Pharmacokinetics of mefloquine administered with artesunate in patients with uncomplicated falciparum malaria from the Brazilian Amazon basin

Malaria Journal
Michelle V D FerreiraAndré M de Siqueira

Abstract

A fixed-dose combination of mefloquine with artesunate was evaluated in cases of falciparum malaria in the Brazilian Amazon basin with acceptable efficacy, safety and tolerability. However, there are no data on the pharmacokinetics of mefloquine in this coformulation in Brazil, which is valuable to evaluate whether Plasmodium is exposed to an effective concentration of the drug. A prospective, single-arm study was conducted in male patients with slide-confirmed infection by Plasmodium falciparum using two tablets of a fixed-dose combination of artesunate (100 mg) and mefloquine base (200 mg) once daily and over 3 consecutive days. Serial blood samples were collected at admission and throughout 672 h post-administration of the drugs. Mefloquine was measured in each blood sample by high-performance liquid chromatography. The pharmacokinetic parameters were determined by non-compartmental analysis. A total of 61 patients were enrolled in the study and 450 whole blood samples were collected for mefloquine measurement. The mefloquine half-life was 10.25 days, the maximum concentration (Cmax) was 2.53 µg/ml, the area-under-the-curve (AUC0-∞) was 359 µg/ml h, the observed clearance (Cl/f) was 0.045 l/kg/h and the volume of distributio...Continue Reading

References

Oct 1, 1990·Clinical Pharmacokinetics·J Karbwang, N J White
Oct 1, 1990·Clinical Pharmacology and Therapeutics·E F BoudreauP Phintuyothin
Aug 1, 1989·British Journal of Clinical Pharmacology·G FranssenF Bricaire
Jan 1, 1988·European Journal of Clinical Pharmacology·J KarbwangA M Breckenridge
Nov 1, 1995·Transactions of the Royal Society of Tropical Medicine and Hygiene·F O ter KuileN J White
Jan 1, 1997·European Journal of Clinical Pharmacology·C CrevoisierC Kleinbloesem
Jan 30, 1999·Antimicrobial Agents and Chemotherapy·R PriceN J White
Dec 1, 1999·Clinical Pharmacology and Therapeutics·J A SimpsonN J White
Mar 23, 2000·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·G LefèvreM S Thomsen
Nov 18, 2000·Antimicrobial Agents and Chemotherapy·J A SimpsonN J White
Oct 7, 2009·Expert Review of Anti-infective Therapy·Liwang Cui, Xin-zhuan Su
Sep 4, 2014·Memórias do Instituto Oswaldo Cruz·Anielle de Pina-CostaCláudio Tadeu Daniel-Ribeiro
Apr 14, 2016·The American Journal of Tropical Medicine and Hygiene·Simone Ladeia-AndradeMarcelo U Ferreira
May 12, 2016·Malaria Journal·Sheila Vitor-SilvaMarcus Vinícius Guimarães Lacerda

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Citations

Mar 19, 2021·Science Translational Medicine·Erin S CoonahanCarole A Long

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