短期拉莫三嗪治疗对卡马西平药代动力学的影响。

Effects of short-term lamotrigine treatment on pharmacokinetics of carbamazepine.

作者信息

Malminiemi K, Keränen T, Kerttula T, Moilanen E, Ylitalo P

机构信息

Department of Clinical Chemistry, Tampere University Hospital, Finland.

出版信息

Int J Clin Pharmacol Ther. 2000 Nov;38(11):540-5. doi: 10.5414/cpp38540.

DOI:10.5414/cpp38540

PMID:11097146

Abstract

AIM AND METHOD

The effects of short-term treatment with lamotrigine (LTG) (100 mg twice daily for one week) on single dose pharmacokinetics of carbamazepine (CBZ, 200 mg) were investigated in a randomized, double-blinded, placebo-controlled cross-over study with 10 healthy volunteers.

RESULTS

Pharmacokinetic parameters for CBZ or for CBZ-10,11-epoxide, the main metabolite of CBZ, were not significantly affected by LTG pretreatment. The mean (+/- SEM) elimination half-life of CBZ was 33.0+/-1.8 h after pretreatment with placebo and 30.1+/-2.0 h after a one-week-pretreatment with LTG (NS). The area under the serum concentration curve to infinity (AUC) of CBZ was 638+/-45 micromol/l after placebo and 624+/-53 micromol/l after LTG (NS). Changes in the peak serum concentration, from 9.0+/-0.3 micromol/l to 9.2+/-0.4 micromol/l (LTG), and in the time to peak serum concentration, from 9.3+/-1.1 h to 9.1+/-1.2 h (LTG), were also not significant.

CONCLUSION

These data support the earlier findings that LTG does not significantly affect the rate or extent of absorption, or elimination of CBZ.

摘要

目的与方法

在一项有10名健康志愿者参与的随机、双盲、安慰剂对照交叉研究中，研究了拉莫三嗪（LTG）短期治疗（每日两次，每次100毫克，持续一周）对卡马西平（CBZ，200毫克）单剂量药代动力学的影响。

结果

LTG预处理对CBZ或其主要代谢产物CBZ - 10,11 - 环氧化物的药代动力学参数无显著影响。安慰剂预处理后CBZ的平均（±标准误）消除半衰期为33.0 ± 1.8小时，LTG预处理一周后为30.1 ± 2.0小时（无显著性差异）。安慰剂组CBZ的血清浓度曲线下面积至无穷大（AUC）为638 ± 45微摩尔/升，LTG组为624 ± 53微摩尔/升（无显著性差异）。血清峰值浓度从9.0 ± 0.3微摩尔/升变为9.2 ± 0.4微摩尔/升（LTG），以及血清峰值浓度出现时间从9.3 ± 1.1小时变为9.1 ± 1.2小时（LTG），变化也均无显著性。