Adjepon-Yamoah K K, Ofori-Adjei D, Woolhouse N M, Lindström B
Ther Drug Monit. 1986;8(2):195-9. doi: 10.1097/00007691-198606000-00012.
The whole-blood kinetics of chloroquine and desethylchloroquine were studied in five healthy Ghanaian subjects. Chloroquine was rapidly absorbed, and peak concentrations were reached within 2 h. The drug disappeared from blood in a multiexponential manner, and the mean terminal half-life from day 7 to day 28 was 13 days. Desethylchloroquine concentrations were generally higher than those of chloroquine after 48 h. Renal clearance accounted for 65% of the apparent total clearance of chloroquine. The estimated mean total urinary recovery of the drug and its desethyl metabolite was 80% of the dose. Whole-blood concentrations of chloroquine offer some advantages compared with plasma concentrations, as this drug concentrates in the formed elements, and special precautions must be taken to obtain representative plasma concentrations.
在五名健康的加纳受试者中研究了氯喹和脱乙基氯喹的全血动力学。氯喹吸收迅速,2小时内达到峰值浓度。药物以多指数方式从血液中消失,第7天至第28天的平均终末半衰期为13天。48小时后,脱乙基氯喹的浓度通常高于氯喹。肾清除率占氯喹表观总清除率的65%。该药物及其脱乙基代谢物的估计平均总尿回收率为给药剂量的80%。与血浆浓度相比,氯喹的全血浓度具有一些优势,因为该药物集中在有形成分中,必须采取特殊预防措施以获得具有代表性的血浆浓度。