Colin Snow
Eflornithine is a drug used to treat late-stage African trypanosomiasis, more commonly known as sleeping sickness. It is effective only against Trypanosoma brucei gambiense, which causes Gambian (or West African) sleeping sickness. Eflornithine is administered by intravenous injection and works by inhibiting an enzyme called ornithine decarboxylase, which is essential for DNA synthesis, cell division, and growth in both normal and parasitic cells. This disruption ultimately causes parasite death.
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What You'll Learn
- Eflornithine is a drug used to treat late-stage African trypanosomiasis (sleeping sickness)
- It is effective only against Trypanosoma brucei gambiense, which causes Gambian sleeping sickness
- It is administered by intravenous injection
- It is safer than melarsoprol, a highly toxic, arsenic-based drug
- Adverse drug reactions during eflornithine therapy are frequent and similar to other cytotoxic drugs
Eflornithine is a drug used to treat late-stage African trypanosomiasis (sleeping sickness)
Eflornithine is a drug used to treat late-stage African trypanosomiasis, also known as sleeping sickness. It is effective only against Trypanosoma brucei gambiense, which causes Gambian (or West African) sleeping sickness. It is not effective against T. brucei rhodesiense, which causes Rhodesian (or East African) sleeping sickness.
Eflornithine is administered by intravenous injection for the treatment of sleeping sickness. The most common dosage regimen consists of 100 mg kg(-1) body weight at intervals of 6 hours for 14 days (150 mg kg(-1) body weight in children) of eflornithine given as short infusions. Adverse drug reactions during eflornithine therapy are frequent and similar to other cytotoxic drugs for cancer treatment. Their occurrence and intensity increase with the duration of treatment and the patient's general condition.
Eflornithine works by inhibiting the enzyme ornithine decarboxylase, which is essential for DNA synthesis, cell division, and growth in both normal and parasitic cells. By disrupting this enzyme, eflornithine slows down parasite growth and replication, ultimately causing parasite death.
In the past, the standard treatment for sleeping sickness was melarsoprol, a highly toxic, arsenic-based drug. However, due to its dangerous toxicity and the rise in cases refractory to melarsoprol, there was a need for an alternative treatment. Eflornithine was introduced as a safer option, and it has been shown to be more effective than melarsoprol in treating late-stage Gambian sleeping sickness.
To prevent the development of eflornithine-resistant trypanosomes, combination therapies have been developed, such as the Nifurtimox-Eflornithine Combination Therapy (NECT). NECT has been found to be safe and effective, with fewer intravenous infusions, shorter treatment length, and improved cost-effectiveness compared to using eflornithine alone.
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It is effective only against Trypanosoma brucei gambiense, which causes Gambian sleeping sickness
Eflornithine is a drug used to treat late-stage African trypanosomiasis, also known as sleeping sickness. It is specifically effective against Trypanosoma brucei gambiense, which causes Gambian (or West African) sleeping sickness. This disease is caused by a protozoan parasite transmitted by the bite of the tsetse fly and poses a significant threat in several sub-Saharan countries.
Eflornithine works by inhibiting an enzyme called ornithine decarboxylase, which is essential for DNA synthesis, cell division, and growth in both normal and parasitic cells. By blocking this enzyme, eflornithine disrupts parasite growth and replication, ultimately leading to parasite death. This mechanism is also the basis for eflornithine's use in treating excessive facial hair growth, as inhibiting ornithine decarboxylase within hair follicles slows down hair growth.
The standard dosage regimen for treating T. b. gambiense sleeping sickness consists of 100 mg/kg body weight of eflornithine administered at intervals of 6 hours for 14 days (with a higher dosage of 150 mg/kg body weight for children). This treatment is given as short intravenous infusions. While eflornithine has shown acceptable safety and effectiveness as a first-line treatment, adverse drug reactions are frequent, and their occurrence and intensity increase with the duration of treatment and the patient's general health condition.
Eflornithine is not effective against T. brucei rhodesiense, which causes Rhodesian (or East African) sleeping sickness. This is due to the innate lack of susceptibility in this parasite based on a higher ornithine decarboxylase turnover. As a result, melarsoprol, a highly toxic arsenic-based drug, was previously the only treatment option for T. b. rhodesiense sleeping sickness. However, the introduction of NECT (Nifurtimox-Eflornithine Combination Therapy) has provided an effective alternative for T. b. gambiense sleeping sickness, reducing the number of intravenous infusions and treatment length compared to eflornithine monotherapy.
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It is administered by intravenous injection
Eflornithine is a drug used to treat late-stage African trypanosomiasis, also known as sleeping sickness. It is specifically effective against Trypanosoma brucei gambiense, which causes Gambian (or West African) sleeping sickness. For this indication, eflornithine is administered by intravenous injection.
The typical dosage regimen for the treatment of T. b. gambiense sleeping sickness consists of 100 mg/kg of body weight administered at intervals of 6 hours for 14 days (150 mg/kg body weight in children) of eflornithine given as short infusions. This equates to a total of 14 intravenous infusions over 7 days.
