Nifurtimox: Drug information

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Contributor Disclosures

(For additional information see "Nifurtimox: Patient drug information" and see "Nifurtimox: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp ( show table)

Brand Names: US
Lampit

Pharmacologic Category
Antiprotozoal

Dosing: Adult

Chagas disease

Chagas disease (T. cruzi infection; American trypanosomiasis) (alternative

agent) (off-label use): Oral: 8 to 10 mg/kg/day in 3 to 4 divided doses for 90
days (Bern 2007; CDC 2019a; HHS [OI adult 2020]; Kappagoda 2011).

West African trypanosomiasis, with confirmed or suspected CNS

involvement

West African trypanosomiasis (T. brucei gambiense infection; sleeping

sickness), with confirmed or suspected CNS involvement (off-label use):
Oral: 15 mg/kg/day in 3 divided doses for 10 days, in combination with
eflornithine (CDC 2019b; Kappagoda 2011; Priotto 2009; WHO 2019).

Missed dose: If a dose is missed, take the next dose as soon as possible; if it is ≤3
hours until the next scheduled dose, skip the missed dose and continue treatment
as scheduled. Do not take a double dose to make up for a missed dose.
Dosing: Kidney Impairment: Adult
There are no dosage adjustments provided in the manufacturer’s labeling (has not
been studied). Nifurtimox concentrations may be increased in patients with end-stage
renal disease on hemodialysis; use with caution.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling (has not
been studied).

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric
(For additional information see "Nifurtimox: Pediatric drug information")

American trypanosomiasis

American trypanosomiasis (Chagas disease; Trypanosoma cruzi infection):

Note: Dose should be adjusted if body weight changes during treatment.

Weight-directed dosing (CDC 2021a; Red Book [AAP 2021]; manufacturer's

labeling):

Infants, Children, and Adolescents <18 years:

Weight 2.5 to <41 kg: Oral: 10 to 20 mg/kg/day in 3 divided doses for

60 days.

Weight ≥41 kg: Oral: 8 to 10 mg/kg/day in 3 divided doses for 60 days.

Weight-band (fixed) dosing (manufacturer's labeling):

Infants, Children, and Adolescents <18 years: Note: Treat for 60 days.

2.5 to 4.5 kg: Oral: 15 mg 3 times daily.

>4.5 to <9 kg: Oral: 30 mg 3 times daily.

 9 to <13 kg: Oral: 45 mg 3 times daily.

13 to <18 kg: Oral: 60 mg 3 times daily.

18 to <22 kg: Oral: 75 mg 3 times daily.

22 to <27 kg: Oral: 90 mg 3 times daily.

27 to <35 kg: Oral: 120 mg 3 times daily.

35 to <41 kg: Oral: 180 mg 3 times daily.

41 to <51 kg: Oral: 120 mg 3 times daily.

51 to <71 kg: Oral: 180 mg 3 times daily.

71 to <91 kg: Oral: 240 mg 3 times daily.

≥91 kg: Oral: 300 mg 3 times daily.

African trypanosomiasis, second-stage disease, caused by Trypanosoma

brucei gambiense

African trypanosomiasis (sleeping sickness), second-stage disease (with

CNS involvement), caused by Trypanosoma brucei gambiense: Limited data
available:

Infants, Children, and Adolescents: Oral: 15 mg/kg/day in 3 divided doses for

10 days in combination with IV eflornithine for 7 days (NECT regimen) (CDC
2021b; Red Book [AAP 2021]; WHO 2019).

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling (has not
been studied). Nifurtimox concentrations may be increased in patients with end-stage
renal disease on hemodialysis; use with caution and monitor closely. Some experts
would avoid use in patients with severe renal dysfunction (Bern 2007; Kappagoda
2011).
Dosing: Hepatic Impairment: Pediatric
There are no dosage adjustments provided in the manufacturer's labeling (has not
been studied); some experts would avoid use in patients with severe hepatic
dysfunction (Bern 2007; Kappagoda 2011).

Adverse Reactions
The following adverse drug reactions and incidences are derived from product
labeling unless otherwise specified.

