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唑尼沙胺(Excegran)辅助治疗对卡马西平蛋白结合及代谢的影响。

Influence of additional therapy with zonisamide (Excegran) on protein binding and metabolism of carbamazepine.

作者信息

Minami T, Ieiri I, Ohtsubo K, Hirakawa Y, Ueda K, Higuchi S, Aoyama T

机构信息

Department of Pediatrics, Faculty of Medicine, Kyushu University, Fukuoka, Japan.

出版信息

Epilepsia. 1994 Sep-Oct;35(5):1023-5. doi: 10.1111/j.1528-1157.1994.tb02548.x.

DOI:10.1111/j.1528-1157.1994.tb02548.x
PMID:7925145
Abstract

The influence of comedication with zonisamide (ZNS) on protein binding and carbamazepine (CBZ) metabolism was studied in 16 pediatric epileptic patients. Correlations were evaluated between ZNS daily dose and individual change of level per dose ratio (L/D ratio), free fraction, and carbamazepine-10,11-epoxide/CBZ level ratio (CBZE/CBZ). Statistical significant negative correlation was observed between L/D ratio and ZNS daily dose. Despite alteration in the L/D ratio, the free fraction of CBZ was unaltered in combination with ZNS. To assess the effect of addition of ZNS on CBZ metabolism, the CBZE/CBZ level ratio was compared; this ratio showed a tendency to increase with increase in ZNS dose. Consequently, ZNS is considered to have a significant effect on CBZ metabolism but not on protein binding.

摘要

在16例小儿癫痫患者中研究了唑尼沙胺(ZNS)合并用药对蛋白质结合及卡马西平(CBZ)代谢的影响。评估了ZNS日剂量与每剂量水平比(L/D比)、游离分数及卡马西平-10,11-环氧化物/CBZ水平比(CBZE/CBZ)的个体变化之间的相关性。观察到L/D比与ZNS日剂量之间存在统计学显著负相关。尽管L/D比发生了改变,但CBZ与ZNS联合使用时的游离分数未改变。为评估添加ZNS对CBZ代谢的影响,比较了CBZE/CBZ水平比;该比值显示出随ZNS剂量增加而增加的趋势。因此,认为ZNS对CBZ代谢有显著影响,但对蛋白质结合无影响。

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