Brain regional pharmacokinetics of 11C-labeled diphenylhydantoin: positron emission tomography in humans.

We used positron emission tomography to study the regional cerebral pharmacokinetics of 11C-labeled diphenylhydantoin (11C-DPH), which was given intravenously to 10 patients (8 intractable partial epileptics and 2 nonepileptics). In the nonaffected hemisphere, 11C-DPH concentration in gray matter reached equilibrium with blood within 20 minutes but was still rising at 60 minutes in white matter, where equilibrium was too slow to be detected owing to the fast physical decay of 11C. Brain-blood concentration ratios at 50 minutes were 1.37 and 1.06 in gray and white matter, respectively, similar but less variable than steady-state DPH ratios reported in human brain surgical samples. There was no indication that normal brain regions of medically resistant epileptics bind DPH less effectively than in nonepileptic patients. Brain and blood 11C-DPH concentrations were well correlated, confirming that the latter gives a reliable estimate of the former in unaffected brain regions.