Subject(s)
Amino Acids/chemistry , Anti-Arrhythmia Agents/toxicity , Animals , Anti-Arrhythmia Agents/chemistry , Injections, Intraperitoneal , Lethal Dose 50 , Mice , Pentanes/chemistry , Pentanes/toxicity , Structure-Activity Relationship , Trimecaine/analogs & derivatives , Trimecaine/chemistry , Trimecaine/toxicityABSTRACT
The antiarrhythmic activity and acute toxicity of polymeric formulations of quinidine, trimecaine, ethacizine, propranolol, verapamil which had been immobilized on a cellulose carrier (monocarboxylcellulose) and low molecular analogues were studied in various experimental animals (rats, mice, dogs). The polymeric formulations of trimecaine and verapamil were found to have a higher antiarrhythmic activity in different arrhythmia models than trimecaine and verapamil. The toxicity of all new compounds was no more than the values of conventional antiarrhythmic drugs.
Subject(s)
Anti-Arrhythmia Agents/therapeutic use , Phenothiazines/therapeutic use , Propranolol/analogs & derivatives , Quinidine/analogs & derivatives , Trimecaine/analogs & derivatives , Verapamil/analogs & derivatives , Animals , Anti-Arrhythmia Agents/toxicity , Arrhythmias, Cardiac/chemically induced , Arrhythmias, Cardiac/drug therapy , Arrhythmias, Cardiac/mortality , Drug Evaluation, Preclinical , Female , Male , Mice , Phenothiazines/toxicity , Polymers , Propranolol/therapeutic use , Propranolol/toxicity , Quinidine/therapeutic use , Quinidine/toxicity , Rats , Trimecaine/therapeutic use , Trimecaine/toxicity , Verapamil/therapeutic use , Verapamil/toxicitySubject(s)
Acetanilides/therapeutic use , Anti-Arrhythmia Agents/therapeutic use , Hemodynamics/drug effects , Trimecaine/therapeutic use , Adrenergic beta-Antagonists/therapeutic use , Animals , Cardiac Complexes, Premature/drug therapy , Cardiac Complexes, Premature/physiopathology , Cats , Dogs , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Drug Synergism , Drug Therapy, Combination , Time Factors , Trimecaine/toxicity , Ventricular Fibrillation/drug therapy , Ventricular Fibrillation/physiopathologyABSTRACT
It has been demonstrated in experiments on cats, rabbits, white rats and mice that the quaternary derivatives of trimecaine (QDT) produce a protective and antiarrhythmic action in atrial (acetylcholine and aconitine) and ventricular (aconitine and calcium chloride) fibrillation. The relationship has been found between the characteristics of the radical at the quaternary nitrogen atom and the antiarrhythmic activity of the QDT. The effect of the QDT on the electrophysiological parameters of the myocardium not on the hemodynamics have been examined. It has been shown that the QDT might be suggested for use as new antiarrhythmic agents.
