Literature DB >> 20508276

Retigabine: the newer potential antiepileptic drug.

Piotr Czuczwar1, Agnieszka Wojtak, Anna Cioczek-Czuczwar, Jolanta Parada-Turska, Ryszard Maciejewski, Stanisław J Czuczwar.   

Abstract

Retigabine represents an antiepileptic drug possessing a completely different mechanism of action when compared to the existing classical and newer antiepileptic drugs. In the therapeutic range, retigabine enhances potassium currents, very likely via destabilization of a closed conformation or stabilization of the open conformation of the potassium Kv7.2-7.3 channels. There are also data indicating that this drug may be a GABA enhancer. Kainate-induced status epilepticus in rats resulted in massive apoptosis in the pyriform cortex and hippocampal area - retigabine inhibited neurodegeneration only in the former brain structure. The metabolism of retigabine has nothing to do with cytochrome P450 enzymes and the drug undergoes glucuronidation and acetylation. Randomized, placebo-controlled multicenter studies have shown that retigabine produced a considerable improvement as an add-on drug in patients with partial drug-resistant epilepsy. The most prominent adverse effects due to retigabine combined with the existing antiepileptic treatment were dizziness, somnolence and fatigue. The preclinical data indicate that this antiepileptic drug may possibly be applied in patients with neuropathic pain and affective disorders. Initial clinical data suggest that retigabine may be also effective in Alzheimer's disease or stroke.

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Year:  2010        PMID: 20508276     DOI: 10.1016/s1734-1140(10)70260-7

Source DB:  PubMed          Journal:  Pharmacol Rep        ISSN: 1734-1140            Impact factor:   3.024


  7 in total

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3.  Activation of KCNQ channels located on the skeletal muscle membrane by retigabine and its influence on the maximal muscle force in rat muscle strips.

Authors:  P Zagorchev; E Apostolova; V Kokova; L Peychev
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2016-01-27       Impact factor: 3.000

4.  The new KCNQ2 activator 4-Chlor-N-(6-chlor-pyridin-3-yl)-benzamid displays anticonvulsant potential.

Authors:  A Boehlen; M Schwake; R Dost; A Kunert; P Fidzinski; U Heinemann; C Gebhardt
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Review 5.  HCN and KV7 (M-) channels as targets for epilepsy treatment.

Authors:  Mala M Shah; Zhuo Huang; Katiuscia Martinello
Journal:  Neuropharmacology       Date:  2012-03-15       Impact factor: 5.250

6.  Identification of putative potassium channel homologues in pathogenic protozoa.

Authors:  David L Prole; Neil V Marrion
Journal:  PLoS One       Date:  2012-02-21       Impact factor: 3.240

7.  Clinical utility of adjunctive retigabine in partial onset seizures in adults.

Authors:  Konrad Rejdak; Jarogniew J Luszczki; Barbara Błaszczyk; Roman Chwedorowicz; Stanislaw J Czuczwar
Journal:  Ther Clin Risk Manag       Date:  2012-01-20       Impact factor: 2.423

  7 in total

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