卡马西平和奥卡西平通过抑制CYP2C19降低苯妥英的代谢。
Carbamazepine and oxcarbazepine decrease phenytoin metabolism through inhibition of CYP2C19.
作者信息
Lakehal F, Wurden C J, Kalhorn T F, Levy R H
机构信息
Department of Pharmaceutics, University of Washington, Seattle, WA 98195-7610, USA.
出版信息
Epilepsy Res. 2002 Dec;52(2):79-83. doi: 10.1016/s0920-1211(02)00188-2.
Multiple studies suggest that phenytoin concentrations increase with CBZ co-medication. This study evaluated the hypothesis that CBZ and/or its major metabolite (CBZE) inhibit CYP2C19-mediated phenytoin metabolism using human liver microsomes and cDNA-expressed CYP2C19. Oxcarbazepine (OXC), and its 10-monohydroxy metabolite (MHD) were also evaluated. CBZ and MHD inhibited CYP2C19-mediated phenytoin metabolism at therapeutic concentrations. Thus, administration of CBZ and OXC with CYP2C19 substrates with narrow therapeutic ranges should be done cautiously.
多项研究表明，与卡马西平（CBZ）联合用药时苯妥英浓度会升高。本研究评估了以下假设：使用人肝微粒体和cDNA表达的CYP2C19，卡马西平和/或其主要代谢物（CBZE）抑制CYP2C19介导的苯妥英代谢。同时也评估了奥卡西平（OXC）及其10-单羟基代谢物（MHD）。在治疗浓度下，卡马西平和MHD抑制CYP2C19介导的苯妥英代谢。因此，将卡马西平和奥卡西平与治疗窗较窄的CYP2C19底物一起给药时应谨慎。
Zotero 插件