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氨氯吡咪在兔体内的处置及效应动力学
Simultaneous Modeling of Amiloride Kinetics and Dynamics in Rabbit
【摘要】 用药动学-药效学结合模型对氨氯吡咪在家兔体内的处置和效应动力学作定量分析。氨氯吡咪的Keo,EC50,Emax,S分别为0.040±0.019 min-1,0.33±0.22 μg/ml,0.22±0.04 ml/min,3.41±0.77,其利尿作用的峰值明显滞后于血药浓度峰值,表明血浆与作用部位属于不同的房室,两者之间存在着一个平衡过程。其滞后时间的长短取决于Keo的大小。
【Abstract】 The Pharmacokinetic and pharmacodynamic profiles of amiloride were analyzed by the combined pharmacokinetic and pharmacodynamic model in rabbits, The pharmacodynamic parameters Keo(the elimination rate constant of the effect compartment), EC50 (the drug concentration at half maximum effect), Emax (the maximum drug effect), S (Hill coefficient) for amiloride were 0.040±0.019 min-1, 0.33±0.22 μg/ml, 0.22±0.04 ml/min, 3.41±0.77 respectively. Following an iv dose of amiloride, its maximal diuretic effect occurred after the peak plasma drug concentration. This indicates that the plasma and effect site belong to different compartments and the equilibrium between the plasma and effect site is not reached instantaneously.
- 【文献出处】 中国药科大学学报 ,Journal of China Pharmaceutical University , 编辑部邮箱 ,1993年01期
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