Nifurtimox/eflornithine

Nifurtimox/eflornithine is a combination therapy used in the treatment of Trypanosoma brucei gambiense human African trypanosomiasis (HAT). This combination therapy is recommended by the World Health Organization (WHO) as the first-line treatment for second-stage gambiense HAT.

Mechanism of Action

Nifurtimox is a nitrofuran compound that is bioactivated within the parasite to form cytotoxic free radicals. These free radicals then cause damage to various structures within the parasite, leading to its death.

Eflornithine, on the other hand, inhibits ornithine decarboxylase, an enzyme essential for the survival and reproduction of the trypanosome parasite. This inhibition leads to a decrease in polyamine levels within the parasite, disrupting its growth and survival.

Clinical Use

Nifurtimox/eflornithine combination therapy (NECT) is used in the treatment of second-stage gambiense HAT, where the parasite has crossed the blood-brain barrier and infected the central nervous system. NECT is preferred over monotherapy due to its shorter treatment duration and lower toxicity.

Side Effects

The most common side effects of NECT include nausea, vomiting, abdominal pain, headache, and seizures. These side effects are generally manageable and subside once treatment is completed.

Resistance

Resistance to Nifurtimox and Eflornithine has been reported in some cases. This resistance is usually due to mutations in the genes encoding for the targets of these drugs.

See Also

• Trypanosoma brucei
• Trypanosomiasis
• Nifurtimox
• Eflornithine

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