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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/12/26 22:03:12」(JST)

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

It is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system.^[1]

Medical uses

Being a nitroaromatic compound, nifurtimox undergoes reduction and eventually creates oxygen radicals such as superoxide. These radicals are toxic to T. cruzi. Mammalian cells are protected by presence of catalase, glutathione, peroxidases, and superoxide dismutase.

Nifurtimox has been used to treat Chagas disease, when it is given for 30 to 60 days,^[2] but gastrointestinal and neurological side effects have meant that benznidazole is now preferred for that indication.^{[citation needed]}

Nifurtimox has also been used to treat African trypanosomiasis (sleeping sickness), and is active in the second stage of the disease (central nervous system involvement). When nifurtimox is given on its own, about half of all patients will relapse,^[3] but the combination of melarsoprol with nifurtimox appears to be efficacious.^[4] Trials are awaited comparing melarsoprol/nifurtimox against melarsoprol alone for African sleeping sickness.^[5]

Combination therapy with eflornithine and nifurtimox is safer and easier than treatment with eflornithine alone, and appears to be equally or more effective. It has been recommended as first-line treatment for second-stage African trypanosomiasis.^[6]

Investigational

Nifurtimox is in a phase-II clinical trial for the treatment of pediatric neuroblastoma and medulloblastoma.^[7]^[8]

Side effects, contraindications, and interactions

Side effects occur following chronic administration, particularly in elderly people. Major toxicities include immediate hypersensitivity such as anaphylaxis and delayed hypersensitivity reaction involving icterus and dermatitis. Gastrointestinal (GI) problems may occur that are severe enough to cause weight loss. Central nervous system disturbances and peripheral neuropathy may also occur. Cell mediated immunity may also be suppressed.

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,^{[citation needed]} where it is sold as 120-mg tablets.

References

^ "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
^ Coura JR, de Castro SL. (2002). "A critical review of Chagas disease chemotherapy". Mem Inst Oswaldo Cruz 97 (1): 3–24. doi:10.1590/S0074-02762002000100001. PMID 11992141.
^ 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 (4): 514–7. doi:10.1016/0035-9203(89)90270-8. PMID 2694491.
^ 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 (3): 322–329. doi:10.1086/510534. PMID 17205469.
^ Pepin J (2007). "Combination Therapy for Sleeping Sickness: A Wake-Up Call". J Infect Dis 195 (3): 311–13. doi:10.1086/510540. PMID 17205466.
^ Priotto G, Kasparian S, Mutombo W, et al. (July 2009). "Nifurtimox-eflornithine combination therapy for second-stage African Trypanosoma brucei gambiense trypanosomiasis: a multicentre, randomised, phase III, non-inferiority trial". Lancet 374 (9683): 56–64. doi:10.1016/S0140-6736(09)61117-X. PMID 19559476.
^ Clinical trial number NCT00601003 at ClinicalTrials.gov . Retrieved on July 10, 2009.
^ "http://www.vai.org/en/vari/research-areas/nmtrc/clinical-trials/phase-ii-nifurtimox.aspx". External link in |title= (help); Missing or empty |url= (help)

UpToDate Contents

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1. 抗原虫治療 antiprotozoal therapies
2. Chagas disease: Antitrypanosomal drug therapy
3. シャーガス病：急性疾患、早期慢性疾患、および免疫不全宿主における疾患のマネージメント chagas disease management of acute disease early chronic disease and disease in immunocompromised hosts
4. Chagas heart disease: Treatment and prognosis
5. アフリカ・トリパノソーマ症の臨床症状、診断、および治療 clinical manifestations diagnosis and treatment of african trypanosomiasis

English Journal

Update in treatment of Chagas disease.

Le Loup G, Pialoux G, Lescure FX.SourceaService des Maladies Infectieuse et Tropicales, Hopitaux Universitaires Paris Est - Tenon, AP-HP, Universite Pierre et Marie Curie, Paris bUMR 216 'Mere et Enfant Face aux Infections Tropicales', Institut de Recherche pour le Developpement, Paris cUniversite Paris Descartes, Sorbonne Paris Cite, Paris, France.
Current opinion in infectious diseases.Curr Opin Infect Dis.2011 Aug 19. [Epub ahead of print]
PURPOSE OF REVIEW: This review discusses the recent data about the pathogenesis of Chagas disease, tolerance of drugs, and follow-up of patients impacting the treatment of Chagas disease in immunocompetent and immunocompromised patients.RECENT FINDINGS: The role of the parasite to promote direct or
PMID 21857512

A Decade of Targets and Patented Drugs for Chemotherapy of Chagas Disease.

