Absorption and urinary excretion of 2-14C-L-alpha-methyldopa (alpha MD) were investigated in 5 healthy human volunteers. The drug was administered alone, with a mixture of amino acids and with a meal consisting of roast beef. The radioactivity in plasma and urine was not decreased significantly by either treatment, and it was concluded that the overall absorption of the drug was virtually unchanged. The amount of unconjugated alpha MD in plasma and urine, however, was significantly decreased following administration of the drug with roast beef. As the acid labile conjugates of alpha MD were practically unchanged an increased biotransformation to other metabolites owing to the protein rich meal was suggested more probable than competition between alpha MD and amino acids in the specific transport systems.