Pharm

Lunesta

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Lunesta, Eszopiclone

  • 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
  • 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
  • Precaution
  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 and to start at 1 mg in all patients (similar to the 2013 Ambien warning)
  4. FDA Warning
    1. 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
  • Advantages
  • Disadvantages
  1. Expensive: Over $100 for 1 month supply