Mental Health Book


Benzodiazepine Receptor Agonist

Aka: Benzodiazepine Receptor Agonist, Nonbenzodiazepine Sedative-Hypnotic, Nonbenzodiazepine Hypnotic Agent, Z-Drug
  1. See Also
    1. Insomnia
  2. Preparations
    1. Zolpidem (Ambien) or Zolpidem CR
    2. Zaleplon (Sonata)
    3. Eszopiclone (Lunesta)
  3. Adverse Effects
    1. Headache
    2. Dizziness
    3. Nausea
  4. Precautions
    1. Avoid in over age 65 years old (See Beers List)
    2. These agents have a duration of effect that extends past the time patients awaken
    3. Long acting agents (e.g. Eszopiclone or Lunesta)
      1. Full dose can impair driving, coordination and memory for up to 11 hours
    4. Since 2013 FDA has moved to lower the maximum doses in women and older patients
      1. Also cautioned about the hang over effect in all patients
    5. FDA Block Box Warning (2019, unusual and potentially dangerous sleep behaviors while on Z-Drugs)
      2. Rare but serious injuries and deaths related to falls, automobile accidents, Medication Overdoses
    6. FDA Warnings (complete list for Z-Drugs)
  5. Pharmacokinetics
    1. All are metabolized by CYP450 3A4
  6. Drug Interactions
    1. Alcohol and other CNS Depressants have additive effect
    2. Narcotic concurrent use may cause excess sedation
  7. Advantages
    1. Less Anticholinergic affect than other hypnotics
    2. Low addictive potential compared with Benzodiazepines
    3. Minimal effect on Sleep Stages
    4. Lack of withdrawal side effects
    5. No rebound Insomnia
    6. Little or no tolerance, effective to 1 year
  8. Disadvantages
    1. Non-pharmacologic therapy for Insomnia (e.g. CBT-I) has better longterm outcomes

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