Alpha-2-delta modulator
Voltage-gated calcium channel alpha-2-delta subunit modulator
- ↓ trafficking of voltage-gated Ca²⁺ channels to synapses
- ↓ glutamate release → ↓ neuropathic pain, seizures, anxiety
- Sedation, dizziness, peripheral edema, weight gain
- Dependence and misuse; withdrawal on abrupt stop
- Not “blocker”
- ↓ Ca²⁺ channel trafficking toward synapse → ↓ glutamate release
Drugs with this mechanism (4)
- Gabapentin — Renally cleared alpha-2-delta ligand for neuralgia and seizures; sedation and misuse.
- Gabapentin ER — Gastroretentive once-daily gabapentin for postherpetic neuralgia; take with the evening meal.
- Phenibut — GABA-B agonist nootropic sold online; tolerance and severe withdrawal.
- Pregabalin — Linear-kinetic alpha-2-delta ligand for neuropathic pain; edema, sedation and misuse.
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