The Sound of Evolution
Gabapentin
Mechanism of action:
Gabapentin is a structural analog of γ-aminobutyric acid (GABA). Gabapentin binds with high affinity to the α₂δ-1 and α₂δ-2 subunits of voltage-gated Ca²⁺ channels. These subunits are mainly located on presynaptic neurons in the central and peripheral nervous systems. During neuronal depolarization, gabapentin reduces calcium influx through calcium channels, suppresses neurotransmitter release, and decreases excessive neuronal firing and synaptic transmission of pain-related signals.
Reference(s):
1. Yagi T et al. (2012). Impact of concomitant antacid administration on gabapentin plasma exposure and oral bioavailability in healthy adult subjects. Drug Metab Pharmacokinet.
2. Czapinski P et al. (2005). Mechanisms of action of antiepileptic drugs. Curr Top Med Chem.
3. Patsalos PN et al. (2008). Antiepileptic drugs--best practice guidelines for therapeutic drug monitoring: a position paper by the subcommission on therapeutic drug monitoring, ILAE Commission on Therapeutic Strategies. Epilepsia.