Gugler R, Shoeman D W, Huffman D H, Cohlmia J B, Azarnoff D L
J Clin Invest. 1975 Jun;55(6):1182-9. doi: 10.1172/JCI108035.
Since the binding of drugs to plasma proteins can significantly after the intensity of pharmacological and toxicological effects of drugs, we studied the pharmacokinetics of three drugs in patients with hypoalbuminemia secondary to the nephrotic syndrome, but with relatively normal renal function. No significant differences were seen in the pharmacokinetic parameters observed for antipyrine, a drug which is less than 10% bound to plasms proteins. The percentage of unbound diphenylhydantoin, a highly plasms protein-bound drug, was found in patients with the nephrotic syndrome to be twice that of healthy individuals (19,2 vs. 10.1%, P smaller than 0.001). However, there was also a lower steady-state plasma concentration of diphenylhydantoin (2.9 plus or minus 0.6 vs. 6.8 plus or minus 0.6 mug/ml, P smaller than 0.001) secondary to an increase in the plasms clearance (0.048 plus or minus 0.019 vs. 0.022 plus or minus 0.006 liter/kg.h, P smaller than 0.001) in the nephrotic patients. The net effect is no difference in the absolute concentration of unbound diphenylhydantoin in healthy individuals (0.69 plus or minus 0.05 mug/ml) and patients with the nephrotic syndrome (0.59 plus or minus 0.06 mug/ml). Qualitatively, similar differences were observed with clofibrate. The dose of these drugs need not be routinely reduced in patients with the nephrotic syndrome as long as they have reasonably normal renal function (creatinine clearance greater than 50 ml/min). With all highly bound acidic drugs, knowledge of the concentration of unbound drug is essential to the proper interpretation of total blood levels and subsequent treatment of the patient.
由于药物与血浆蛋白的结合能显著影响药物的药理和毒理作用强度,我们研究了三种药物在肾病综合征继发低白蛋白血症但肾功能相对正常的患者体内的药代动力学。对于安替比林(一种与血浆蛋白结合率低于10%的药物),观察到的药代动力学参数无显著差异。在肾病综合征患者中,发现高血浆蛋白结合药物苯妥英的未结合百分比是健康个体的两倍(19.2%对10.1%,P小于0.001)。然而,由于肾病患者血浆清除率增加(0.048±0.019对0.022±0.006升/千克·小时,P小于0.001),苯妥英的稳态血浆浓度也较低(2.9±0.6对6.8±0.6微克/毫升,P小于0.001)。净效应是健康个体和肾病综合征患者中未结合苯妥英的绝对浓度无差异(0.69±0.05微克/毫升对0.59±0.06微克/毫升)。在氯贝丁酯方面也观察到了定性的类似差异。只要肾病综合征患者肾功能合理正常(肌酐清除率大于50毫升/分钟),这些药物的剂量无需常规减少。对于所有高度结合的酸性药物,了解未结合药物的浓度对于正确解释全血水平及后续治疗患者至关重要。