Axelsson R, Mårtensson E, Alling C
Eur J Clin Pharmacol. 1982 Oct;23(4):359-63. doi: 10.1007/BF00613621.
The blood chemistry and clinical pharmacokinetics of thioridazine and its metabolites, side-chain sulphoxide, side-chain sulphone and ring sulphoxide, were studied in 31 alcoholics and were compared with values in 17 thioridazine-treated controls without alcoholism. Pathological blood chemistry values, including abnormal liver function and protein concentrations, were common among the alcoholics. In relation to dosage, the majority had a low serum concentration of thioridazine and at a given concentration of thioridazine they had high serum concentrations of its metabolites. Positive intercorrelations were found between pathological liver function tests, prolonged serum half-life and increased serum concentration of thioridazine. The free fractions of thioridazine, side-chain sulphoxide and ring sulphoxide were significantly higher and those of the side-chain sulphone lower in the alcoholics than in the controls. The free fractions of side-chain and ring sulphoxide were significantly increased in patients with a low concentration of alpha 1-acid glycoprotein.
对31名酗酒者的硫利达嗪及其代谢产物（侧链亚砜、侧链砜和环亚砜）的血液化学和临床药代动力学进行了研究，并与17名未患酒精中毒的硫利达嗪治疗对照者的值进行了比较。包括肝功能和蛋白质浓度异常在内的病理性血液化学值在酗酒者中很常见。就剂量而言，大多数人硫利达嗪的血清浓度较低，在给定的硫利达嗪浓度下，其代谢产物的血清浓度较高。在病理性肝功能检查、硫利达嗪血清半衰期延长和血清浓度升高之间发现了正相关。酗酒者中硫利达嗪、侧链亚砜和环亚砜的游离分数显著高于对照组，而侧链砜的游离分数则较低。α1-酸性糖蛋白浓度低的患者侧链和环亚砜的游离分数显著增加。
