artemether (an artemisinin derivative) is an antimalarial agent used in combination with lumefantrine for the treatment of acute uncomplicated malaria caused by Plasmodium falciparum
is administered in combination with lumefantrine for improved efficacy
artemisinin-based combination therapies are highly effective first-line malaria treatments (1)
artemether-lumefantrine is the most widely used and the current WHO guidelines, which recommend weight-based dosing regimens for children, were extrapolated from adult clinical studies
artemisinin derivatives allow more parasite clearance than any other anti-malarial drug (parasite numbers can be reduced by a factor of 10^5 per asexual cycle, compared with 10^2-10^3 with other anti-malarial drugs) (2)
combination therapy exerts its effects against the erythrocytic stages of Plasmodium spp. and may be used to treat infections caused by P. falciparum and unidentified Plasmodium species, including infections acquired in chloroquine-resistant areas
artemether works against the erythrocytic stages of P. falciparum via inhibition of nucleic acid and protein synthesis
has a rapid onset of action and is rapidly cleared from the body
provides rapid symptomatic relief by reducing the number of malarial parasites
is administered in combination with lumefantrine for improved efficacy
when combined with efficacious anti-malarials with slower elimination rates, such as lumefantrine, shorter courses of treatment (three days) become effective (2)
in comparison to artemether, lumefantrine has a much longer half life and is believed to clear residual parasites
lumefantrine exposure is crucial to prevent malaria recrudescence, and the day 7 concentration is a significant factor in determining therapeutic response
Reference:
Simeon S et al. Optimizing Lumefantrine Dosing for Young Children in High-Malaria-Burden Countries Using Pharmacokinetic-Pharmacodynamic Simulations. Open Forum Infect Dis. 2024 Oct 17;11(11):ofae627.
Makanga M, Krudsood S. The clinical efficacy of artemether/lumefantrine (Coartem). Malar J. 2009 Oct 12;8 Suppl 1(Suppl 1):S5. doi: 10.1186/1475-2875-8-S1-S5.
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