Morris R G, Black A B, Lam E, Westley I S
Department of Clinical Pharmacology, The Queen Elizabeth Hospital, Woodville, South Australia.
Ther Drug Monit. 2000 Dec;22(6):656-60. doi: 10.1097/00007691-200012000-00003.
Lamotrigine (LTG) is one of the newer antiepileptic drugs which has been shown to have a spectrum of drug interactions (including with other epilepsy drugs) that can have a pronounced effect on LTG kinetics. The present study examined the LTG metabolic inhibition dose-response relationship with valproic acid (VPA) in eight patients with epilepsy with a view to using this to benefit the patient. This could benefit the patient not only by attaining higher plasma LTG concentrations with "standard" dosages of LTG, but also possibly by achieving better seizure control through providing a less variable peak-to-trough fluctuation in LTG concentrations as a result of extending the half-life of LTG. The dosages of VPA trialed were 0, 200, 500, and 1,000 mg/d which resulted in a mean increase in LTG area under the curve of 83.7 +/- 14.7% at 200 mg VPA/d, to and 160 +/- 37.9% at 1,000 mg VPA/d. The presence of concomitant enzyme inducers in some patients did not influence the percentage increase from baseline in half-life observed, although clearly those on inducers started from a lower absolute half-life as a result of the induction. The effect was shown to be quite variable, particularly at the highest dosage of VPA tested (1,000 mg/d), suggesting that this effect could be best applied with the support of the therapeutic drug monitoring laboratory determining plasma LTG concentrations to allow individualization of the LTG dosage.
拉莫三嗪(LTG)是一种较新的抗癫痫药物,已被证明具有一系列药物相互作用(包括与其他抗癫痫药物的相互作用),这些相互作用可对LTG的药代动力学产生显著影响。本研究检测了8例癫痫患者中LTG与丙戊酸(VPA)的代谢抑制剂量反应关系,以期借此使患者受益。这不仅可以通过使用“标准”剂量的LTG达到更高的血浆LTG浓度使患者受益,还可能通过延长LTG的半衰期,使LTG浓度的峰谷波动更小,从而更好地控制癫痫发作。所试验的VPA剂量分别为0、200、500和1000mg/d,结果显示,VPA剂量为200mg/d时,LTG曲线下面积平均增加83.7±14.7%,VPA剂量为1000mg/d时,增加至160±37.9%。一些患者同时使用酶诱导剂,这并未影响观察到的半衰期相对于基线的增加百分比,不过显然,使用诱导剂的患者由于诱导作用,其绝对半衰期较低。结果显示这种效应变化很大,尤其是在测试的最高VPA剂量(1000mg/d)时,这表明在治疗药物监测实验室测定血浆LTG浓度以实现LTG剂量个体化的支持下,这种效应能得到最佳应用。