Retigabine: the newer potential antiepileptic drug.
Journal Title: Pharmacological Reports - Year 2010, Vol 62, Issue 2
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.
Authors and Affiliations
Piotr Czuczwar, Agnieszka Wojtak, Anna Cioczek-Czuczwar, Jolanta Parada-Turska, Ryszard Maciejewski, Stanisław Czuczwar
Keywords
Related Articles
- EP ID EP129213
- DOI -
- Views 95
- Downloads 0
Prodrugs: A challenge for the drug development.
It is estimated that about 10% of the drugs approved worldwide can be classified as prodrugs. Prodrugs, which have no or poor biological activity, are chemically modified versions of a pharmacologically active agent, whi...
ESR techniques for the detection of nitric oxide in vivo as an index of endothelial function.
Plasma nitrite/nitrate levels reflect oxidation of formed nitric oxide (NO ) but are not indicative of endothelial nitric oxide synthase (eNOS) function due to interference by dietary nitrates and reactive oxygen species...
Vane blood-bathed technique reveals the significance of adrenergic reaction in myocardial infarction.
Using the blood-bathed technique of Vane we induced acute coronary occlusion in the dog and subsequently detected adrenaline release into the circulatory system, determined the rate of release and documented its signific...
Pulmonary endothelium in the perinatal period.
The pulmonary circulation is the only system in the body which does not have a dress rehearsal in utero. The pulmonary endothelium plays a pivotal role in ensuring that the resistance falls rapidly after birth so that th...
Antiproliferative activity of various Uncaria tomentosa preparations on HL-60 promyelocytic leukemia cells.
The woody Amazonian vine Uncaria tomentosa (cat's claw) has been recently more and more popular all over the world as an immunomodulatory, antiinflammatory and anti-cancer remedy. This study investigates anti-proliferati...