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丙戊酸钠可急性抑制拉莫三嗪的代谢。

Sodium valproate acutely inhibits lamotrigine metabolism.

作者信息

Yuen A W, Land G, Weatherley B C, Peck A W

机构信息

Wellcome Research Laboratories, Beckenham, Kent.

出版信息

Br J Clin Pharmacol. 1992 May;33(5):511-3. doi: 10.1111/j.1365-2125.1992.tb04079.x.

Abstract

Concomitant administration of sodium valproate (VPA) reduced lamotrigine (LTG) total clearance by approximately 21% and increased elimination half-life and AUC. Reduced elimination occurred acutely within the first hour. Renal elimination of LTG was not impaired. The most probable explanation for this effect is hepatic competition between VPA and LTG for glucuronidation. Volume of distribution and parameters related to absorption, Cmax and tmax were unchanged.

摘要

丙戊酸钠(VPA)与拉莫三嗪(LTG)同时给药可使拉莫三嗪的总清除率降低约21%,并延长消除半衰期和增加药时曲线下面积(AUC)。在给药后的第一小时内即迅速出现清除率降低的情况。拉莫三嗪的肾排泄未受损害。对此效应最可能的解释是VPA与LTG在肝脏中竞争葡萄糖醛酸化。分布容积以及与吸收相关的参数、最大血药浓度(Cmax)和达峰时间(tmax)均未改变。

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