Partial Agonists at GABA Receptors

Partial Agonists at GABA_A Receptors

• Full GABA agonists (i.e., benzodiazepines) are effective anxiolytics

  • use is limited though by their potential for rebound anxiety, physical dependence, abuse potential, and side effects (i.e., ataxia, sedation, memory impairment, etc.)

• Partial agonists provide effective anxiolytics without the limiting side effects

  • Alpidem

    • Partial agonist of GABA₁ and GABA₃ receptors

    • More anxiolytic than full agonists, with less sedation and no interaction with EtOH

    • May induce hepatitis though

  • Etizolam

    • Potent anxiolytic

      • “lower incidence of side effects at comparable efficacy”

  • Imidazenil

  • Abecarnil

  • Bretazenil

Category: Pharmacology Notes