Азимилид

Использование

Cardiac depressant (anti-arrhythmic).

Общее описание

Azimilide, E-1-[[[5-(4-chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl]-2,4-imidazolidinedione, is a class III agent that significantlyblocks the delayed rectifier potassium current,Iks, including the Ikr component. Its ability to block multichannelsmay be caused by a lack of the methane sulfonamidegroup that is common to other class III agents, whichselectively block the Ikr potassium current. It is believedthat blocking both Ikr and Iks potassium currents yields consistentclass III antiarrhythmic effects at any heart rate.

Клиническое использование

Azimilde is another Class III antiarrhythmic agent structurally unrelated to any of the above agents. Azimilide is not available in the United States; it is only available in Europe. Following oral administration, the drug is completely absorbed, with no effect of food. Protein binding is 94%. It is metabolized in the liver to an active carboxylate metabolite, but its concentration in plasma is less than 5% of the parent compound. Thus, it is considered to be therapeutically inactive. Renal excretion is approximately 10%. Its elimination half-life is 3 to 4 days.

Ферментативный ингибитор

This class ΙΙΙ antiarrhythmic drug and ion channel blocker (FW = 457.95 g/mol; CAS 149908-53-2), also known by the code name NE-10064 and systematic name, 1-({(E)-[5-(4-chlorophenyl)furan-2-yl]methylidene} amino)-3-[4-(4-methylpiperazin-1-yl)butyl]-imidazolidine-2,4-dione, blocks both the slow-activating IKs and rapidly activating IKr components of the delayed rectifier potassium current, distinguishing its action from conventional potassium channel blockers such as sotalol and dofetilide,which block only IKr. Azimilide prolongs the cardiac refractory period in a dose-dependent manner, as manifested by increases in action potential duration, QTc interval, and effective refractory period.