Benznidazole

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Benznidazole
Benznidazole.svg
Systematic (IUPAC) name
N-benzyl-2-(2-nitro-1H-imidazol-1-yl)acetamide
Clinical data
Trade namesRochagan, Radanil
AHFS/Drugs.comMicromedex Detailed Consumer Information
Legal status?
RoutesOral
Pharmacokinetic data
BioavailabilityHigh
MetabolismHepatic
Half-life12 hours
ExcretionRenal and fecal
Identifiers
CAS number22994-85-0 YesY
ATC codeP01CA02
PubChemCID 31593
ChemSpider29299 YesY
UNIIYC42NRJ1ZD YesY
KEGGD02489 YesY
ChEMBLCHEMBL110 YesY
Chemical data
FormulaC12H12N4O3 
Mol. mass260.249 g/mol
 YesY (what is this?)  (verify)
 
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Benznidazole
Benznidazole.svg
Systematic (IUPAC) name
N-benzyl-2-(2-nitro-1H-imidazol-1-yl)acetamide
Clinical data
Trade namesRochagan, Radanil
AHFS/Drugs.comMicromedex Detailed Consumer Information
Legal status?
RoutesOral
Pharmacokinetic data
BioavailabilityHigh
MetabolismHepatic
Half-life12 hours
ExcretionRenal and fecal
Identifiers
CAS number22994-85-0 YesY
ATC codeP01CA02
PubChemCID 31593
ChemSpider29299 YesY
UNIIYC42NRJ1ZD YesY
KEGGD02489 YesY
ChEMBLCHEMBL110 YesY
Chemical data
FormulaC12H12N4O3 
Mol. mass260.249 g/mol
 YesY (what is this?)  (verify)

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, a list of the most important medication needed in a basic health system.[3]

Medical uses[edit]

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[edit]

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[edit]

  1. ^ a b c d 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[edit]