2011
DOI: 10.1111/j.1528-1167.2011.03140.x
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In vitro transport profile of carbamazepine, oxcarbazepine, eslicarbazepine acetate, and their active metabolites by human P-glycoprotein

Abstract: Summary Purpose:  Antiepileptic drugs (AEDs) are widely used not only in the treatment of epilepsy but also as treatments for psychiatric disorders. Pharmacoresistance of AEDs in the treatment of epilepsy and psychiatric disorders is a serious problem. Transport of antiepileptic drugs by P‐glycoprotein (Pgp, ABCB1, or MDR1), which is overexpressed in the blood–brain barrier, may be a mechanism for resistance of AEDs. For most AEDs, conflicting evidence precludes consensus on whether they are substrates of Pgp.… Show more

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Cited by 85 publications
(44 citation statements)
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“…The relevance of ABC transporter function for the therapy of epilepsy could be shown in a pilocarpine seizure model in rats, where co-administration of the P-gp inhibitor verapamil significantly potentiated the anticonvulsant activity of the AED oxcarbazepine [79]. In addition, it was reported that combined treatment with verapamil and AEDs improved overall seizure control in an epileptic patient [80].…”
Section: Neuropathologies and Abc Transporters At The Bbbmentioning
confidence: 98%
“…The relevance of ABC transporter function for the therapy of epilepsy could be shown in a pilocarpine seizure model in rats, where co-administration of the P-gp inhibitor verapamil significantly potentiated the anticonvulsant activity of the AED oxcarbazepine [79]. In addition, it was reported that combined treatment with verapamil and AEDs improved overall seizure control in an epileptic patient [80].…”
Section: Neuropathologies and Abc Transporters At The Bbbmentioning
confidence: 98%
“…The most common SNPs in the ABCB1 gene were c.1236C>T (rs1128503), c.2677G>T/A (rs2032582) and c.3435C>T (rs1045642). It is still unclear whether CBZ is an active substrate of P-gp [4][5][6], and conflicting results have been reported for different ethnic groups in regard to the influence of the above three SNPs on CBZ disposition [7,8]. Although Chinese epileptic patients with 3435TT had lower adjusted CBZ concentrations than those with 3435CC [9], a larger study should be carried out to validate the results.…”
Section: Introductionmentioning
confidence: 93%
“…Although Chinese epileptic patients with 3435TT had lower adjusted CBZ concentrations than those with 3435CC [9], a larger study should be carried out to validate the results. Meanwhile, carbamazepine-10,11-epoxide (CBZE), an active and stable metabolite [10], is considered to be a substrate of P-gp in vitro [5]. However, the contribution of ABCB1 gene polymorphisms to CBZE disposition has not been studied.…”
Section: Introductionmentioning
confidence: 99%
“…Cell viability was tested using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays [58]. Briefly, cells were seeded onto a flat-bottom 96-well plate (Corning Life Science, USA) at a density of 1.5 Â 10 4 cells/ well.…”
Section: Cell Viability Testmentioning
confidence: 99%