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Eszopiclone

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Eszopiclone, Lunesta

  • See Also
  1. Insomnia
  2. Benzodiazepine Receptor Agonist
  • Mechanism
  1. Nonbenzodiazepine Hypnotic Agent (Benzodiazepine Receptor Agonist)
  2. Acts at Gamma-Aminobutyric Acid receptors
  3. Isomer of Zopiclone (Imovane)
  4. Schedule IV Controlled Substance
  • Indication
  1. Insomnia
  • Dosing
  1. Starting dose: 1 mg orally at bedtime
  2. Maximum dosing of 1 mg indications
    1. Severe liver disease
    2. Concurrent use of CYP 3A4 inhibitor
  3. Maximum dosing of 2 mg indications
    1. Older patients (age over 65 years old): 1 mg
  4. Maximum of 3 mg indications
    1. Younger, healthy patients
  • Precautions
  1. These agents have a duration of effect that extends past the time patients awaken
  2. Eszopiclone (Lunesta) at 3 mg dose can impair driving, coordination and memory for up to 11 hours
  3. In 2014 FDA released a safety warning to limit maximum dosing of Lunesta
    1. Start at 1 mg in all patients (similar to the 2013 Ambien warning)
    2. http://www.fda.gov/Drugs/DrugSafety/ucm397260.htm
  • Pharmacokinetics
  1. Onset of action: 10-18 minutes
  2. Half-Life: 4-6 hours (5-7 hours in some reviews)
  3. Duration of action: 6-8 hours
  4. Metabolism: CYP450 3A4
  5. Delayed activity if taken after a fatty meal
  • Adverse effects
  1. Nonbenzodiazepine Hypnotic Agent for common effects
  2. Metallic Taste
    1. Reported in up to 34% of patients on 3 mg
    2. Very bothersome - discontinuation is common
  3. Amnesia
  4. Hallucinations
  5. Worsening depression
  • Resources
  1. Eszopiclone (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=fd047b2b-05a6-4d99-95cb-955f14bf329f
  • References
  1. (2005) Med Lett Drugs Ther 47:17-9 [PubMed]
  2. Wessel (2005) Am Fam Physician 71(12):2359-60 [PubMed]