THE PHARMACOKINETICS OF A SINGLE-DOSE OF ARTEMISININ IN PATIENTS WITHUNCOMPLICATED FALCIPARUM-MALARIA

The pharmacokinetics of artemisinin was studied in 11 Vietnamese patie nts with uncomplicated falciparum malaria after a single 500 mg oral d ose, Curative treatment with mefloquine (15 mg/kg) was provided 24 hr after the artemisinin dose, Artemisinin concentrations were measured b y high-performance liquid chromatography with electrochemical detectio n. The following pharmacokinetic results were found (all mean +/- SD): calculated volume of distribution/bioavailability = 22.8 +/- 16.6 L.k g(-1), mean absorption time = 1.16 +/- 0.92 hr, calculated maximum con centration = 364 +/- 250 mu g.L-1 occurring at 2.88 +/- 1.71 hr after drug intake, and an elimination half-life of 2.72 +/- 1.76 hr. Bioavai lability was low, These results do not differ from results in healthy subjects. Parasites disappeared rapidly, with a mean parasite clearanc e time of 36 hr. No relationship was found between pharmacokinetics an d the parasite elimination rate, Tolerance to the single dose of artem isinin was good, No adverse effects were detected, In conclusion, phar macokinetics of a single dose of artemisinin for uncomplicated falcipa rum malaria is not different from findings in healthy subjects. A sing le dose of 500 mg of artemisinin is effective in reducing parasitemia in nonsevere falciparum malaria and is well-tolerated.