The aim of the present work was to evaluate the possible influence of amiodarone on some basic parameters of acute oral digoxin kinetics. A single oral dose of digoxin (0.50 mg) was administered to six healthy volunteers both before and at the end of a 7-day treatment with with amiodarone. This treatment caused a clear-cut rise in peak serum digoxin levels (Cmax) from 2.92 +/- 1.09 to 5.87 +/- 1.68 ng/ml (p less than 0.005) and a decrease of the peak time (Tmax) in four out of the six subjects. The area under the serum concentration-time curve (AUC) was increased by amiodarone with a high individual variability (30.71 +/- 6.15 vs 40.63 +/- 10.04 ng X h X ml-1). Also the 72-hour recovery of the glycoside in the urine was higher (258.77 +/- 68.41 vs 357.62 +/- 62.98 micrograms; p less than 0.01), while renal clearance (Clr) was not altered. These results show that amiodarone increases digoxin bioavailability by a mechanism which appears to be independent of changes in drug elimination.