Investigations of the metabolites of the trypanocidal drug melarsoprol

@article{Keiser2000InvestigationsOT,
  title={Investigations of the metabolites of the trypanocidal drug melarsoprol},
  author={Jennifer Keiser and {\"O}rjan Ericsson and Christian Burri},
  journal={Clinical Pharmacology \& Therapeutics},
  year={2000},
  volume={67}
}
Melarsoprol remains the first‐choice drug for trypanosomiasis (human African sleeping sickness). To contribute to the sparse pharmacologic data and to better understand the cause of the frequent serious adverse reactions, we investigated the metabolism of this 50–year‐old organoarsenic compound. 
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TLDR
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  • M. Barrett
  • Biology
    Current opinion in infectious diseases
  • 2000
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References

SHOWING 1-10 OF 40 REFERENCES
Mel B in the treatment of human trypanosomiasis.
  • E. Friedheim
  • Medicine, Biology
    The American journal of tropical medicine and hygiene
  • 1949
TLDR
“Mel B” penetrates into the CSF and exerts a strong parasiticidal effect on the trypanosomes in the central nervous system and may restore the pathological CSF changes of advanced meningoencephalitis Sleeping Sickness cases to normal co-incident with clinical recovery.
Discrepancy in plasma melarsoprol concentrations between HPLC and bioassay methods in patients with T. gambiense sleeping sickness indicates that melarsoprol is metabolized
TLDR
In patients with late‐stage Trypanosoma gambiense sleeping sickness, the aim was to unravel to what extent the bioassay codetermines biologically active metabolites of melarsoprol.
Adverse Effects of Chemotherapeutic Agents Used in Tropical Medicine
  • G. Cook
  • Biology, Medicine
    Drug safety
  • 1995
TLDR
There remains a very long way to go before a single preparation is available to combat all major protozoan and/or helminthic infections; such an agent would also need to be 100% effective when given as a single dose, safe not only in the healthy adult but also during pregnancy and lactation, stable at high ambient temperature and relatively low in cost.
Pharmacokinetic properties of the trypanocidal drug melarsoprol.
TLDR
The results of these first pharmacokinetic studies on melarsoprol were used to simulate possible alternative therapy schemes which might avoid some of the problems that arise with melarsiprol use.
Clinical and pathological aspects of human African trypanosomiasis (T. b. gambiense) with particular reference to reactive arsenical encephalopathy.
TLDR
Clinical and laboratory findings point rather to a drug-related, delayed immune response in patients treated with melarsoprol for human African trypanosomiasis developing a severe reactive arsenical encephalopathy (RAE).
African trypanosomiasis and drug-induced encephalopathy: risk factors and pathogenesis.
  • J. Pépin, F. Milord
  • Medicine, Biology
    Transactions of the Royal Society of Tropical Medicine and Hygiene
  • 1991
Relapsed parasitaemia following chemotherapy of chronic T. brucei infections in mice and its relation to cerebral trypanosomes.
TLDR
Combined treatment of chronic T. brucei infections with either diminazene aceturate or suramin followed by 5-substituted nitroimidazoles at appropriate dose levels will completely eliminate the infective trypanosomes from the brain and the mice are permanently cured.
...
...