Bisaramil (hydrochloride)

Bisaramil hydrochloride is an antiarrhythmic compound with activity in inhibiting free radical generation. Bisaramil hydrochloride directly blocks sodium currents and exhibits enhanced sodium channel blocking ability. Bisaramil hydrochloride inhibits isoproterenol-induced slow calcium action potentials in cardiomyocytes. Bisaramil hydrochloride reduces heart rate and prolongs the PR, QRS, and QT intervals in the electrocardiogram, showing blocking effects on sodium and potassium channels. Bisaramil hydrochloride reduces cardiac conduction velocity, increases the threshold current for capture and atrial fibrillation, and prolongs the effective refractory period. Bisaramil hydrochloride reduces ventricular arrhythmias and eliminates mortality caused by ventricular fibrillation in ischemic rat hearts[1].

[1]M K Pugsley, et al. Effects of bisaramil, a novel class I antiarrhythmic agent, on heart, skeletal muscle and brain Na+ channels. Eur J Pharmacol. 1998 Jan 19;342(1):93-104.|[2]M Paróczai, et al. Bisaramil and antiarrhythmics as inhibitors of free radical generation. Pharmacol Res. 1997 Apr;35(4):279-85.|[3]The antiarrhythmic actions of bisaramil and penticainide result from mixed cardiac ion channel blockade