Abstract
The protein binding of racemic chloroquine, its enantiomers and desethylchloroquine to plasma, purified human albumin, and alpha 1-acid glycoprotein (alpha 1-AGP) was determined by equilibrium dialysis. The binding was not concentration dependent. (+)-Chloroquine bound more to plasma (66.6 +/- 1.9%) and albumin (45.9 +/- 0.8%) than (-)-chloroquine (48.5 +/- 2.4% and 35.3 +/- 0.6%, respectively). These differences were statistically significant. (-)-Chloroquine bound more to alpha 1-AGP (47.5 +/- 0.7%) than (+)-chloroquine (34.5 +/- 0.5%). The binding of desethylchloroquine to alpha 1-AGP is higher than to albumin (38.9 +/- 0.9% and 21.1 +/- 0.4%, respectively.
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- Aderounmu A. F. In vitro assessment of the antimalarial activity of chloroquine and its major metabolites. Ann Trop Med Parasitol. 1984 Dec;78(6):581–585. doi: 10.1080/00034983.1984.11811868. [DOI] [PubMed] [Google Scholar]
- Alván G., Ekman L., Lindström B. Determination of chloroquine and its desethyl metabolite in plasma, red blood cells and urine by liquid chromatography. J Chromatogr. 1982 Apr 16;229(1):241–247. doi: 10.1016/s0378-4347(00)86059-4. [DOI] [PubMed] [Google Scholar]
- Fu S., Björkman A., Wåhlin B., Ofori-Adjei D., Ericsson O., Sjöqvist F. In vitro activity of chloroquine, the two enantiomers of chloroquine, desethylchloroquine and pyronaridine against Plasmodium falciparum. Br J Clin Pharmacol. 1986 Jul;22(1):93–96. [PMC free article] [PubMed] [Google Scholar]
- Haberkorn A., Kraft H. P., Blaschke G. Antimalarial activity of the optical isomers of chloroquine diphosphate. Tropenmed Parasitol. 1979 Sep;30(3):308–312. [PubMed] [Google Scholar]
- Verdier F., Le Bras J., Clavier F., Hatin I. Blood levels and in vitro activity of desethylchloroquine against Plasmodium falciparum. Lancet. 1984 May 26;1(8387):1186–1187. doi: 10.1016/s0140-6736(84)91436-3. [DOI] [PubMed] [Google Scholar]
- Walker O., Birkett D. J., Alván G., Gustafsson L. L., Sjöqvist F. Characterization of chloroquine plasma protein binding in man. Br J Clin Pharmacol. 1983 Mar;15(3):375–377. doi: 10.1111/j.1365-2125.1983.tb01513.x. [DOI] [PMC free article] [PubMed] [Google Scholar]