Hellgren U, Alván G, Jerling M
Department of Clinical Pharmacology, Karolinska Institute, Huddinge Hospital, Sweden.
Eur J Clin Pharmacol. 1993;45(4):383-5. doi: 10.1007/BF00265960.
In a review of studies using appropriate methods for drug determinations and controlled intake, an interindividual variation in chloroquine concentrations of 2.3 to 5.6-fold was found. In our department, steady-state concentrations were evaluated in 40 patients with rheumatic diseases. The variation in whole blood concentrations was 11-fold for chloroquine and 10-fold for the desethylchloroquine metabolite. The mean ratio between desethylchloroquine and chloroquine concentrations was 0.53 and the Spearman-Rank correlation 0.92. The correlation between age and the ratio of chloroquine concentration/dose was 0.36 (P < 0.05) and the corresponding correlation for body weight was -0.43 (P < 0.05). Our data indicate that body weight and age are important independent factors for the disposition of chloroquine. However, when extensive 100-fold variations in concentrations are found between individuals we suggest that the reliability of the dose intake should be questioned.
在一项对采用适当药物测定方法和控制摄入量的研究的综述中,发现氯喹浓度的个体间差异为2.3至5.6倍。在我们科室,对40例风湿性疾病患者的稳态浓度进行了评估。氯喹全血浓度的差异为11倍,去乙基氯喹代谢物为10倍。去乙基氯喹与氯喹浓度的平均比值为0.53,Spearman秩相关系数为0.92。年龄与氯喹浓度/剂量比值之间的相关性为0.36(P<0.05),体重的相应相关性为-0.43(P<0.05)。我们的数据表明,体重和年龄是氯喹处置的重要独立因素。然而,当个体间浓度存在100倍的广泛差异时,我们建议应质疑剂量摄入的可靠性。