benznidazole

Contraindicated in:

Hypersensitivity to benznidazole or other nitroimidazole derivatives (cross-sensitivity may occur);
Current or previous use (in past 2 wk) of disulfiram;
Concurrent use of products containing alcohol or propylene glycol;
Cockayne syndrome (↑ risk of hepatotoxicity and death);
OB: Pregnancy (may cause fetal harm);
Lactation: Lactation.

Use Cautiously in:

Rep: Women of reproductive potential;
Pedi: Children <2 yr and >12 yr (safety and effectiveness not established).

Adv. Reactions/Side Effects ⬆ ⬇

Derm: rash, ACUTE GENERALIZED EXANTHEMATOUS PUSTULOSIS, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS, ERYTHEMA MULTIFORME, TOXIC EPIDERMAL NECROLYSIS, urticaria

GI: abdominal pain, ↓appetite, ↑liver enzymes, diarrhea, nausea, vomiting

GU: ↓fertility (males)

Hemat: anemia, eosinophilia, leukopenia, neutropenia, thrombocytopenia

Metab: ↓weight

MS: arthralgia

Neuro: dizziness, headache, peripheral neuropathy, tremor

Interactions ⬆ ⬇

Drug-drug:

Concurrent use with disulfiram may result in psychotic reactions; concurrent use and use of disulfiram in past 2 wk contraindicated.
Disulfiram-like reaction may occur with ingestion of products containing alcohol or propylene glycol; use during and ≥3 days after therapy contraindicated.

Availability ⬆ ⬇

(Generic available)

Tablets: 12.5 mg; 100 mg

Route/Dosage ⬆ ⬇

PO (Children 2–12 yr and ≥60 kg): 200 mg every 12 hr for 60 days.
PO (Children 2–12 yr and 40–59 kg): 150 mg every 12 hr for 60 days.
PO (Children 2–12 yr and 30–39 kg): 100 mg every 12 hr for 60 days.
PO (Children 2–12 yr and 20–29 kg): 75 mg every 12 hr for 60 days.
PO (Children 2–12 yr and 15–19 kg): 62.5 mg every 12 hr for 60 days.
PO (Children 2–12 yr and <15 kg): 50 mg every 12 hr for 60 days.

Action ⬆ ⬇

Disrupts DNA, RNA, and protein synthesis in susceptible organisms.

Therapeutic effects:

Resolution of infection.

Spectrum:

Active against Trypanosoma cruzi.

Classifications ⬆ ⬇

Therapeutic Classification: antiprotozoals

Pharmacologic Classification: imidazoles

Pharmacokinetics ⬆ ⬇

Absorption: Rapidly and completely absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Metabolic pathway unknown; excreted in urine and feces.

Half-Life: 13 hr.

Time/Action Profile ⬆ ⬇

(plasma levels)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2 hr	12 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient and parents to take benznidazole as directed for 60 days.
Caution patient to avoid intake of alcoholic beverages or preparations containing alcohol during and for at least 3 days after treatment with benznidazole. May cause a disulfiram-like reaction (flushing, nausea, vomiting, headache, abdominal cramps).
Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception during and for at least 5 days after last dose and to avoid breast feeding during therapy. Inform male patients that benznidazole may impair fertility.

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Indications ⬇

Contraind./Precautions ⬆ ⬇