Drug intelligence / Profile preview

amiodarone + flecainide + propafenone + quinidine + dofetilide + sotalol + cibenzoline

Development stage
Unknown
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of seven antiarrhythmic drugs, each used to manage and prevent cardiac arrhythmias, particularly atrial fibrillation and ventricular tachyarrhythmias. These agents represent different classes within the Vaughan Williams classification system: - **Amiodarone** (Class III): A potassium channel blocker that prolongs repolarization and the action potential duration in cardiac tissue. It also has sodium channel blocking, beta-blocking, and calcium channel blocking properties. - **Flecainide** (Class IC): A sodium channel blocker with slow offset kinetics that suppresses phase 0 depolarization in cardiac cells. - **Propafenone** (Class IC): Similar to flecainide, it blocks sodium channels with slow offset kinetics but also exhibits beta-blocking activity. - **Quinidine** (Class IA): A sodium channel blocker with intermediate offset kinetics; it also blocks potassium channels to prolong repolarization. - **Dofetilide** (Class III): A selective potassium channel blocker that prolongs action potential duration without significant effects on other ion channels. - **Sotalol** (Class III/II): Both a non-selective beta-blocker and a potassium channel blocker; it prolongs repolarization while reducing adrenergic stimulation of the heart. - **Cibenzoline** (Class IA): Like quinidine, it is a sodium channel blocker with intermediate offset kinetics. These drugs are primarily indicated for rhythm control in atrial fibrillation or flutter, as well as for certain ventricular arrhythmias. Their use depends on patient-specific factors such as structural heart disease or heart failure[1][2][3][4][5][6].

02

Targets

ADRB1 (β1)SCN5A (Sodium channel protein type 5 subunit alpha)KCNH2 (Voltage-gated potassium channel subfamily H member 2)

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