Piotrovskiĭ V K, Veĭko N N, Golovanova I V, Gus'kova T A, Polievktov M K
Biull Eksp Biol Med. 1987 Jan;103(1):73-5.
Serum concentration profiles of prazosin and its metabolite 2-(1-piperazinyl)-4-amine-6,7-dimethoxyquinazoline after intravenous bolus administration to rabbits (0.5 mg/kg) were shown to be biphasic. Rapid decline related to distribution was followed by a terminal slope lasting for up to 24 hours. Prazosin level in this phase decreased, its elimination half-life being about 9 hours, while the metabolite serum level was almost constant between 4 and 24 hours and averaged 0.9 mumol/l. This is in keeping with the earlier suggested extremely low elimination rate of this metabolite. Enterohepatic recirculation may account for this phenomenon, as well as a significant rise in the metabolite serum concentration I hour after the injection.
给兔子静脉推注哌唑嗪(0.5mg/kg)后,其血清浓度曲线及代谢产物2-(1-哌嗪基)-4-氨基-6,7-二甲氧基喹唑啉呈双相。与分布相关的快速下降之后是持续长达24小时的终末斜率。此阶段哌唑嗪水平下降,其消除半衰期约为9小时,而代谢产物血清水平在4至24小时之间几乎恒定,平均为0.9μmol/L。这与之前提出的该代谢产物极低的消除率一致。肠肝循环可能是导致此现象的原因,注射后1小时代谢产物血清浓度也显著升高。