Publication: Ex vivo blood schizontocidal activities of artemisinin derivatives against Plasmodium falciparum
Issued Date
1999-06-01
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ISSN
01251562
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2-s2.0-0033139574
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Mahidol University
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SCOPUS
Bibliographic Citation
Southeast Asian Journal of Tropical Medicine and Public Health. Vol.30, No.2 (1999), 225-231
Suggested Citation
Ratawan Ubalee, Dujdao Songthammawat, Kesara Na-Bangchang, Peerapan Tan-Ariya, Juntra Karbwang Ex vivo blood schizontocidal activities of artemisinin derivatives against Plasmodium falciparum. Southeast Asian Journal of Tropical Medicine and Public Health. Vol.30, No.2 (1999), 225-231. Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/25633
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Title
Ex vivo blood schizontocidal activities of artemisinin derivatives against Plasmodium falciparum
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Abstract
Serum samples collected at intervals from eight healthy volunteers after the administration of the six regimens of artemisinin derivatives were investigated for their ex vivo blood schizontocidal activities against K1 strain Plasmodium falciparum. The regimens included single doses of (a) 300 mg oral artemether; (b) 300 mg intramuscular artemether; (c) 100 mg suppository artemether; (d) 300 mg oral artesunate (Guillin formulation); (e) 300 mg oral artesunate (Arenco formulation); (f) 300 mg oral dihydroartemisinin. Sera collected after various regimens of artemisinin derivatives showed distinct degree of ex vivo blood schizontocidal activities. Activity of sera after suppository dosing was remarkably low and variable comparing to the other two formulations (oral, intramuscular). Median values for Amax (the maximum activity normalized with dose) of sera from oral dosing were 2.4- and 118-fold, while AUA (the area under activity-time curve, normalized with dose) were 0.82- and 2,370-fold of that after the intramuscular and suppository dosing, respectively. Sera from artesunate-Arenco dosing exhibited significantly higher Amax and AUA (medians: Amax 12.4 vs 5.13 nmol/l/mg dose; AUA: 21.9 vs 8.8 nmol.h/ml/mg dose), compared to that from artesunate-Guillin dosing. Among the oral formulations of artemisinin derivatives investigated (artemether, artesunate, dihydroartemisinin), sera collected following a single dose of oral dihydroartemisinin exhibited lowest bioactivity (Amax 2.35 nmol/l/mg dose: AUA: 44 nmol.h/ml/mg dose).