Single and multiple dose kinetics of a new antiepileptic drug, Org 6370, and its desmethyl metabolite, Org 6363

The pharmacokinetic parameters of the new antiepileptic drug, Org 6370, and its desmethyl metabolite, Org 6363, were studied in healthy male volunteers. Plasma concentrations of the compounds were determined by a new method using liquid-solid extraction and capillary gas-chromatographic separation w...

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Bibliographic Details
Published inTherapeutic drug monitoring Vol. 8; no. 2; p. 140
Main Authors Kapetanovic, I M, Yonekawa, W D, Kupferberg, H J, Cos, L, Rollins, D E, Tolman, K G
Format Journal Article
LanguageEnglish
Published United States 01.01.1986
Subjects
Adult
Anticonvulsants - administration & dosage
Anticonvulsants - metabolism
Bridged Bicyclo Compounds - metabolism
Bridged Bicyclo Compounds - therapeutic use
Bridged-Ring Compounds - metabolism
Chromatography, Gas
Epilepsy - drug therapy
Half-Life
Humans
Kinetics
Male
Time Factors
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Summary:The pharmacokinetic parameters of the new antiepileptic drug, Org 6370, and its desmethyl metabolite, Org 6363, were studied in healthy male volunteers. Plasma concentrations of the compounds were determined by a new method using liquid-solid extraction and capillary gas-chromatographic separation with a nitrogen-selective detector. The kinetic parameters obtained after a single oral dose of Org 6370 were not good predictors of multiple-dose parameters. With long-term treatment, there was unanticipated accumulation of the parent drug and especially the metabolite. The clinical implication of these findings is that caution must be exercised in clinical trials of Org 6370.
ISSN:0163-4356
DOI:10.1097/00007691-198606000-00002