Tocainidum
Tocainidum Uses, Dosage, Side Effects, Food Interaction and all others data.
An antiarrhythmic agent which exerts a potential- and frequency-dependent block of sodium channels.
Tocainidum is a primary amine analog of lidocaine with antiarrhythmic properties useful in the treatment of ventricular arrhythmias. Tocainidum, 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. Tocainidum is a Class I antiarrhythmic compound with electrophysiologic properties in man similar to those of lidocaine, but dissimilar from quinidine, procainamide, and disopyramide.
| Trade Name | Tocainidum |
| Availability | Discontinued |
| Generic | Tocainide |
| Tocainide Other Names | Tocainida, Tocainide, Tocainidum |
| Related Drugs | propranolol, amiodarone, lidocaine, verapamil, sotalol, magnesium sulfate, Inderal, dofetilide, acebutolol, Epsom Salt |
| Type | |
| Formula | C11H16N2O |
| Weight | Average: 192.2575 Monoisotopic: 192.126263144 |
| Protein binding | Approximately 10 percent bound to plasma protein. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Tocainidum is an orally active class 1b antiarrhythmic agent that interferes with cardiac sodium channels and typically used to treat ventricular arrhythmias.
For the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that, in the judgment of the physician, are life-threatening.
How Tocainidum works
Tocainidum acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. Tocainidum binds preferentially to the inactive state of the sodium channels.The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers.
Toxicity
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.
Tocainidum Drug Interaction
Moderate: carvedilol, metoprololUnknown: spironolactone, trolamine salicylate topical, ipratropium, amoxicillin / clavulanate, sulfamethoxazole / trimethoprim, diphenhydramine, dicyclomine, bumetanide, ergocalciferol, ciprofloxacin, ubiquinone, docusate, colchicine, albuterol / ipratropium, warfarin, apixaban, sacubitril / valsartan, ascorbic acid
Tocainidum Disease Interaction
Major: cardiovascular dysfunction, proarrhythmic effectsModerate: electrolyte imbalance
Elimination Route
Following oral administration, the bioavailability approaches 100 percent, and is unaffected by food.
Half Life
The average plasma half-life in patients is approximately 15 hours. May be prolonged up to 35 hours in patients with severe renal function impairment (creatinine clearance less than 30 mL per min per 1.73 square meters of body surface area.
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