Benznidazole

N- benzyl-2- nitroimidazole -1 - ylacetamide

P01CA02

Antiprotozoic

189 ° C.

400 mg · l - 1 in water

Attention

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Benznidazole (trade name, among others Rochagan ® ( BR); initial manufacturer Hoffmann -La Roche) is a drug from the group of nitroimidazoles, which is used in the treatment of the acute phase of Chagas disease.

Clinical information

Benznidazole is recommended by the WHO for the treatment of acute Chagas disease. The effectiveness of chronic disease is controversial and is currently being tested in a co-sponsored by the WHO clinical trial. The use of benznidazole is limited by some significant side effects. The most serious are thrombocytopenic purpura and agranulocytosis; in such cases, the therapy must be discontinued immediately.

Pharmacological properties

Benznidazole acts via the generation of free radicals during its metabolism. The causative agent of Chagas disease, Trypanosoma cruzi, is very sensitive to free radicals because enzymes to break down such radicals are missing or have only low activity. In animal studies, after administration of benznidazole damage to the adrenal gland, colon and esophagus were observed. Benznidazole is considered to be mutagenic and carcinogenicity was demonstrated in some non-clinical studies, but it was found in treated patients have no evidence for such effects in humans. The nitro group of the substance must be reduced enzymatically for the toxic effect.

Other Information

Benznidazole was developed in the early 1970s at Roche (Ro - 71051 ). Since the early 1980s, it is next to nifurtimox the standard treatment for Chagas disease in Latin America; WHO has benznidazole added to the list of the indispensable drug. In Europe and the U.S. does not benznidazole preparations are approved; benznidazole in Latin America is in the form of tablets containing 100 mg of the market.