LAMPIT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LAMPIT (LAMPIT).
Inhibits the enzyme G6PD (glucose-6-phosphate dehydrogenase) in Trypanosoma cruzi, leading to oxidative stress and parasite death.
| Metabolism | Hepatic metabolism primarily by cytochrome P450 enzymes, including CYP2D6 and others; undergoes extensive biotransformation. |
| Excretion | Renal excretion of unchanged drug accounts for 10% of the dose; biliary/fecal excretion accounts for approximately 90%, mainly as metabolites. |
| Half-life | Terminal elimination half-life is approximately 20 hours. In hepatic impairment, half-life may be prolonged by up to 2-fold. |
| Protein binding | Extensively bound to plasma proteins, primarily albumin; approximately 90% bound. |
| Volume of Distribution | Volume of distribution is approximately 10 L/kg, indicating extensive tissue penetration and distribution beyond plasma. |
| Bioavailability | Oral bioavailability is approximately 50% due to first-pass metabolism. |
| Onset of Action | Oral administration: Clinical effect (reduction in parasitemia) typically observed within 24-48 hours. |
| Duration of Action | Duration of action is approximately 24 hours, requiring once-daily dosing. Clinical effect persists for the duration of treatment (e.g., 60 days for Chagas disease). |
Nifurtimox (Lampit) for Chagas disease: adult dose 8-10 mg/kg/day orally in 3 divided doses for 90 days. For Chagas disease in children: 15-20 mg/kg/day orally in 3 divided doses for 90 days.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment needed for mild-to-moderate renal impairment. For severe renal impairment (CrCl <30 mL/min) or ESRD, use with caution; dose reduction or discontinuation may be necessary due to lack of safety data. Not studied in dialysis. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh C). For mild-to-moderate (Child-Pugh A or B), use with caution; dose adjustment not defined, monitor liver function. |
| Pediatric use | Children <10 kg: no established dose. ≥10 kg: 15-20 mg/kg/day orally in 3 divided doses for 90 days. |
| Geriatric use | No specific dose adjustment; use with caution due to potential for increased sensitivity, comorbidities, and polypharmacy. Monitor for adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LAMPIT (LAMPIT).
| Breastfeeding | Excreted in breast milk; M/P ratio unknown. Avoid breastfeeding due to potential adverse effects. Consider alternative therapy or discontinue breastfeeding. |
| Teratogenic Risk | LAMPIT (nifurtimox) is contraindicated in pregnancy; teratogenic effects observed in animal studies. Use during first trimester associated with increased risk of congenital anomalies. Second and third trimester: potential fetal harm; use only if benefit justifies risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
Nifurtimox is contraindicated in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency due to risk of severe hemolytic anemia.
| Serious Effects |
Hypersensitivity to nifurtimox or any component; G6PD deficiency; active severe neurological or psychiatric disorders; pregnancy (relative contraindication).
| Precautions | Monitor for gastrointestinal intolerance, neurological symptoms (e.g., peripheral neuropathy, convulsions), and weight loss. Caution in patients with hepatic or renal impairment. |
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| Monitor CBC, liver function tests, and renal function in mother. Fetal ultrasound for anomalies if exposure occurs. Monitor for signs of peripheral neuropathy and GI intolerance. |
| Fertility Effects | No specific human data; animal studies show reduced fertility at high doses. May impair spermatogenesis or ovarian function. Advise effective contraception during therapy. |