Furet Y, Breteau M, Etienne T
Laboratoire de Pharmacologie, C.H.R. Bretonneau, Tours.
Therapie. 1991 Mar-Apr;46(2):119-23.
Pharmacokinetics of the depot antipsychotics are unclear and mainly depend on releasing from the depot site (according to a "flip-flop" model). Few data are available on residual plasma concentrations of those drugs. We have practiced 38 blood determinations among 15 patients treated by long-acting neuroleptics (10 by fluphenazine decanoate, 4 by flupentixol decanoate and 1 by pipotiazine palmitate). Radio Receptor Assay method was used (based on competition for dopamine receptors binding), with results expressed as chlorpromazine equivalents. They showed; a wide interindividual variability; considering each subject, intraindividual variability is attenuated; blood measurements are mainly higher than therapeutic ranges (especially for patients on fluphenazine decanoate). Those results might involve that some patients are overdosed, but other studies are needed in this way.
长效抗精神病药物的药代动力学尚不清楚,主要取决于从长效注射部位的释放情况(根据“翻转”模型)。关于这些药物的血浆残留浓度的数据很少。我们对15例接受长效抗精神病药物治疗的患者进行了38次血液检测(10例接受癸酸氟奋乃静治疗,4例接受癸酸氟哌噻吨治疗,1例接受棕榈酸哌泊噻嗪治疗)。采用放射受体分析法(基于对多巴胺受体结合的竞争),结果以氯丙嗪等效物表示。结果显示:个体间差异很大;就每个受试者而言,个体内差异较小;血液检测结果大多高于治疗范围(尤其是接受癸酸氟奋乃静治疗的患者)。这些结果可能意味着一些患者用药过量,但还需要进行其他研究来证实。