Chau N P, Weiss Y A, Safar M E, Lavene D E, Georges D R, Milliez P L
Clin Pharmacol Ther. 1977 Nov;22(5 Pt 1):505-10. doi: 10.1002/cpt1977225part1505.
Intravenous and oral pharmacokinetics of pinlolol were studied in 18 hypertensive patients-9 with normal renal function and 9 with impaired renal function. Analysis of data showed that a linear two-compartment model was suitable to describe the pindolol kinetics. Compared with patients with normal renal function, patients with chronic renal failure exhibited: (1) unchanged transfer rate constants and distribution volumes and (2) decreased total body clearance with decreased renal clearance and unchanged nonrenal clearance. Analysis of oral data by the Loo-Riegelman method showed that the pindolol absorption kinetic was not first order. Compared with patients with normal renal function, patients with chronic renal failure exhibited decreased fraction of dose effectively absorbed and increased initial rate of absorption. The initial rate of absorption was inversely correlated with the creatinine clearance. The study disclosed evidence that absorption was modified in chronic renal failure.
在18例高血压患者中研究了心得平的静脉和口服药代动力学，其中9例肾功能正常，9例肾功能受损。数据分析表明，线性二室模型适合描述心得平的动力学。与肾功能正常的患者相比，慢性肾衰竭患者表现为：（1）转运速率常数和分布容积不变；（2）全身清除率降低，肾清除率降低而非肾清除率不变。用Loo-Riegelman方法分析口服数据表明，心得平的吸收动力学不是一级的。与肾功能正常的患者相比，慢性肾衰竭患者有效吸收剂量分数降低，初始吸收速率增加。初始吸收速率与肌酐清除率呈负相关。该研究揭示了慢性肾衰竭时吸收发生改变的证据。
