Abstract
The concentration-time profile of [ 14C]gabapentin (GBP) in plasma and brain interstitial fluid (ISF) was determined following a single 15 mg/kg intravenous bolus dose to rats. Brain ISF was sampled with a microdialysis probe in striatum. Blood was also collected serially to 4 h postdose. At termination, brain was sectioned into regions and [ 14C]GBP concentrations were determined. Anticonvulsant effects were determined by maximal electroshock in rats with identical dosing. Plasma [ 14C]GBP declined linearly after dosing while brain ISF [ 14C]GBP concentration peaked at approximately 1 h and then declined in parallel with plasma concentration. Throughout, brain ISF [ 14C]GBP concentration was approximately 3–6% of [ 14C]GBP concentration in plasma. However, at 4 h postdose, whole brain tissue [ 14C]GBP concentration was equal to or greater than the concentration of [ 14C]GBP in plasma. Maximal anticonvulsant effect lagged behind both plasma and brain ISF GBP concentrations. The anticonvulsant effect of GBP is delayed by time-dependent events other than distribution from blood to brain.
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