Carbamazepine-10,11-Epoxide in Epilepsy A Pilot Study

• The effects of carbamazepine-10,11-epoxide, an active metabolite of carbamazepine, were evaluated in seven outpatients with frequent epileptic seizures. The study included an initial 4-week period with the carbamazepine dose optimized for each patient. Patients were then crossed over, dose by dose...

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Published inArchives of neurology (Chicago) Vol. 47; no. 8; pp. 888 - 892
Main Authors Tomson, Torbjörn, Almkvist, Ove, Nilsson, Bengt Y, Svensson, Jan-Olof, Bertilsson, Leif
Format Journal Article
LanguageEnglish
Published Chicago, IL American Medical Association 01.08.1990
Subjects
Adult
Anticonvulsants. Antiepileptics. Antiparkinson agents
Biological and medical sciences
Carbamazepine - analogs & derivatives
Carbamazepine - blood
Carbamazepine - therapeutic use
Dose-Response Relationship, Drug
Epilepsy - blood
Epilepsy - drug therapy
Female
Humans
Male
Medical sciences
Middle Aged
Neuropharmacology
Neuropsychological Tests
Pharmacology. Drug treatments
Pilot Projects
Single-Blind Method
Human
Chemotherapy
Nervous system diseases
Treatment
Convulsion
Metabolite
Epilepsy
HPLC chromatography
Anticonvulsant
Metabolism
Pharmacokinetics
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Summary:• The effects of carbamazepine-10,11-epoxide, an active metabolite of carbamazepine, were evaluated in seven outpatients with frequent epileptic seizures. The study included an initial 4-week period with the carbamazepine dose optimized for each patient. Patients were then crossed over, dose by dose, to carbamazepine-10,11-epoxide and followed up for another 4 weeks. Dosing was single blind. The evaluation of the anticonvulsant effect was hampered by marked fluctuations in plasma levels during treatment with carbamazepine-10,11-epoxide. There was, however, no significant change in seizure control. During epoxide treatment, no subjective side effects were reported despite epoxide plasma concentrations up to 57 μmol/L. Neuropsychological assessment revealed a significant improvement in finger motor speed and logical reasoning during the carbamazepine-10,11-epoxide period. Subnormal serum sodium levels in two patients were normalized after switching from carbamazepine to the epoxide. Continued investigations with this active metabolite of carbamazepine in epilepsy are therefore justified.
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ISSN:0003-9942
1538-3687
DOI:10.1001/archneur.1990.00530080072013