Drug/Small Molecule:

tocainide

An antiarrhythmic agent which exerts a potential- and frequency-dependent block of sodium channels. PubChem (source: Drug Bank)

For the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that, in the judgment of the physician, are life-threatening. (source: Drug Bank)

Tocainide acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers. (source: Drug Bank)

Tocainide is a primary amine analog of lidocaine with antiarrhythmic properties useful in the treatment of ventricular arrhythmias. Tocainide, like lidocaine, produces dose dependent decreases in sodium and potassium conductance, thereby decreasing the excitability of myocardial cells. In experimental animal models, the dose-related depression of sodium current is more pronounced in ischemic tissue than in normal tissue. Tocainide is a Class I antiarrhythmic compound with electrophysiologic properties in man similar to those of lidocaine, but dissimilar from quinidine, procainamide, and disopyramide. (source: Drug Bank)

Negligible first pass hepatic degradation. No active metabolites have been found. (source: Drug Bank)

Approximately 10 percent bound to plasma protein. (source: Drug Bank)

Following oral administration, the bioavailability approaches 100 percent, and is unaffected by food. (source: Drug Bank)

The oral LD₅₀ of tocainide was calculated to be about 800 mg/kg in mice, 1000 mg/kg in rats, and 230 mg/kg in guinea pigs; deaths were usually preceded by convulsions. (source: Drug Bank)

Cc1cccc(c1NC(=O)C(C)N)C (source: Drug Bank)