药代动力学相互作用retigabine和拉莫三嗪在健康受试者。

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赫尔曼·R, Knebel NG Niebch G,理查兹L, Borlak J,打孔机

药代动力学相互作用retigabine和拉莫三嗪在健康受试者。

欧元中国新药杂志。2003年4月,58 (12):795 - 802。Epub 2003年2月28日。

PubMed ID

12698305 (在PubMed

]

文摘

用途:抗癫痫药物(aed) retigabine (RGB)和拉莫三嗪(LTG)进行主要N-glucuronidation和肾排泄。这项研究进行了评估潜在aed药代动力学之间的相互作用。方法:29岁健康男性受试者参与了这项研究。A组(n = 14)接受单剂量口服200毫克RGB第一天和第七天,25毫克o.i.d。LTG天3 - 8。B组(n = 15)接受单剂量口服200毫克LTG 1天17天,300毫克,up-titrated RGB b.i.d.天6 20。收集血液样本比较aed的药物动力学和RGB (awd21 - 360)的n -乙酰代谢物单后和伴随的治疗。结果:RGB迅速吸收和消除平均半衰期(t (1/2)) 6.3 + / - -1.1 h和明显的间隙(CL / F) 0.69 + / - -1.4 l / h /公斤。在合并施打LTG,意思是RGB t(1/2)和血浆浓度时间曲线下面积(AUC)增加了7.5% (P = 0.045)和15% (P = 0.006),分别在CL / F下降了13% (P = 0.06)。awd21 - 360年结果一致。LTG适度迅速吸收,消除平均t (1/2) 37 + / - -10.4 h和CL / F (0.028 + / - -0.007 l / h /公斤。 Under co-administration of RGB, mean LTG t(1/2) and AUC decreased by 15% and 18%, respectively, while CL/F increased by 22% (all parameters, P=0.001). CONCLUSIONS: RGB and LTG exhibit a modest pharmacokinetic interaction on each other. The slight decline in RGB clearance due to LTG is believed to result from competition for renal elimination rather than competition for glucuronidation. The induction of LTG clearance due to retigabine was unexpected since RGB did not show enzyme induction in various other drug-drug interaction studies. Further studies in patients are needed to assess the clinical relevance of these findings for concomitant treatment with both drugs in the upper recommended dose range.

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药物

Ezogabine