Eflornithine exerts its therapeutic effects by inhibiting the enzyme ornithine decarboxylase, which plays a crucial role in the synthesis of polyamine-based compounds involved in cell division and differentiation. This disruption of polyamine synthesis impairs parasite growth and replication, ultimately leading to parasite death.
Prior to 2009, eflornithine was considered the best treatment for sleeping sickness. However, its complex distribution and administration in affected regions posed significant challenges. Doctors often had no choice but to use melarsoprol, a highly toxic alternative that resulted in the death of one out of every 20 patients.
To overcome these challenges, a combination therapy known as NECT (Nifurtimox-Eflornithine Combination Therapy) was introduced. NECT combines nifurtimox, a nitrofuran compound, with eflornithine. This combination therapy offers several advantages, including a reduced number of intravenous infusions (14 instead of 56), a shorter treatment duration, and improved cost-effectiveness compared to using eflornithine alone.
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It is safer than melarsoprol, a highly toxic, arsenic-based drug
Eflornithine is a drug used to treat late-stage African trypanosomiasis, also known as sleeping sickness. It is effective only against Trypanosoma brucei gambiense, which causes Gambian (or West African) sleeping sickness. It is not effective against T. brucei rhodesiense, which causes Rhodesian (or East African) sleeping sickness.
Eflornithine is safer than melarsoprol, a highly toxic, arsenic-based drug that was previously used to treat sleeping sickness. Melarsoprol's high toxicity has been well-documented, and it is known to have killed one out of every 20 patients it was meant to cure. In addition, the rapid rise in cases refractory to melarsoprol in Central Africa further emphasised the need for an alternative treatment.
Eflornithine works by inhibiting an enzyme called ornithine decarboxylase, which is essential for DNA synthesis, cell division, and growth in both normal and parasitic cells. By blocking this enzyme, eflornithine disrupts parasite growth and replication, ultimately leading to parasite death. This mechanism of action is selective at the target level, which contributes to its improved safety profile compared to melarsoprol.
The development of eflornithine as a treatment for sleeping sickness was driven by the need for a less toxic and more cost-effective option than melarsoprol. While eflornithine has shown acceptable safety and effectiveness as a first-line treatment, it is important to note that adverse drug reactions during eflornithine therapy are frequent, and their occurrence and intensity increase with the duration of treatment and the severity of the patient's general condition.
In summary, eflornithine is a safer alternative to melarsoprol for the treatment of late-stage Gambian sleeping sickness. It works by inhibiting parasite growth and has been shown to be effective and relatively safe in clinical trials and cohort studies. However, it is important to monitor for potential adverse drug reactions, especially in patients with more severe underlying conditions.
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Adverse drug reactions during eflornithine therapy are frequent and similar to other cytotoxic drugs
Eflornithine is a drug used to treat late-stage African trypanosomiasis, also known as sleeping sickness. It is effective only against Trypanosoma brucei gambiense, which causes Gambian (or West African) sleeping sickness. It is not effective against T. brucei rhodesiense, which causes Rhodesian (or East African) sleeping sickness.
Adverse drug reactions during eflornithine therapy are frequent and similar in nature to other cytotoxic drugs used to treat cancer. The occurrence and intensity of these reactions increase with the duration of treatment and the patient's general condition. While a severe allergic reaction to eflornithine is rare, medical help should be sought immediately if any symptoms of an allergic reaction are observed, such as a rash, itching, swelling (especially of the face, tongue, or throat), severe dizziness, or breathing difficulties.
Other potential side effects of eflornithine include hearing problems like tinnitus or hearing loss, and liver problems, including loss of appetite, nausea, vomiting, upper right abdominal pain, fatigue, itching, dark urine, clay-coloured stools, and jaundice. Eflornithine may also cause low blood cell counts, resulting in fever, chills, fatigue, mouth sores, skin sores, easy bruising, unusual bleeding, pale skin, cold hands and feet, light-headedness, and shortness of breath.
In addition, eflornithine can have adverse effects on foetal development, and both men and women are advised to use birth control while taking the medication and for at least one week after the last dose. Before initiating treatment, a complete blood count, liver function tests, and baseline audiogram tests are recommended.
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Frequently asked questions
It is a drug used to treat late-stage African trypanosomiasis (sleeping sickness).
It works by inhibiting an enzyme called ornithine decarboxylase, which is essential for DNA synthesis, cell division, and growth in both normal and parasitic cells. By inhibiting this enzyme, eflornithine disrupts parasite growth and replication, ultimately causing parasite death.
The typical dosage regimen for the treatment of sleeping sickness consists of 100 mg/kg body weight of eflornithine given as short infusions every 6 hours for 14 days. For children, the dosage is slightly higher at 150 mg/kg body weight.
Yes, adverse drug reactions during eflornithine therapy are frequent and similar to those of other cytotoxic drugs for cancer treatment. The occurrence and intensity of these reactions increase with the duration of treatment and the severity of the patient's condition. Severe reactions, including seizures, fever, diarrhoea, and bacterial infections, have been reported in some patients, and relapses can occur more than 12 months after treatment.
