Tocainide antiarrhythmic effect

Nyquist O, Forssell G, Nordlander R, Schenck-Gustafsson K. Hemodynamic and antiarrhythmic effects of tocainide in patients with acute myocardial infarction. Am Heart J 1980 100(6 Pt 2) 1000-5. 

Mechanism of action. Na -channel blocking antiarrhythmics resemble most local anesthetics in being cationic amphiphilic molecules (p.206 exception phenytoin, p.191). Possible molecular mechanisms of their inhibitory effects are outlined on p.202 in more detail. Their low structural specificity is reflected by a low selectivity toward different cation channels. Besides the Na channel. Carotid 1C channels are also likely to be blocked. Accordingly, cationic amphiphilic antiarrhythmics affect both the depolarization and repolarization phases. Depending on the substance, AP duration can be increased (Class IA), decreased (Class IB), or remain the same (Class IC). Antiarrhythmics representative of these categories include Class IA—quinidine, procainamide, ajmaline, disopyramide Class IB—lidocaine, mexile-tine, tocainide Class IC—flecainide, propafenone. 

Moricizine (600 to 900 mg/day given every 8 hours in three equally divided doses) is indicated in the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that are life threatening. Because of the proarrhythmic effects of moricizine, its use should be reserved for patients in whom the benefits of treatment outweigh the risks. Moricizine is a class 1C antiarrhythmic agent with potent local anesthetic activity and myocardial-membrane-stabilizing effects. It shares some of the characteristics of the class lA (disopyramide, procainamide, or quinidine), of class IB (lidocaine, mexiletene, phenytoin, or tocainide), or class 1C agents (encainide, flecainide, or propafenone) in that it reduces the fast inward current carried by sodium ions. Moricizine shortens phase 2 and 3... 

For this reason, tolycaine lacks any CNS side effects, even though it still contains the N-ethyl groups. It should be noted, however, that both tocainide and tolycaine are primarily used clinically as antiarrhythmic agents. 

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