Nitazoxanide

[6] Chemically, nitazoxanide is the prototype member of the thiazolides, a class of drugs which are synthetic nitrothiazolyl-salicylamide derivatives with antiparasitic and antiviral activity.

[1] It is also an effective treatment option for infections caused by other protozoa and helminths (e.g., Entamoeba histolytica,[13] Hymenolepis nana,[14] Ascaris lumbricoides,[15] and Cyclospora cayetanensis[16]).

Seven of 8 HBeAg-negative patients treated with nitazoxanide 500 mg twice daily had undetectable HBV DNA and 2 had loss of HBsAg.

The authors concluded that more randomized trials with low risk of bias are needed to determine if Nitazoxanide can be used as an effective treatment for chronic hepatitis C patients.

[1] The anti-protozoal activity of nitazoxanide is believed to be due to interference with the pyruvate:ferredoxin oxidoreductase (PFOR) enzyme-dependent electron-transfer reaction that is essential to anaerobic energy metabolism.

[24] The mechanism appears to be by selectively blocking the maturation of the viral hemagglutinin at a stage preceding resistance to endoglycosidase H digestion.

[23] Following oral administration, nitazoxanide is rapidly hydrolyzed to the pharmacologically active metabolite, tizoxanide, which is 99% protein bound.

It is a broad-spectrum anti-infective drug that significantly modulates the survival, growth, and proliferation of a range of extracellular and intracellular protozoa, helminths, anaerobic and microaerophilic bacteria, in addition to viruses.

IUPAC Name: [[[2-[(5-nitro-1,3-thiazol-2-yl)carbamoyl]phenyl] acetate2]][26] Canonical SMILES: CC(=O)OC1=CC=CC=C1C(=O)NC2=NC=C(S2)N+[O-]2[27] MeSH Synonyms: 1) 2-(acetolyloxy)-n-(5-nitro-2-thiazolyl)benzamide 2) Alinia 3) Colufase 4) Cryptaz 5) Daxon 6) Heliton 7) Ntz 8) Taenitaz[28] Nitazoxanide was originally discovered in the 1980s by Jean-François Rossignol at the Pasteur Institute.

Initial studies in the USA were conducted in collaboration with Unimed Pharmaceuticals, Inc. (Marietta, GA) and focused on development of the drug for treatment of cryptosporidiosis in AIDS.

A placebo-controlled study of nitazoxanide in cryptosporidiosis demonstrated significant clinical improvement in adults and children with mild illness.

In Zambia and in a study conducted in Mexico, nitazoxanide was not successful in the treatment of cryptosporidiosis in advanced infection with human immunodeficiency virus at the doses used.

[1] An extended release tablet (675 mg) has been used in clinical trials for chronic hepatitis C; however, this form is not currently marketed or available for prescription.

[20] Nitazoxanide is sold under the brand names Adonid, Alinia,[30] Allpar, Annita, Celectan, Colufase, Daxon, Dexidex, Diatazox, Kidonax, Mitafar, Nanazoxid,[31] Parazoxanide, Netazox, Niazid, Nitamax, Nitax, Nitaxide, Nitaz, Nizonide, NT-TOX, Pacovanton, Paramix, Toza, and Zox.