LAMPIT Dosage & Rx Info | Uses, Side Effects

Lampit Generic Name & Formulations

Legal Class

General Description

Nifurtimox 30mg, 120mg; scored tabs.

Pharmacological Class

Antiprotozoal.

How Supplied

Tabs—100

Manufacturer

Bayer Corporation

Generic Availability

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/or reactive oxygen species that induce DNA damage and cell death of both intracellular and extracellular forms of T. cruzi.

Lampit Indications

Indications

Chagas disease (American Trypanosomiasis) caused by Trypanosoma cruzi in pediatric patients (birth to <18yrs of age and weighing ≥2.5kg).

Lampit Dosage and Administration

Adult

Not applicable.

Children

Swallow whole or divide in half by hand; do not use a tablet splitting device. If unable to swallow, tabs may be dispersed in water and administered as a slurry. Give 3 times daily with food for 60 days. Total daily dose: <18yrs (<41kg): 10–20mg/kg; (≥41kg): 8–10mg/kg. Individual dose: <18yrs (<2.5kg): not established; (2.5–4.5kg): 15mg; (4.6–<9kg): 30mg; (9–<13kg): 45mg; (13–<18kg): 60mg; (18–<22kg): 75mg; (22–<27kg): 90mg; (27–<35kg): 120mg; (35–<41kg): 180mg; (41–<51kg): 120mg; (51–<71kg): 180mg; (71–<91kg): 240mg; (≥91kg): 300mg.

Lampit Contraindications

Contraindications

Consuming alcohol during treatment.

Lampit Boxed Warnings

Not Applicable

Lampit Warnings/Precautions

Warnings/Precautions

Discontinue at the 1^st sign of serious hypersensitivity. History of brain injury, seizures, psychiatric disease, serious behavioral alterations, neurological disturbances, psychiatric drug reactions, porphyria: administer under close medical supervision. Monitor body weight every 14 days; dose adjustment may be needed. Renal or hepatic impairment. Embryo-fetal toxicity. Advise to use effective contraception during and for 6 months (females of reproductive potential) or for 3 months (males w. female partners to use condoms) after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: monitor infants.

Lampit Pharmacokinetics

Absorption

The mean (%CV) nifurtimox AUC estimates ranged between 1676–2670 μg∙h/L (19–32%) and C_max estimates ranged between 425–568 μg/L (26–50%) following administration of single dose 120mg nifurtimox with food in adult Chagas patients. The median time to reach maximum concentration (T_max) of nifurtimox under fed conditions was 4 hours (range: 2–8 hours).

Effect of Food: Following administration of a single oral dose of 120 mg Lampit in adult Chagas patients, nifurtimox C_max increased 68%, AUC increased 71%, and T_max increased by 1 hour with a high-fat meal (800–1000 calorie, ~60% fat) compared to fasted conditions.

Distribution

Plasma protein bound: 42%; passes the blood brain barrier and the placental barrier.

Metabolism

Primary mediated via nitroreductases.

Elimination

Renal (~44% and 27% under fed and fasted conditions, respectively). Half-life: 2.4–3.6 hours.

Lampit Interactions

Interactions

See Contraindications. Potentiated by alcohol.

Lampit Adverse Reactions

Adverse Reactions

Vomiting, abdominal pain, headache, decreased appetite, nausea, pyrexia, rash; worsening of neurological and psychiatric conditions, hypersensitivity, weight loss, porphyria; potential for genotoxicity and carcinogenicity.

Lampit Clinical Trials

See Literature

Lampit Note