Pharm

Nifurtimox

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Nifurtimox, Lampit

  • Indications
  1. African Trypanosomiasis
    1. Used in NECT combination with Eflornithine
  2. American Trypanosomiasis (Chagas Disease, T. cruzi)
    1. FDA approved in U.S. for use in children age <18 years (and at least 2.5 kg)
  • Contraindications
  1. Pregnancy
  • Mechanism
  1. Nitrofuran derivative with Antiprotozoal activity
  2. Nifurtimox is cytotoxic to targeted Protozoa
    1. Nifurtimox is reduced by Protozoal enzymes to a free radical, triggering cytotoxic superoxide anion (02-)
    2. Superoxides alkylate parasitic Nucleic Acids and Proteins, disrupting Protozoal Cell Structure and function
  • Medications
  1. Tablets: 30 mg, 120 mg
  1. General
    1. Avoid in weight <2.5 kg
    2. Dose to closest available 1/2 tablet
  2. Weight <41 kg
    1. Give 10-20 mg/kg DIVIDED three times daily orally with food for 60 days
  3. Weight >41 kg
    1. Give 8-10 mg/kg DIVIDED three times daily orally with food for 60 days
  1. See Eflornithine
  2. See African Trypanosomiasis
  3. Eflornithine renal dose adjustment needed for eGFR <30 ml/min
  4. NECT (Eflornithine/Nifurtimox)
    1. Indications
      1. Severe Stage 2 West African Trypanosomiasis with CSF Leukocytes >100 wbc/uL (any age)
    2. Dosing
      1. Eflornithine 400 mg/kg/day IV divided every 12 hours for 7 days AND
      2. Nifurtimox 15 mg/kg/day divided every 8 hours for 10 days
  • Adverse Effects
  1. Gastrointestinal
    1. Decreased appetite
    2. Nausea and Vomiting
    3. Abdominal Pain
  2. Miscellaneous
    1. Headache
    2. Fever
    3. Rash
  • Safety
  1. Pregnancy
    1. Avoid in pregnancy based on animal studies (Miscarriage, IUGR risk, skeletal malformations)
  2. Lactation
    1. Is present in Breastmilk (at <15% of the recommended pediatric dose), with no reported adverse effects
    2. Monitor for decreased oral intake, Vomiting, rash, fever and irritability