Possible Interaction: Gamma-Aminobutyric Acid and Pregabalin

“A deficiency of gamma‐aminobutyric acid (GABA) has been described in the cerebellum in CCA, and pregabalin has been shown to enhance GABA release in rat hippocampus.”

“The preclinical studies indicated that pregabalin possesses modulatory effects on the GABA and glutamate systems, leaving room for an abuse potential.”

“ Pregabalin , a GABA analogue, presumably interacts with brain glutamate and GABA neurotransmission.”

“Valproate, gabapentin, pregabalin , and vigabatrin increase brain GABA levels or neurotransmission at least in part by targeting the metabolic pathways of GABA.”

“Exocytotic release of [3H]GABA from synaptosomes decreased in the presence of FGABAs 1-3 and pregabalin , and the effects of FGABAs 1 &3 were more significant than those of FGABAs 2 and pregabalin.”

“Recently, we have shown that … acid (GABA), bioisosters of pregabalin (β-i-Bu-GABA), i.e. β-polyfluoroalkyl-GABAs (FGABAs), with substituents: β-… (2); β-CF2CF2H (3), are able to increase the initial rate of [3H]GABA uptake by isolated rat brain nerve … is higher than that of pregabalin.”

“Prolonged incubation of hippocampal cultures, which endogenously express GAT1, with gabapentin and pregabalin caused a 2-fold increase in subsequent GABA uptake, which was concentration- and time-dependent.”