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Lookup NU author(s): Professor Alan Boddy
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The anticonvulsant potency and pharmacokinetics of the enantiomers of stiripentol were compared using the intravenous pentyl-enetetrazol infusion seizure model in the rat. Enantioselectivity was observed with respect to both the anticonvulsant activity and elimination kinetics of this compound. (+)-Stiripentol was 2.4 times more potent than its antipode against pentylenetetrazol-induced clonic seizure (brain EC50 of 15.2-mu-g/ml versus 36.1-mu-g/ml). The (+)-enantiomer was eliminated more rapidly than the (-)-enantiomer, as reflected in a higher plasma clearance (1.64 l/h/kg versus 0.557 1/h/kg) and a shorter half-life (2.83 h versus 6.50 h). Parallel studies with the racemate of stiripentol indicated that the anticonvulsant potency of the racemate was between the potency of the two enantiomers, suggesting that the combined activity reflects the additive action of (+)- and (-)-stiripentol. However, a marked metabolic interaction between enantiomers was evident after racemate administration. These results point to the need for information on the differential pharmacokinetics of stiripentol enantiomers following racemic drug administration.
Author(s): Shen, D. D., Levy, R. H., Savitch, J. L., Boddy, A. V., Tombret, F., Lepage, F.
Publication type: Article
Publication status: Published
Journal: Epilepsy Research
Print publication date: 01/06/1992
ISSN (print): 0920-1211
ISSN (electronic): 1872-6844
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