Metabolism and urinary excretion of esmolol in humans.

The urinary excretion patterns of esmolol, a short-acting beta blocker, and its major metabolite were investigated in eight healthy men after intravenous infusion of 50, 100, 200, and 300 micrograms/kg/min of esmolol for six hours and 150 micrograms/kg/min for 24 hours. Esmolol and the metabolite concentrations in urine were determined by high-performance liquid chromatography. The mean urinary recoveries of the unchanged drug were 0.64%, 0.67%, 0.69%, 0.77%, and 0.98% after the 50, 100, 150, 200, and 300 micrograms/kg/min dose, respectively. Recovery of the metabolite was independent of dose, and the overall mean recovery accounted for 73% of administered dose. The results of this study indicate that esmolol is extensively metabolized, and the extent of the metabolism is not dose related in the dosage range used. The renal route plays a very minor role in the elimination of the drug but is important for the elimination of the metabolite.