Nitazoxanide

(BAN, USAN, rINN)
Nitazoxanide Chemical formula
Synonyms: Nitazoxanida; Nitazoxanidum; PH-5776. N-(5-Nitro-2-thiazolyl)salicylamide acetate.
Cyrillic synonym: Нитазоксанид.

💊 Chemical information

Chemical formula: C12H9N3O5S = 307.3.
CAS — 55981-09-4.
ATC — P01AX11.

💊 Adverse Effects

The most common adverse effects associated with nitazoxanide are abdominal pain and diarrhoea. Nausea and vomiting, flatulence, and increased appetite have also been reported. Headache may occur. Other reported adverse effects include fever, malaise, pruritus, sweating, dizziness, and rhinitis. Discoloration of urine and of the eyes has been reported rarely. Increased creatinine and liver enzyme values have been noted.

💊 Pharmacokinetics

Nitazoxanide is absorbed from the gastrointestinal tract after oral dosage and is rapidly hydrolysed to an active desacetyl metabolite, tizoxanide. Tizoxanide then partially undergoes conjugation, primarily by glucuronidation. The extent of absorption is enhanced if given with food and peak plasma concentrations of tizoxanide and the glucuronide are seen 1 to 4 hours after an oral dose. The parent drug is not detected in plasma. Tizoxanide is more than 99% bound to plasma proteins. About two-thirds of an oral dose of nitazoxanide is eliminated in the faeces and one-third in the urine; tizoxanide is excreted in the urine, bile, and faeces, while the glucuronide is excreted in only the urine and bile.

💊 Uses and Administration

Nitazoxanide is used for the treatment of cryptosporidiosis and giardiasis in immunocompetent patients. It is given orally and should be taken with food. Doses are 100 mg twice daily for 3 days in those aged 1 to 3 years, 200 mg twice daily for 3 days in those aged 4 to 11 years, and 500 mg twice daily for 3 days in adults. Nitazoxanide has also been tried in a number of other protozoal and helminth infections, particularly in immunocompromised patients, including those with HIV infection. It is also being investigated for the treatment
of rotavirus disease and Clostridium difficile colitis.
1. Bailey JM, Erramouspe J. Nitazoxanide treatment for giardiasis and cryptosporidiosis in children. Ann Pharmacother 2004; 38: 634–40
2. Fox LM, Saravolatz LD. Nitazoxanide: a new thiazolide antiparasitic agent. Clin Infect Dis 2005; 40: 1173–80
3. Musher DM, et al. Nitazoxanide for the treatment of Clostridium difficile colitis. Clin Infect Dis 2006; 43: 421–7
4. Anderson VR, Curran MP. Nitazoxanide: a review of its use in the treatment of gastrointestinal infections. Drugs 2007; 67: 1947–67.

Protozoal infections.

As well as its established use in cryptosporidiosis and giardiasis, nitazoxanide has been used in other protozoal infections including intestinal amoebiasis, blastocytosis, and microsporidiosis.

Rotavirus diarrhoea.

A randomised double-blind placebocontrolled study1 in 38 young children (median age 11 months) with confirmed rotavirus diarrhoea found that oral nitazoxanide 7.5 mg/kg twice daily for 3 days significantly reduced the duration of rotavirus disease. The median time to resolution of illness after the first dose was 31 hours for those given nitazoxanide compared with 75 hours for those in the placebo group.
1. Rossignol J-F, et al. Effect of nitazoxanide for treatment of severe rotavirus diarrhoea: randomised double-blind placebo-controlled trial. Lancet 2006; 368: 124–9.

Worm infections.

Nitazoxanide has been used in various helminthiases, including ascariasis, hymenolepiasis, the liver fluke infection fascioliasis, and trichuriasis.

💊 Preparations

Proprietary Preparations

Arg.: Heliton†; Nixoran; Braz.: Annita; Mex.: Bionit; Daxon; Kidonax; Mitafar; NTZ†; Padovan Ton; Paramix; Rosanil; USA: Alinia; Venez.: Celectan. Multi-ingredient: Mex.: Heliton.
Published December 13, 2018.