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The combination of artemether and lumefantrine (benflumetol) is a new and very well tolerated oral antimalarial drug effective even against multidrug-resistant falciparum malaria. The artemether component is absorbed rapidly and biotransformed to dihydroartemisinin, and both are eliminated with terminal half-lives of around 1 hour. These are very active antimalarials which give a rapid reduction in parasite biomass and consequent rapid resolution of symptoms. The lumefantrine component is absorbed variably in malaria, and is eliminated more slowly (half-life of 3 to 6 days). Absorption is very dependent on coadministration with fat, and so improves markedly with recovery from malaria. Thus artemether clears most of the infection, and the lumefantrine concentrations that remain at the end of the 3- to 5-day treatment course are responsible for eliminating the residual 100 to 10 000 parasites. The area under the curve of plasma lumefantrine concentrations versus time, or its correlate the plasma concentration on day 7. has proved an important determinant of therapeutic response. Characterisation of these pharmacokinetic-pharmacodynamic relationships provided the basis for dosage optimisation, an approach that could be applied to other antimalarial drugs.

Original publication

DOI

10.2165/00003088-199937020-00002

Type

Journal article

Journal

Clinical pharmacokinetics

Publication Date

08/1999

Volume

37

Pages

105 - 125

Addresses

Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand. fnnjw@diamond.mahidol.ac.th

Keywords

Animals, Humans, Plasmodium falciparum, Malaria, Ethanolamines, Sesquiterpenes, Artemisinins, Fluorenes, Drug Combinations, Antimalarials, Drug Resistance, Microbial, Drug Resistance, Multiple, Food-Drug Interactions, Clinical Trials as Topic