Lumefantrine

Lumefantrine is a synthetic antimalarial medication used in combination with artemether as part of artemisinin-based combination therapy (ACT). In fixed-dose formulations it is widely marketed with artemether under names such as Coartem. The combination is recommended for the treatment of uncomplicated malaria caused by Plasmodium falciparum, and is used in both adults and children, especially in areas with resistance to other antimalarials.

Lumefantrine acts by interfering with the parasite’s ability to detoxify heme, inhibiting the formation of hemozoin in the parasite’s digestive vacuole. This leads to accumulation of toxic heme and death of the parasite. The drug is long-acting, providing a sustained antimalarial effect, which complements the rapid action of artemether.

Pharmacokinetics and administration: lumefantrine is highly lipophilic with poor water solubility. Absorption is enhanced when taken with a fatty meal or milk. It has a long elimination half-life, measured in days, and is primarily metabolized by cytochrome P450 3A4 to active and inactive metabolites. The drug and its metabolites are largely excreted in feces. It is administered as part of a multi-dose course over several days; taking doses with meals containing fat improves absorption and efficacy.

Safety and interactions: common adverse effects include headache, dizziness, nausea, vomiting, and fever. Serious adverse events are rare but may include QT interval prolongation, particularly when combined with other QT-prolonging drugs or CYP3A4 modulators. Lumefantrine should be used under medical supervision according to local guidelines, with consideration of pregnancy, liver function, and potential drug interactions. It is not used for severe malaria, which requires parenteral therapy.