阿那普明：对阿尔茨海默型痴呆患者的药代动力学和生化研究

Alaproclate: a pharmacokinetic and biochemical study in patients with dementia of Alzheimer type.

作者信息

Bergman I, Bråne G, Gottfries C G, Jostell K G, Karlsson I, Svennerholm L

出版信息

Psychopharmacology (Berl). 1983;80(3):279-83. doi: 10.1007/BF00436170.

Abstract

Alaproclate, a specific inhibitor of neuronal serotonin re-uptake, was given to 12 patients with dementia of Alzheimer type. The drug was rapidly absorbed and an elimination half-life of 7.1 +/- 0.9 h (+/- SD, n = 8) was calculated. Plasma protein binding for alaproclate was 82 +/- 1%. Two weeks of repeated administration produced plasma concentrations of alaproclate similar to those predicted from a single dose. The pharmacological effect of the drug was demonstrated by an inhibition of serotonin uptake in the patients' platelets and a reduction of the serotonin concentration in blood. Global rating of clinical efficacy showed a positive effect of alaproclate in five of the patients, mainly regarding emotional functions.

摘要

阿那普明，一种神经元5-羟色胺再摄取的特异性抑制剂，被给予12名阿尔茨海默型痴呆患者。该药吸收迅速，计算出消除半衰期为7.1±0.9小时（±标准差，n = 8）。阿那普明的血浆蛋白结合率为82±1%。两周的重复给药产生的阿那普明血浆浓度与单剂量预测的浓度相似。该药的药理作用通过抑制患者血小板对5-羟色胺的摄取以及降低血液中5-羟色胺浓度得以证明。临床疗效的整体评定显示，阿那普明对5名患者有积极作用，主要涉及情感功能。