We studied the time course of three electrophysiologic effects of propranolol after intravenous and oral administration and their relationship with plasma levels within the same subjects. Ten patients who had undergone cardiac catheterization for diagnostic purposes received 0.1 mg/kg of propranolol intravenously. Blood was drawn at intervals for 12 hr and heart rate and the effective refractory periods of the atrium (ERPA) and the atrioventricular node (ERPAVN) were determined at the same time. Eight patients continued treatment with propranolol by the oral route for up to 4 days (40 mg every 12 hr). Blood was sampled after each morning dose. Plasma concentrations of propranolol were measured by gas chromatography. Maximal lengthening of ERPA after propranolol (15.1% i.v. and 9.4% oral) was much less marked than that of ERPAVN (23.2% i.v. and 19.4% oral). Heart rate decreased 23.5% (i.v.) and 13.1% (oral). Effects were seen much sooner after intravenous (5-8 min) than after oral administration (86-146 min), but they lasted about twice as long after oral as after intravenous treatment.