新的抗癫痫药物的临床药理学概要perampanel:一种新颖的非竞争性AMPA受体拮抗剂。
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Patsalos PN
新的抗癫痫药物的临床药理学概要perampanel:一种新颖的非竞争性AMPA受体拮抗剂。
Epilepsia。2015年1月;56(1):12日到27日。doi: 10.1111 / epi.12865。Epub 2014年12月13日。
- PubMed ID
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25495693 (在PubMed]
- 文摘
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临床药理学的药物非常确定其治疗,和本文总结了特征与抗癫痫药物(AED) perampanel有关。perampanel PubMed进行文必威国际app献检索。国会抽象数据包括在必要时和卫材公司提供未发表的数据文件。口服摄入后,perampanel迅速吸收和血浆浓度峰值出现0.5 - -2.5 h后;其生物利用度~ 100%。尽管perampanel吸收的速度放缓了食品co-ingestion吸收程度保持不变;因此,perampanel可以不考虑吃饭时间管理。perampanel的药物代谢动力学情况是线性和可预测的临床相关的剂量范围(2毫克);perampanel 95%蛋白结合的白蛋白和alpha1-acid糖蛋白。Perampanel广泛(> 90%)在肝脏代谢,主要由细胞色素P450 (CYP) 3 a4,各种药物活性代谢物。 In healthy volunteers, the apparent terminal half-life is ~105 h, whereas the calculated effective half-life is 48 h. These half-life values allow for once-daily dosing, which will aid patient compliance and in the event of a missed dose, will have minimal impact on seizure control. In healthy volunteers prescribed carbamazepine, half-life decreases to 25 h. Clearance values are not significantly different in adolescents (~13.0 ml/min) and the elderly (~10.5 ml/min) compared with adults (10.9 ml/min). Perampanel has minimal propensity to cause pharmacokinetic interactions. However, it is the target of such interactions and CYP3A4-inducing AEDs enhance its clearance; this can be used to advantage because dose titration can be faster and thus optimum therapeutic outcome can be achieved sooner. Perampanel 12 mg, but not 4 or 8 mg, enhances the metabolism of the progesterone component of the oral contraceptive pill, necessitating the need for an additional reliable contraceptive method. Overall, perampanel has a favorable clinical pharmacology profile, which should aid its clinical use.
DrugBank数据引用了这篇文章
- 药物酶
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药物 酶 类 生物 药理作用 行动 Perampanel 细胞色素P450 3 a4 蛋白质 人类 没有底物诱导物细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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药物 交互 整合药物之间
在您的软件的交互Perampanel 苯妥英 的血清浓度Perampanel时可以减少与苯妥英相结合。 Perampanel Fosphenytoin 的血清浓度Perampanel可以结合Fosphenytoin时下降。
