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Melarsoprol

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Melarsoprol
Clinical data
Pregnancy
category
  • ?
Routes of
administration
IV
ATC code
Legal status
Legal status
  • ?
Pharmacokinetic data
Bioavailability?
Metabolism?
Elimination half-life35 hours
ExcretionRenal
Identifiers
  • (2-(4-(4,6-diamino-1,3,5-triazin-2-ylamino)phenyl)-
    1,3,2-dithiarsolan-4-yl)methanol
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.007.086 Edit this at Wikidata
Chemical and physical data
FormulaC12H15AsN6OS2
Molar mass398.341 g/mol g·mol−1

Melarsoprol (INN) is a medicinal drug used in the treatment of Human African trypanosomiasis.[1] It is also sold under the trade names “Mel B” and “Melarsen Oxide-BAL.”

Melarsoprol is also used in the treatment of Chagas disease[citation needed] and sleeping sickness, the former cause by trypanosoma cruzi and the latter by trypanosoma brucei.

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.

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[2].

Alternatives

Eflornithine is a more modern and far less dangerous treatment for sleeping sickness,[3] but is expensive, not widely available on the market, and most of its supply comes from donations from its manufacturer. Moreover, eflornithine is effective only for West African Sleeping Sickness; it has no effect on East African Sleeping Sickness.

References

  1. ^ Bisser S, N'Siesi FX, 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): 322–9. doi:10.1086/510534. PMID 17205469. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  2. ^ Bulletin of the World Health Organization vol.84 no.10 Genebra Oct. 2006 - Melarsoprol versus eflornithine for treating late-stage Gambian trypanosomiasis in the Republic of the Congo
  3. ^ Chappuis F, Udayraj N, Stietenroth K, Meussen A, Bovier PA (2005). "Eflornithine is safer than melarsoprol for the treatment of second-stage Trypanosoma brucei gambiense human African trypanosomiasis". Clin. Infect. Dis. 41 (5): 748–51. doi:10.1086/432576. PMID 16080099.{{cite journal}}: CS1 maint: multiple names: authors list (link)