GABA-A agonist
GABA-A receptor agonist
- Directly opens GABA-A chloride channels rather than potentiating GABA
- No ceiling from endogenous GABA availability → profound CNS depression possible if BBB-crossing
- Sedation
- Anxiolysis
- Anticonvulsant effects
- Motor impairment / ataxia
- Respiratory depression
- Barbiturates at high concentrations
- OTC GABA supplements
- ➔ does not readily enter brain
- ➔ possible effect on peripheral GABA receptors
Drugs with this mechanism (2)
- Gamma-Aminobutyric Acid — The primary inhibitory neurotransmitter of the CNS.
- Taurine — Endogenous amino acid; a glycine/GABA-A modulator and common supplement.
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