Melarsoprol

Aka: Melarsoprol

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II. Indications

  1. East African Trypanosomiasis (T. rhodesiense)
    1. Stage 2 AND (Age <6 years OR body weight >20kg)
    2. Fexindazole is preferred in other cases

III. Contraindications

  1. G6PD Deficiency
  2. Pregnancy

IV. Mechanism

  1. Arsenical agent used in Trypanosomias

V. Dosing

  1. Melarsoprol 2.2 mg/kg/day IV for 10 days
  2. Consider Corticosteroid pretreatment to prevent encephalopathy
  3. Consider pretreatment with Suramin to treat blood stages before Melarsoprol

VI. Pharmacokinetics

  1. Penetrates the blood brain barrier and CNS

VII. Adverse Effects

  1. Encephalopathy (5-10% of patients)
    1. High mortality (>50%)
    2. Consider Corticosteroid pretreatment to prevent encephalopathy
  2. Jarisch-Herxheimer Reaction
  3. Hemolysis in G6PD Deficiency
  4. Blood Pressure elevation
  5. Gastrointestinal symptoms (Nausea, Vomiting, Abdominal Pain)
  6. Peripheral Neuropathy
  7. Pruritus
  8. Phlebitis

VIII. Safety

  1. Pregnancy
    1. Avoid unless used as rescue therapy in severe disease
  2. Lactation
    1. May continue to Breast feed while on therapy

IX. Resources

  1. African Trypanosomiasis (WHO)
    1. https://www.who.int/news-room/fact-sheets/detail/trypanosomiasis-human-african-(sleeping-sickness)
  2. African Trypanosomiasis (Stat Pearls)
    1. https://www.ncbi.nlm.nih.gov/books/NBK535413/

X. References

  1. Gladwin, Trattler and Mahan (2014) Clinical Microbiology, Medmaster, Fl, p. 349
  2. Freedman (2025) Sanford Guide, accessed 7/11/2025 on IOS
  3. Ortiz-Martínez (2023) Curr Trop Med Rep 10(4):222-34 +PMID: 38939748 [PubMed]

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