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Please use this identifier to cite or link to this item: http://repository.li.mahidol.ac.th/dspace/handle/123456789/26678
Title: A comparison of oral artesunate and artemether antimalarial bioactivities in acute falciparum malaria
Authors: Yupin Suputtamongkol
Paul N. Newton
Brian Angus
Paktiya Teja-Isavadharm
Duangsuda Keeratithakul
Maneerat Rasameesoraj
Sasithon Pukrittayakamee
Nicholas J. White
Faculty of Medicine, Siriraj Hospital, Mahidol University
Mahidol University
John Radcliffe Hospital
Armed Forces Research Institute of Medical Sciences, Thailand
Keywords: Medicine;Pharmacology, Toxicology and Pharmaceutics
Issue Date: 1-Dec-2001
Citation: British Journal of Clinical Pharmacology. Vol.52, No.6 (2001), 655-661
Abstract: Aims: Artesunate and artemether are the two most widely used artemisinin derivatives in the treatment of uncomplicated Plasmodium falciparum malaria, but there is little information on their comparative pharmacokinetics. The aim of this study was to examine the relative oral antimalarial bioavailability and pharmacokinetics of the two derivatives. Methods: The pharmacokinetic properties of oral artesunate and artemether (4 mg kg-1) were compared in a randomized cross-over study of 14 adult patients in western Thailand with acute uncomplicated Plasmodium falciparum malaria. Antimalarial activity was compared using a previously validated, sensitive bioassay. Results: Despite a 29% lower molar dose, oral artesunate administration resulted in significantly larger mean area under the plasma antimalarial activity time curve and median maximum plasma antimalarial activity than after oral artemether (P≤0.02). The mean (95% CI) oral antimalarial bioavailability of artemether, relative to oral artesunate, corrected for molar dose was 58 (40-76)%. The mean (95% CI) relative antimalarial bioavailability of artemether was lower on the first day of treatment, 31 (17-100)%, compared to the second day, 72 (44-118)% (P=0.018). In vivo parasite clearance and time above the in vitro IC90were similar for the two drugs, despite considerable differences in Cmaxand AUC. Conclusions: The oral antimalarial bioavailability following artemether was significantly lower than that after artesunate. Artemether oral antimalarial bioavailability is reduced in acute malaria.
URI: https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=0035668954&origin=inward
http://repository.li.mahidol.ac.th/dspace/handle/123456789/26678
ISSN: 03065251
Appears in Collections:Scopus 2001-2005

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