets [see Warnings and Precautions (5.1) ]. • Eszopiclone tablet is contraindicated in patients with known hypersensitivity to eszopiclone.contraindicated

DOSAGE & ADMINISTRATION Use the lowest effective dose for the patient. • Use the lowest dose effective for the patient ( 2 ) • Recommended initial dose is 1 mg, immediately before bedtime, with at least 7 to 8 hours remaining before the planned time of awakening. May increase dose if clinically indicated, to a maximum of 3 mg ( 2.1 ) • Geriatric or debilitated patients: Dose should not exceed 2 mg ( 2.2 ) • Patients with severe hepatic impairment, or taking potent CYP3A4 inhibitors: Dose should not exceed 2 mg ( 2.3 ) • Do not take with or immediately after a meal ( 2.5 ) 2.1 Dosage in Adults The recommended starting dose is 1 mg. Dosing can be raised to 2 mg or 3 mg if clinically indicated. In some patients, the higher morning blood levels of eszopiclone tablets following use of the 2 mg or 3 mg dose increase the risk of next day impairment of driving and other activities that require full alertness [ see Warnings and Precautions (5.1) ]. The total dose of eszopiclone tablets should not exceed 3 mg, once daily immediately before bedtime [ see Warnings and Precautions (5.6) ]. 2.2 Geriatric or Debilitated Patients The total dose of eszopiclone tablets should not exceed 2 mg in elderly or debilitated patients. 2.3 Patients with Severe Hepatic Impairment, or Taking Potent CYP3A4 Inhibitors In patients with severe hepatic impairment, or in patients coadministered eszopiclone tablets with potent CYP3A4 inhibitors, the total dose of eszopiclone tablets should not exceed 2 mg [ see Warnings and Precautions (5.7) ].

• CNS Depressant Effects Impaired alertness and motor coordination, including risk of morning impairment. Risk increases with dose and use with other CNS depressants and alcohol. Caution patients taking 3 mg dose against driving and against activities requiring complete mental alertness during the morning after use. ( 5.2 ) • Evaluate for Comborbid Diagnoses Reevaluate if insomnia persists after 7 to 10 days of use ( 5.3 ) • Severe Anaphylactic/Anaphylactoid Reactions (angioedema and anaphylaxis have been reported): Do not rechallenge if such reactions occur ( 5.4 ) • Abnormal Thinking amd Behavioral Changes including decreased inhibition, bizarre behavior, agitation and depersonalization have been reported. Immediately evaluate any new onset of behavioral changes ( 5.5 ) • Worsening of Depression or Suicidal Thinking may occur: Prescribe the least number of tablets feasible to avoid intentional overdose ( 5.5 , 5.8 ) • Withdrawal Effects Symptoms may occur with rapid dose reduction or discontinuation ( 5.6 , 9.3 ) • Elderly Patients Use lower dose due to impaired motor, cognitive performance and increased sensitivity ( 2.2 , 5.8 ) • Patients with Hepatic Impairment, Impaired Respiratory Function, Impaired Drug Metabolism or Hemodynamic Responses Use with caution ( 5.8 ) 5.1 Complex Sleep Behaviours Complex sleepbehaviors including sleep-walking, sleep-driving, and engaging in other activities while not fully awake may occur following the first or any subsequent use of eszopiclone tablet. Patients can be seriously injured or injure others during complex sleep behaviors.

The following are described in more detail in the Warnings and Precautions section of the label: • Complex Sleep Behaviors [see Boxed Warning and Warnings and Precautions (5.1) ] • CNS Depressant Effects and Next-Day Impairment [see Warnings and Precautions (5.2) ] • Need to Evaluate for Comorbid Diagnoses [see Warnings and Precautions (5.3) ] • Severe Anaphylactic and Anaphylactoid Reactions [see Warnings and Precautions (5.4) ] • Abnormal Thinking and Behavioral Changes [see Warnings and Precautions (5.5) ] • Withdrawal Effects [see Warnings and Precautions (5.6) ] • Timing of Drug Administration [see Warnings and Precautions (5.7) ] • Special Populations [see Warnings and Precautions (5.8) ] Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The premarketing development program for eszopiclone tablets included eszopiclone exposures in patients and/or normal subjects from two different groups of studies: approximately 400 normal subjects in clinical pharmacology/pharmacokinetic studies, and approximately 1550 patients in placebo-controlled clinical effectiveness studies, corresponding to approximately 263 patient-exposure years.

• Pediatric Use Safety and effectiveness not established. Dizziness, dysgeusia, hallucinations, suicidal ideation reported ( 8.4 ) 8.1 Pregnancy Risk Summary Available pharmacovigilance data with eszopiclone use in pregnant women are insufficient to identify a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction studies conducted in pregnant rats and rabbits throughout organogenesis, there was no evidence of teratogenicity. Administration of eszopiclone to rats throughout pregnancy and lactation resulted in offspring toxicities at all doses tested; the lowest dose was approximately 200 times the maximum recommended human dose (MRHD) of 3 mg/day based on mg/m 2 body surface area (See Data). The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data Oral administration of eszopiclone to pregnant rats (62.5, 125, or 250 mg/kg/day) and rabbits (4, 8, or 16 mg/kg/day) throughout organogenesis showed no evidence of teratogenicity up to the highest doses tested.

