Lampit® (nifurtimox) borromeo
- 2. · 30MG · 120MG DOSAGE FORM & STRENGTHS
- 3. MECHANISM OF ACTION The mechanism of action of nifurtimox is not fully understood. Studies suggest that: Nifurtimox is metabolized/activated, by Type I (oxygen insensitive) and Type II (oxygen sensitive) nitoreductases (NTR) leading to production of toxic intermediate metabolites and reactive oxygen species that induce DNA damage and cell death of both intracellular and extracellular forms of T. cruzi.
- 4. Antimicrobial Activity of Nifurtimox is active against all three stages, trypomastigotes, amastigotes, and epimastigotes, of T. cruzi. Nitroreductase (NTR)- are mitochondrial enzymes that appear to be essential for parasite growth
- 5. INDICATION -Nifurtimox is indicated in pediatric patients under 18 years of age weighing at least 2.5 kg (5.5 pounds) -Treatment of Chagas disease (American Trypanosomiasis) caused by Trypanosoma cruzi.
- 8. PHARMACOKINETICS Absorption: Peak plasma time: 4 hr Peak Plasma concentration: 425-568 mcg/L (single 120-mg dose) Distribution: The plasma proteins binding of nifurtimox is 42%. Elimination: elimination half-life of nifurtimox ranged between 2.4–3.6 hours (12–37%)
- 9. • headache • vomiting • nausea • rash • decreased appetite • abdominal pain • fever · weight loss ADVERSE EFFECTS
- 10. DRUG-DRUG INTERACTION No clinical studies evaluating the drug interaction potential of nifurtimox have been conducted.
- 11. WARNING -Hypersensitivity reactions could be accompanied by hypotension, angioedema, dyspnea, pruritus, rash or other severe skin reactions. -At the first sign of serious hypersensitivity, discontinue treatment with LAMPIT -Gastrointestinal irritation
- 12. PRECAUTION -Take with food -Avoid drinking alcoholic beverages
- 13. ADMINISTRATION -Tablets should be taken in three times a day, preferably in the morning, at noon and at night, after meals. -Lactating infants may take it pulverized and mixed with a small amount of food. In this case it is convenient to give the medication before the full meal. -If patient cant swallow tablet, LAMPIT can be mixed in water
- 14. approximately one-half teaspoonful (2.5ml) of water into a spoon Lampit tablet Preparing a Tablet and Water Mixture (Slurry)
- 15. PREGNANCY -Studies have not been done in pregnant women. -Based on animal studies, LAMPIT may cause fetal harm when administered to a pregnant woman. -Doses over 50 mg/kg per day in rats and 125 mg/kg per day in mice resulted in retarded growth of the fetuses.
- 16. CLINICAL STUDY The study was randomized, double-blind study assessed the efficacy, safety, and pharmacokinetics of nifurtimox in 330 pediatric patients with serologic evidence of T. cruzi infection/ with Chagas disease. It was followed up for one year after end of treatment. The results showed superiority in favor of the nifurtimox 60-day compared to the nifurtimox 30-day (not an approved dosing regimen).