GABA-B agonist
GABA-B receptor agonist
- Gi-coupled → ↓ transmitter release and postsynaptic hyperpolarization
- Suppresses spinal reflexes → muscle relaxation
- Sedation
- Abrupt withdrawal → seizures
GABA-B agonist (1/2)
- Spinal reflex suppression → muscle relaxation / antispasticity
- Improved sleep architecture
- ➔ oxybate
- CNS depression → potential coma in overdose
- ➔ may produce EEG burst suppression mimicking brain death
- Analgesic effects
GABA-B agonist (2/2)
- May ↑ appetite
- ➔ agitation, delirium, autonomic instability, seizures
Drugs with this mechanism (5)
- Baclofen — GABA-B agonist muscle relaxant; studied for alcohol craving.
- Gamma-Aminobutyric Acid — The primary inhibitory neurotransmitter of the CNS.
- GHB (Oxybate) — Oxybate GHB/GABA-B agonist for narcolepsy; powerful respiratory depressant with abuse risk.
- Phenibut — GABA-B agonist nootropic sold online; tolerance and severe withdrawal.
- Mixed-salt oxybates — Lower-sodium mixed oxybate for narcolepsy and idiopathic hypersomnia; dispensed under a REMS.
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