Induction of microsomal enzymes in rat liver by oxcarbazepine, 10,11-dihydro-10-hydroxy-carbamazepine and carbamazepine.
1. The effects of the new anti-epileptic drug, oxcarbazepine, its major metabolite in man, 10,11-dihydro-10-hydroxy-carbamazepine, and carbamazepine, on hepatic microsomal enzyme activities have been studied in rats after repeated administration of equimolar doses. 2. All three compounds caused a qualitatively similar induction of the mono-oxygenase system, the greatest increase being observed in the activity of 4-nitroanisole O-demethylase. Oxcarbazepine is as potent as carbamazepine, while 10,11-dihydro-10-hydroxy-carbamazepine is a weak inducer. 3. The observation that oxcarbazepine is a potent inducer in rats but not in man is explained by the species differences in its metabolism.
Wagner
J
J
Research and Development Department, CIBA-GEIGY Limited, Basle, Switzerland.
Schmid
K
K
D000818:Animals; D002220:Carbamazepine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D004790:Enzyme Induction / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology*; D051381:Rats; D011919:Rats, Inbred Strains
C039775:10,11-dihydro-10-hydroxycarbamazepine; D002220:Carbamazepine