>10%:

Gastrointestinal: Abdominal pain (13%), decreased appetite (11%), vomiting

(15%)

Nervous system: Headache (13%)

1% to 10%:

Dermatologic: Skin rash (6%), urticaria (2%)

Endocrine & metabolic: Weight loss (3%)

Gastrointestinal: Diarrhea (5%), nausea (8%)

Hematologic & oncologic: Anemia (3%), eosinophilia (2%)

Nervous system: Dizziness (3%)

Miscellaneous: Fever (7%)

<1%:

Cardiovascular: Syncope

Dermatologic: Pruritus

Hematologic & oncologic: Leukopenia, neutropenia

Nervous system: Anxiety, drowsiness, fatigue, irritability, paresthesia, seizure,

vertigo
 Neuromuscular & skeletal: Arthralgia, asthenia, myalgia, tremor

Postmarketing:

Hematologic & oncologic: Thrombocytopenia

Hypersensitivity: Anaphylaxis, angioedema, hypersensitivity reaction

Immunologic: Drug reaction with eosinophilia and systemic symptoms

Nervous system: Agitation, amnesia, apathy, myasthenia, polyneuropathy,

psychotic symptoms, sleep disorder

Contraindications
Hypersensitivity to nifurtimox or any component of the formulation; alcohol
consumption during treatment.

Significant drug interactions exist, requiring dose/frequency adjustment or

avoidance. Consult drug interactions database for more information.

Warnings/Precautions
Concerns related to adverse effects:

• CNS effects: May cause muscle weakness or tremors, which may impair
physical abilities; patients must be cautioned about performing tasks such as
operating machinery or driving if weakness or tremors occur.

• GI effects: Loss of appetite and nausea/vomiting leading to weight loss have

been reported. Monitor body weight every 2 weeks during treatment and
adjust dosage based on weight as needed.

• Hypersensitivity reaction: Hypersensitivity reactions, sometimes accompanied

by angioedema (including laryngeal or facial edema), dyspnea, hypotension,
pruritus, rash, or other severe skin reactions, have been reported. The
hypersensitivity may be due to nifurtimox or an immune response caused by
Chagas disease during treatment. Discontinue use at the first sign of serious
hypersensitivity.
 • Peripheral neuropathy: Use has been associated with peripheral neuropathy;
monitor for signs and symptoms during therapy (Crespillo-Andujar 2018;
Forsyth 2016; Kappagoda 2011).

Disease-related concerns:

• Hepatic impairment: Use with caution and close monitoring in patients with
hepatic impairment.

• Neurological conditions: Use with caution and close monitoring in patients

with a history of brain injury or seizures; worsening of the condition may occur.

• Porphyria: Use with caution in patients with porphyria; nitrofuran derivatives

may precipitate acute attacks of porphyria.

• Psychiatric disease: Use with caution and close monitoring in patients with a
history of psychiatric disease or serious behavioral alterations; worsening of
the condition may occur.

• Renal impairment: Use with caution and close monitoring in patients with
end-stage renal disease requiring hemodialysis (serum concentrations are
increased).

Dosage Forms: US
Excipient information presented when available (limited, particularly for generics);
consult specific product labeling.

Tablet, Oral:

Lampit: 30 mg, 120 mg [contains corn starch]

Generic Equivalent Available: US

No

Pricing: US
Tablets (Lampit Oral)

30 mg (per each): $3.00

 120 mg (per each): $3.60

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is

provided as reference price only. A range is provided when more than one
manufacturer's AWP price is available and uses the low and high price reported by the
manufacturers to determine the range. The pricing data should be used for
benchmarking purposes only, and as such should not be used alone to set or
adjudicate any prices for reimbursement or purchasing functions or considered to be
an exact price for a single product and/or manufacturer. Medi-Span expressly
disclaims all warranties of any kind or nature, whether express or implied, and
assumes no liability with respect to accuracy of price or price range data published in
its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or
consequential damages arising from use of price or price range data. Pricing data is
updated monthly.

Prescribing and Access Restrictions

Nifurtimox is only available for the treatment of African trypanosomiasis (in
combination with eflornithine) with an individual IND from the FDA. Additional IND
information is available at [Link]
applications/investigational-new-drug-ind-application.

Administration: Adult
Oral: Administer with food. Tablets are functionally scored and may be split at the
scored lines by hand; do not break mechanically with a tablet splitting device. In
patients unable to swallow whole or half tablets, tablet may be dispersed in water.
Place ~2.5 mL of water in a spoon and place the prescribed dose into the water.
Allow the tablet(s) to disintegrate (usually <30 seconds) until a slurry is formed.
Administer the slurry immediately with food.

