Medical Pharmacology: Sedative Hypnotics Drugs

Medical Pharmacology Chapter 12: Anxiolytics and Sedative-Hypnotics

Pharmacological hypnosis: major drugs /drug classes
- Introduction
  - If non-pharmacological treatment of insomnia (such as moderate exercise) is not effective, drugs may have to be used.
  - Untreated chronic insomnia may have many adverse effects including a four-fold increase in serious accidents.
  - In addition to use of pharmacological agents, management of insomnia should include (a) a search for an underlying cause, elimination of "performance anxiety" related to falling asleep, adjusting the patient's biological clock such that sleepiness corresponds to the time of attempted sleep, and suppression of the use of alcohol or over-the-counter sleep aids
- Ethanol
  - Ethanol should not be used to manage insomnia because of numerous adverse effects.
    - For insomnia, despite reducing sleep latency, it may cause sleep fragmentation.
- Barbiturates and non-barbiturates for hypnosis
  - Barbiturates and non-barbiturates such as meprobamate have been used in the past for pharmacological hypnosis.
  - However, these drugs should be avoided:
    - Liabilities associated with barbiturate use include abuse potential, physical potentially life-threatening withdrawal reactions, dependence, and life-threatening toxicity with overdosage.
- Benzodiazepines
  - Hypnotics that act at benzodiazepine receptors and newer agents such as zolpidem (Ambien) are preferable to barbiturates because of:
    - Greater therapeutic index, less disruption of sleep patterns and less danger of overdosage toxicity.
  - In the absence of daytime anxiety benzodiazepines with short half-lives (no active metabolites or only short-acting metabolites) are preferable.
  - Triazolam (Halcion) is an example of a short-acting agent that has been used as a hypnotic.
    - Short acting benzodiazepines may, however cause amnesia, early morning awakening, rebound daytime anxiety
  - Some patients who have insomnia also have daytime anxiety.
    - To manage those patients a longer-acting benzodiazepine may be appropriate.
      - Use of these agents may result in: next-day cognitive impairment or delayed cognitive impairment as metabolites accumulate

Hobbs, W.R, Rall, T.W., and Verdoorn, T.A., Hypnotics and Sedatives: Ethanol In, Goodman and Gillman's The Pharmacologial Basis of Therapeutics,(Hardman, J.G, Limbird, L.E, Molinoff, P.B., Ruddon, R.W, and Gilman, A.G.,eds) TheMcGraw-Hill Companies, Inc.,1996, pp. 385-386.

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