In vitro susceptibility of Gabonese wild isolates of Plasmodium falciparum to artemether, and comparison with chloroquine, quinine, halofantrine and amodiaquine

Parasitology. 1998 Dec:117 ( Pt 6):541-5. doi: 10.1017/s0031182098003400.

Abstract

The in vitro activity of artemether against 63 African isolates of Plasmodium falciparum from Libreville, Gabon was evaluated using an isotopic drug susceptibility semi-microtest. The 50% inhibitory concentration (IC50) values for artemether were in a narrow range from 0.8 to 34.8 nM (mean IC50 5.0 nM) and the 95% confidence interval (CI95%) was 3.6-6.3 nM. In vitro decreased susceptibility or resistance were observed with artemether (14%), to chloroquine (90%), to quinine (32%). Isolate susceptibility to amodiaquine and halofantrine was high i.e. 100% and 98%, respectively. There was a significant positive correlation between responses to artemether and amodiaquine (r2 = 0.45, P < 0.001), artemether and chloroquine (r2 = 0.36, P < 0.001), artemether and quinine (r2 = 0.31, P < 0.001), and artemether and halofantrine (r2 = 0.19, P < 0.01). Positive correlation between these drugs suggests in vitro cross-resistance or at least common features in drug uptake and/or mode of action or resistance.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Amodiaquine / pharmacology
  • Animals
  • Antimalarials / pharmacology*
  • Artemether
  • Artemisinins*
  • Child
  • Child, Preschool
  • Chloroquine / pharmacology
  • Drug Resistance, Microbial
  • Gabon
  • Humans
  • Infant
  • Malaria, Falciparum / drug therapy
  • Malaria, Falciparum / parasitology
  • Phenanthrenes / pharmacology
  • Plasmodium falciparum / drug effects*
  • Quinine / pharmacology
  • Sesquiterpenes / pharmacology*

Substances

  • Antimalarials
  • Artemisinins
  • Phenanthrenes
  • Sesquiterpenes
  • Amodiaquine
  • Chloroquine
  • Quinine
  • Artemether
  • halofantrine