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Please use this identifier to cite or link to this item: http://repository.li.mahidol.ac.th/dspace/handle/123456789/25777
Title: Pharmacokinetics of benflumetol given as a fixed combination artemether-benflumetol (CGP 56697) in Thai patients with uncomplicated falciparum malaria
Authors: K. Na-Bangchang
J. Karbwang
U. Tasanor
A. Thanavibul
E. Farkad
R. Mull
Mahidol University
Novartis International AG
Thammasat University
Keywords: Pharmacology, Toxicology and Pharmaceutics
Issue Date: 1-Dec-1999
Citation: International Journal of Clinical Pharmacology Research. Vol.19, No.2 (1999), 41-46
Abstract: The pharmacokinetics of benflumetol as a fixed combination, artemether-benflumetol (CGP 56697), following three regimens [regimen A: four tablets at 0, 8, 24 and 48 h (320 mg artemether, 1920 mg benflumetol); regimen B: two tablets at 0, 8, 24 and 48 h (160 mg artemether; 960 mg benflumetol); regimen C: four tablets at 0, 8 and 24 h (240 mg artemether; 1440 mg benflumetol)] were investigated in 39 patients with acute uncomplicated falciparum malaria. All patients showed a rapid initial response with a median parasite clearance time of 40, 41 and 39.5 h and a fever clearance time of 27.8, 32 and 24.5 h for regimens A, B and C, respectively. In nine patients (two, four and three patients in regimens A, B and C, respectively), however parasitemia reappeared in the peripheral blood smear between days 9 and 23. The pharmacokinetics of benflumetol were highly variable with coefficients of variation in pharmacokinetic parameters ranging from 14.9% to 144%. Absorption and elimination of benflumetol were relatively slow. Median C(max) per dose (first dose) was significantly higher in regimen B (6.29 ng/ml/mg dose) than in regimen A (2.6 ng/ml/mg dose) and regimen C (3.06 ng/ml/mg dose). Mean t(1/2z) in regimen C (2.65 h) was significantly shorter than in regimen A (4.5 h) and regimen B (3.89 h). In patients on regimens A and B who showed a sensitive response, plasma concentrations of benflumetol were significantly higher than in those with treatment failure.
URI: https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=0033402421&origin=inward
http://repository.li.mahidol.ac.th/dspace/handle/123456789/25777
ISSN: 02511649
Appears in Collections:Scopus 1991-2000

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