Rufinamide儿科Lennox-Gastaut综合症患者:一个全面的概述。

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Rufinamide儿科Lennox-Gastaut综合症患者:一个全面的概述。

Paediatr药物。2011年4月1;13 (2):97 - 106。doi: 10.2165 / 11586920-000000000-00000。

PubMed ID
21351809 (在PubMed
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文摘

Rufinamide三唑衍生物有广谱抗癫痫作用,无关任何抗癫痫药物目前在市场上。欧盟委员会和美国FDA批准rufinamide在2007年和2008年,分别为辅助治疗癫痫与Lennox-Gastaut综合症4岁以上儿童和成人。rufinamide的作用机制并不完全清楚,但被认为延长钠离子通道的活性状态,因此限制过度放电sodium-dependent动作电位。Rufinamide吸收当用食品,绝对生物利用度在70%和85%之间。药物的消除半衰期约为6 - 10小时,与一次最大血浆浓度(C (max))约4 - 6小时。C (max) 10毫克/公斤/天的剂量30毫克/公斤/天4.01杯/毫升和8.68杯/毫升,分别和血浆浓度时间曲线下的面积是37.8 + / - 0到12个小时47个杯子。h /毫升和89.3 + / - 58杯子。分别h /毫升。Rufinamide产生非线性增加剂量的药物动力学。的体积分布在儿童与成人相似(0.8 - -1.2 L /公斤)和药物血浆蛋白结合不大舒服(26.2 -34.8%)。 Rufinamide is mainly metabolized by carboxylesterases to an inactive metabolite (CGP 47292), and the majority of the metabolites are excreted in the urine (91%). No dosage adjustment is required in patients with renal dysfunction. Rufinamide does not affect the plasma concentration of other antiepileptics, but phenytoin, phenobarbital, valproate, and primidone affect the clearance of rufinamide. In a clinical study of 138 patients averaging 12 years of age, rufinamide used as an adjunctive therapy (with an initial dosage of 10 mg/kg/day up to a target dosage of 45 mg/kg/day) in patients with Lennox-Gastaut syndrome reduced the median total seizure frequency by 32.7% versus 11.7% in the placebo group (p = 0.0015). Similar reduction in total seizure frequency was maintained in the extension phase of this study. In other studies, rufinamide also seemed to provide improvement in both partial seizures and refractory epilepsy, but further studies need to validate this observation and to identify its clinical significance. Rufinamide is usually started orally at 10 mg/kg/day, titrating up by 10 mg/kg/day every 2 days to a target dosage of 45 mg/kg/day divided twice daily (maximum dosage of 3200 mg/day). Dosing of rufinamide has not been established in patients <4 years of age. Rufinamide is available as 100, 200, and 400 mg tablets in Europe, and 200 and 400 mg tablets in the US; a suspension of 40 mg/mL can be prepared extemporaneously. Rufinamide is well tolerated, with the most common adverse effects being dizziness, fatigue, nausea, vomiting, diplopia, and somnolence. From the current data, rufinamide serves as an adjunctive therapy in the management of Lennox-Gastaut syndrome. Further studies need to evaluate its efficacy as a first-line agent in the management of this neurologic disorder.

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药物
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药物 目标 类 生物 药理作用 行动
Rufinamide Metabotropic谷氨酸受体5 蛋白质 人类
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