First dose and steady-state pharmacokinetics of oxcarbazepine and its 10-hydroxy metabolite |
| |
Authors: | R G Dickinson W D Hooper P R Dunstan M J Eadie |
| |
Institution: | (1) Clinical Neuropharmacology and Drug Metabolism Group, Department of Medicine, University of Queensland, Brisbane, Australia |
| |
Abstract: | Summary The pharmacokinetics of oxcarbazepine (a new anticonvulsant which is a congener of carbamazepine) and of its 10-hydroxy metabolite were studied at the outset of therapy in 8 adult epileptics comedicated with other anticonvulsants. The pharmacokinetic study was repeated under steady-state conditions after 3 months of drug intake in 6 of these subjects.The plasma elimination half-life of oxcarbazepine appeared to lie in the range 1.0–2.5 h, and that of its 10-hydroxy metabolite averaged 8.4 h. The apparent oral clearance of the parent drug (averaging 2.51·kg–1·h–1) was high enough to suggest substantial presystemic elimination. The oral clearance fell after 3 months of drug intake, but the half-lives of the drug and metabolite showed no statistically significant change over this time. Steady-state plasma levels of both drug and metabolite were linearly related to drug dose, metabolite levels averaging 9 times those of the parent substance. |
| |
Keywords: | oxcarbazepine pharmacokinetics drug metabolism |
本文献已被 SpringerLink 等数据库收录! |