USMLE

Zolpidem Zaleplon Eszopiclone

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Other Neuro Pharm
  1. Ramelteon
  2. Triptans
  3. Benzodiazepines - Function
  4. Zolpidem Zaleplon Eszopiclone
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Summary

Zolpidem, Zaleplon, and Eszopiclone are non-benzodiazepine hypnotics informally called the Z-drugs, which are used to treat insomnia. These drugs work by binding to and potentiating BZ1 receptors, a type of GABA receptor. The resulting GABA signalling induces sleep. Compared to traditional benzo drugs, these Z-drugs have a lower risk of dependence and less residual daytime effects.

Key Points

  • BZ1-GABA Hypnotics
    • Also known as the non-benzodiazepine hypnotics
    • Drug Names
      • Zolpidem, zaleplon, eszopiclone
    • Mechanism
      • Act via BZ1 subtype of the GABA receptor to increase frequency of chloride channel opening
        • Same binding site as benzodiazepines; effects also reversed by flumazenil
        • But chemically unrelated to benzos (hence, non-benzodiazepine)
    • Clinical Use
      • Insomnia
        • Sleep cycle less affected compared to benzodiazepine hypnotics
        • Short duration of action due to rapid metabolism by liver
        • Unlike older sedative-hypnotics, BZ1 hypnotics cause only modest day-after psychomotor depression and few amnestic effects
    • Adverse Effects
      • Lower dependence risk than benzodiazepines
      • May cause ataxia, headaches, confusion