Sonmezturk Hasan H, Azar Nabil J
Department of Neurology, Vanderbilt University Medical Center, Nashville, Tennessee, USA.
J Cent Nerv Syst Dis. 2011 Feb 14;3:17-25. doi: 10.4137/JCNSD.S4126. Print 2011.
Extended release (XR) formulation of levetiracetam (LEV) is approved by the Food and Drug Administration as an add-on to other antiepileptic drugs (AEDs) for adults with partial onset seizures. This is based on class-I evidence demonstrating significant seizure reduction in once daily dosing. Keppra-XR is marketed with the brand name of Keppra XR since 2008 (UCB Pharma). Its original immediate release (IR) formulation has been in the market since 2000. LEV has a unique molecular structure which is chemically unrelated to existing AEDs. The precise mechanism of action is unknown. Animal studies showed binding to synaptic vesicle protein SV2A, thought to be involved in modulating synaptic neurotransmitter release. LEV-IR is proven effective as adjunctive therapy for partial-onset seizures, primary generalized tonic-clonic seizures and myoclonic seizures. It was shown to be equivalent to carbamazepine as first-line treatment for partial-onset seizures. The extended release formulation added advantages such as better tolerance and increased compliance.
左乙拉西坦(LEV)缓释(XR)制剂已获美国食品药品监督管理局批准,可作为其他抗癫痫药物(AEDs)的附加用药,用于治疗成人部分性发作癫痫。这一批准基于I类证据,表明每日一次给药可显著减少癫痫发作。自2008年以来,开浦兰缓释片(Keppra-XR)以Keppra XR的品牌名称上市(优时比制药公司)。其最初的速释(IR)制剂自2000年起已投放市场。左乙拉西坦具有独特的分子结构,在化学上与现有的抗癫痫药物无关。其确切作用机制尚不清楚。动物研究表明,它与突触囊泡蛋白SV2A结合,据认为这与调节突触神经递质释放有关。左乙拉西坦速释片(LEV-IR)已被证明作为辅助疗法对部分性发作、原发性全身性强直阵挛发作和肌阵挛发作有效。它被证明作为部分性发作的一线治疗药物与卡马西平等效。缓释制剂具有更好的耐受性和更高的依从性等优点。