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- W2011056884 abstract "PurposeData on the blood pharmacokinetics of vigabatrin, an antiepileptic drug with a unique and novel mechanism of action, in the rat are sparse. Additionally, little is known of the kinetics of vigabatrin in the central cerebrospinal fluid (CSF) compartment. We therefore investigated the rate of penetration into and the inter-relationship between serum and CSF compartments following systemic administration of vigabatrin in the rat.MethodsSprague–Dawley rats were implanted with a jugular vein catheter and a cisterna magna catheter for blood and CSF sampling, respectively. Vigabatrin was administered by intraperitonial injection at three different doses (250, 500 and 1000 mg/kg) and blood and CSF collected at timed intervals up to 8 h. Vigabatrin concentrations in sera and CSF were determined by high performance liquid chromatography.ResultsVigabatrin concentrations in blood and CSF rose linearly and dose-dependently and the time to maximum concentration (Tmax) was 0.4 and 1.0 h, respectively. Vigabatrin is not protein bound in serum and its elimination from serum (mean t1/2 values, 1.1–1.4 h) is rapid and dose-independent. The efflux of vigabatrin from CSF was significantly slower than that seen for serum (mean t1/2 values, 2.2–3.3 h).ConclusionsThe kinetics of vigabatrin are linear with rapid entry into CSF. However, although vigabatrin CSF kinetics parallel that seen in serum, CSF vigabatrin concentrations represent only 2% of concentrations seen in serum and do not reflect free drug concentrations in serum." @default.
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- W2011056884 date "2007-01-01" @default.
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- W2011056884 title "The pharmacokinetics of vigabatrin in rat blood and cerebrospinal fluid" @default.
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- W2011056884 doi "https://doi.org/10.1016/j.seizure.2006.10.003" @default.
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