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Antimicrobial Agents and Chemotherapy, April 2002, p. 1026-1031, Vol. 46, No. 4
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.4.1026-1031.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

Artemisinin Pharmacokinetics and Efficacy in Uncomplicated-Malaria Patients Treated with Two Different Dosage Regimens

Toufigh Gordi,1,{dagger}* Dinh Xuan Huong,2 Trinh Ngoc Hai,2 Nguyen Thi Nieu,2 and Michael Ashton1,{ddagger}

Division of Pharmacokinetics and Drug Therapy, Faculty of Pharmacy Uppsala University, Uppsala, Sweden,1 National Institute of Malariology, Parasitology, and Entomology, Hanoi, Vietnam2

Received 14 February 2001/ Returned for modification 15 September 2001/ Accepted 26 December 2001

The immediate efficacies of two oral dosage regimens of artemisinin were investigated in 77 male and female adult Vietnamese falciparum malaria patients randomly assigned to treatment with either 500 mg of artemisinin daily for 5 days (group A; n = 40) or artemisinin at a dose of 100 mg per day for 2 days, with the dose increased to 250 mg per day for 2 consecutive days and with a final dose of 500 mg on the fifth day (group B; n = 37). Parasitemia was monitored every 4 h. The average parasite clearance time was longer in group B than in group A (means ± standard deviations, 50 ± 23 and 34 ± 14 h, respectively; P < 0.01). Artemisinin concentrations in saliva samples obtained on days 1 and 5 were quantified by high-performance liquid chromatography. The average oral clearance, based on saliva drug concentrations in group B patients, was twofold higher than that in group A patients on day 1 (P < 0.01), with no differences in drug half-lives (P = 0.40), indicating a saturable first-pass metabolism. Female patients had higher oral clearance values on day 1. Artemisinin's pharmacokinetic parameters were similar on day 5 in both groups, although a significant increase in oral clearance from day 1 to day 5 was evident. Thus, artemisinin exhibited both dose- and time-dependent pharmacokinetics. The escalating dose studied did not result in higher artemisinin concentrations toward the end of the treatment period.

* Corresponding author. Present address: Pharmacia Singapore Clinical Pharmacology Unit 101 Thomson Rd., No. 17-01 United Square Singapore 307591, Singapore. Phone: 65-358-0111. Fax: 65-258-3075. E-mail: toufigh.gordi{at}pharmacia.com.

{dagger} Present address: Pharmacia Singapore Clinical Pharmacology, Singapore 307591, Singapore.

{ddagger} Present address: Unit for Pharmacokinetics and Drug Metabolism, Göteborg University, Göteborg, Sweden.

Antimicrobial Agents and Chemotherapy, April 2002, p. 1026-1031, Vol. 46, No. 4
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.4.1026-1031.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.



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