Zaccara G
Unit of Neurology, Department of Medicine, Florence Health Authority, Firenze, Italy.
Drugs Today (Barc). 2016 Apr;52(4):219-27. doi: 10.1358/dot.2016.52.4.2480987.
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.
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。