On the mechanism for the red-cell accumulation of mefloquine, an antimalarial drug

Biochim Biophys Acta. 1984 Mar 23;803(3):174-81. doi: 10.1016/0167-4889(84)90007-7.


The accumulation of the antimalarial drug mefloquine by human red blood cells has been studied by 19F-NMR spectroscopy. The uptake process was nonlinearly dependent on the external drug concentration. Concentrations inside cells as high as 60-times greater than those in the extracellular phosphate-buffered-saline were observed. Red-cell ghosts were also found to accumulate mefloquine with high-affinity binding sites for the drug. Hemoglobin was found to bind mefloquine with low affinity, but due to the high concentration of this protein it is a significant drug compartment in the red cell. Analysis of the 19F-NMR chemical shifts and linewidths of mefloquine in the presence of red cells, red-cells ghosts and hemoglobin indicates restricted mobility of the drug in the membrane-bound state and slow exchange with the extracellular medium. This is a significant characteristic of the reaction in connection with the prophylactic activity of the drug. Exchange of the drug between hemoglobin and the red-cell membrane, however, is fast and may play an important role in the bioavailability of the drug to the parasite.

MeSH terms

  • Antimalarials / blood*
  • Biological Transport
  • Erythrocyte Membrane / metabolism
  • Erythrocytes / metabolism*
  • Humans
  • Kinetics
  • Magnetic Resonance Spectroscopy
  • Mefloquine
  • Quinolines / blood*


  • Antimalarials
  • Quinolines
  • Mefloquine