兔体内普鲁卡因胺对致颤阈影响的药动学和药效学模型  

COMBINED PHARMACOKINETIC—PHARMACODYNAMIC MODEL OF PROCAINAMIDE IN RABBITS WITH IN-DUCED VENTRICULAR FIBRILLATION THRESHOD (VFT) CHANGES

作　　者：路洪[1] 黄圣凯[1] 杨金玉[1] 陆丹玉[1] 卢建丰[1] 

机构地区：[1]中国药科大学药理教研室

出　　处：《药学学报》1991年第7期481-487,共7页Acta Pharmaceutica Sinica

基　　金：江苏省科技基金

摘　　要：本文以电刺激兔心室致颤阈作为效应指标,观察了iv PA后药效变化的时间过程,并用药动学、药效学结合模型分析了代谢物形成过程中PA和NAPA的动力学性质,从原药PA和代谢物NAPA不同转运性质角度阐明了两者的效应贡献;它们的效应室内药量与药效符合线性相加模型。The change of electrically induced VFT was chosen as index of effect in anesthetized rabbits for study of pharmacodynamics of PA and NAPA. We analyzed the pharmacokinetic propertics of PA and NAPA and elucidated tbeir offect kinetics with a pharmacokinetic - pharmacodynamic (PK/PD) model in view of different transfer qualities. A linear - addition effect model was used to describe the relationship between the effect and the amount of drug and its metabolite in the effect compartment. PA was found to be eliminated faster than NAPA and distributed more extensively in rabbits. The effect per unit concentration of PA was shown to be larger than that of NAPA.

关 键 词：普鲁卡因胺 药代动力学 

分 类 号：R969.1[医药卫生—药理学]