Possible Interaction: Gamma-Aminobutyric Acid and Gabapentin

“ Gabapentin is an antiepileptic drug that increases the synthesis and release of GABA.”

“ GABA rose 48% at 6 hours with gabapentin but not with lamotrigine.”

“With long-term dosing and once target doses were achieved at 4 weeks, significant elevations in GABA were observed compared with baseline for all three drugs (topiramate 46%, gabapentin 25%, lamotrigine 25%).”

“OBJECTIVE Gabapentin is an antiepileptic drug of new generation that increases brain GABA levels.”

“ GABA was elevated in patients taking gabapentin compared with 14 complex partial epilepsy patients, matched for antiepileptic drug treatment.”

“ Gabapentin appears to increase human brain GABA levels.”

“We and others demonstrated that gabapentin inhibits presynaptic GABA release and induces glutamate release from astrocytes in the locus coeruleus (LC), thereby increasing LC neuron activity and spinal noradrenaline release, and that gabapentin relies on this action in the LC for its analgesia.”

“ GABA and NMDA receptors are also involved in the antinociceptive actions of gabapentin and ketamine, respectively.”

“ Gabapentin , designed as a precursor of GABA easily entering the brain, was shown to increase brain synaptic GABA.”

“This transporter-mediated GABA release is enhanced by the anticonvulsants gabapentin and vigabatrin.”

“ Gabapentin significantly increased GABA concentrations by 13% (P<0.02) in human neocortical slices made from tissue resected during epilepsy surgery.”

“These results confirm our MRS studies in vivo that gabapentin increases GABA levels in epileptic patients, but has minimal or no effect in a healthy rodent model.”

“ Gabapentin increases the concentration and probably the rate of synthesis of GABA in brain, which may enhance non-vesicular GABA release during seizures.”