Neurology Unit, Ospedale dell'Angelo , Venezia-Mestre, Italy.
Neurology Unit, Department of Neurosciences, University Hospital of Udine , Udine, Italy.
Expert Opin Drug Metab Toxicol. 2020 Oct;16(10):853-863. doi: 10.1080/17425255.2020.1813277. Epub 2020 Sep 20.
The goal of pharmacologic therapy with antiseizure medications (ASMs) is to achieve a seizure-free state with minimal side effects. About one third of patients treated with available ASMs continue to experience uncontrolled seizures. There is still need for new ASMs with enhanced effectiveness and tolerability.
The present manuscript is based on an extensive Internet and PubMed search from 1999 to 2020. It is focused on the clinical and pharmacological properties of brivaracetam (BRV) in the treatment of epilepsy.
BRV is approved as add-on or monotherapy (in US) for the treatment of focal-onset seizures with or without secondary generalization. BRV is a high affinity synaptic vesicle glycoprotein 2A ligand, with 15-30-fold higher affinity than levetiracetam. The selectivity of BRV may be associated with fewer clinical adverse effects. BRV shares many of the pharmacokinetic characteristics of an ideal ASMs. Additionally, BRV has a low potential for clinically relevant drug-drug interactions. Its pharmacokinetic profile makes BRV a promising agent for the treatment of status epilepticus (SE). Although BRV is not approved for the treatment of SE, it has demonstrated promising preliminary results. Further studies are needed to explore the efficacy and tolerability of BRV in SE.
抗癫痫药物（ASMs）的药理治疗目标是在最小副作用的情况下实现无癫痫发作状态。大约三分之一接受现有 ASMs 治疗的患者仍会出现不受控制的癫痫发作。仍然需要具有增强疗效和耐受性的新型 ASMs。
本手稿基于 1999 年至 2020 年的广泛互联网和 PubMed 搜索。它重点介绍了 brivaracetam（BRV）在治疗癫痫中的临床和药理学特性。
BRV 被批准为附加或单药治疗（在美国），用于治疗伴有或不伴有继发性泛化的局灶性发作癫痫。BRV 是一种高亲和力突触囊泡糖蛋白 2A 配体，与左乙拉西坦的亲和力高 15-30 倍。BRV 的选择性可能与较少的临床不良反应有关。BRV 具有许多理想 ASMs 的药代动力学特征。此外，BRV 具有较低的临床相关药物相互作用的潜力。其药代动力学特征使 BRV 成为治疗癫痫持续状态（SE）的有前途的药物。尽管 BRV 尚未被批准用于治疗 SE，但它已显示出有希望的初步结果。需要进一步的研究来探索 BRV 在 SE 中的疗效和耐受性。
