Suppr超能文献

α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体拮抗剂吡仑帕奈是癫痫治疗的新希望。

The AMPA receptor antagonist perampanel is a new hope in the treatment for epilepsy.

作者信息

El Desoky Ehab S

机构信息

Department of Pharmacology, Faculty of Medicine, Assiut University, 71515, Assiut, Egypt.

出版信息

Fundam Clin Pharmacol. 2014 Oct;28(5):473-80. doi: 10.1111/fcp.12081. Epub 2014 May 14.

Abstract

Perampanel is a novel drug recently approved as adjunctive therapy in epileptic patients aged 12 years and older who have drug-resistant partial epilepsy with and without secondary generalization. Pharmacological researches revealed that perampanel reduces neuronal excitability by a non-competitive antagonistic activity against the ionotropic alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors causing modulation of glutamatergic neurotransmission. The pharmacological profile of the drug showed complete absorption following oral administration, and extensive metabolism in the liver by oxidation followed by glucuronidation with an elimination half-life of approximately 53-165 h (average: 105 h), allowing once-daily administration. Randomized placebo-controlled trials demonstrated an effective dose range of the drug, between 4 and 12 mg/day, to significantly reduce seizure frequency in patients with partial-onset seizure that are pharmacoresistant with a favorable tolerability profile. The most frequent adverse events of the drug reported in phase III clinical trials were dizziness, somnolence, fatigue, and headache. However, the data raised from the studies can give a hope that perampanel offers a valuable option as an adjuvant therapy for pharmacoresistant partial-onset and secondarily generalized seizures.

摘要

吡仑帕奈是一种新型药物,最近被批准作为辅助疗法用于12岁及以上患有耐药性部分性癫痫(伴或不伴继发全面性发作)的癫痫患者。药理学研究表明,吡仑帕奈通过对离子型α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体的非竞争性拮抗活性来降低神经元兴奋性,从而调节谷氨酸能神经传递。该药物的药理学特征显示口服给药后可完全吸收,在肝脏中通过氧化然后与葡萄糖醛酸结合进行广泛代谢,消除半衰期约为53 - 165小时(平均:105小时),允许每日一次给药。随机安慰剂对照试验证明该药物的有效剂量范围为4至12毫克/天,可显著降低对药物耐药的部分性发作患者的癫痫发作频率,且耐受性良好。在III期临床试验中报告的该药物最常见的不良事件为头晕、嗜睡、疲劳和头痛。然而,这些研究所得的数据带来了希望,即吡仑帕奈作为耐药性部分性发作和继发全面性发作的辅助治疗提供了一个有价值的选择。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验