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癫痫的药物治疗:新批准和正在研发的药物。

Pharmacotherapy of epilepsy: newly approved and developmental agents.

机构信息

Epilepsy Unit, Division of Cardiovascular and Medical Sciences, Western Infirmary, Glasgow, Scotland.

出版信息

CNS Drugs. 2011 Feb;25(2):89-107. doi: 10.2165/11584860-000000000-00000.

Abstract

This article discusses seven newly available antiepileptic drugs (AEDs) and agents in phase III development. Lacosamide, licensed as an adjunctive treatment for partial-onset seizures, primarily acts by enhancing sodium channel slow inactivation. At daily doses of 200-600 mg, the drug significantly reduced partial-onset seizures in adults with refractory epilepsy. The most common adverse effects are CNS related. Rufinamide, available as adjunctive treatment for seizures associated with Lennox-Gastaut syndrome, has an unclear mechanism of action, although it does block voltage-dependent sodium channels. Coadministration of valproic acid significantly increases rufinamide circulating concentrations. The drug has been shown to have efficacy for partial-onset, primary generalized tonic-clonic, tonic-atonic, absence and atypical absence seizures. Adverse effects are mainly somnolence, nausea and vomiting. Eslicarbazepine acetate, a carbamazepine analogue, was recently licensed as adjunctive treatment for partial-onset seizures. Eslicarbazepine acetate acts at voltage-gated sodium channels, although the precise mechanism of action is unclear. The drug had efficacy for partial-onset seizures in three randomized, double-blind, placebo-controlled studies, using 400, 800 or 1200 mg/day. Adverse effects include dizziness and somnolence. Retigabine (ezogabine) exerts its anticonvulsant effect through the opening of neuronal voltage-gated potassium channels. Following significant seizure reduction rates at dosages of 600, 900 and 1200 mg/day, license applications have been submitted for its use as adjunctive treatment for patients with partial-onset seizures. Dose-related adverse effects include somnolence, confusion and dizziness. Brivaracetam is the n-propyl analogue of levetiracetam. Mixed results have been obtained in phase III studies in patients with partial-onset seizures, and further trials in children, patients with photosensitive epilepsy and patients with partial-onset seizures are ongoing. Dizziness, headache and somnolence are the most common adverse effects reported. Perampanel was designed as an AMPA-type glutamate receptor antagonist. Following encouraging results from phase II studies in patients with refractory partial-onset seizures, recruitment for phase III trials is almost complete. Ganaxolone is a neurosteroid with potent antiepileptic activity that modulates GABA(A) receptors in the CNS. Ganaxolone has shown promise in a variety of seizure types. Dizziness and somnolence have been reported in some patients. The availability of new AEDs has widened the choices for clinicians treating patients with epilepsy. However, given the minimal improvement in prognosis and disappointing efficacy outcomes in double-blind, placebo-controlled, dose-ranging regulatory trials, it seems unlikely that these novel agents will have a major impact on outcomes for people with epilepsy.

摘要

本文讨论了七种新的抗癫痫药物(AEDs)和处于 III 期开发阶段的药物。拉考沙胺被批准作为部分发作性癫痫的辅助治疗药物,主要通过增强钠通道慢失活而起作用。在每日 200-600mg 的剂量下,该药物可显著减少难治性癫痫成人的部分发作性癫痫发作。最常见的不良反应与中枢神经系统有关。鲁非酰胺可作为 Lennox-Gastaut 综合征相关癫痫发作的辅助治疗药物,其作用机制尚不清楚,尽管它确实可以阻断电压依赖性钠通道。丙戊酸的联合用药可显著增加鲁非酰胺的循环浓度。该药物已被证明对部分发作、原发性全身性强直阵挛、强直阵挛、失神和非典型失神发作有效。不良反应主要为嗜睡、恶心和呕吐。乙酰左乙拉西坦是一种卡马西平类似物,最近被批准作为部分发作性癫痫的辅助治疗药物。乙酰左乙拉西坦作用于电压门控钠通道,但其确切作用机制尚不清楚。该药物在三项随机、双盲、安慰剂对照研究中,使用 400、800 或 1200mg/天的剂量,对部分发作性癫痫发作具有疗效。不良反应包括头晕和嗜睡。瑞替加滨(依佐加滨)通过开放神经元电压门控钾通道发挥其抗惊厥作用。在每日 600、900 和 1200mg 的剂量下显著减少癫痫发作后,已提交其作为部分发作性癫痫患者辅助治疗的许可申请。剂量相关的不良反应包括嗜睡、意识混乱和头晕。布立西坦是左乙拉西坦的 n-丙基类似物。在部分发作性癫痫患者的 III 期研究中,混合结果已经获得,在儿童、光敏性癫痫患者和部分发作性癫痫患者中的进一步试验正在进行中。最常见的不良反应包括头晕、头痛和嗜睡。吡仑帕奈是一种 AMPA 型谷氨酸受体拮抗剂。在难治性部分发作性癫痫患者的 II 期研究中取得令人鼓舞的结果后,III 期试验的招募工作几乎已经完成。甘氨酰胺是一种具有强大抗惊厥活性的神经甾体,可调节中枢神经系统中的 GABA(A)受体。甘氨酰胺酮在各种癫痫发作类型中都有良好的表现。一些患者报告有头晕和嗜睡。加那索酮是一种神经甾体,具有很强的抗癫痫活性,可调节中枢神经系统中的 GABA(A)受体。加那索酮酮在各种癫痫发作类型中都有良好的表现。一些患者报告有头晕和嗜睡。加那索酮是一种神经甾体,具有很强的抗癫痫活性,可调节中枢神经系统中的 GABA(A)受体。加那索酮酮在各种癫痫发作类型中都有良好的表现。一些患者报告有头晕和嗜睡。

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