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A. Types of Agents navigator

  1. Anti-Histamines
  2. Benzodiazepines
  3. Trazodone (Desyrel®) and Zolpidem (Ambien®)
  4. Neuroleptics: Phenothiazines and Butyrphenones
  5. Systemic Agents for Sedation / Anesthesia
    1. Opiates and derivatives - fentanyl for short duration, morphine for longer
    2. Ketamine - analgesia, sedation, amnesia, immobilization
    3. Propofol - ultrashort acting agent

B. Anti-Histamines navigator

  1. Combination of anihistamine and anticholinergic activities induce lethargy
  2. Diphenhydramine (Benadryl®): 25-50mg. qhs.
  3. Hydroxyzine (Atarax®): also for nausea, severe allergic reactions
  4. Caution in elderly patients who often have significant CNS effects and some tachycardia

C. Benzodiazepines navigator

  1. Diazepam (Valium®): 5-10mg. Long t1/2 ~40 hours
  2. Lorazepam (Ativan®): 2-5mg. Moderate t1/2 ~6 hours
  3. Midazolam (Versed®): 0.4mg/kg. Rapid onset, shorter t1/2 ~2 hours
  4. Quazepam (Doral®): 15mg. Receptor specificity, decreased rebound insomnia
  5. Triazolam (Halcion®): 0.25mg.
  6. Temazepam (Restoril®): 7.5mg
  7. Alprazolam (Xanax®): 0.5-2mg po qhs up to tid
  8. These agents should be avoided in patients with history of substance abuse [4]
  9. Benzodiazepine effects may be reversed using flumazenil (Romazicon®)
  10. Not generally recommended for chronic administration
  11. Withdrawal from benzodiazepine dependence is similar to alcohol withdrawal [5]

D. Phenothiazines and Butyrphenones navigator

  1. Should generally be avoided unless patient is psychotic or delirious
  2. Thioridazine (Mellaril®) - good agent in elderly persons in low doses (10mg qhs)
  3. Haloperidol (Haldol®) - high risk of acute dystonic reactions (add anticholinergic)

E. Other Agents navigator

  1. Zolpidem (Ambien®) [1]
    1. Imidazopyridine hypnotic agent binds to benzodiazapine receptor type 1 (BZ1)
    2. Well absorbed orally; dose is 10mg po qhs (5mg for elderly or hepatic disease)
    3. Well tolerated, especially in elderly with no evidence yet for addictive potential
    4. Minimal effect on stages of sleep
    5. Generally recommended instead of benzodiazepines
  2. Zaleplon (Sonata®) []
    1. Pyrazolopyridimine hypnotic for short term treatment of insomnia
    2. Binds to benzodiazepine receptors (Schedule 4 Controlled Substance)
    3. Rapid onset of action (amy be slightly faster than zolpidem)
    4. Shorter half life than zolpidem, with increased frequency of early awakening
    5. Usual dose is 10mg po qhs (reduce dose by 50% for elderly or hepatic impairment)
    6. Dose may be increased to 20mg qhs, but increased risk of transient visual halucinations
    7. Metabolized in part by CYP3A4 so caution with drugs that inhibit this enzyme
  3. Chloral Hydrate
    1. 250-500mg po qhs
    2. Well tolerated, minimal effects on sleep stages
    3. Rapid tolerance (3-4 days)
  4. Trazodone (Desyrel®)
    1. Little anti-depressant activity but excellent sleep agent
    2. Dose is 50-100mg (max 150mg) po qhs
    3. Avoid if bipolar disorder is present
    4. May cause priapism (~1/1000 men)
    5. Effective in most patients with no addictive potential
  5. Dexmedetomidine [6]
    1. Highly selective alpha2-adrenergic receptor agonist
    2. Acts on locus ceruleus and spinal cord
    3. Produces both sedation and analgesia
    4. Superior clinical results versus lorazepam in mechanically ventilated brain injury
    5. Reduced days of delirium or coma compared with lorazepam

References navigator

  1. Krauss B and Green SM. 2000. NEJM. 342(13):938 abstract
  2. Zolpidem. 1993. Med Let. 35(895):35 abstract
  3. Zaleplon. 1999. Med Let. 41(1063):93 abstract
  4. Acute Reactions to Drugs of Abuse. 2002. Med Let. 44(1125):21 abstract
  5. Kosten TR and O'Connor PG. 2003. NEJM. 348(18):1786 abstract
  6. Pandharipande PP, Pun BT, Herr DL, et al. 2007. JAMA. 298(22):2645