The KCNQ/KV7 potassium channel opener Retigabine as add-on therapy for partial epilepsy. Pharmacological and clinical data

被引:0
|
作者
Orhan, Goekce [1 ]
Wuttke, Thomas V. [2 ,3 ,4 ,5 ]
Nies, Anne T. [6 ]
Schwab, Matthias [6 ,7 ]
Lerche, Holger [1 ]
机构
[1] Univ Tubingen, Hertie Inst Klin Hirnforsch, Abt Neurol Schwerpunkt Epileptol, D-72076 Tubingen, Germany
[2] Harvard Univ, Sch Med, Dept Neurosurg, MGH HMS Ctr Nervous Syst Repair, Boston, MA 02114 USA
[3] Harvard Univ, Sch Med, Dept Neurol, MGH HMS Ctr Nervous Syst Repair, Boston, MA 02114 USA
[4] Harvard Univ, Program Neurosci, Sch Med, Boston, MA 02114 USA
[5] Massachusetts Gen Hosp, Nayef Al Rodhan Labs, Boston, MA 02114 USA
[6] Dr Margarete Fischer Bosch Inst Clin Pharmacol, D-70376 Stuttgart, Germany
[7] Univ Klinikum Tubingen, Klin Pharmakol Abt, Inst Expt & Klin Pharmakol & Toxikol, D-72076 Tubingen, Germany
来源
PSYCHOPHARMAKOTHERAPIE | 2011年 / 18卷 / 04期
关键词
Epilepsy; potassium channel; pharmacotherapy; antiepileptic drug; retigabine; ANTICONVULSANT RETIGABINE; PHARMACOKINETIC INTERACTION; DIFFERENT PATTERNS; N-GLUCURONIDATION; HUMAN LIVER; D-23129; ACTIVATION; MODEL; CURRENTS; BINDING;
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中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The KCNQ/K(V)7 potassium channel opener Retigabine as add-on therapy for partial epilepsy. Pharmacological and clinical data This review summarizes the pharmacological, preclinical and clinical data on the new anticonvulsant compound retigabine (RGB) and discusses the impact of this drug for patients with refractory partial epilepsy. Retigabine increases the activity of voltage-gated KCNQ/K(V)7 channels and thus exhibits a novel mechanism of action as compared to available anticonvulsive drugs. Retigabine has been investigated in three multicenter, randomized, double-blind and placebo-controlled clinical phase 11 and III trials in adults with >= 4 partialonset seizures per month and showed efficacy in pharmacoresistant epilepsy. In march 2011, Retigabine received approval in Europe as Trobalt (R).
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页码:148 / +
页数:8
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