Department of Pharmacy: Clinical and Administrative Sciences, University of Oklahoma Health Sciences Center, College of Pharmacy, Oklahoma City, Oklahoma, USA.
Clin Ther. 2012 Sep;34(9):1845-56.e1. doi: 10.1016/j.clinthera.2012.07.009. Epub 2012 Aug 21.
Ezogabine, also known as retigabine, is a recently approved anticonvulsant medication with a novel mechanism of action. It activates low-threshold voltage-gated potassium channels, leading to hyperpolarization of the membrane potential, stabilization of the resting membrane potential, and suppression of repetitive firing.
This review identified the efficacy and tolerability of ezogabine in the treatment of partial-onset seizures reported in randomized controlled trials. Additional characteristics of the medication, including mechanism of action, pharmacokinetic properties, drug interactions, and additional applications under investigation are also addressed.
MEDLINE and EMBASE were systematically searched, using the search terms retigabine and ezogabine, for randomized trials published from 1980 through February 8, 2012. Trials of the effects of adjunctive ezogabine in patients aged ≥16 years with partial seizures were included for analysis of clinical efficacy and tolerability. Articles that did not pertain to clinical efficacy and that did not report on randomized controlled trials were excluded. Articles relating to additional properties were reviewed for inclusion in the review.
One Phase IIb and 2 Phase III trials were identified. Ezogabine has reported dose-dependent efficacy at doses of 600, 900, and 1200 mg/d. As with most anticonvulsant medications, the most common adverse events associated with ezogabine were central nervous system effects. Because potassium channels in the urothelium of the bladder are activated by ezogabine, a Risk Evaluation and Mitigation Strategy is in place regarding the risk for urinary retention and symptoms of acute urinary retention. There are limited drug interactions with ezogabine because it does not undergo metabolism by the cytochrome P450 system and is not highly protein bound.
Ezogabine is a newly approved anticonvulsant for adjunctive therapy in partial-onset seizures in adults with a novel mechanism of action, activating low-threshold voltage-gated potassium channels. It has advantages over many of the available anticonvulsants in that it is not metabolized through the cytochrome P450 system and is not highly protein bound, therefore limiting its potential for drug-drug interactions. Unique to ezogabine compared with other anticonvulsants is its association with urinary retention due to its effect on potassium channels in the urothelium of the bladder.
依佐加滨，也称为瑞替加滨，是一种最近批准的抗癫痫药物，具有新颖的作用机制。它激活低阈值电压门控钾通道，导致膜电位超极化、静息膜电位稳定和重复放电抑制。
本综述确定了依佐加滨在随机对照试验中治疗部分发作性癫痫的疗效和耐受性。还介绍了药物的其他特征，包括作用机制、药代动力学特性、药物相互作用以及正在研究的其他应用。
系统检索 MEDLINE 和 EMBASE，使用检索词瑞替加滨和依佐加滨，检索 1980 年至 2012 年 2 月 8 日发表的随机试验。纳入分析临床疗效和耐受性的年龄≥16 岁部分发作性癫痫患者辅助应用依佐加滨的试验。排除与临床疗效无关且未报告随机对照试验的文章。审查与其他特性相关的文章，以纳入综述。
确定了 1 项 IIb 期和 2 项 III 期试验。依佐加滨在 600、900 和 1200mg/d 的剂量下具有剂量依赖性疗效。与大多数抗癫痫药物一样，依佐加滨最常见的不良反应是中枢神经系统效应。由于膀胱尿路上皮的钾通道被依佐加滨激活，因此存在与尿潴留和急性尿潴留症状相关的风险评估和缓解策略。依佐加滨与药物的相互作用有限，因为它不通过细胞色素 P450 系统代谢，也不高度结合蛋白。
依佐加滨是一种新批准的抗癫痫药物，用于成人部分发作性癫痫的辅助治疗，具有新颖的作用机制，激活低阈值电压门控钾通道。与许多现有抗癫痫药物相比，它具有优势，因为它不通过细胞色素 P450 系统代谢，也不高度结合蛋白，因此限制了其与药物相互作用的潜力。与其他抗癫痫药物相比，依佐加滨独特的是它与尿潴留有关，这是由于它对膀胱尿路上皮钾通道的作用。
