Pharmacokinetics of mefloquine, when given alone and in combination with artemether, in patients with uncomplicated falciparum malaria

Fundam Clin Pharmacol. 1995;9(6):576-82. doi: 10.1111/j.1472-8206.1995.tb00536.x.

Abstract

The pharmacokinetics of mefloquine at a single oral dose of 750 mg, when given alone or 24 hours after a single oral dose of artemether (300 mg) was investigated in 27 Thai patients with acute uncomplicated falciparum malaria (17 with mefloquine alone, 10 with the combination). The oral bioavailabiiity of mefloquine was significantly decreased when administered 24 hours after an oral dose of artemether. This was evident by the significantly lower values of Cmax, AUC[0-24 h], AUC[0-48 h], AUC[0-72 h], as well as total AUC[Cmax: 1,290 (827-2,619) vs 1,820 (1,283-2,531) ng.ml-1; AUC[0-24 h]: 0.99 (0.64-1.41) vs 1.33 (1.07-1.95) micrograms.day.ml-1; AUC[0-48 h]: 1.78(1.23-2.58) vs 2.67 (2.09-3.84) micrograms.day.ml-1; AUC[0-72 h]: 2.74 (1.63-3.6) vs 4.54 (2.88-5.38) micrograms.day.ml-1; AUC: 11.11 (6-20.96) vs 15.29 (9.3-36.71) micrograms.day.ml-1]. Tmax was also delayed with the combination regimen [14 (5-24) vs 6 (4-16) h]. Terminal elimination half-lives were comparable [t1/2z: 11.1 (6.8-14.3) vs 13.4 (10.5-19.1) h].

Publication types

  • Clinical Trial
  • Controlled Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adolescent
  • Adult
  • Antimalarials / adverse effects
  • Antimalarials / pharmacokinetics*
  • Artemether
  • Artemisinins*
  • Biological Availability
  • Drug Interactions
  • Humans
  • Malaria, Falciparum / metabolism*
  • Malaria, Falciparum / parasitology
  • Male
  • Mefloquine / adverse effects
  • Mefloquine / pharmacokinetics*
  • Sesquiterpenes / adverse effects
  • Sesquiterpenes / pharmacology*

Substances

  • Antimalarials
  • Artemisinins
  • Sesquiterpenes
  • Artemether
  • Mefloquine