Fexinidazole
African Trypanosomiasis
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Drug Status
Government Approvals
US(FDA)
WHO Essential Medicine
YES
Known Teratogen
No
Pharmaceutical Class
Nitroimidazole Antimicrobial
Controlled Drug Substance
No
Fexinidazole
Summary
Fexinidazole is used to treat a disease called human African trypanosomiasis, also known as sleeping sickness. It can treat both the early stage, where the disease is in the blood and lymph system, and the later stage, where it affects the brain and spinal cord.
Fexinidazole works by getting transformed into reactive substances in the body. These substances damage the DNA and proteins of the parasites causing sleeping sickness, leading to their death.
Fexinidazole is taken orally, once daily with food. For adults and children weighing 35 kg or more, the usual dose is 1800 mg for the first 4 days, followed by 1200 mg for the next 6 days. For children weighing 20 kg to less than 35 kg, the dose is 1200 mg for the first 4 days and 600 mg for the next 6 days.
Common side effects of Fexinidazole include headache, vomiting, insomnia, nausea, and weakness. More serious side effects can include changes in heart rhythm, mental health issues, and a decrease in white blood cells.
Fexinidazole should not be used by people who are allergic to similar drugs, have severe liver problems, or have a condition called Cockayne syndrome. It can cause a reaction if taken with alcohol, and it may not work as well in severe cases of sleeping sickness. It can also have effects on the heart and mental health, and can reduce white blood cells.
Indications and Purpose
How does Fexinidazole work?
Fexinidazole is metabolized into active compounds that target and kill the trypanosome parasites responsible for human African trypanosomiasis. It interferes with the parasites' DNA and protein synthesis, leading to their death.
Is Fexinidazole effective?
Fexinidazole's efficacy was demonstrated in a clinical trial where it was compared to nifurtimox-eflornithine combination therapy (NECT) for treating late second-stage human African trypanosomiasis (HAT). The success rate at 18 months was 91.2% for Fexinidazole, although it was slightly lower than NECT. Additional trials in early-stage HAT and pediatric patients showed success rates of 98.7% and 97.6%, respectively, at 12 months.
What is Fexinidazole?
Fexinidazole is used to treat human African trypanosomiasis (HAT), also known as sleeping sickness, in both its first and second stages. It works by being metabolized into active compounds that kill the trypanosome parasites. The drug is taken orally and is effective when administered with food.
Directions for Use
For how long do I take Fexinidazole?
The typical duration of use for Fexinidazole is 10 days, consisting of a loading dose for the first 4 days and a maintenance dose for the remaining 6 days.
How do I dispose of Fexinidazole?
If you can, bring unused medicines to a drug take-back program or collection site at a pharmacy or hospital. They will dispose of this medicine properly so they don't harm people or the environment. If you can't find a take-back program, you can throw most medicines in the trash at home. But first, take them out of their original containers, mix them with something undesirable like used coffee grounds, seal the mixture in a plastic bag and throw it away.
How do I take Fexinidazole?
Fexinidazole should be taken orally once daily with food, ideally at the same time each day. It is important to avoid alcohol during treatment and for at least 48 hours after completing the therapy to prevent adverse reactions.
How long does it take for Fexinidazole to start working?
Fexinidazole typically starts working within a few days, but the time to achieve its full therapeutic effect can vary depending on the condition being treated. Factors like your overall health, the severity of the infection, and how your body processes the medicine can affect how quickly it works. It's important to follow your healthcare provider's instructions and complete the full course of treatment to ensure the best outcome. If you have concerns about how the medicine is working, consult your healthcare provider.
How should I store Fexinidazole?
Fexinidazole should be stored below 30°C (86°F) in its original package to protect it from light and moisture. Ensure it is kept out of reach of children and pets.
What is the usual dose of Fexinidazole?
For adults and children weighing 35 kg or more, the usual daily dose is 1,800 mg for the first 4 days (loading dose), followed by 1,200 mg for the next 6 days (maintenance dose). For children weighing 20 kg to less than 35 kg, the dose is 1,200 mg for the first 4 days, followed by 600 mg for the next 6 days.
Warnings and Precautions
Can Fexinidazole be taken safely while breastfeeding?
