Arroyo Santiago
Eisai Global Clinical Development, Ridgefield Park, New Jersey 07660, USA.
Neurotherapeutics. 2007 Jan;4(1):155-62. doi: 10.1016/j.nurt.2006.11.006.
Rufinamide is a triazole derivative structurally unrelated to currently marketed antiepileptic drugs. Rufinamide was profiled for anticonvulsant activity at the National Institutes of Health and showed broad-spectrum anticonvulsant properties at nontoxic doses in animal models. The principal mechanism of action of rufinamide is considered to be the modulation of the activity of sodium channels and, in particular, prolongation of the inactive state of the channel. Rufinamide provides an efficacious and well-tolerated treatment option for use as adjunctive therapy in patients with partial seizures and with Lennox-Gastaut syndrome (LGS). In LGS, rufinamide is effective in controlling multiple seizure types and in reducing the severity of the seizures. The most commonly observed (> or =10%) adverse experiences seen in association with rufinamide are headache, dizziness, fatigue, somnolence and nausea. Rufinamide is generally well tolerated, and its safety profile is well-established.
鲁非酰胺是一种三唑衍生物，其结构与目前上市的抗癫痫药物无关。在美国国立卫生研究院，鲁非酰胺被测定了抗惊厥活性，并且在动物模型中，其在无毒剂量下显示出广谱抗惊厥特性。鲁非酰胺的主要作用机制被认为是调节钠通道的活性，尤其是延长通道的失活状态。鲁非酰胺为部分性发作和伦诺克斯-加斯托综合征（LGS）患者提供了一种有效且耐受性良好的辅助治疗选择。在LGS中，鲁非酰胺可有效控制多种发作类型并减轻发作的严重程度。与鲁非酰胺相关的最常见（≥10%）不良事件是头痛、头晕、疲劳、嗜睡和恶心。鲁非酰胺通常耐受性良好，其安全性已得到充分确立。
