Disposition and pharmacodynamics of dichloroacetate (DCA) and oxalate following oral DCA doses

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Abstract
Healthy volunteers received intravenous and/or oral doses of sodium dichloroacetate (DCA) in various single and multiple dose regimens. A crossover bioavailability study proved abortive because second and subsequent doses showed significantly longer terminal elimination half‐lives (means 3·64 h and 9·9 h, respectively) than was the case for initial doses (1·58 h). A parallel bioavailability comparison failed to show that oral doses were significantly different from 100 per cent bioavailability (AUCoral, 604μgh−1 ml−1; AUCi.v., 489μgh−1 ml−1). The time required to elapse between individual doses, in order to prevent second doses having relatively long half‐life values, varied in different individuals from 1 week to greater than 3 months. No cardiac or central nervous system effects were recorded by echocardiography and digit symbol substitution tests, respectively. The mean renal clearance of DCA was 42·9 ml h−1. No differences were observed in DCA kinetics between male and female subjects.