Furazolidone and nitrofurantoin, oral nitrofuran derivatives with broad-spectrum antimicrobial properties already in clinical use, were compared for activity against Pneumocystis carinii in an immunosuppressed rat model of P. carinii pneumonia. Furazolidone exhibited only slight activity as a prophylactic agent but was moderately effective in the therapy of pneumocystosis. The median histologic score and organism count fell from 4+ and 10(8) to 10(9) cysts per lung, respectively, in the controls to 1+ to 2+ and 10(7) to 10(8) cysts per lung, respectively, in the furazolidone-treated groups. However, these results were not as good as those obtained with the standard drug, trimethoprim-sulfamethoxazole (0+, 10(6) to 10(7) cysts per lung). Nitrofurantoin showed little anti-P. carinii activity despite different doses or drug preparations. The high doses of furazolidone used here and their toxic effects on the rats will probably discourage investigation of this drug in the treatment of pneumocystosis in humans. Nevertheless, since many nitrofurans have been synthesized, further exploration of this class of compounds might be helpful in developing new anti-P. carinii agents or in studying structure-activity relationships
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