Product Name

Tocainide

CAS Number

41708-72-9

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Product Name:
Tocainide
CAS Number:
41708-72-9
Indication:
For the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that, in the judgment of the physician, are life-threatening.
Mode of Action:

Tocainide acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. Tocainide binds preferentially to the inactive state of the sodium channels.The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers.

Pharmacodynamics:

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.

Metabolism:

Negligible first pass hepatic degradation. No active metabolites have been found.

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.

IUPAC:
2-amino-N-(2, 6-dimethylphenyl)propanamide
ATC:
C01BB03
PubChem:
38945
DrugBank:
DB01056 (APRD01266)
Formula:
C10H12N2
Molecular Mass:
192.2575
Synonyms:
Tocainida [INN-Spanish] Tocainidum [INN-Latin]
SMILES:
CC(N)C(=O)NC1=C(C)C=CC=C1C
InChi:
BUJAGSGYPOAWEI-UHFFFAOYSA-N

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