Lumefantrine
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Lumefantrine is an antimalarial drug used in combination with artemether to treat malaria. It is part of the artemisinin-based combination therapies (ACTs) recommended by the World Health Organization for the treatment of uncomplicated Plasmodium falciparum malaria.
Pharmacology[edit]
Lumefantrine is a lipophilic compound that is poorly soluble in water. It is absorbed in the gastrointestinal tract and is metabolized in the liver by the cytochrome P450 system, primarily by the enzyme CYP3A4. The drug has a long half-life, which helps in maintaining therapeutic levels in the blood for an extended period, thus aiding in the prevention of malaria recurrence.
Mechanism of Action[edit]
Lumefantrine works by interfering with the haem polymerization process in the Plasmodium parasites. This process is crucial for the parasite's survival as it detoxifies the free haem released during the digestion of hemoglobin. By inhibiting this process, lumefantrine causes the accumulation of toxic haem, leading to the death of the parasite.
Clinical Use[edit]
Lumefantrine is used in combination with artemether, marketed under the brand name Coartem. This combination is effective against chloroquine-resistant strains of Plasmodium falciparum. The combination therapy is administered orally and is typically given over a three-day course.
Side Effects[edit]
Common side effects of lumefantrine include headache, dizziness, anorexia, and nausea. Serious side effects are rare but may include allergic reactions and QT interval prolongation, which can lead to arrhythmias.
History[edit]
Lumefantrine was developed in the 1980s and was initially used in China. It gained international recognition after being included in the World Health Organization's List of Essential Medicines. The combination with artemether was developed to enhance efficacy and reduce the risk of resistance.
Related pages[edit]
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Lumefantrine
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