Nifurtimox

IUPAC: (RS )-N- (3-methyl -1 ,1- dioxo -1 ,4- thiazinan -4-yl ) - 1 - (5 -nitro- 2-furyl) methanimine

P01CC01

Antiprotozoic

180-182 ° C

2 mg · kg -1 ( LD50, rabbit, oral)

Template: Infobox chemical / molecular formula search available

Nifurtimox (trade name Lampit ®) is a drug from the group of nitrofurans, which is used as antiprotozoal for the treatment of Chagas disease.

Clinical information

Nifurtimox is by the WHO for the treatment of acute Chagas' disease, an infection with Trypanosoma cruzi, is recommended. For a demonstration of efficacy also in chronic Chagas' disease, there is insufficient information.

In addition to the Chagas disease is currently the use of nifurtimox in combination therapy with eflornithine for treating late stage of West African sleeping sickness, an infection with a subspecies of Trypanosoma brucei examined. Also an effect in the treatment of neuroblastoma and medulloblastoma is currently being tested after a remission of neuroblastoma had been observed in the treatment of patients suffering from Chagas patient.

Among the more common side effects include weight loss, anorexia, mental changes, irritability or drowsiness, and gastrointestinal disturbances such as diarrhea and vomiting. From animal studies there is evidence of neurotoxicity, Toxozität in testes and ovaries as well as adverse effects in the adrenal glands, colon, esophagus and breast.

Nifurtimox should not be used during pregnancy; there is evidence that the substance is mutagenic.

Pharmacological properties

After oral administration it is well absorbed and almost completely metabolized. Nifurtimox presumably acts on the formation of free radicals, which can be hardly degraded by the parasite.

Other Information

AG was nifurtimox in the 1960s under the name " Bayer 2502 " at Bayer developed. Since 1967 the fabric against Chagas disease is used; he is next to benznidazole, the only substance that is used to treat this disease. Currently no nifurtimox preparations in Germany, Austria or Switzerland are approved; in South America are tablets containing 120 mg of active ingredient are available. After Bayer had production stopped for lack of demand in 1997, the production was started again in 2000 to allow clinical studies in African sleeping sickness. Through agreements between WHO and Bayer and drug donations by the manufacturer's supply of nifurtimox is now regarded again as backed up.