Metabolic fate of bromperidol in humans: comparison with rats and dogs

The metabolic fate of an oral dose of 2 mg of 3H-bromperidol has been studied in two human subjects. During 5 days, about 50% of the radioactive dose was excreted by both subjects, somewhat more in the urine than in the faeces. Excretion rates were slow. Concentrations of radioactivity in plasma were low reaching a peak of 6-10 ng equivalents/ml during 1.5-4 hours, but concentrations of the parent drug were less than 0.5 ng/ml at all times. A major metabolite, more polar than bromperidol was present in human urine and is under investigation. The metabolic fate of bromperidol in humans is different from that in rats or dogs.