Melarsoprol

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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
Identifiers
CAS number 494-79-1
ATC code P01CD01
PubChem 10311
Chemical data
Formula C12H15AsN6S2 
Mol. mass 398.341 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 35 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

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Legal status

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Routes IV

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].

Contents

[edit] 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 a significant fraction of cases.

[edit] Administration

As it melts plastic, melarsoprol must be administered in glass syringes and special I.V. tubes.

[edit] Alternatives

Eflornithine is a more modern and far less dangerous treatment for sleeping sickness,[2] but is expensive, not widely available on the market, and most of its supply comes from donations from its manufacturer.

[edit] 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. 
  2. ^ 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.