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Severe overdosage with the antiepileptic drug oxcarbazepine
Author(s) -
Van Opstal J. M.,
Janknegt R.,
Cilissen J.,
L’Ortije W. H. V. M.,
Nel J. E.,
De Heer F.
Publication year - 2004
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.2004.02129.x
Subject(s) - oxcarbazepine , prodrug , pharmacology , active metabolite , antiepileptic drug , metabolite , toxicity , drug , medicine , anticonvulsant , pharmacokinetics , epilepsy , carbamazepine , psychiatry
Few published human data are available concerning the acute toxicity of the new antiepileptic drug oxcarbazepine of which the metabolite 10‐ monohydroxy derivate (MHD) is the pharmacologically effective compound. Two hours after a documented overdosage of more than 100 tablets oxcarbazepine, the serum level of the parent compound was 10‐fold higher than the therapeutic dosage (31.6 mg l −1 ). However, the concentration of MHD, which peaked 7 h after intake, was only twofold higher (59.0 mg l −1 ). No life‐threatening situations occurred and the patient fully recovered. The fact that oxcarbazepine is a prodrug and that the formation of the active MHD metabolite is a rate‐limiting process may contribute to the relative low toxicity of the drug in overdose.