Studies on 3, 4-Dimethyl-5-Sulfanilamido-Isoxazole (Nu-445) in Humans.

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Abstract
A new sulfonamide prepn. has been presented which, on the basis of its high solubility in buffer soln.,would be expected to greatly diminish the danger of sulfonamide crystallization in the kidney, with or without the concomitant adm. of alkali. Neither crystallization nor the signs of renal irritation in the absence of crystallization were observed. The antibacterial activity in vivo and in vitro and the low toxicity in animals combined to recommend an investigation of the clinical pharmacology of this compound. The blood and urine levels attained were found to be satisfactory and they were achieved and maintained with an 8-hr, dosage schedule. The entry of this drug into the spinal fluid of the normal individual is low, but in the presence of meningeal inflammation it was markedly increased in the one patient studied. The toxicity of the compound is low.
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