Indications
Lumefantrine, in combination with artemether, is primarily indicated for the treatment of acute uncomplicated malaria caused by Plasmodium falciparum. This therapy is particularly effective in regions where malaria is resistant to chloroquine. It is also prescribed for cases of uncomplicated malaria when the specific Plasmodium species has not been identified. The regimen is suitable for adults as well as children who weigh more than 5 kilograms.
Pharmacodynamics
Lumefantrine acts as a blood schizonticide that targets the erythrocytic stages of Plasmodium falciparum. When combined with artemether, the two drugs work synergistically to enhance antimalarial efficacy. Artemether is characterized by its rapid onset of action and quick clearance from the body, which provides prompt relief by swiftly reducing the malarial parasite load. Lumefantrine, with its longer half-life, ensures the clearance of residual parasites, contributing to sustained therapeutic effects.
Absorption
The absorption of lumefantrine is significantly enhanced when taken with food. This increase in absorption is crucial for achieving optimal therapeutic levels of the drug in the bloodstream.
Metabolism
Lumefantrine undergoes extensive hepatic metabolism, primarily through the cytochrome P450 3A4 enzyme. During this process, the principal metabolite formed and detected in plasma is desbutyl-lumefantrine. This metabolic pathway plays a vital role in the drug's pharmacokinetics and efficacy.
Mechanism of Action
The precise mechanism through which lumefantrine achieves its antimalarial effect remains unidentified. Nonetheless, current evidence indicates that lumefantrine acts by inhibiting the formation of β-hematin. This process involves the compound forming a complex with hemin, thereby interfering with the synthesis of nucleic acids and proteins.
