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瑞替加滨:用于部分性癫痫发作。

Retigabine: in partial seizures.

作者信息

Plosker Greg L, Scott Lesley J

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

CNS Drugs. 2006;20(7):601-8; discussion 609-10. doi: 10.2165/00023210-200620070-00005.

DOI:10.2165/00023210-200620070-00005
PMID:16800718
Abstract

Retigabine has anticonvulsant properties that appear to be primarily mediated by opening neuronal voltage-gated potassium channels. This action has been shown in neuronal KCNQ2/3 and KCNQ3/5 potassium channels. In addition to this unique action, retigabine also potentiates GABA-evoked currents in cortical neurons at high concentrations. When used as adjunctive therapy in patients with partial seizures, retigabine 600-1200 mg/day (200-400 mg three times daily) was associated with significant linear dose-dependent reductions in monthly seizure frequency compared with placebo in a large 16-week randomised phase II trial. Median monthly seizure frequency decreased from baseline by up to 35% among patients in the retigabine treatment arms compared with 13% in the placebo group. Retigabine 1200 mg/day was also significantly more effective than retigabine 600 mg/day. Responder rates, defined as the proportion of patients with > or = 50% reduction in seizure frequency, were significantly higher among patients in the retigabine 900 and 1200 mg/day groups than in those who received placebo. CNS-related adverse events were the most commonly reported treatment-emergent adverse events associated with retigabine in clinical trials. Across all three retigabine groups in the large phase II trial, somnolence (20.3%), dizziness (14.6%), confusion (12.3%) and speech disorder (11.3%) were the most frequent CNS-related adverse events.

摘要

瑞替加滨具有抗惊厥特性,其作用似乎主要通过打开神经元电压门控钾通道介导。这种作用已在神经元KCNQ2/3和KCNQ3/5钾通道中得到证实。除了这种独特作用外,瑞替加滨在高浓度时还能增强皮质神经元中γ-氨基丁酸(GABA)诱发的电流。在一项为期16周的大型随机II期试验中,当瑞替加滨作为部分性癫痫患者的辅助治疗药物使用时,与安慰剂相比,600 - 1200毫克/天(200 - 400毫克,每日三次)的瑞替加滨与每月癫痫发作频率呈显著的线性剂量依赖性降低相关。与安慰剂组13%的降低率相比,瑞替加滨治疗组患者的每月癫痫发作频率中位数从基线水平降低了高达35%。1200毫克/天的瑞替加滨也比600毫克/天的瑞替加滨显著更有效。反应率定义为癫痫发作频率降低≥50%的患者比例,瑞替加滨900毫克/天和1200毫克/天组的患者反应率显著高于接受安慰剂的患者。在临床试验中,中枢神经系统(CNS)相关不良事件是与瑞替加滨相关的最常见的治疗中出现的不良事件。在大型II期试验的所有三个瑞替加滨组中,嗜睡(20.3%)、头晕(14.6%)、意识模糊(12.3%)和言语障碍(11.3%)是最常见的CNS相关不良事件。

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本文引用的文献

1
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Neurochem Res. 2005 Dec;30(12):1557-65. doi: 10.1007/s11064-005-8834-8.
2
Retigabine: chemical synthesis to clinical application.瑞替加滨:从化学合成到临床应用
CNS Drug Rev. 2005 Spring;11(1):1-20. doi: 10.1111/j.1527-3458.2005.tb00033.x.
3
Lack of pharmacokinetic interaction between retigabine and phenobarbitone at steady-state in healthy subjects.
Front Neurol. 2021 Jul 23;12:688362. doi: 10.3389/fneur.2021.688362. eCollection 2021.
4
K7 channels are potential regulators of the exercise pressor reflex.K7 通道可能是运动升压反射的调节因子。
J Neurophysiol. 2021 Jul 1;126(1):1-10. doi: 10.1152/jn.00700.2020. Epub 2021 May 26.
5
An Updated Overview on Therapeutic Drug Monitoring of Recent Antiepileptic Drugs.近期抗癫痫药物治疗药物监测的最新综述
Drugs R D. 2016 Dec;16(4):303-316. doi: 10.1007/s40268-016-0148-6.
6
Clinical utility of adjunctive retigabine in partial onset seizures in adults.辅助瑞替加滨治疗成人部分发作性癫痫的临床效用。
Ther Clin Risk Manag. 2012;8:7-14. doi: 10.2147/TCRM.S22605. Epub 2012 Jan 20.
7
Neuronal potassium channel openers in the management of epilepsy: role and potential of retigabine.神经元钾通道开放剂在癫痫治疗中的作用:瑞替加滨的作用及潜力
Clin Pharmacol. 2010;2:225-36. doi: 10.2147/CPAA.S15369. Epub 2010 Dec 7.
8
Novel medications for epilepsy.新型抗癫痫药物。
Drugs. 2011 Nov 12;71(16):2151-78. doi: 10.2165/11594640-000000000-00000.
9
Retigabine (ezogabine): in partial-onset seizures in adults with epilepsy.雷替加滨(依佐加滨):用于治疗成人癫痫部分发作。
CNS Drugs. 2011 Oct 1;25(10):887-900. doi: 10.2165/11205950-000000000-00000.
10
Voltage-gated potassium channels as therapeutic targets.电压门控钾通道作为治疗靶点。
Nat Rev Drug Discov. 2009 Dec;8(12):982-1001. doi: 10.1038/nrd2983.
在健康受试者中,稳态时瑞替加滨与苯巴比妥之间不存在药代动力学相互作用。
Br J Clin Pharmacol. 2003 Jul;56(1):39-45. doi: 10.1046/j.1365-2125.2003.01825.x.
4
Pharmacokinetic interaction between retigabine and lamotrigine in healthy subjects.瑞替加滨与拉莫三嗪在健康受试者中的药代动力学相互作用。
Eur J Clin Pharmacol. 2003 Apr;58(12):795-802. doi: 10.1007/s00228-003-0558-6. Epub 2003 Feb 28.
5
Effects of age and sex on the disposition of retigabine.年龄和性别对瑞替加滨处置的影响。
Clin Pharmacol Ther. 2003 Jan;73(1):61-70. doi: 10.1067/mcp.2003.12.
6
Novel anticonvulsant medications in development.正在研发的新型抗惊厥药物。
Expert Opin Investig Drugs. 2002 Oct;11(10):1387-406. doi: 10.1517/13543784.11.10.1387.
7
Multiple-dose, linear, dose-proportional pharmacokinetics of retigabine in healthy volunteers.瑞替加滨在健康志愿者中的多剂量、线性、剂量比例药代动力学。
J Clin Pharmacol. 2002 Feb;42(2):175-82. doi: 10.1177/00912700222011210.
8
Investigations into the mechanism of action of the new anticonvulsant retigabine. Interaction with GABAergic and glutamatergic neurotransmission and with voltage gated ion channels.新型抗惊厥药瑞替加滨的作用机制研究。与γ-氨基丁酸能和谷氨酸能神经传递以及电压门控离子通道的相互作用。
Arzneimittelforschung. 2000 Dec;50(12):1063-70. doi: 10.1055/s-0031-1300346.
9
Characterization of KCNQ5/Q3 potassium channels expressed in mammalian cells.在哺乳动物细胞中表达的KCNQ5/Q3钾通道的特性
Br J Pharmacol. 2001 Jan;132(2):381-4. doi: 10.1038/sj.bjp.0703861.
10
New anti-epileptic drugs.
Expert Opin Investig Drugs. 1999 Oct;8(10):1497-1510. doi: 10.1517/13543784.8.10.1497.