De Schepper P J, Vranckx C, Verbeeck R, Van den Berghe M L
Arzneimittelforschung. 1979;29(7):1056-62.
Plasma kinetics of pipotiazine, a phenothiazine neuroleptic, have been studied in five chronic schizophrenic patients after both oral (25 mg) and i.v. (5 mg) administration of pipotiazine tritiated in the 3- and 4-positions of the piperidine ring. Peak plasma concentrations of unchanged pipotiazine were reached between 1 and 2 h after oral administration and showed a five-fold inter-individual variation. The mean terminal elimination half-life was 11.2 h. After i.v. administration plasma concentration declined bi-exponentially with mean half-life values of 2.7 and 8.8 h. Data indicate that biotranformation of the drug was not dependent on the route of administration and that there were no qualitative differences in biotransformation between individuals. The large apparent distribution volumes (mean value 545 l) indicated extensive binding to tissue components. After 25 mg p.o. effect on the handwriting area was manifest from 8 to 48 h after administration and reached maximum intensity between 24 and 36 h. This is consistent with rather a large duration of action observed clinically.
哌泊噻嗪是一种吩噻嗪类抗精神病药，研究人员在5例慢性精神分裂症患者口服（25毫克）和静脉注射（5毫克）哌啶环3位和4位用氚标记的哌泊噻嗪后，对其血浆动力学进行了研究。口服给药后1至2小时内达到未变化的哌泊噻嗪的血浆峰值浓度，个体间差异为5倍。平均终末消除半衰期为11.2小时。静脉注射后，血浆浓度呈双指数下降，平均半衰期值分别为2.7小时和8.8小时。数据表明，药物的生物转化不依赖于给药途径，个体间生物转化没有质的差异。较大的表观分布容积（平均值545升）表明药物与组织成分广泛结合。口服25毫克后，给药后8至48小时对手写区域产生影响，在24至36小时达到最大强度。这与临床上观察到的较长作用持续时间一致。