Metabolism

The pharmacokinetics of eszopiclone have been investigated in healthy subjects (adult and elderly) and in patients with hepatic disease or renal disease. In healthy subjects, the pharmacokinetic profile was examined after single doses of up to 7.5 mg and after once-daily administration of 1, 3, and 6 mg for 7 days.

In clinical trials with eszopiclone, one case of overdose with up to 36 mg of eszopiclone was reported in which the subject fully recovered. Since commercial marketing began, spontaneous cases of eszopiclone overdoses up to 270 mg (90 times the maximum recommended dose of eszopiclone) have been reported, in which patients have recovered. Fatalities related to eszopiclone tablets overdoses were reported only in combination with other CNS drugs or alcohol. 10.1 Signs and Symptoms Signs and symptoms of overdose effects of CNS depressants can be expected to present as exaggerations of the pharmacological effects noted in preclinical testing. Impairment of consciousness ranging from somnolence to coma has been described. Rare individual instances of fatal outcomes following overdose with racemic zopiclone have been reported in European postmarketing reports, most often associated with overdose with other CNS-depressant agents. Methemoglobinemia in association with overdoses of racemic zopiclone has been reported. 10.2 Recommended Treatment General symptomatic and supportive measures should be used along with immediate gastric lavage where appropriate.

• Dec 15, 2004NDANDA021476Waylis Therap
• May 23, 2011ANDAANDA091169Teva
• Sep 13, 2011ANDAANDA091124Lupin Ltd
• Mar 26, 2013ANDAANDA091151Mylan Pharms Inc
• Apr 3, 2013ANDAANDA091103Sun Pharm
• Apr 15, 2014ANDAANDA091024Dr Reddys
• Apr 15, 2014ANDAANDA091166Glenmark Pharms Ltd
• Jun 10, 2014ANDAANDA091113Orbion Pharms

Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

• Eszopiclone, Tablet, 1 mg (NDC 0093-5537-56)To be discontinued
  Sponsor: Teva Pharmaceuticals USA, Inc.
  Updated Jun 26, 2025
• Eszopiclone, Tablet, 2 mg (NDC 0093-5538-01)To be discontinued
  Sponsor: Teva Pharmaceuticals USA, Inc.
  Updated Jun 26, 2025
• Eszopiclone, Tablet, 3 mg (NDC 0093-5539-01)To be discontinued
  Sponsor: Teva Pharmaceuticals USA, Inc.
  Updated Jun 26, 2025

1. 1Drug Ineffective4,84719%
2. 2Insomnia3,89116%
3. 3Dysgeusia3,85415%
4. 4Nausea1,4055.6%
5. 5Middle Insomnia1,2144.8%
6. 6Fatigue1,1974.8%
7. 7Headache1,1744.7%
8. 8Somnolence8863.5%
9. 9Dizziness8793.5%
10. 10Anxiety8603.4%
11. 11Initial Insomnia8563.4%
12. 12Pain8163.3%
13. 13Diarrhoea7603.0%
14. 14Depression7162.9%
15. 15Fall6572.6%

Recent PubMed references pinned to Eszopiclone as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Evidence-based pharmacological interventions for insomnia: a systematic review on the effects of eszopiclone on insomnia comorbid with mental disturbances.
  The world journal of biological psychiatry : the official journal of the World Federation of Societies of Biological Psychiatry · 2026 · Palagini L, Dell'Osso BM, Ferini Strambi L, et al.
  PMID 41840848DOI 10.1080/15622975.2026.2641481
• Evaluation of the stability and cross-reactivity of zopiclone and eszopiclone using immunoassay kits.
  The Journal of toxicological sciences · 2026 · Saito T, Namera A, Yamamoto R, et al.
  PMID 41765457DOI 10.2131/jts.51.173
• Suicide adverse events associated with zopiclone and eszopiclone: A pharmacovigilance analysis based on FAERS, JADER and CVARD.
  PloS one · 2026 · Xu Y, Li F, Zhang M, et al.
  PMID 41505484DOI 10.1371/journal.pone.0340357
• Cognitive Behavioral Therapy Alone or in Combination with Eszopiclone in Comorbid Insomnia and Obstructive Sleep Apnea in Veterans with Posttraumatic Stress Disorder: A Randomized Trial.
  The Psychiatric quarterly · 2025 · El-Solh AA, Lawson Y, Martinson A, et al.
  PMID 40202618DOI 10.1007/s11126-025-10143-9
• Comparative analysis of warm needle moxibustion and gua sha nursing care on sleep quality and psychological stress in insomnia patients undergoing eszopiclone tablet treatment: A retrospective study.
  Medicine · 2025 · Fan L, Wu C, Lu C, et al.
  PMID 39792767DOI 10.1097/MD.0000000000041025
• Z hypnotics in the management of narcolepsy: a case series.
  Journal of clinical sleep medicine : JCSM : official publication of the American Academy of Sleep Medicine · 2025 · Aboukasm A, Reffi AN, Drake CL, et al.
  PMID 39745471DOI 10.5664/jcsm.11546
• Combination Drug Therapy with Acetazolamide, Eszopiclone ± Venlafaxine for Obstructive Sleep Apnea (RESCUE-Combo): A Randomized, Double-Blind, Placebo-controlled Clinical Trial.
  Annals of the American Thoracic Society · 2025 · Schmickl CN, Orr JE, Alex RM, et al.
  PMID 39514000DOI 10.1513/AnnalsATS.202407-736OC
• Efficacy and safety of eszopiclone combined with drug therapy in the treatment of insomnia after stroke: A network meta-analysis and systematic review.
  PloS one · 2024 · Li RY, Zhu DL, Chen KY, et al.
  PMID 38315683DOI 10.1371/journal.pone.0297064

