Weiss Y A, Safar M E, Chevillard C, Frydman A, Simon A, Lemaire P, Alexandre J M
Eur J Clin Pharmacol. 1976;10(6):387-93. doi: 10.1007/BF00563074.
In borderline and permanent hypertensives after rapid i.v. injection of dl-propranolol 0.2 mg/kg plasma levels were measured and were fitted to a two-compartment open-model. In borderline patients, characterized by a high basal cardiac output (CO), plasma levels were always lower than in permanent hypertensives. The biological half-life was reduced and the central volume of distribution, volume of distribution at pseudo-equilibrium and total clearance (TC) were markedly increased. In the overall population, there was a significant positive correlation between CO and TC. Rapid achievement of a predetermined plateau in each group constituted experimental proof of the validity of the two-compartment open-model for kinetic analysis of propranolol i.v. If kinetic parameters from permanent hypertensive were applied to borderline hypertensives a lower plateau was obtained. Thus, in so far as beta-blockade is related to plasma level of propranolol, an increased intravenous dose may be required in patients with high CO.
在临界高血压和持续性高血压患者中，快速静脉注射0.2mg/kg的dl-普萘洛尔后，测定血浆水平，并将其拟合为二室开放模型。在以高基础心输出量（CO）为特征的临界高血压患者中，血浆水平始终低于持续性高血压患者。生物半衰期缩短，中央分布容积、准平衡时分布容积和总清除率（TC）显著增加。在总体人群中，CO与TC之间存在显著正相关。每组快速达到预定平台期构成了二室开放模型用于静脉注射普萘洛尔动力学分析有效性的实验证据。如果将持续性高血压患者的动力学参数应用于临界高血压患者，则会得到较低的平台期。因此，就β受体阻滞与普萘洛尔血浆水平相关而言，高CO患者可能需要增加静脉剂量。
