Article date: February 1980
By: EILEEN WINSLOW in Volume 71, Issue 2, pages 615-622
Antagonism of aconitine‐induced dysrhythmias in mice as a method of detecting and assessing antidysrhythmic activity was evaluated.
Aconitine‐induced dysrhythmias in mice appear to be selectively sensitive to antidysrhythmic agents (administered intraperitoneally) which reduce the inward sodium current in cardiac cells.
Antidysrhythmic agents whose mechanism of action is thought to depend on β‐adrenoceptor blockade, prolongation of cardiac monophasic action potentials or calcium antagonism are ineffective in delaying the onset of aconitine‐induced dysrhythmias in mice. The inactive drugs were practolol, sotalol, bretylium, amiodarone and verapamil.
Comparisons of anti‐dysrhythmic activities of test drugs should be based on more than one ED value and should take account of efficacy as well as potency.
The mouse aconitine test is a useful and rapid method of evaluating oral antidysrhythmic activity in terms of potency, efficacy and duration of action.
With respect to potency, efficacy, oral activity, duration of action and safety, 3α‐amino‐5α‐androstan‐2β‐ol‐17‐one hydrochloride (Org 6001) offered the most satisfactory overall profile of the active drugs tested (Org 6001, aprindine, quinidine, disopyramide, lignocaine, mexiletine, procainamide and propranolol).
Antagonism of aconitine‐induced dysrhythmias in mice as a method of detecting and assessing antidysrhythmic activity was evaluated.
Aconitine‐induced dysrhythmias in mice appear to be selectively sensitive to antidysrhythmic agents (administered intraperitoneally) which reduce the inward sodium current in cardiac cells.
Antidysrhythmic agents whose mechanism of action is thought to depend on β‐adrenoceptor blockade, prolongation of cardiac monophasic action potentials or calcium antagonism are ineffective in delaying the onset of aconitine‐induced dysrhythmias in mice. The inactive drugs were practolol, sotalol, bretylium, amiodarone and verapamil.
Comparisons of anti‐dysrhythmic activities of test drugs should be based on more than one ED value and should take account of efficacy as well as potency.
The mouse aconitine test is a useful and rapid method of evaluating oral antidysrhythmic activity in terms of potency, efficacy and duration of action.
With respect to potency, efficacy, oral activity, duration of action and safety, 3α‐amino‐5α‐androstan‐2β‐ol‐17‐one hydrochloride (Org 6001) offered the most satisfactory overall profile of the active drugs tested (Org 6001, aprindine, quinidine, disopyramide, lignocaine, mexiletine, procainamide and propranolol).
DOI: 10.1111/j.1476-5381.1980.tb10981.x
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