Owen Richard T
Drugs Today (Barc). 2010 Jan;46(1):23-31. doi: 10.1358/dot.2010.46.1.1437709.
Eslicarbazepine acetate, a novel antiepileptic agent, has recently been marketed as an adjunctive therapy in adults with partial onset seizures with or without secondary generalization. Its mode of action is not fully elucidated but it is believed that it and its metabolites stabilize the inactivated state of voltage-gated sodium channels, preventing their return to the inactivated state. Eslicarbazepine acetate is extensively converted to eslicarbazepine, its major active metabolite. Its pharmacokinetic profile is unaffected by food, gender, age or moderate hepatic impairment; clearance is dependent on renal function and dose reduction is recommended in patients with a creatinine clearance < 60 ml/min. Eslicarbazepine acetate does not induce its own metabolism or clearance. Clinical trials have demonstrated efficacy in short and long term studies (up to 1 year) together with improvements in quality of life outcomes and depressive symptoms where these existed at baseline. Most adverse events were mild to moderate in intensity and occurred early in treatment; the most frequently reported events were dizziness, somnolence and headache. Trials using eslicarbazepine acetate as monotherapy are ongoing.
醋酸艾司利卡西平是一种新型抗癫痫药物，最近已作为辅助疗法用于治疗伴有或不伴有继发性全身性发作的成人部分性发作。其作用机制尚未完全阐明，但据信它及其代谢产物可稳定电压门控钠通道的失活状态，防止其恢复到失活状态。醋酸艾司利卡西平可广泛转化为其主要活性代谢产物艾司利卡西平。其药代动力学特征不受食物、性别、年龄或中度肝功能损害的影响；清除率取决于肾功能，肌酐清除率<60 ml/min的患者建议减少剂量。醋酸艾司利卡西平不会诱导自身的代谢或清除。临床试验已证明其在短期和长期研究（长达1年）中有效，同时在基线时存在生活质量结果和抑郁症状的情况下也有所改善。大多数不良事件的强度为轻度至中度，且在治疗早期出现；最常报告的事件是头晕、嗜睡和头痛。使用醋酸艾司利卡西平作为单一疗法的试验正在进行中。
