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布瓦西坦:一种获批用于治疗癫痫的新型化合物。

Brivaracetam: new compound approved for the treatment of epilepsy.

作者信息

Zaccara G

机构信息

Unit of Neurology, Department of Medicine, Florence Health Authority, Firenze, Italy.

出版信息

Drugs Today (Barc). 2016 Apr;52(4):219-27. doi: 10.1358/dot.2016.52.4.2480987.

Abstract

Brivaracetam was approved in the E.U. and U.S. at the beginning of 2016 for the adjunctive treatment of focal epilepsies in patients over 16 years of age. This compound is a novel high-affinity synaptic vesicle glycoprotein 2A (SV2A) ligand, with a selectivity for this protein that is 10- to 30-fold higher than that shown by levetiracetam. Preclinical studies show that brivaracetam might have a stronger anticonvulsant effect and distributes in the brain more quickly, when compared to levetiracetam. The agent has linear and simple pharmacokinetics and a low interaction potential. Six double-blind placebo-controlled studies have assessed doses from 5 to 200 mg/day. Significant efficacy has been observed from doses of 50 mg/day, but there was not a clear dose-effect relationship. Short-term tolerability was excellent with all doses. Adverse events significantly associated with brivaracetam were dizziness, somnolence, fatigue and irritability. An excellent tolerability profile has been found after administration of a formulation for intravenous use.

摘要

布立西坦于2016年初在欧盟和美国获批,用于辅助治疗16岁以上患者的局灶性癫痫。该化合物是一种新型的高亲和力突触囊泡糖蛋白2A(SV2A)配体,对该蛋白的选择性比对左乙拉西坦高10至30倍。临床前研究表明,与左乙拉西坦相比,布立西坦可能具有更强的抗惊厥作用,且在脑内分布更快。该药物具有线性且简单的药代动力学,药物相互作用可能性低。六项双盲安慰剂对照研究评估了每日5至200毫克的剂量。从每日50毫克的剂量开始就观察到了显著疗效,但未发现明确的剂量效应关系。所有剂量的短期耐受性都很好。与布立西坦显著相关的不良事件有头晕、嗜睡、疲劳和易怒。静脉用制剂给药后耐受性良好。

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