Nifurtimox: Mechanism of Action, Uses, Interactions, and Adverse Effects

Benznidazole and Nifurtimox

The trypanosomatid parasite Trypanosoma cruzi causes Chagas disease, which threatens millions of people in South America. As with other neglected diseases, there is essentially no pharmaceutical industry research and development effort, and treatment is based on two medications, Nifurtimox and Benznidazole, which were found empirically more than thirty years ago.

Nifurtimox Mechanism of Action

The exact mechanism of action of nifurtimox is unknown, although the biological activity of nifurtimox, a nitrofuran derivative, is thought to be mediated by the bio-reduction of the nitro-group to a nitro-anion-radical, which then undergoes redox-cycling with molecular oxygen. While there have been counter-arguments to this notion, it is widely accepted.

Nifurtimox Pharmacokinetics

The blood-brain barrier and the placenta are both crossed by this drug. 42% of the drug shows plasma protein binding. The drug is primarily bound with albumin. It is mostly metabolized by nitroreductase enzymes. In the fed condition, 44 percent of the administered dosage was retrieved primarily as metabolites in the urine. The half-life of nifurtimox is between 2.4 and 3.6 hours.

Nifurtimox and Benznidazole side effects

Side effects associated with the use of Nifurtimox and Benznidazole are given below:

  • Nausea and vomiting
  • Peripheral neuropathy
  • Leukopenia
  • Weight loss
  • Anorexia

Side effects of Nifurtimox

Side effects associated with Nifurtimox include:

  • Anorexia
  • Nausea
  • Headache
  • Amnesia
  • Restlessness
  • Disorientation
  • Forgetfulness
  • Insomnia
  • Spasms
  • Paresthesia
  • Polyneuritis
  • Convulsive seizures

The majority of side effects (93%) are minor and go away when the dose is reduced or the medication is stopped.

Nifurtimox Uses

It is used to treat Chagas disease which is a parasitic infection caused by Trypanosoma cruzi.

Nifurtimox Interactions

Drug-drug interactions

There are no listed drug interactions associated with Nifurtimox.

Drug-food interactions

Avoid consuming alcoholic beverages. If you drink alcohol while taking nifurtimox, you may experience more negative side effects. Take with a meal.


Following are given some conditions where the use of the drug is contraindicated

  • Previous anti- T. cruzi treatment
  • Clinically significant psychiatric disorders including
  • Moderate to severe depression
  • Severe anxiety
  • Psychosis
  • Peripheral neuropathy
  • Epilepsy
  • Pregnancy
  • Hepatic or renal failure
  • Incapability to attend follow-up visits
Severe Anxiety

Is Benznidazole an antibiotic?

An antibiotic called benznidazole is used to treat a parasite infection (Chagas disease). It works by preventing the spread of a certain parasite. This antibiotic is only used to treat Chagas disease.

How long does Chagas disease last?

Chagas disease includes two stages: acute and chronic. Infection can last a lifetime if left untreated. Acute Chagas illness develops soon after infection and can continue for several weeks to months. Parasites may be discovered in the circulating blood during the acute phase.

Chronic Chagas disease includes complicated symptoms like abnormalities in heart rhythm (that may result in death), dilated heart, dilated esophagus, and difficulty in passing stool or eating.

What type of drug is Nifurtimox?

It is a nitrofuran classified as an anti-protozoal drug, that works against both African and American trypanosomiasis (T. cruzi and Chagas disease).

Nifurtimox Brand name

Lampit by Bayer


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