GABA-A agonist

GABA-A receptor agonist

GABA-A receptor agonist — mechanism peg (Ballicules) — GABA-A agonist — mechanism card

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 — Primary inhibitory CNS neurotransmitter.
Taurine — Endogenous amino acid; a glycine/GABA-A modulator and common supplement.

Self-check

Does direct GABA-A agonism merely potentiate existing GABA?
No; it directly opens chloride channels.
What permits profound CNS depression with a BBB-crossing direct GABA-A agonist?
No ceiling from endogenous GABA availability.

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