Chen B H, Taylor E H, Pappas A A
Clin Chim Acta. 1987 Feb 27;163(1):75-80. doi: 10.1016/0009-8981(87)90035-0.
Disopyramide is an antiarrhythmic drug with concentration dependent protein binding within the therapeutic range. We found good agreement between fluorescence polarization immunoassay (FPIA, Abbott TDX) and high performance liquid chromatography (HPLC) for total disopyramide among 27 admission patients' sera (FPIA = 1.12 (HPLC) -0.002, r = 0.982, SEE = 0.378 mg/l). Agreement between FPIA and HPLC for free disopyramide was similarly good (FPIA = 0.867 (HPLC) -0.003, r = 0.986, SEE = 0.09 mg/l, n = 27). Serum alpha 1 acid glycoprotein concentration (AAG) and free fraction (FF) percent of disopyramide correlated inversely (FF = -0.0112 (AAG) + 31.3 r = 0.707, SEE = 6.41 mg/l, n = 24), and the free disopyramide fraction varied greatly. For two pooled sera with 12 different disopyramide concentrations (range from 0.5-20.0 mg/l), the proportion of free fraction ranged from 6.5 to 73.2%. Overall, we found the free disopyramide fraction variable with each individual, total drug, and protein concentration. Therefore, free drug concentration should be monitored in disopyramide therapy, and FPIA is reliable for free as well as total drug assay.
丙吡胺是一种抗心律失常药物，在治疗范围内具有浓度依赖性蛋白结合。我们发现，在27例入院患者血清中，荧光偏振免疫分析法（FPIA，雅培TDX）与高效液相色谱法（HPLC）测定的丙吡胺总量具有良好的一致性（FPIA = 1.12（HPLC）-0.002，r = 0.982，标准误 = 0.378 mg/l）。FPIA与HPLC测定游离丙吡胺的一致性同样良好（FPIA = 0.867（HPLC）-0.003，r = 0.986，标准误 = 0.09 mg/l，n = 27）。血清α1酸性糖蛋白浓度（AAG）与丙吡胺的游离分数（FF）百分比呈负相关（FF = -0.0112（AAG）+ 31.3，r = 0.707，标准误 = 6.41 mg/l，n = 24），且游离丙吡胺分数变化很大。对于两种含有12种不同丙吡胺浓度（范围为0.5 - 20.0 mg/l）的混合血清，游离分数比例在6.5%至73.2%之间。总体而言，我们发现游离丙吡胺分数因个体、总药物浓度和蛋白质浓度而异。因此，在丙吡胺治疗中应监测游离药物浓度，FPIA对于游离药物和总药物测定都是可靠的。
