Eleven healthy subjects received five doses of intravenous sodium dichloroacetate (DCA) at 2-hr intervals. Determinations of DCA in plasma and of lactate and glucose in blood were made at various times until 24 hr after starting the first infusion. Twenty-four-hour urinary oxalate excretion was also measured. DCA levels rose and fell during and after each dose, with higher levels induced by higher doses. Lactate levels fell as the result of DCA treatment, with greater falls after higher doses, and returned to normal after 24 hr at the two lower dose levels but not at the level of 50 mg/kg. Lactate levels did not change parallel to changes in DCA levels. Only the doses of 50 mg/kg prevented postprandial rises in lactate levels. Blood glucose levels were not altered. The mean DCA t1/2 after the initial doses was 63.3 min (range 15.0 to 112.2 min), while that after the final doses was 374.0 min (range 37.8 to 1386.0 min). The AUC and the DCA-induced increase in urinary oxalate excretion were linearly related to dose. Mean DCA apparent volume of distribution was 0.30 l/kg (range 0.09 to 0.60 l/kg).