Felbamate in vitro metabolism by rat liver microsomes.
Incubation of [14C]felbamate at 37 degrees C for 60 min with liver microsomes from untreated Sprague-Dawley rats converted 10% of the drug to the p-hydroxy (6%) and 2-hydroxy (4%) metabolites. With microsomes from phenobarbital-pretreated rats, 21% of the drug was metabolized to the p-hydroxy (7.5%) and 2-hydroxy (13.5%) metabolites. With microsomes from felbamate-pretreated rats, up to 25% of drug was metabolized to the p-hydroxy (5%) and 2-hydroxy (20%) metabolites. In addition, a small amount of the monocarbamate metabolite was also present, but no other metabolites were formed. Coincubations of [14C]phenytoin with felbamate had no effect on the metabolism of phenytoin, whereas the amount of [14C]felbamate metabolized in the presence of phenytoin decreased by 30-38%.
Wallace Laboratories, Division of Carter-Wallace, Inc., Cranbury, NJ 08512.
V E
VE
Adusumalli
K K
KK
Wong
N
N
Kucharczyk
R D
RD
Sofia
D000818:Animals; D000927:Anticonvulsants / Q000378:metabolism* / Q000494:pharmacology; D004347:Drug Interactions; D000078328:Felbamate; D006900:Hydroxylation; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism*; D010634:Phenobarbital / Q000494:pharmacology; D048448:Phenylcarbamates; D010672:Phenytoin / Q000378:metabolism / Q000494:pharmacology; D011409:Propylene Glycols / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013997:Time Factors
D000927:Anticonvulsants; D048448:Phenylcarbamates; D011409:Propylene Glycols; D010672:Phenytoin; D000078328:Felbamate; D010634:Phenobarbital