Nifurtimox

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Nifurtimox
Nifurtimox.png
Clinical data
Pregnancy
category
  • Undetermined
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • ℞ Prescription only
    Not available in U.S. or Canada
Pharmacokinetic data
BioavailabilityLow
MetabolismHepatic (CYP involved)
Elimination half-life2.95 ± 1.19 hours
ExcretionRenal, very low
Identifiers
CAS Number
PubChem CID
E number{{#property:P628}}
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Chemical and physical data
FormulaC10H13N3O5S
Molar mass287.293 g/mol

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List of terms related to Nifurtimox

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Nifurtimox is a 5-nitrofuran and is used to treat diseases caused by trypanosomes (Chagas disease and sleeping sickness). It is given by mouth and not by injection.

Uses

Nifurtimox has been used to treat Chagas disease, when it is given for 30 to 60 days,[1] but gastrointestinal and neurological side effects have meant that benznidazole is now preferred for that indication.

Nifurtimox has also been used to treat African sleeping sickness and is active in the second stage of African sleeping sickness (CNS disease). Unfortunately, when nifurtimox is given on its own, about half of all patients will relapse,[2] but the combination of melarsoprol with nifurtimox appears to be efficacious.[3] Trials are awaited comparing melarsoprol/nifurtimox against melarsoprol alone for African sleeping sickness.[4]

Dosing

Nifurtimox is dosed as 15 mg/kg/day in two to three divided doses. It is given by mouth. Refer to the articles on Chagas disease and sleeping sickness for more detailed information on dosing for these diseases.

Manufacturing and availability

Nifurtimox is sold as Lampit® by Bayer. It was previously known as Bayer 2502.

Nifurtimox is only licensed for use in Argentina and Germany, where it is sold as 120 mg tablets.

References

  1. Coura JR, de Castro SL. (2002). "A critical review of Chagas disease chemotherapy". Mem Inst Oswaldo Cruz. 97: 3&ndash, 24.
  2. Pepin J, Milord F, Mpia B; et al. (1989). "An open clinical trial of nifurtimox for arseno-resistant T.b. gambiense sleeping sickness in central Zaire". Trans R Soc Trop Med Hyg. 83: 514&ndash, 7.
  3. Bisser S, N'Siesi F-X, Lejon V; et al. (2007). "Equivalence Trial of Melarsoprol and Nifurtimox Monotherapy and Combination Therapy for the Treatment of Second-Stage Trypanosoma brucei gambiense Sleeping Sickness". J Infect Dis. 195: 322&ndash, 329.
  4. Jacques Pepin (2007). "Combination Therapy for Sleeping Sickness: A Wake-Up Call". J Infect Dis. 195: 311&ndash, 13.



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