BACKGROUND The determination of dosing regimens for the treatment of malaria is largely empirical and thus a better understanding of the pharmacokinetic/pharmacodynamic properties of antimalarial agents is required to assess the adequacy of current treatment regimens and identify sources of suboptimal dosing that could select for drug-resistant parasites. Mefloquine is a widely used antimalaria...

The pharmacokinetics of mefloquine at the therapeutic dose of 750 mg single orally were compared between cured and recrudescent patients with acute uncomplicated falciparum malaria. Mefloquine was well-tolerated during the study. The side-effects found were nausea, vomiting and diarrhea. Five patients showed R-I and two showed R-II types of response. All recrudescent patients came from the east...

BACKGROUND Malaria is a major public health problem representing 2.3% of the overall global disease burden. The cost of treatment of malaria continues to rise as older drugs and insecticides become less effective and are replaced by more effective, but also more expensive products. METHODS A post-hoc pharmacoeconomic analysis (direct and indirect costs only) of three antimalarials, chloroquin...

We studied the polymorphism of msp-1, which encodes a major surface protein on the merozoite, isolated from blood samples from western Thailand in 1999. Our study area was a low-transmission area for malaria, where mefloquine has been used as an antimalarial drug since 1994. Forty-nine patients were confirmed to have contracted falciparum malaria twice within 24 weeks. The number of detected ha...

BACKGROUND During the period of 1996-1999, we prospectively monitored 243 Javanese adults and children after arriving in Papua, Indonesia, and microscopically documented each new case of malaria by active surveillance. METHODS In a randomized, open-label, comparative malaria treatment trial, 72 adults and 50 children received chloroquine for each incident case of malaria, and 74 adults and 47...

The in vitro activity of artemether against 56 African isolates of Plasmodium falciparum from Senegal was evaluated using an isotope-based drug susceptibility semi-microtest. The 50% inhibitory concentration (IC50) values for artemether were in a narrow range from 0.8 to 15.2 nM (mean IC50 = 3.43 nM) and the 95% confidence interval (CI) was 2.50-4.36 nM. Artemether was equally effective on chlo...

Eight naturally occurring monoindole alkaloids were evaluated in vitro for their ability to inhibit Plasmodium falciparum growth and, in drug combination, to reverse the resistance of a chloroquine-resistant strain of Plasmodium falciparum. None of these indole alkaloids has significant intrinsic antiplasmodial activity (IC(50) > 10 microM or 5 microg/ml). Nevertheless, three alkaloids (icajine...

Pulmonary toxicity with mefloquine. E. Udry, F. Bailly, M. Dusmet, P. Schnyder, R. Lemoine, J.W. Fitting. #ERS Journals Ltd 2001. ABSTRACT: This report presents a case of acute lung injury developing within hours after administration of mefloquine for a low-level Plasmodium falciparum malaria, which was persistent despite halofantrine therapy. Extensive microbiological investigation remained ne...

We have analyzed artemisinin sensitivity in Plasmodium falciparum isolates obtained from patients in South Vietnam and show that artemisinin sensitivity does not differ before and after drug treatment. There was an increase in the level of mefloquine resistance in the isolates after drug treatment that was concomitant with a decrease in chloroquine resistance, suggesting that treatment with art...

Resistance to many antimalaria drugs developed on the Cambodia-Thailand border long before developing elsewhere. Because antimalaria resistance is now a global problem, artemisinin-based combination therapies (ACTs) are the first-line therapies in most malaria-endemic countries. However, recent clinical and molecular studies suggest the emergence of ACT-resistant Plasmodium falciparum infection...