The 10 most recently updated of 76 ClinicalTrials.gov registrations naming Eszopiclone as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• National Adaptive Trial for PTSD Related Insomnia
  Completed · Phase 3 · Interventional · 673 enrolled · VA Office of Research and Development
  NCT03668041updated 2026-06-03
• Continuous Positive Airway Pressure, Arousability and Links to Mechanisms in Obstructive Sleep Apnea
  Recruiting · Phase 3 · Interventional · 250 enrolled · Yale University
  NCT07332442updated 2026-06-03
• Effect of Eszopiclone on Adherence to CPAP and Severity of Insomnia in Patients With COMISA
  Completed · Phase 4 · Interventional · 60 enrolled · University of Sao Paulo General Hospital
  NCT06017921updated 2026-05-29
• The Study in Outpatient Medicine Using Nudges to Improve Sleep
  Enrolling by invitation · Interventional · 444 enrolled · University of Southern California
  NCT06640023updated 2026-04-27
• Endotype-Targeted Therapy to Rescue OSA Patients Struggling With CPAP Adherence (TOP-CPAP)
  Completed · Phase 2 · Interventional · 42 enrolled · University of California, San Diego
  NCT05951023updated 2025-11-25
• Effectiveness of Combining Behavioral and Pharmacologic Therapy for Complex Insomnia in Veterans With PTSD
  Completed · Phase 4 · Interventional · 53 enrolled · VA Office of Research and Development
  NCT03937713updated 2025-10-21
• Endotypic Traits and Obstructive Sleep Apnea Surgery
  Recruiting · Phase 2 · Interventional · 150 enrolled · University of California, Los Angeles
  NCT05953610updated 2025-06-27
• Impact of Eszopiclone on Blood Pressure in Patients With Insomnia and Hypertension (PRYSMA-HTN)
  Recruiting · Phase 4 · Interventional · 150 enrolled · University of Sao Paulo
  NCT07018557updated 2025-06-12
• Grain Moxibustion Treatment on Insomnia: a Randomized Controlled Trial
  Not yet recruiting · Interventional · 102 enrolled · Shanghai Institute of Acupuncture, Moxibustion and Meridian
  NCT04980703updated 2025-05-14
• Effects of Eszopiclone and Lemborexant in People With OSA With a Low Arousal Threshold Who Have Difficulty Sleeping
  Not yet recruiting · Phase 2 · Interventional · 15 enrolled · Flinders University
  NCT06928766updated 2025-04-18

Frequently asked questions

How does Eszopiclone work?

The mechanism of action of eszopiclone as a hypnotic is unclear; however, its effect could be related to its interaction with GABA-receptor complexes at binding domains located close to or allosterically coupled to benzodiazepine receptors.

What is Eszopiclone used for?

According to FDA labeling, Eszopiclone carries indications including: & USAGE Eszopiclone tablets are indicated for the treatment of insomnia. In controlled outpatient and sleep laboratory studies, eszopiclone tablets administered at bedtime decreased sleep latency and improved sleep maintenance.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Eszopiclone?

Eszopiclone is classified as Benzodiazepine related drugs, Gamma Amino Butyric Acid (GABA) Activity Alteration.

What are the brand names for Eszopiclone?

Eszopiclone is marketed under brand names including Lunesta.

What are the contraindications for Eszopiclone?

Eszopiclone labeling lists contraindications including: • Eszopiclonetablet is contraindicated in patients who have experienced complex sleep behaviors after taking eszopiclone tablets [see Warnings and Precautions (5.1) ]. • Eszopiclone tablet is contraindicated in patients with known hypersensitivity to eszopiclone.. Always consult the full prescribing information and a clinician.