Nitazoxanide appears to interfere with the PFOR enzyme-dependent electron-transfer reaction, which is essential in anaerobic metabolism. No resistance to nitazoxanide in infectious agents previously known to be susceptible to the drug has yet been reported.
ABSORPTION, FATE, AND EXCRETION
Following oral administration, nitazoxanide is hydrolyzed rapidly to its active metabolite tizoxanide, which undergoes conjugation primarily to tizoxanide glucuronide. Bioavailability after an oral dose is excellent, and maximum plasma concentrations of metabolites are detected within 1—4 hours of administration of the parent compound. Tizoxanide is >99.9% bound to plasma proteins. Tizoxanide is excreted in the urine, bile, and feces, whereas tizoxanide glucuronide is excreted in urine and bile.
THERAPEUTIC USES In the U.S., nitazoxanide (alinia) is available as an oral suspension and as tablets. It is approved for the treatment of G. intestinalis infections in adults and in children and for the treatment of diarrhea in children under 12 caused by cryptosporidia. The efficacy of nitazoxanide in children (or adults) with cryptosporidia infection and AIDS is not clearly established. For children between the ages of 12 and 47 months, the recommended dose is 100 mg every 12 hours for 3 days; for children between 4 and 11 years of age, the dose is 200 mg every 12 hours for 3 days. A 500-mg nitazoxanide tablet, suitable for adult dosing (every 12 hours), is not available in the U.S.
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