Benznidazole

Benznidazole
Systematic (IUPAC) name
N-benzyl-2-(2-nitro-1H-imidazol-1-yl)acetamide
Clinical data
Trade names Rochagan, Radanil
AHFS/Drugs.com Micromedex Detailed Consumer Information
Oral
Pharmacokinetic data
Bioavailability High
Metabolism Hepatic
Half-life 12 hours
Excretion Renal and fecal
Identifiers
22994-85-0 Yes
P01CA02
PubChem CID 31593
ChemSpider 29299 Yes
UNII YC42NRJ1ZD Yes
KEGG D02489 Yes
ChEMBL CHEMBL110 Yes
Chemical data
Formula C12H12N4O3
260.249 g/mol
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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]

It is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system.[3]

Medical uses

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 T. 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 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. ↑ 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.
  2. ↑ http://www.itg.be/evde/04_Chagas_diseasep12.htm
  3. ↑ "WHO Model List of EssentialMedicines". World Health Organization. October 2013. Retrieved 22 April 2014.

External links