Colvin R A, Ashavaid T F, Katz A M, Messineo F C
Department of Zoological and Biomedical Sciences, Ohio University College of Osteopathic Medicine, Athens 45701.
J Cardiovasc Pharmacol. 1990 Oct;16(4):519-22. doi: 10.1097/00005344-199010000-00001.
The binding of [3H]digoxin to purified canine cardiac sarcolemmal vesicles was characterized. Scatchard analysis of saturation isotherms yielded linear plots with a maximal binding capacity of 174 +/- 31.9 pmol/mg, a dissociation constant of 31.7 +/- 4.59 nM, and a Hill coefficient of 0.947 +/- 0.02 (mean +/- SEM), suggesting that [3H]digoxin bound to a single class of sites. In contrast to their marked effect on steady-state serum digoxin levels when administered in combination, quinidine, verapamil, and amiodarone were without effect on equilibrium binding of [3H]digoxin. Thus, increased steady-state serum concentrations of digoxin resulting from combination therapy with these particular drugs probably will have cardiac effects that may increase the risk of digitoxicity to the patient.
对[3H]地高辛与纯化的犬心肌肌膜囊泡的结合特性进行了表征。对饱和等温线进行Scatchard分析得到线性图,最大结合容量为174±31.9 pmol/mg,解离常数为31.7±4.59 nM,希尔系数为0.947±0.02(平均值±标准误),表明[3H]地高辛与单一类别的位点结合。与联合给药时对稳态血清地高辛水平有显著影响相反,奎尼丁、维拉帕米和胺碘酮对[3H]地高辛的平衡结合没有影响。因此,与这些特定药物联合治疗导致的地高辛稳态血清浓度升高可能会对心脏产生影响,从而增加患者发生洋地黄中毒的风险。