Gabapentin has come into clinical use as adjunctive therapy in the tre
atment of epilepsy. Designed to mimic gamma-aminobutyric acid (GABA),
its mechanism of action remains elusive. In vivo measurements of GABA
in human brain were made using H-1 magnetic resonance spectroscopy. We
used a 2.1-T magnetic resonance imager-spectrometer and an 8-cm surfa
ce coil to measure a 13.5-cm(3) volume in the occipital cortex. GABA l
evels were measured in 14 patients enrolled in an open-label trial of
gabapentin. GABA was elevated in patients taking gabapentin compared w
ith 14 complex partial epilepsy patients, matched for antiepileptic dr
ug treatment. Brain GABA levels appeared to be higher in patients taki
ng high-dose gabapentin (3,300-3,600 mg/day) than in those taking stan
dard doses (1,200-2,400 mg/day). Gabapentin appears to increase human
brain GABA levels.