Notterman D A, Drayer D E, Metakis L, Reidenberg M M
Clin Pharmacol Ther. 1986 Nov;40(5):511-7. doi: 10.1038/clpt.1986.216.
Quinidine and quinine are stereoisomers. When given sequentially or simultaneously, the renal clearance of values of quinidine and quinine were measured in seven healthy volunteers and when given simultaneously, to an additional five elderly men. Analytic specificity was provided by an HPLC drug assay. Protein binding was measured by equilibrium dialysis. The quinidine clearance exceeded the quinine clearance in every individual. The mean (+/- SD) ratio of these clearances was 4.2 +/- 1.4 when the drugs were given together and 4.4 +/- 2.3 when they were given separately in the younger subjects and 3.4 +/- 0.5 when given simultaneously to the elderly. Calculating clearance of drug in serum water (unbound drug clearance) revealed a quinidine clearance of 6.1 +/- 2.3 times that of creatinine measured simultaneously, and for quinine it was 1.5 +/- 0.6 times that of creatinine. We conclude that there is stereoselective net renal tubular secretion of quinidine over quinine indicating stereoselectivity of this renal tubular transport process.
奎尼丁和奎宁是立体异构体。在七名健康志愿者中依次或同时给予这两种药物后，测量了奎尼丁和奎宁的肾清除率，并在另外五名老年男性中同时给予这两种药物。通过高效液相色谱法药物分析提供分析特异性。通过平衡透析测量蛋白质结合。在每个个体中，奎尼丁的清除率均超过奎宁的清除率。在年轻受试者中，当两种药物一起给予时，这些清除率的平均（±标准差）比值为4.2±1.4，分开给予时为4.4±2.3，在老年受试者中同时给予时为3.4±0.5。计算血清水中药物的清除率（未结合药物清除率）显示，奎尼丁的清除率是同时测量的肌酐清除率的6.1±2.3倍，而奎宁的清除率是肌酐清除率的1.5±0.6倍。我们得出结论，与奎宁相比，存在对奎尼丁的立体选择性净肾小管分泌，表明该肾小管转运过程具有立体选择性。
