健康青年人丙咪嗪及其代谢产物去甲丙咪嗪的药代动力学  

PHARMACOKINETICS OF IMIPRAMINE IN HEALTHY YOUNG ADULT VOLUNTEERS WITH CONSIDERATION OF ITS METABOLITE DESIPRAMINE

作　　者：刘平[1] 刘家良[1] 沈渔邨[1] 舒良[1] 孙丽丽[1] 胡裕雯 张艾琳[1] 

机构地区：[1]北京医科大学精神卫生研究所,北京100083

出　　处：《中国临床药理学杂志》1991年第4期228-232,227,共6页The Chinese Journal of Clinical Pharmacology

摘　　要：本文报道7例健康青年志愿者口服50mg丙咪嗪的药代动力学参数。丙咪嗪药时曲线符合二室线性动力学。其V/F(c)=1088±157 1;t1/2β=28.6±11.5h;t1/2Ka=0.688±0.280h;CL(s)=70.56±18.90 l/h。主要代谢产物去甲丙咪嗪药时曲线符合一室线性动力学。其t1/2=44.5±33.9h;t1/2Ka=2.01±1.60h;CL(s)=16O±118 l/h。统计学处理表明,去甲丙咪嗪的达峰时间较丙咪嗪显著延迟,其t1/2Ka相应延长,峰浓度亦低于原型药物。本文讨论了代谢产物药代动力学参数的临床意义。Pharmacokinetic parameters of imipramine were studied onseven healthy young adult volunteers. The concentration-time curve ofimipramine fitted in with a two-compartment kinetic model. The parametersof it were as follows: V/F(c)=1088±1570 l; t1/2β=28.6±11.5h; t1/2Ka=0.69±0.28 h; CL(s)=70.6±18.9l/h. The concentration-time curve of desi-pramine, the major metabolite of imipramine, fitted in with a one-compar-tment kinetic model. The parameters of it were as follows: t1/2Ke=44.5±33.9h; t1/2Ka=2.01±1.60h; CL=160±118 l/h. It was discovered in statisticalanalysis that the T_(peak) of desipramine was significantly longer than thatof imipramine; the t1/2Ka of it was correspondingly longer and the C_(max) ofdesipramine was lower too. The t1/2β of it was longer than that of the parentdrug. The clinical significance of the pharmacokinetics of the metabolitewas discussed.

关 键 词：丙咪嗪 去甲丙咪嗪 药代动力学 

分 类 号：R971.43[医药卫生—药品]