文章基本信息

标题：In Vitro-in Vivo Correlation of Pharmacodynamics of Felodipine in Essential Hypertensive Patients Based on an Ion-Channel Binding Model
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作者：Yukiko NAKAJIMA ; Koujirou YAMAMOTO ; Shuji SHIMADA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1996
卷号：19
期号：8
页码：1097-1099
DOI：10.1248/bpb.19.1097
出版社：The Pharmaceutical Society of Japan
摘要：The relationship between the plasma drug concentration and the antihypertensive effect of felodipine was analyzed by an ion-channel binding model which takes into consideration the slow association/dissociation process of a drug at the calcium channel. The in vitro dissociation constant (K_d) of felodipine to the calcium channel in the heart of rats was determined, and was compared to the in vivo dissociation constant (D_{d, calc}) estimated by the pharmacodynamic analysis of the concentration-effect data in Japanese essential hypertensive patients obtained from literature. The relative relationship between K_d and K of felodipine was substantially identical with eight other calcium channel blocking agents reported previously. This result suggested the possibility that we can predict the pharmacodynamic behavior of newly developed calcium channel blocking agents from the in vitro K_d value and plasma concentration-time profile in human using the ion-channel binding model.
关键词：felodipine;calcium channel blocker;pharmacodynamic model