Jørgensen A, Andersen J, Bjørndal N, Dencker S J, Lundin L, Malm U
Psychopharmacology (Berl). 1982;77(1):58-65. doi: 10.1007/BF00436100.
Nine chronic schizophrenic patients selected from three hospital departments were treated with flupentixol (orally and IV) and cis(Z)-flupentixol decanoate in Viscoleo (IM) in a three-phase pharmacokinetic study. Oral administration (single and repeated dosage) showed a relatively slow absorption with maximum serum concentration around 4 h after administration. Intravenous injection indicated multicompartment kinetics for cis(Z)-flupentixol. The biological half-lives calculated after the different doses were the same, indicating that the pharmacokinetics of cis(Z)-flupentixol does not differ between single and repeated administration and does not change when moderately higher doses are given. The bioavailability of orally administered cis(Z)-flupentixol was calculated to be about 40% with IV injection as reference. After IM administration maximum serum concentration was seen between 4 and 10 days in most patients. Calculation of a disappearance half-life gave very variable results, indicating that the release of the drug from the oil depot is not a monoexponential process. The intramuscular depot had a much lower bioavailability than IV injection, which means that steady state has not been obtained after 8 weeks of depot treatment. Serum prolactin concentrations were elevated during neuroleptic treatment, but no correlation was found between prolactin concentrations and the serum concentrations of cis(Z)-flupentixol. A correlation between the changes in clinical ratings and concentrations of cis(Z)-flupentixol or prolactin was not found.
从三个医院科室挑选出的9名慢性精神分裂症患者，在一项三相药代动力学研究中接受了氟哌噻吨（口服和静脉注射）和顺式（Z）-癸酸氟哌噻吨油剂（肌肉注射）治疗。口服给药（单次和重复剂量）显示吸收相对缓慢，给药后约4小时达到血清浓度最大值。静脉注射表明顺式（Z）-氟哌噻吨具有多室动力学特征。不同剂量后计算出的生物半衰期相同，表明顺式（Z）-氟哌噻吨的药代动力学在单次给药和重复给药之间没有差异，且给予稍高剂量时也不会改变。以静脉注射为参照，口服顺式（Z）-氟哌噻吨的生物利用度计算约为40%。大多数患者肌肉注射给药后4至10天出现血清浓度最大值。计算消除半衰期得到的结果差异很大，表明药物从油剂储存库中的释放不是单指数过程。肌肉注射储存库的生物利用度远低于静脉注射，这意味着在进行8周的储存库治疗后尚未达到稳态。在抗精神病药物治疗期间血清催乳素浓度升高，但未发现催乳素浓度与顺式（Z）-氟哌噻吨血清浓度之间存在相关性。未发现临床评分变化与顺式（Z）-氟哌噻吨或催乳素浓度之间存在相关性。
