EFFECT OF FELBAMATE ON PLASMA-LEVELS OF CARBAMAZEPINE AND ITS METABOLITES

被引:73
作者
ALBANI, F
THEODORE, WH
WASHINGTON, P
DEVINSKY, O
BROMFIELD, E
PORTER, RJ
NICE, FJ
机构
[1] NINCDS,EPILEPSY BRANCH,PRECLIN PHARMACOL SECT,BETHESDA,MD 20892
[2] NINCDS,MED NEUROL BRANCH,CLIN EPILEPSY SECT,BETHESDA,MD 20892
关键词
ANTICONVULSANTS; FELBAMATE; CARBAMAZEPINE; CARBAMAZEPINE-10,11-EPOXIDE; CARBAMAZEPINE-DIOL; DRUG INTERACTIONS;
D O I
10.1111/j.1528-1157.1991.tb05624.x
中图分类号
R74 [神经病学与精神病学];
学科分类号
摘要
Felbamate (FBM) is a novel antiepileptic drug (AED) currently undergoing clinical evaluation in the United States. During a controlled clinical trial conducted at the National Institutes of Health Clinical Center, FBM was added to constant carbamazepine (CBZ) monotherapy. CBZ total concentrations were reduced during active FBM treatment (mean reduction 25%, range 10-42%, p < 0.001). The effect was evident after the first week of treatment and reached a plateau in 2-4 weeks. To clarify the interaction mechanism, free and total concentrations of CBZ and its plasma metabolites were determined by high-performance liquid chromatography (HPLC) and ultrafiltration in four patients. In these patients, FBM treatment reduced CBZ concentrations and increased CBZ-epoxide (CBZ-E) concentrations (p < 0.01). Free fractions of all compounds were unmodified. FBM appears to be capable of inducing CBZ metabolism. CBZ-FBM interaction may be clinically relevant.
引用
收藏
页码:130 / 132
页数:3
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