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Chiral aspects of the human metabolism of ethosuximide

✍ Scribed by J. S. Millership; J. Mifsud; D. Galea; W. C. McRoberts; J. T. G. Hamilton

Publisher
John Wiley and Sons
Year
2005
Tongue
English
Weight
121 KB
Volume
26
Category
Article
ISSN
0142-2782

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✦ Synopsis

Abstract

Ethosuximide is a chiral drug substance primarily indicated for the treatment of absence seizures. This drug is used clinically as the racemate. The human urinary metabolites of ethosuximide (I) have been studied using chiral gas chromatography (GC) and gas chromatography/mass spectrometry (GC/MS). The metabolites identified were the previously reported unchanged ethosuximide (I) enantiomers, all four stereoisomers of 2‐(1‐hydroxyethyl)‐2‐methylsuccinimide (II), and the four stereoisomers of 2‐ethyl‐3‐hydroxy‐2‐methylsuccinimide (III). Through chemical derivatization methodology and GC/MS (using electron impact ionization [EI] and chemical ionization [CI] techniques) two enantiomers of a previously unreported metabolite of ethosuximide, 2‐ethyl‐2‐hydroxymethylsuccinimide (VI), have been identified. Copyright © 2005 John Wiley & Sons, Ltd.

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