Fichtl B, Meister W, Schmied R
Int J Clin Pharmacol Ther Toxicol. 1983 May;21(5):241-4.
The aim of this study was to investigate whether serum protein binding of drugs is altered in patients with severe chronic cardiac failure. A total of 27 patients of the cardiac unit participated in the study. One group comprised 15 subjects with chronic cardiac failure (grade III-IV according to the New York Heart Association); 12 patients served as controls (grade I-II). The extent of binding was determined in the therapeutic concentration range by means of equilibrium dialysis at pH 7.4 and 37 degrees C. The binding of six marker drugs shows no difference between controls and patients with chronic cardiac failure. Furthermore, measured free fractions were in the range reported in the literature for healthy, untreated individuals. Our selection of drugs comprised substances that are representative of the three major drug-binding sites on human albumin (diazepam-digitoxin-warfarin/phenytoin). Furthermore, propranolol and imipramine represent examples of drugs binding mainly to lipo- and glycoproteins. The results suggest that the binding of most drugs encountered in clinical practice will be unchanged in patients with chronic cardiac failure.
本研究旨在调查重度慢性心力衰竭患者的药物血清蛋白结合率是否发生改变。心脏科共有27名患者参与了该研究。一组包括15名慢性心力衰竭患者（根据纽约心脏协会分级为III-IV级）；12名患者作为对照组（I-II级）。在pH 7.4和37摄氏度条件下，通过平衡透析法在治疗浓度范围内测定结合程度。六种标记药物在对照组和慢性心力衰竭患者之间的结合情况无差异。此外，测得的游离分数在文献报道的健康未治疗个体范围内。我们选择的药物包括代表人类白蛋白上三个主要药物结合位点的物质（地西泮-洋地黄毒苷-华法林/苯妥英）。此外，普萘洛尔和丙咪嗪是主要与脂蛋白和糖蛋白结合的药物实例。结果表明，临床实践中遇到的大多数药物在慢性心力衰竭患者中的结合情况将保持不变。
