Benznidazole
Systematic (IUPAC) name | |
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N-benzyl-2-(2-nitro-1H-imidazol-1-yl)acetamide | |
Clinical data | |
Trade names | Rochagan, Radanil |
AHFS/Drugs.com | Micromedex Detailed Consumer Information |
Legal status | ? |
Routes | Oral |
Pharmacokinetic data | |
Bioavailability | High |
Metabolism | Hepatic |
Half-life | 12 hours |
Excretion | Renal and fecal |
Identifiers | |
CAS number | 22994-85-0 |
ATC code | P01CA02 |
PubChem | CID 31593 |
ChemSpider | 29299 |
UNII | YC42NRJ1ZD |
KEGG | D02489 |
ChEMBL | CHEMBL110 |
Chemical data | |
Formula | C12H12N4O3 |
Mol. mass | 260.249 g/mol |
SMILES
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Benznidazole (INN, formerly marketed by Hoffman-La Roche under the trade names Rochagan and Radanil) is an antiparasitic medication used in the treatment of Chagas disease. Its mechanism of action is the production of free radicals, to which the Trypanosoma cruzi is particularly sensitive given its reduced detoxification capabilities.[1] Roche donated the technology and rights to produce benznidazole to the Brazilian government.[2]
Effectiveness
Benznidazole has a significant activity during the acute phase of the disease, with a therapeutical success rate of up to 80%. Its curative capabilities during the chronic phase are, however, limited. Some studies have found parasitologic cure (a complete elimination of Trypanosoma cruzi from the body) in pediatric and young patients during the early stage of the chronic phase, but overall failure rate in chronically infected individuals is typically above 80%.[1]
However, some studies indicate that the treatment with benznidazole in chronic patients, even if incapable of producing parasitologic cure, carries a significative reduction of occurrence of electrocardiographic changes and a delayed worsening of the clinical condition of the patient.[1]
Benznidazole has proven to be effective in the treatment of reactivated T. cruzi infections caused by immunosuppression, such as AIDS patients or those under immunosuppressive therapy related to organ transplants.[1]
Side effects
The side effects most commonly associated with benznidazole therapy are rash and gastrointestinal symptoms such as nausea. Rarely, peripheral neuropathy may present after prolonged treatment.
References
- ↑ 1.0 1.1 1.2 1.3 Urbina, Julio A. "Nuevas drogas para el tratamiento etiológico de la Enfermedad de Chagas" (in Spanish). Retrieved March 24, 2012.
- ↑ http://www.itg.be/evde/04_Chagas_diseasep12.htm
External links
- (Portuguese) "Rochagan [Patient Information]" (PDF). Hoffmann-La Roche. Retrieved 2006-11-27.
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