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交沙霉素对卡马西平药代动力学的影响。

Effects of josamycin on carbamazepine kinetics.

作者信息

Vinçon G, Albin H, Demotes-Mainard F, Guyot M, Bistue C, Loiseau P

出版信息

Eur J Clin Pharmacol. 1987;32(3):321-3. doi: 10.1007/BF00607583.

Abstract

The steady state pharmacokinetics of oral carbamazepine in epileptic patients (n = 8) was compared before and after one week of treatment with josamycin (2 g/day). There was a small but statistically significant decrease in oral clearance of total (17%) and unbound (21.5%) drug. In spite of an unchanged AUC of 10,11-epoxide carbamazepine the ratio of metabolite to parent drug AUC was significantly decreased (20.2%). The plasma protein binding of carbamazepine and its 10,11-epoxide metabolite did not vary. The results demonstrate impairment by josamycin of the apparent clearance of carbamazepine. Care should be taken in patient receiving both carbamazepine and josamycin.

摘要

在8名癫痫患者中比较了口服卡马西平的稳态药代动力学,这些患者在接受一周的交沙霉素(2克/天)治疗前后进行了比较。总药物(17%)和游离药物(21.5%)的口服清除率有小幅但具有统计学意义的下降。尽管10,11-环氧卡马西平的AUC没有变化,但代谢物与母体药物AUC的比值显著降低(20.2%)。卡马西平及其10,11-环氧代谢物的血浆蛋白结合率没有变化。结果表明交沙霉素会损害卡马西平的表观清除率。同时接受卡马西平和交沙霉素治疗的患者应谨慎用药。

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