Laboratory of Pharmacokinetics of Antimalarial Drugs, Para Federal University, Belém, Brazil.
Trop Med Int Health. 2020 Sep;25(9):1093-1097. doi: 10.1111/tmi.13459. Epub 2020 Jul 27.
To evaluate the extent of chloroquine underdosing and to measure the concentrations of chloroquine and desethylchloroquine in adult patients with P. vivax malaria in the Brazilian Amazon basin.
Prospective study of cases in male adult patients with malaria by Plasmodium vivax treated with a total dose of 1500 mg chloroquine over three days and a short course of primaquine. Patients were weighed at admission, and the dose per mg/kg was determined. Blood samples were collected at 24 and 168 h after enrolment, and the concentrations of chloroquine and desethylchloroquine were measured in plasma by high-performance liquid chromatography with fluorescence detection.
Of 61 patients were included in the study, and 60% received a total dose of chloroquine below 25 mg/kg. Plasma chloroquine concentrations ranged from 90 to 184 ng/ml and from 175 to 827 ng/ml at 24 and 168 hours. For desethylchloroquine, the values ranged from 32 to 144 ng/ml and from 90 to 440 ng/ml at 24 and 168 h. There were no significant correlations between the plasma levels of chloroquine and the doses administered (mg/kg) at 24 and 196 h. Similar results were found for desethylchloroquine.
There is widespread suboptimal dosing of chloroquine that is probably due to the dosing regimen based on patient age, which reduces the drug exposure with a possible influence on parasite clearance.
评估氯喹的用药不足程度，并测量巴西亚马逊流域成人间日疟患者体内氯喹和去乙基氯喹的浓度。
前瞻性研究了在成年男性疟疾病例中，采用总剂量为 1500mg 氯喹，分三天给予，同时短程给予伯氨喹。患者入院时称重，确定每毫克/公斤的剂量。在入组后 24 小时和 168 小时采集血样，采用高效液相色谱法-荧光检测法测定血浆中氯喹和去乙基氯喹的浓度。
共有 61 例患者纳入研究，其中 60%的患者总氯喹剂量低于 25mg/kg。血浆氯喹浓度在 24 小时和 168 小时时分别为 90 至 184ng/ml 和 175 至 827ng/ml。去乙基氯喹的浓度分别为 32 至 144ng/ml 和 90 至 440ng/ml。在 24 小时和 168 小时时，氯喹的血浆水平与给予的剂量（mg/kg）之间均无显著相关性。去乙基氯喹也存在类似结果。
氯喹的用药不足现象普遍存在，这可能是由于基于患者年龄的给药方案导致药物暴露减少，从而可能影响寄生虫清除。
