Possible Interaction: Leucine and Gabapentin

“… gabapentin significantly attenuated the rise in … 3 to 5 min between L and G; P<0.001 at 1 to 4 min and <0.05 at 5 min between L and ….001 at 1 to 2 min and <0.05 at 3 to 5 min between L and GL).”

“Although the neuroprotective mechanism of action of gabapentin is currently unknown, it is hypothesized here that gabapentin decreases the rate of formation of glutamate derived from the branched-chain amino acids (BCAAs) leucine , isoleucine, and valine.”

“4 Gabapentin and L‐leucine mutually inhibit their uptake.”

“At 100 μm, gabapentin significantly inhibited initial rate of uptake of [3H]‐glycine (29%), L‐[3H]‐glutamate (22%) and L‐[3H]‐leucine (40%).”

“The steady-state kinetic study in astrocytes and CHO cells indicates that the intracellular concentrations of gabapentin are about two to four times higher than that of leucine.”

“The presence of a submaximal concentration of leucine reduced [3H]gabapentin binding affinity but did not affect the maximum number of binding sites, suggesting a competitive interaction between leucine and the binding protein.”

“Pre-steady state kinetics show that 1.3 mm gabapentin can completely inhibit the binding of leucine to reduced hBCATc, whereas 65.4 mm gabapentin is required to inhibit leucine binding to hBCATm.”