SULFADIAZINE AND SODIUM SULFADIAZINE: A COMPARISON OF CERTAIN OF THEIR CLINICAL AND PHARMACOLOGIC VALUES

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Abstract
The absorption, excretion, acetylation, diffusion and toxicity of sulfadiazine given orally and of Na sulfadiazine given both orally and intraven. were studied in 218 patients who received these drugs over long periods of time. It was observed that sulfadiazine given orally yields a higher concn. of free drug in the blood and smaller proportions of acetylated drug in the blood and in the urine than do any of the other sulfonamide drugs in general use, except sulfanilamide. Na sulfadiazine given orally yields even higher concns. of free drug in the blood than does sulfadiazine, and like the latter is acetylated to only a slight degree in the blood and urine. Initial doses of 4 g. of both sulfadiazine and Na sulfadiazine were much more effective than initial doses of 2 g. in establishing high concs. in the blood, were acetylated to only a slight degree, and were relatively non-toxic. The toxic reactions observed after treatment with sulfadiazine and Na sulfadiazine were of the same general type as those observed after other sulfonamide drugs but were less frequent and less severe. Nausea and vomiting, anemia, agranulocytosis. jaundice, cerebral effects and cyanosis were not observed at all. On the basis of these facts it appears that pharmacologically sulfadiazine and Na sulfadiazine possess definite advantages over the other sulfonamide drugs in general use.