West African trypanosomiasis: If vomiting occurs within 30 minutes of dose,

repeat the same dose. If vomiting occurs within 30 to 60 minutes of dose, a half
dose should be given. If vomiting occurs >1 hour after dose, no additional dose is
necessary. If nausea or vomiting persists, consider administering domperidone or
 metoclopramide before subsequent doses. If treatment is interrupted, the missing
doses should be added at the end of treatment for a total of 30 doses of
nifurtimox (WHO 2019).

Administration: Pediatric
Oral: Administer with food. Tablets are functionally scored and may be split at the
scored lines by hand; do not break mechanically with a tablet splitting device. In
patients unable to swallow whole or half tablets, tablet may be dispersed in water.
Place ~2.5 mL of water in a spoon and place the prescribed dose into the water. Allow
the tablet(s) to disintegrate (usually <30 seconds) until a slurry is formed. Administer
the slurry immediately with food.

African trypanosomiasis (sleeping sickness; T. brucei gambiense infection): If

vomiting occurs within 30 minutes of dose, repeat the same dose. If vomiting
occurs within 30 to 60 minutes of dose, a half dose should be given. If vomiting
occurs >1 hour after dose, no additional dose is necessary. If nausea or vomiting
persists, consider administering domperidone (not available in the United States)
or metoclopramide before subsequent doses (WHO 2019).

Missed doses:

American trypanosomiasis (Chagas disease; T. cruzi infection): If a dose is

missed, administer as soon as possible; if it is ≤3 hours until the next scheduled
dose, skip the missed dose and continue treatment as scheduled. Do not take
a double dose to make up for a missed dose.

African trypanosomiasis (sleeping sickness; T. brucei gambiense

infection): If treatment is interrupted, the missing doses should be added at
the end of treatment for a total of 30 doses of nifurtimox (WHO 2019).

Hazardous Drugs Handling Considerations

This medication is not on the NIOSH (2016) list; however, it may meet the criteria for a
hazardous drug. Nifurtimox may cause teratogenicity, reproductive toxicity, and
genotoxicity.
Use appropriate precautions for receiving, handling, storage, preparation, dispensing,
transporting, administration, and disposal. Follow NIOSH and USP 800
recommendations and institution-specific policies/procedures for appropriate
containment strategy (NIOSH 2016; USP-NF 2020).

Note: Facilities may perform risk assessment of some hazardous drugs to determine
if appropriate for alternative handling and containment strategies (USP-NF 2020).
Refer to institution-specific handling policies/procedures.

Use: Labeled Indications

Chagas disease (Trypanosoma cruzi infection; American trypanosomiasis):
Treatment of Chagas disease in pediatric patients <18 years of age and weighing ≥2.5
kg.

Use: Off-Label: Adult

West African trypanosomiasis (Trypanosoma brucei gambiense infection; sleeping
sickness), with confirmed or suspected CNS involvement

Medication Safety Issues

Sound-alike/look-alike issues:

Nifurtimox may be confused with nifuroxazide, nitrofurantoin, nitazoxanide.

Metabolism/Transport Effects
None known.

Drug Interactions
(For additional information: Launch drug interactions program)

Note: Interacting drugs may not be individually listed below if they are part of a
group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT
listed). For a complete list of drug interactions by individual drug name and detailed
management recommendations, use the Lexicomp drug interactions program by
clicking on the “Launch drug interactions program” link above.
 Alcohol (Ethyl): May enhance the adverse/toxic effect of Nifurtimox. Risk X: Avoid
combination

Food Interactions
Food increases Cmax, AUC, and Tmax. Management: Administer with food.

Reproductive Considerations
Evaluate pregnancy status prior to use; pregnancy testing is required prior to use in
patients who could become pregnant. Patients who could become pregnant should
use effective contraception during therapy and for 6 months after the last nifurtimox
dose. Patients with partners who could become pregnant should use condoms during
therapy and for 3 months after the last nifurtimox dose.

Pregnancy Considerations
Based on data from animal reproduction studies, in utero exposure to nifurtimox may
cause fetal harm.

Outcome data related to the use of nifurtimox in pregnancy are limited (Kuemmerle
2022; Schmid 2012).

