Pharmacological action
Venakaran works by blocking peak sodium currents by blocking overdrive-activated delayed rectifier currents (IKur). IKur, encoded by the Kv1.5 channel protein, is abundantly expressed in atrial myocytes, is the main current mediating atrial repolarization in humans, and is activated during atrial fibrillation. Venakalan inhibition of IKur can prolong the action potential duration of the atrium, thereby prolonging the atrial effective refractory period and slowing down atrial conduction, so as to shorten the time of atrial fibrillation and quickly achieve the effect of atrial fibrillation conversion.
Description
Vernakalant is a potassium channel blocker that was approved in
Europe in 2010 for treatment of atrial fibrillation (AF), a condition of
cardiac arrhythmia in which the atria of the heart beat irregularly due to
changes in cardiac ion channel function and distribution.
Vernakalant has activity for cardiac Na+ and K+ channels and also for the
atrial-selective Kv1.5 channel. Vernakalant (RSD1235) was characterized
in animal models to assess efficacy, atrial selectivity, and reduction in side effects.
Originator
Cardiome Pharma Corp. (Canada)
Definition
ChEBI: Vernakalant is an alcohol and a member of phenols.