There is no data on the presence of Fexinidazole in human milk, but it is present in rat milk. The benefits of breastfeeding should be weighed against the mother's need for Fexinidazole and any potential effects on the breastfed child. Consult a healthcare provider for personalized advice.
Can Fexinidazole be taken safely while pregnant?
There is insufficient data from human studies to evaluate the risk of fetal harm with Fexinidazole use during pregnancy. Pregnant women should be treated for HAT to prevent vertical transmission, considering the benefits to the mother and potential risks to the fetus. Animal studies showed no prenatal development effects at clinical doses, but effects were observed at higher doses.
Can I take Fexinidazole with other prescription drugs?
Fexinidazole should not be used with drugs that prolong the QT interval or induce bradycardia, such as certain antiarrhythmics and antimalarials. It can also interact with CYP450 inducers and inhibitors, affecting the metabolism of other drugs. Patients should avoid using herbal medicines and supplements during treatment.
Does Fexinidazole have adverse effects?
Adverse effects are unwanted or harmful effects that can occur with medication use. Fexinidazole may cause nausea, headache, vomiting, dizziness, and trouble sleeping. These are generally mild and not very common. However, serious adverse effects, though rare, can include severe allergic reactions like rash, itching, or swelling, which need immediate medical attention. It's important to report any new or worsening symptoms to your healthcare provider and not stop the medication without their guidance.
Does Fexinidazole have any safety warnings?
Fexinidazole comes with safety warnings, including the risk of allergic reactions, which can cause symptoms like rash, itching, or swelling. It's important to monitor for these signs and seek medical help if they occur. The medicine can also affect liver function, so regular liver tests may be needed. If you experience symptoms like yellowing of the skin or eyes, dark urine, or severe fatigue, contact your doctor immediately. Always follow your healthcare provider's instructions and report any unusual symptoms.
Is Fexinidazole addictive?
Fexinidazole has no known potential for dependence or addiction. It is not habit-forming, and there are no behaviors or warning signs associated with physical or psychological dependence on this medicine. You can take it as prescribed without worrying about addiction. However, always follow your healthcare provider's instructions and complete the full course of treatment to ensure the infection is fully treated.
Is Fexinidazole safe for the elderly?
There is limited data on the use of Fexinidazole in elderly patients, as only 11 subjects aged 65 or older were included in clinical trials. Therefore, it is important for elderly patients to use Fexinidazole under close medical supervision to monitor for any potential side effects or interactions.
Is it safe to drink alcohol while taking Fexinidazole?
Drinking alcohol while taking Fexinidazole can cause a disulfiram-like reaction, which includes symptoms like flushing, nausea, and headache. It is advised to avoid alcohol during treatment and for at least 48 hours after completing the therapy.
Is it safe to exercise while taking Fexinidazole?
Most people tolerate Fexinidazole well, and it should not limit your ability to exercise. There is no information suggesting that this medicine affects exercise capacity, physical strength, or endurance. However, if you experience symptoms like dizziness or fatigue during physical activity, it may be wise to take precautions, such as avoiding strenuous activities or high-impact sports. Always listen to your body and consult your healthcare provider if you have concerns.
Is it safe to stop Fexinidazole?
Fexinidazole is used for treating temporary or acute conditions, such as infections. Stopping it abruptly can lead to the infection not being fully treated, which might cause it to return or worsen. There are no known withdrawal symptoms, but it's crucial to complete the full course as prescribed. Stopping early can lead to resistance, making future treatments less effective. Always consult your doctor before stopping any medication to ensure it's safe and appropriate for your situation.
What are the most common side effects of Fexinidazole?
A side effect is an unwanted reaction to a medicine. Common side effects of Fexinidazole include headache, nausea, vomiting, dizziness, and trouble sleeping. These effects are not very common and are usually mild. It's important to note that new symptoms can occur when starting any new medicine, and they might not be related to the medicine itself. Always talk to your healthcare provider before stopping any medication to ensure it's safe to do so.
Who should avoid taking Fexinidazole?
Fexinidazole is contraindicated in patients with known hypersensitivity to the drug, severe hepatic impairment, and Cockayne syndrome. Important warnings include decreased efficacy in severe HAT, QT interval prolongation, neuropsychiatric adverse reactions, neutropenia, potential hepatotoxicity, and disulfiram-like reactions with alcohol. Patients should avoid alcohol and certain medications that prolong the QT interval.