Other agents may be preferred for the treatment of West African trypanosomiasis in
pregnant patients when therapy cannot be postponed until after delivery. Nifurtimox
should not be used during pregnancy unless treatment is considered life-saving for
the mother (WHO 2019). Treatment of Chagas disease in pregnancy does not prevent
transmission to the newborn; maternal treatment with nifurtimox is considered
contraindicated by some guidelines and use should be postponed until after delivery
(Carlier 2019; Meymandi 2018).

Data collection to monitor pregnancy and infant outcomes following exposure to

nifurtimox is ongoing. Health care providers are encouraged to enroll patients who
become pregnant within 6 months of the last dose or who are exposed to nifurtimox
during pregnancy in the pregnancy safety study (1-888-842-2937).
Breastfeeding Considerations
Nifurtimox is present in breast milk (Moroni 2019).

Data related to the presence of nifurtimox in breast milk are available from a study
of 10 lactating patients, 1 to 11 months postpartum, treated for Chagas disease.
Patients were administered nifurtimox 8 to 12 mg/kg/day for 30 days and breast
milk was sampled after ~3 and ~10 days of treatment. The highest breast milk
concentration was 9.5 mg/L. Using the highest breast milk concentration from one
patient, the authors of the study calculated the relative infant dose (RID) of
nifurtimox to be 14.54%, based on the weight-adjusted maternal dose of 9.8
mg/kg/day, providing an estimated dose to the breastfed infant of 1.42
mg/kg/day. Using data from all 10 patients, the median concentration of
nifurtimox in breast milk was 2.15 mg/L, providing a RID of 6.7%. Adverse events
were not observed in the breastfed infants. Two infants required treatment for
congenital Chagas disease (Moroni 2019). In general, breastfeeding is considered
acceptable when the RID of a medication is <10% (Anderson 2016; Ito 2000).

Data related to the use of nifurtimox for the treatment of West African
trypanosomiasis in breastfeeding patients are limited (Kuemmerle 2022; Schmid
2012).

According to the manufacturer, the decision to breastfeed during therapy should

consider the risk of infant exposure, the benefits of breastfeeding to the infant,
and the benefits of treatment to the mother. However, breastfeeding may
continue when nifurtimox is used for the treatment of West African
trypanosomiasis in lactating patients (WHO 2019). Infants exposed to nifurtimox
via breast milk should be monitored for adverse events, including decreased
appetite, irritability, pyrexia, rash, or vomiting.

Dietary Considerations
Take with food. Avoid alcohol.

Monitoring Parameters
Pregnancy test prior to use in patients who could become pregnant.
 Additional monitoring is dependent on the anticipated length of treatment:

Treatment course ≤10 days: Renal function, hepatic function, and CBC at
baseline and during treatment if clinically indicated.

Treatment course >10 days: Renal function, hepatic function, and CBC at
baseline, at least once during treatment (some experts recommend every 4 to
6 weeks [Bern 2020]), and at therapy completion; periodically screen for
peripheral neuropathy during treatment (Kappagoda 2011; Olivera 2017).
Monitor body weight every 2 weeks during therapy.

Mechanism of Action
Not well described. It has been suggested that nifurtimox is metabolized/activated by
type I (oxygen insensitive) and type II (oxygen sensitive) nitroreductases, 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.

Pharmacokinetics (Adult Data Unless Noted)

Absorption: Rapidly absorbed (WHO 1995). Administration with a high-fat meal
(800 to 1,000 calories; ~60% fat) increased Cmax and AUC by 68% and 71%,
respectively.

Protein binding: 42%.

Metabolism: Extensively metabolized in the liver, where nitroreduction occurs

through CYP450 reductase (Bern 2007; WHO 1995).

Half-life elimination: 2.4 to 3.6 hours.

Time to peak: Median: 4 hours (range: 2 to 8 hours).

Excretion: Urine: ~27% (fasted conditions) to 44% (fed conditions), primarily as

metabolites.

Brand Names: International

Find brand name(s) by country (for United States and Canada see separate Brand
Names sections)

Enter a Country or Country Code

International Brand Names by Country

For country code abbreviations ( show table)

(AR) Argentina: Furtimox; (PR) Puerto Rico: Lampit; (PT) Portugal: Lampit

REFERENCES

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