Andreasen F, Husted S
Acta Pharmacol Toxicol (Copenh). 1980 Sep;47(3):202-7. doi: 10.1111/j.1600-0773.1980.tb01560.x.
The percentual binding of furosemide (5 micrograms/ml) was slightly but significantly lower in serum from elderly patients than in serum from normal blood donors (96.5 +/- 0.7 versus 97.9 +/- 0.3). A significant positive correlation was demonstrated between protein binding and albumin concentration in serum. The reduced binding in the elderly could be explained by an observed decrease in the concentration of albumin in the elderly. The percentual binding did not change in samples obtained during the first hour after the intravenous administration of 40 mg furosemide. Of 4-chloro-5-sulfamoyl antranilic acid (CSA) and antranilic acid (A) about 60% were bound to serum proteins in vitro and none of these two compounds affected the protein binding of furosemide. The addition of phenprocoumon (PPC) caused significant decreases in the percentual binding of furosemide in serum (5 microgram/ml) at PPC values of 10 microgram/ml and more. The effect of PPC on the binding of furosemide was studied in vivo in 7 patients receiving 40 mg furosemide intravenously without and with the simultaneous intravenous administration of PPC (3 mg per 10 kg body weight). In good accordance with the in vitro experiments the modest average decrease in furosemide binding, caused by concentrations of PPC not exceeding 6.2 micrograms/ml, was not significant.
老年患者血清中呋塞米(5微克/毫升)的结合百分比略低于正常献血者血清中的结合百分比,但具有统计学意义(96.5±0.7对97.9±0.3)。血清中蛋白质结合与白蛋白浓度之间呈显著正相关。老年人结合能力降低可归因于观察到的老年人白蛋白浓度下降。静脉注射40毫克呋塞米后第一小时内采集的样本中,结合百分比没有变化。在体外,4-氯-5-氨磺酰基邻氨基苯甲酸(CSA)和邻氨基苯甲酸(A)约60%与血清蛋白结合,且这两种化合物均不影响呋塞米的蛋白结合。当苯丙香豆素(PPC)浓度达到10微克/毫升及以上时,会导致血清中呋塞米(5微克/毫升)的结合百分比显著下降。在7名接受静脉注射40毫克呋塞米的患者中,在未同时静脉注射PPC(每10千克体重3毫克)和同时静脉注射PPC的情况下,对PPC对呋塞米结合的影响进行了体内研究。与体外实验结果高度一致,由浓度不超过6.2微克/毫升的PPC引起的呋塞米结合的适度平均下降并不显著。