Duschak VG.SourceInstituto Nacional de Parasitologia "Dr. Mario Fatala Chaben", ANLIS-Malbran, Ministerio de Salud de la nacion. Av. Paseo Colon 568 (1063), Buenos Aires, Argentina. vduschak@conicet.gov.ar.
Recent patents on anti-infective drug discovery.Recent Pat Antiinfect Drug Discov.2011 Aug 9. [Epub ahead of print]
Chagas disease, a parasitic infection typically spread by triatomine bugs, affects millions of people throughout Latin America. Current chemotherapy based on the nitroaromatic compounds, benznidazole and nifurtimox provides unsatisfactory results and suffers from considerable side effects. Therefore
PMID 21824073

Japanese Journal

Antichagasic Activities of Natural Products against Trypanosoma cruzi

Uchiyama Nahoko
Journal of health science 55(1), 31-39, 2009-02-01
… New chemotherapeutic agents are desired because of the lack of effective vaccines, undesirable side effects of anti-chagasic drugs in use such as nifurtimox and benznidazole, and the emergence of parasite resistance to these drugs. …
NAID 110007055938

Research for New Antichagasic Drugs

MESTER Brenda,CLARAMUNT Rosa M.,ELGUERO Jose,ATIENZA Juan,GOMEZ BARRIO Alicia,ESCARIO Jose Antonio
Chemical & pharmaceutical bulletin 39(8), 1990-1993, 1991-08-25
… The antiprotozoal activity has been tested against Trypanosoma cruzi, comparative to Nifurtimox (Lampit). …
NAID 110003629482

Related Pictures

★リンクテーブル★

リンク元	「シャーガス病」「ニフルチモックス」

「シャーガス病」

Nifurtimox
Systematic (IUPAC) name
	(RS)-3-methyl-N-[(1E)-(5-nitro-2-furyl)methylene]thiomorpholin-4-amine 1,1-dioxide
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy; category	Undetermined;
Legal status	℞ Prescription only; Not available in U.S. or Canada;
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	Low
Metabolism	Hepatic (CYP involved)
Biological half-life	2.95 ± 1.19 hours
Excretion	Renal, very low
Identifiers
CAS Number	23256-30-6
ATC code	P01CC01 QP51AC01
PubChem	CID: 31772
ChemSpider	29464
UNII	M84I3K7C2O
KEGG	D00833
ChEMBL	CHEMBL290960
Chemical data
Formula	C10H13N3O5S
Molecular mass	287.293 g/mol
	SMILES O=S2(=O)CC(N(N=Cc1oc([N+]([O-])=O)cc1)CC2)C ;
	InChI InChI=1S/C10H13N3O5S/c1-8-7-19(16,17)5-4-12(8)11-6-9-2-3-10(18-9)13(14)15/h2-3,6,8H,4-5,7H2,1H3 ; Key:ARFHIAQFJWUCFH-UHFFFAOYSA-N ;
Physical data
Melting point	180 to 182 °C (356 to 360 °F)
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　　[★]

英: Chagas disease, Chagas' disease
同: Chagas病
関: アメリカトリパノソーマ病アメリカ・トリパノソーマ症 American trypanosomiasis、スキゾトリパノソーマ症 schizotrypanosomiasis、ブラジル・トリパノソーマ症 Brazilian trypanosomiasis、シャーガス-クルース病 Chagas-Cruz disease; トリパノソーマ属、原虫

アメリカでは感染者は献血が制限される
クルース・トリパノソーマ Trypanosoma cruziの感染
人獣共通感染症

特徴

ウイルス学

病原体

クルース・トリパノソーマ Trypanosoma cruzi

疫学

南アメリカ、中央アメリカ

潜伏期間

感染経路

サシガメ(Triatoma)の糞中に排出される感染型虫体から皮膚・眼の結膜へ

皮膚
眼の結膜　→　eye edema ロマニャ徴候

症状

拡張型心筋症、巨大結腸、巨大食道
慢性期に移行しやすい(初期に見つかるのは感染者のうち1-2%)。
多くの場合発熱を呈する
初期：

原虫侵入部の腫脹と領域リンパ節の腫脹
(眼の結膜)ロマニャ徴候

全身への移行：筋組織を好む

乳児では脳炎、心筋炎が重症化しやすい

脳：脳炎
心臓：不整脈、拡張型心筋症
筋肉：心筋炎

合併症

経過

無症状期：10-20年の無症状期
発症　　：抗体陽性者の半数以上が心症状(拡張型心筋症)、消化器症状(巨大食道、巨大結腸)を呈する

治療

nifurtimox

検査

予防

-Chagas病

「ニフルチモックス」

　　[★]

英: nifurtimox

(米)クルース・トリパノソーマ Trypanosoma cruzi：シャーガス病

[1] "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.

[2] Coura JR, de Castro SL. (2002). "A critical review of Chagas disease chemotherapy". Mem Inst Oswaldo Cruz 97 (1): 3–24. doi:10.1590/S0074-02762002000100001. PMID 11992141.

[3] 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 (4): 514–7. doi:10.1016/0035-9203(89)90270-8. PMID 2694491.

[4] 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 (3): 322–329. doi:10.1086/510534. PMID 17205469.

[5] Pepin J (2007). "Combination Therapy for Sleeping Sickness: A Wake-Up Call". J Infect Dis 195 (3): 311–13. doi:10.1086/510540. PMID 17205466.

[6] Priotto G, Kasparian S, Mutombo W, et al. (July 2009). "Nifurtimox-eflornithine combination therapy for second-stage African Trypanosoma brucei gambiense trypanosomiasis: a multicentre, randomised, phase III, non-inferiority trial". Lancet 374 (9683): 56–64. doi:10.1016/S0140-6736(09)61117-X. PMID 19559476.

[7] Clinical trial number NCT00601003 at ClinicalTrials.gov . Retrieved on July 10, 2009.

[8] "http://www.vai.org/en/vari/research-areas/nmtrc/clinical-trials/phase-ii-nifurtimox.aspx". External link in |title= (help); Missing or empty |url= (help)

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案内

nifurtimox