Nifurtimox: Difference between revisions
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{{drugbox | | {{drugbox | | ||
| IUPAC_name = ''N''-(3-methyl-1,1-dioxo-1,4-thiazinan-4-yl)-<br>1-(5-nitro-2-furyl)methanimine | | IUPAC_name = ''N''-(3-methyl-1,1-dioxo-1,4-thiazinan-4-yl)-<br>1-(5-nitro-2-furyl)methanimine | ||
| image = Nifurtimox. | | image =Nifurtimox.png | ||
| CAS_number = 23256-30-6 | | CAS_number = 23256-30-6 | ||
| ATC_prefix = P01 | | ATC_prefix = P01 | ||
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| routes_of_administration = Oral | | routes_of_administration = Oral | ||
}} | }} | ||
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==Overview== | |||
'''Nifurtimox''' is a [[5-nitrofuran]] and is used to treat diseases caused by [[trypanosome]]s ([[Chagas disease]] and [[sleeping sickness]]). It is given by mouth and not by injection. | '''Nifurtimox''' is a [[5-nitrofuran]] and is used to treat diseases caused by [[trypanosome]]s ([[Chagas disease]] and [[sleeping sickness]]). It is given by mouth and not by injection. | ||
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==References== | ==References== | ||
{{Reflist|2}} | |||
{{Agents against leishmaniasis and trypanosomiasis}} | {{Agents against leishmaniasis and trypanosomiasis}} | ||
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[[Category:Furans]] | [[Category:Furans]] | ||
[[Category:Nitro compounds]] | [[Category:Nitro compounds]] | ||
[[Category:Drug]] | |||
{{WikiDoc Sources}} | {{WikiDoc Sources}} | ||
Latest revision as of 17:31, 10 April 2015
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| Clinical data | |
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| Pregnancy category |
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| Routes of administration | Oral |
| ATC code | |
| Legal status | |
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| Pharmacokinetic data | |
| Bioavailability | Low |
| Metabolism | Hepatic (CYP involved) |
| Elimination half-life | 2.95 ± 1.19 hours |
| Excretion | Renal, very low |
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| CAS Number | |
| PubChem CID | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
| Chemical and physical data | |
| Formula | C10H13N3O5S |
| Molar mass | 287.293 g/mol |
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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
- ↑ Coura JR, de Castro SL. (2002). "A critical review of Chagas disease chemotherapy". Mem Inst Oswaldo Cruz. 97: 3&ndash, 24.
- ↑ 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.
- ↑ 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.
- ↑ Jacques Pepin (2007). "Combination Therapy for Sleeping Sickness: A Wake-Up Call". J Infect Dis. 195: 311&ndash, 13.
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