Benznidazole

260.25

260.25

200-659-6

YC42NRJ1ZD

299972

DTXSID9046570

C1013

White to Off-White

P - Antiparasitic products, insecticides and repellents

0.91 (LogP)

1.35±0.1 g/cm3(Predicted)

189-192 °C (lit.)

0.4g/L(temperature not stated)

14+-.0.46(Predicted)

Sealed in dry,Room Temperature

3

Xi

26-36

NI3340000

36/37/38

|Warning|H315 (97.44%): Causes skin irritation [Warning Skin corrosion/irritation]|P261, P264, P271, P280, P302+P352, P304+P340, P305+P351+P338, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 39 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

At clinically relevant dosages, benznidazole can produce hepatotoxicity, peripheral neuropathy, and angioedema.

Benznidazole therapy is associated with an appreciable rate of serum enzyme elevations, found in at least 10% of patients. The abnormalities, however, are generally mild, transient and without accompanying symptoms or jaundice. In clinical trials there were no reported instances of clinically apparent liver injury with jaundice attributed to benznidazole. However, there have been case reports of drug rash with eosinophilia and systemic symptoms (DRESS syndrome) accompanied by serum enzyme elevations associated with benznidazole therapy, and cases of immunoallergic hepatitis have been reported with other nitroimidazoles such as metronidazole and ornidazole, some of which have been severe. Thus, while benznidazole therapy has been linked to instances of DRESS syndrome accompanied by serum enzyme elevations it has not been directly linked to cases of clinically apparent liver injury with jaundice. On the other hand, it has had limited clinical use and its structural similarity to other nitroimidazoles suggests that it might cause rare cases of immunoallergic hepatitis.

For use in the treatment of Chagas disease in children 2-12 years of age.

Benznidazole is an orally available, broad spectrum antimicrobial agent used in the treatment of Chagas disease. Benznidazole is a nitroimidazole similar to metronidazole and is associated with serum enzyme elevations during therapy in up to 10% of patients but has not linked to cases of clinically apparent acute liver injury.

Antiinfective Agents

Benznidazole is a trypanocidal agent which kills the causative organism in Chagas disease, *Trypanosoma cruzi*.

Chemical agents that increase the rate of genetic mutation by interfering with the function of nucleic acids. A clastogen is a specific mutagen that causes breaks in chromosomes. (See all compounds classified as Mutagens.)|Agents destructive to the protozoal organisms belonging to the suborder TRYPANOSOMATINA. (See all compounds classified as Trypanocidal Agents.)|Agents that suppress immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-CELLS or by inhibiting the activation of HELPER CELLS. While immunosuppression has been brought about in the past primarily to prevent rejection of transplanted organs, new applications involving mediation of the effects of INTERLEUKINS and other CYTOKINES are emerging. (See all compounds classified as Immunosuppressive Agents.)

Benznidazole has a bioavailability of 91.7% and a Tmax of 2.93 h.|The metabolites of benznidazole appear to be primarily exreted in the urine.|The apparent volume of distribution is 39.19 L.|The apparent oral clearance is 2.04 L/h.

Benznidazole is metabolized by nitroreductases in *Trypanosoma cruzi* and by cytochrome P450 enzymes.

The half life of elimination is 13.27 h.

Benznidazole is thought to be reduced to various electrophilic metabolites by nitroreductases present in *Trypanosoma cruzi*. These metabolites likely bind to proteins, lipids, DNA, and RNA resulting in damage to these macromolecules. Benznidazole has been found to increase trypanosomal death through interferon-γ which is likely present in increased amounts due to inflammation caused by macromolecule damage. DNA in parasites affected by benznidazole has been found to undergo extensive unpacking with overexpression of DNA repair proteins supporting the idea of DNA damage contributing to the mechanism of the drug.

2-nitroimidazole benznidazole

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients