Department of Neurology, Medical University of Lublin, Lublin.
Ther Clin Risk Manag. 2012;8:7-14. doi: 10.2147/TCRM.S22605. Epub 2012 Jan 20.
In ~30% of epileptic patients, full seizure control is not possible, which is why the search for novel antiepileptic drugs continues. Retigabine exhibits a mechanism of action that is not shared by the available antiepileptic drugs. This antiepileptic enhances potassium currents via Kv7.2-7.3 channels, which very likely results from destabilization of a closed conformation or stabilization of the open conformation of the channels. Generally, the pharmacokinetics of retigabine are linear and the drug undergoes glucuronidation and acetylation. Results from clinical trials indicate that, in the form of an add-on therapy, retigabine proves an effective drug in refractory epileptic patients. The major adverse effects of the add-on treatment are dizziness, somnolence, and fatigue. This epileptic drug is also considered for other conditions - neuropathic pain, affective disorders, stroke, or even Alzheimer's disease.
在约 30%的癫痫患者中,无法实现完全的癫痫发作控制,这就是为什么人们仍在继续寻找新型抗癫痫药物。瑞替加滨的作用机制与现有的抗癫痫药物不同。这种抗癫痫药物通过 Kv7.2-7.3 通道增强钾电流,这很可能是由于通道的关闭构象不稳定或开放构象稳定。一般来说,瑞替加滨的药代动力学呈线性,药物经葡萄糖醛酸化和乙酰化代谢。临床试验结果表明,作为附加治疗,瑞替加滨对难治性癫痫患者是一种有效的药物。附加治疗的主要不良反应是头晕、嗜睡和疲劳。这种抗癫痫药物也被考虑用于其他疾病,如神经病理性疼痛、情感障碍、中风,甚至阿尔茨海默病。