Dichloroacetate tissue concentrations and its relationship to hypolactatemia and pyruvate dehydrogenase activation.

Following a single oral dose of DCA to laboratory rats, peak hepatic tissue DCA concentration occurred at 3 hr. When given chronically for 7 days, DCA caused activation of the pyruvate dehydrogenase complex which returned to basal activity 24 hr following the final dose. Hepatic tissue DCA concentrations were maximally increased at 3 hr following the final dose, and the drug was eliminated slowly over 72 hr with a half-life of 9.74 hr. Liver and muscle showed similar DCA tissue concentrations following chronic administration.