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The Pharmacology and Mechanisms of Action of New Generation, Non-Benzodiazepine Hypnotic Agents

CNS Drugs volume 18, pages 9–15 (2004)Cite this article

Abstract

The new generation hypnotic drugs, zolpidem, zopiclone and zaleplon, are at least as efficacious in the clinic as benzodiazepines and may offer advantages in terms of safety. These drugs act through the BZ binding sites associated with GABAA receptors, but show some differences from benzodiazepines in pharmacological effects and mechanisms of action. Of particular interest is the finding that zolpidem shows a wide separation between doses producing sedative effects and those giving rise to other behavioural actions, and induces less tolerance and dependence than benzodiazepines. Zolpidem also demonstrates selectivity for GABAA receptors containing α1 subunits. Recent studies using genetically modified mice have confirmed that receptors containing alpha1 subunits play a particularly important role in mediating sedative activity, thus providing an explanation for the pharmacological profile of zolpidem.

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  1. Sanofi-Synthelabo Research, 31 Avenue Paul-Vaillaint Couturier, 92220, Bagneux, Paris, France

    David J. Sanger

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  1. David J. Sanger
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Correspondence to David J. Sanger.

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Sanger, D.J. The Pharmacology and Mechanisms of Action of New Generation, Non-Benzodiazepine Hypnotic Agents. CNS Drugs 18, 9–15 (2004). https://doi.org/10.2165/00023210-200418001-00004

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  • DOI: https://doi.org/10.2165/00023210-200418001-00004

Keywords

  • GABAA Receptor
  • Zolpidem
  • Flumazenil
  • Sedative Effect
  • Zopiclone