Gabapentin

Category: pharmacological

Aliases: Neurontin

Pharmacological Mechanism

α2δ subunit of voltage-gated Ca²⁺ channels — reduces excitatory neurotransmitter release. Used for neuropathic pain + adjunctive seizure therapy + RLS. Renally cleared; no CYP. Dose-dependent absorption (saturable LAT1) — high-dose AUC plateaus.

Half-Life (t½)

PO: 6h

Dosing Guidelines

• PO: Typical 600 mg (Range: 100–1200 mg)

Target Organ Systems

• nervous

Pathways It Modulates

• Metabotropic glutamate receptors (inhibitor) — α2δ Ca channel → ↓glutamate release
• Voltage-gated calcium channels (inhibitor) — α2δ-1 subunit (presynaptic Ca channel)

Chemical Identifiers

• PubChem CID: 3446
• Formula: C9H17NO2
• Molecular weight: 171.24 g/mol
• InChIKey: UGJMXCAKCUNAIE-UHFFFAOYSA-N
• SMILES: C1CCC(CC1)(CC(=O)O)CN

References

• PMID 8022536