Stereoselectivity in the disposition of chloroquine and desethylchloroquine in rabbits.
Stereoselective pharmacokinetic properties of chloroquine (CAS 54-05-7) and desethylchloroquine were investigated in rabbits by administration of the separate enantiomers according to a cross-over design. The terminal half-life was longer for (R)-chloroquine than for (S)-chloroquine. A striking difference was revealed in the concentrations of metabolites. The levels of (R)-desethylchloroquine were higher than those of (S)-desethylchloroquine, resulting in a statistically significant higher AUC for the (R)-metabolite than for the (S)-metabolite.
Augustijns
P
P
Laboratory of Clinical Pharmacy, University of Leuven, Belgium.
Verbeke
N
N
D000818:Animals; D002738:Chloroquine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D005260:Female; D006207:Half-Life; D007273:Injections, Intramuscular; D008297:Male; D011817:Rabbits; D013237:Stereoisomerism; D014018:Tissue Distribution
D002738:Chloroquine; C007278:desethylchloroquine