PMID: 6608378Mar 23, 1984Paper

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

Biochimica Et Biophysica Acta
R C San GeorgeM E Fabry

Abstract

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.

References

Nov 19, 1979·Life Sciences·R E BrownA D Wolfe
Jun 1, 1978·Antimicrobial Agents and Chemotherapy·L H SchmidtD Vaughan
Feb 14, 1975·Biochimica Et Biophysica Acta·S FischerI Tellez-Nagel
Dec 1, 1977·Annals of Tropical Medicine and Parasitology·W PetersD C Warhurst
Jan 1, 1978·Methods in Enzymology·F W Dahlquist
Feb 1, 1979·Antimicrobial Agents and Chemotherapy·C D FitchR Chevli
Jan 1, 1979·Advances in Pharmacology and Chemotherapy·R S Rozman, C J Canfield
Dec 1, 1979·Antimicrobial Agents and Chemotherapy·R E DesjardinsJ D Chulay
Mar 1, 1976·Antimicrobial Agents and Chemotherapy·D F ClydeR B Hornick
Nov 21, 1975·Science·C M TrenholmeC J Canfield
Jul 1, 1974·The Journal of Clinical Investigation·C D FitchY Gonzalez
Oct 1, 1971·Journal of Medicinal Chemistry·C J OhnmachtR E Lutz
Sep 1, 1980·Analytical Biochemistry·P J Munson, D Rodbard
Jan 1, 1981·Medicinal Research Reviews·T R Sweeney

❮ Previous
Next ❯

Citations

Jun 26, 2001·European Journal of Drug Metabolism and Pharmacokinetics·J A KolawoleN Ochekpe
Oct 1, 1988·Biochemical Pharmacology·G VanderkooiY Yuthavong
Feb 1, 1997·International Journal for Parasitology·M Foley, L Tilley
Aug 27, 1998·Pharmacology & Therapeutics·M Foley, L Tilley
May 6, 2010·Parasitology·E Holmes
Dec 26, 2001·Antimicrobial Agents and Chemotherapy·Nehal VyasChristy M Wyandt
Jan 1, 1995·Critical Reviews in Biochemistry and Molecular Biology·B GiardinaM Castagnola
Oct 15, 2013·The Journal of Pharmacy and Pharmacology·Lissinda H du PlessisAwie F Kotzé
Oct 1, 1986·Chemico-biological Interactions·J H Riviere, D J Back
Aug 1, 1989·British Journal of Clinical Pharmacology·G FranssenF Bricaire
Nov 1, 1985·British Journal of Clinical Pharmacology·J H RivièreR E Howells
Aug 21, 2016·The Brazilian Journal of Infectious Diseases : an Official Publication of the Brazilian Society of Infectious Diseases·José Luiz Fernandes VieiraMargarete do Socorro Mendonça Gomes
Jul 28, 2012·Biology of Reproduction·Remington Lee Nevin
Sep 5, 2013·The American Journal of Tropical Medicine and Hygiene·Nongluk SeethornKesara Na-Bangchang
Jun 16, 2007·Experimental Parasitology·Kesara Na-BangchangSteven A Ward
Jan 1, 1993·Biopharmaceutics & Drug Disposition·H Tajerzadeh, D J Cutler
Mar 19, 2002·Therapeutic Drug Monitoring·Marion L Williams, Irving W Wainer
Jun 1, 1986·Annals of Tropical Medicine and Parasitology·T G GearyH Ginsburg
Dec 5, 2020·Future Medicinal Chemistry·Ranjeet P DashNuggehally R Srinivas

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antimalarial Agents

Antimalarial agents, also known as antimalarials, are designed to prevent or cure malaria. Discover the latest research on antimalarial agents here.

Antimalarial Agents (ASM)

Antimalarial agents, also known as antimalarials, are designed to prevent or cure malaria. Discover the latest research on antimalarial agents here.