Toggle Main Menu Toggle Search

Open Access padlockePrints

Comparative anticonvulsant potency and pharmacokinetics of (+)- and (−)-enantiomers of stiripentol

Lookup NU author(s): Professor Alan Boddy


Full text for this publication is not currently held within this repository. Alternative links are provided below where available.


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.

Publication metadata

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

Year: 1992

Volume: 12

Issue: 1

Pages: 29-36

Print publication date: 01/06/1992

ISSN (print): 0920-1211

ISSN (electronic): 1872-6844


DOI: 10.1016/0920-1211(92)90088-B


Altmetrics provided by Altmetric