melarsoprol

メラルソプロール

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/12/30 19:17:32」(JST)

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Melarsoprol

Systematic (IUPAC) name
(2-(4-(4,6-diamino-1,3,5-triazin-2-ylamino)phenyl)- 1,3,2-dithiarsolan-4-yl)methanol
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy cat.	?
Legal status	?
Routes	IV
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half-life	35 hours
Excretion	Renal
Identifiers
CAS number	494-79-1 N
ATC code	P01CD01 QP51AD04
PubChem	CID 10311
ChemSpider	9889 Y
UNII	ZF3786Q2E8 Y
KEGG	D00832 Y
ChEMBL	CHEMBL166 Y
Chemical data
Formula	C12H15AsN6OS2
Mol. mass	398.341 g/mol
SMILES OCC1S[As](SC1)c3ccc(Nc2nc(nc(n2)N)N)cc3
InChI InChI=1S/C12H15AsN6OS2/c14-10-17-11(15)19-12(18-10)16-8-3-1-7(2-4-8)13-21-6-9(5-20)22-13/h1-4,9,20H,5-6H2,(H5,14,15,16,17,18,19) Y Key:JCYZMTMYPZHVBF-UHFFFAOYSA-N Y
N (what is this?)  (verify)

Melarsoprol (INN) is a medicinal drug used in the treatment of East African, (AKA rhodesiense) human African trypanosomiasis. It is also sold under the trade names “Mel B” and “Melarsen Oxide-BAL.”

Melarsoprol is also used in the treatment of trypanosomiasis, such as Chagas disease and West African sleeping sickness, the former caused by Trypanosoma cruzi and the latter by Trypanosoma brucei gambiense.

Side effects

Being a toxic organic compound of arsenic, melarsoprol is a highly dangerous treatment which is only administered by injection under the supervision of a physician, as it can produce similar effects as arsenic poisoning. Among clinicians, it is colloquially referred to as "Arsenic in antifreeze".

It is known to cause a range of side effects including convulsions, fever, loss of consciousness, rashes, bloody stools, nausea, and vomiting. It is fatal in and of itself in around 8% of cases.

Alternatives

Eflornithine is a more modern and far less dangerous treatment for sleeping sickness, but it is expensive, it is not widely available on the market, and most of its supply comes from donations from its manufacturer.

References

UpToDate Contents

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• 1. 抗原虫治療 antiprotozoal therapies
• 2. 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
• 3. ヒ素曝露と中毒 arsenic exposure and poisoning

English Journal

• HIV-1 Replication in Monocyte-derived Dendritic Cells is Stimulated by Melarsoprol, One of the Main Drugs Against Human African Trypanosomiasis.

• Barat C, Pepin J, Tremblay MJ.SourceCentre de Recherche en Infectiologie, Centre Hospitalier Universitaire de Quebec-CHUL, and Departement de Microbiologie-Infectiologie et Immunologie, Faculte de Medecine, Universite Laval, Quebec (QC), Canada.
• Journal of molecular biology.J Mol Biol.2011 Jul 29;410(5):1052-64.
• Human African trypanosomiasis (HAT) is a disease caused by the protozoan parasite Trypanosoma brucei, the causative agent of sleeping sickness that is still endemic in well defined regions of sub-Saharan Africa. Co-infections with this human pathogen and human immunodeficiency virus (HIV) are not un
• PMID 21763506

• Influence of trypanocidal therapy on the haematology of vervet monkeys experimentally infected with Trypanosoma brucei rhodesiense.

• Ngotho M, Kagira JM, Kariuki C, Maina N, Thuita JK, Mwangangi DM, Farah IO, Hau J.SourceInstitute of Primate Research, Nairobi, Kenya.
• Acta tropica.Acta Trop.2011 Jul;119(1):14-8. Epub 2011 Mar 21.
• The aim of this study was to characterise the sequential haematological changes in vervet monkeys infected with Trypanosoma brucei rhodesiense and subsequently treated with sub-curative diminazene aceturate (DA) and curative melarsoprol (MelB) trypanocidal drugs. Fourteen vervet monkeys, on a serial
• PMID 21420376

Japanese Journal

• Combination chemotherapy with a substance P receptor antagonist (aprepitant) and melarsoprol in a mouse model of human African trypanosomiasis

• RODGERS Jean,BRADLEY Barbara,KENNEDY Peter GE
• Parasitology international : official journal of the Japanese Society of Parasitology 56(4), 321-324, 2007-12-01
• NAID 10019777866

• Human African trypanosomiasis : Potential therapeutic benefits of an alternative suramin and melarsoprol regimen

• JENNINGS Frank W.,RODGERS Jean,BRADLEY Barbara,GETTINBY George,KENNEDY Peter G. E.,MURRAY Max
• Parasitology international : official journal of the Japanese Society of Parasitology 51(4), 381-388, 2002-12-01
• NAID 50000698960

Related Links

• Melarsoprol - Wikipedia, the free encyclopedia

Melarsoprol (INN) is a medicinal drug used in the treatment of human African trypanosomiasis. It is also sold under the trade names “Mel B” and “Melarsen Oxide-BAL.” Melarsoprol is also used in the treatment of trypanosomiasis, such as ...

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