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Title: Pharmacokinetics of mefloquine alone or in combination with artesunate
Authors: J. Karbwang
K. Na Bangchang
A. Thanavibul
D. J. Back
D. Bunnag
T. Harinasuta
Mahidol University
Keywords: Medicine
Issue Date: 25-Mar-1994
Citation: Bulletin of the World Health Organization. Vol.72, No.1 (1994), 83-87
Abstract: A randomized comparative trial of the pharmacokinetics and pharmacodynamics of oral doses of mefloquine and of mefloquine in combination with artesunate was carried out on 20 Thai male patients with acute, uncomplicated falciparum malaria. The patients were randomized to receive either mefloquine alone (8 patients; 1250 mg of mefloquine-initial dose, 750 mg; followed 6 hours later by 500 mg), or in combination with oral artesunate (12 patients - initial dose, 200 mg of artesunate; followed by 750 mg and 500 mg of mefloquine 6 hours and 12 hours later, respectively). The patients who received mefloquine alone all showed initially good responses to the treatment, with mean ± SD values for the fever clearance time (FCT) and parasite clearance time (PCT) of 44.7 ± 43.1 hours and 82.3 ± 52.3 hours, respectively. Two patients had recrudescences on day 20 and day 31 (RI response). The cure rate was 75%, and one patient had Plasmodium vivax in his peripheral blood on day 52. The patients who received the combination treatment were clinically markedly improved, with a relatively shorter FCT (31.2 ± 12.4 hours) and significantly shorter PCT (47.5 ± 19.6 hours). Four had recrudescences on days 12, 18, 26 and 33; the cure rate was 66%. Artesunate caused three significant changes in mefloquine pharmacokinetics: a decrease in the maximum concentration (C(max): 1623 -1 versus 2212 -1 ); an increase in the clearance rate (Cl/f: 2.9 ml.min -1 .kg -1 versus 1.1 ml.min -1 .kg -1 ); and an expansion of the volume of distribution (Vd(z)/f: 31.8 -1 versus 25.0 -1 ).
ISSN: 00429686
Appears in Collections:Scopus 1991-2000

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