Anti-arrhythmic, local anaesthetic, and adrenergic blocking activity of some beta-receptor antagonists.
1. The antagonistic effect of the beta-receptor blocking compounds propranolol, Ph QA 33 and INPEA on ouabain-induced cardiac fibrillations in guinea-pigs was compared with their local anaesthetic and beta-receptor blocking properties.2. All three compounds were found capable of increasing the tolerance to ouabain and of reversing ouabain-induced fibrillations, the ED50 being 0.3 mg/kg intravenously, 0.5 mg/kg intravenously, and 1.5 mg/kg intravenously, respectively for propranolol, Ph QA 33 and INPEA.3. Propranolol and Ph QA 33 were found to be moderate to strong local anaesthetics while INPEA had a considerably weaker though significant effect.4. The order of potency as beta-receptor blocking compounds was propranolol >/= Ph QA 33 >> INPEA, the latter compound being less than 1% as active as propranolol.5. Despite the surprising finding that INPEA was effective against non-catecholamine-induced arrhythmias, the results support the general assumption that the anti-arrhythmic effect of beta-receptor blocking compounds is related to their local anaesthetic action rather than to their beta-blocking ability.
D000605:Amino Alcohols / Q000494:pharmacology*; D000772:Anesthesia, Local; D000779:Anesthetics, Local / Q000494:pharmacology; D000818:Animals; D001145:Arrhythmias, Cardiac / Q000188:drug therapy*; D001282:Atrial Flutter / Q000139:chemically induced; D003315:Cornea / Q000187:drug effects; D006168:Guinea Pigs; D007275:Injections, Intravenous; D008297:Male; D009578:Nitrobenzenes / Q000494:pharmacology*; D010042:Ouabain / Q000037:antagonists & inhibitors; D011433:Propranolol / Q000494:pharmacology*; D013565:Sympatholytics / Q000494:pharmacology*
D000605:Amino Alcohols; D000779:Anesthetics, Local; D009578:Nitrobenzenes; D013565:Sympatholytics; D010042:Ouabain; D011433:Propranolol