Lingjaerde O
Eur J Clin Pharmacol. 1979 Jun 12;15(5):335-40. doi: 10.1007/BF00558437.
The inhibition of serotonin uptake by platelets has been measured in blood from 20 patients on amitriptyline (50--225 mg daily), 14 patients on clomipramine (25--200 mg daily), and in an untreated group of 21 depressed patients. A complete kinetic analysis was carried out in each patient. Using the increase in the kinetic parameter Km as a measure of uptake inhibition, there was high correlation between the daily dose and inhibition within each drug group, clomipramine being about 10 times more potent than amitriptyline. The inhibition did not vary with age, sex, duration of treatment (up to 3 years), or concomitant use of moderate doses of benzodiazepines, neuroleptics or lithium. In the amitriptyline group the inhibition was significantly smaller in smokers than in non-smokers. The kinetic parameter Vmax was essentially unchanged in the amitriptyline group, and was markedly reduced in the clomipramine group, but without any correlation with dose. The mixed competitive-noncompetitive effect of clomipramine confirms previous in vitro findings.
对20名服用阿米替林（每日50 - 225毫克）的患者、14名服用氯米帕明（每日25 - 200毫克）的患者以及21名未接受治疗的抑郁症患者的血液进行了血小板对血清素摄取抑制作用的测定。对每位患者进行了完整的动力学分析。以动力学参数Km的增加作为摄取抑制的指标，在每个药物组中，每日剂量与抑制作用之间存在高度相关性，氯米帕明的效力约为阿米替林的10倍。抑制作用不随年龄、性别、治疗持续时间（长达3年）或同时使用中等剂量的苯二氮䓬类药物、抗精神病药物或锂而变化。在阿米替林组中，吸烟者的抑制作用明显小于不吸烟者。阿米替林组的动力学参数Vmax基本未变，氯米帕明组的Vmax则显著降低，但与剂量无任何相关性。氯米帕明的混合竞争性 - 非竞争性作用证实了先前的体外研究结果。
