Nifurtimox

Nifurtimox

File:Nifurtimox.svg
Clinical data
Pregnancy category	Undetermined
Routes of administration	Oral
ATC code	P01CC01 (WHO)
Legal status
Legal status	℞ Prescription only Not available in U.S. or Canada
Pharmacokinetic data
Bioavailability	Low
Metabolism	Hepatic (CYP involved)
Elimination half-life	2.95 ± 1.19 hours
Excretion	Renal, very low
Identifiers
IUPAC name N-(3-methyl-1,1-dioxo-1,4-thiazinan-4-yl)- 1-(5-nitro-2-furyl)methanimine
CAS Number	23256-30-6
PubChem CID	6842999
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C10H13N3O5S
Molar mass	287.293 g/mol

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, 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, but the combination of melarsoprol with nifurtimox appears to be efficacious. Trials are awaited comparing melarsoprol/nifurtimox against melarsoprol alone for African sleeping sickness.

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.