Nitazoxanide

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Abstract
Nitazoxanide (Alinia®, Daxon®, Dexidex®, Paramix®, Kidonax®, Colufase®, Annita®) has in vitro activity against a variety of microorganisms, including a broad range of protozoa and helminths. Nitazoxanide is effective in the treatment of protozoal and helminthic infections, including Cryptosporidium parvum or Giardia lamblia, in immunocompetent adults and children, and is generally well tolerated. Nitazoxanide is a first-line choice for the treatment of illness caused by C. parvum or G. lamblia infection in immunocompetent adults and children, and is an option to be considered in the treatment of illnesses caused by other protozoa and/or helminths. Nitazoxanide is a nitrothiazolyl-salicylamide derivative that is thought to inhibit the pyruvate:ferredoxin/flavodoxin oxidoreductase enzyme-dependent electron transfer reaction. This prodrug is metabolised to form the main active metabolite, tizoxanide. The in vitro activity of nitazoxanide and tizoxanide has been demonstrated against a wide range of organisms, including the protozoal species Blastocystis hominis, C. parvum, Entamoeba histolytica, G. lamblia and Trichomonas vaginalis. In addition, the in vitro activity of anaerobic bacteria and rotavirus have been shown to be inhibited by nitazoxanide. Over 99% of tizoxanide formed after a dose of nitazoxanide is protein bound in the plasma and the bioavailability of tizoxanide is increased when nitazoxanide is administered with food. The bioavailability of the nitazoxanide suspension is 70% relative to the nitazoxanide tablets. The maximum plasma tizoxanide concentration in adults is reached 3.5 hours after oral administration of nitazoxanide 500mg (twice daily for 7 days). Tizoxanide is excreted in the urine (one-third) and faeces (two-thirds). The mean terminal elimination half-life of tizoxanide in adults is 1.8 hours. There appears to be no inhibition of cytochrome P450 enzymes by tizoxanide and no drug interactions have been reported. In well controlled clinical trials, clinical and parasitological cure rates were higher with nitazoxanide than with placebo in adults and children infected with a range of protozoa including C. parvum, G. lamblia, B. hominis and E. histolytica. The clinical cure rates with nitazoxanide were similar to those with metronidazole in paediatric patients with G. lamblia infection.Nitazoxanide was as effective as albendazole and praziquantel in the treatment of ascariasis and hymenolepiasis in children. In patients with trichuriasis, nitazoxanide was significantly more effective than albendazole in the subgroup of patients with light infections, but not in the overall study population. In children and/or adults with mixed protozoal and helminth infections, nitazoxanide was as effective as mebendazole and/or quinfamide or albendazole. Although nitazoxanide was not effective in achieving clinical or parasitological cure in the intent-to-treat population of hospitalised children with HIV and C. parvum infection, higher parasitological cure rates than those with placebo were obtained in the subgroup of evaluable adults and in those with CD4+ counts >50µL. In a compassionate-use open-label study, approximately two-thirds of the patients with HIV and C. parvum infection had a clinical cure. Nitazoxanide has also shown efficacy against nonindicated organisms; nitazoxanide was more effective than placebo in the treatment of rotavirus infection in children and viral gastroenteritis in adults, and noninferior to metronidazole in the treatment of Clostridium difficile infection. Nitazoxanide at various dosages is generally well tolerated in immunocompetent adults, adolescents and children. The majority of adverse events are mild in severity and are usually associated with the gastrointestinal system. The most frequently reported adverse events in both adults, adolescents and children include abdominal pain, headache, diarrhoea and nausea. Adverse events have led to discontinuation of treatment in none of the children and in <1% of adults, and no clinically significant changes in laboratory parameters have been reported.

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