Strzelczyk Adam, Willems Laurent M, Willig Sophia, Rosenow Felix, Bauer Sebastian
a 1 Epilepsy Center Frankfurt Rhine-Main and Department of Neurology, Goethe-University , Frankfurt am Main, Germany.
b 2 Epilepsy Center Hessen and Department of Neurology, Philipps-University , Marburg, Germany.
Expert Rev Clin Pharmacol. 2015;8(6):733-40. doi: 10.1586/17512433.2015.1091303. Epub 2015 Oct 5.
Perampanel is the latest approved antiepileptic drug in focal and generalized epilepsies and has a distinct and selective mode of action on AMPA-receptors. Several thousand patients have received perampanel within randomized placebo-controlled trials, open-label extension trials and post-marketing observational studies. Significant median partial-onset seizure reduction rates of 23% for 4 mg/day, 26-31% for 8 mg/day and 18-35% for 12 mg/day were reported. Likewise 50 percent responder rates were 29% for 4 mg/day, 33-38% for 8 mg/day and 34-36% for 12 mg/day. Primary generalized tonic-clonic seizures were reduced by 76.5% (8 mg) vs 38.4% (placebo) in a recent controlled trial. Overall, perampanel is well tolerated and the main adverse events are dizziness, somnolence and fatigue. There are also anecdotal reports on use in progressive myoclonic epilepsies and status epilepticus. Perampanel will likely remain an important, possibly broad-spectrum AED with a significant market share, especially in patients with drug-refractory epilepsies.
吡仑帕奈是最新获批用于局灶性和全身性癫痫的抗癫痫药物,对α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体具有独特的选择性作用方式。在随机安慰剂对照试验、开放标签扩展试验和上市后观察性研究中,已有数千名患者使用过吡仑帕奈。据报道,每日4毫克时,部分发作性癫痫的显著中位缓解率为23%;每日8毫克时为26%-31%;每日12毫克时为18%-35%。同样,每日4毫克时50%缓解率为29%,每日8毫克时为33%-38%,每日12毫克时为34%-36%。在最近一项对照试验中,原发性全身性强直-阵挛性发作在服用8毫克吡仑帕奈时减少了76.5%,而服用安慰剂时减少了38.4%。总体而言,吡仑帕奈耐受性良好,主要不良事件为头晕、嗜睡和疲劳。也有关于其用于进行性肌阵挛性癫痫和癫痫持续状态的传闻报道。吡仑帕奈可能仍将是一种重要的、可能具有广谱性的抗癫痫药物,拥有显著的市场份额,尤其是在药物难治性癫痫患者中。