Gram L F, Reisby N, Ibsen I, Nagy A, Dencker S J, Bech P, Petersen G O, Christiansen J
Clin Pharmacol Ther. 1976 Mar;19(3):318-24. doi: 10.1002/cpt1976193318.
The relationship between the antidepressive effect of imipramine and the plasma concentrations of imipramine and the active metabolite desipramine was studied in 24 patients suffering from endogenous depression. After a placebo period of 7 days, the patients received imipramine, 75 mg 3 times a day. The dose was reduced in patients with pronounced side effects. Blood samples for drug assay were drawn in the morning, 15 hr after the last drug intake. Imipramine and desipramine in plasma were assayed by quantitative in situ thin-layer chromatography. Individual variations in plasma concentration were 20- to 30-fold in both imipramine and desipramine. Severity of depression was assessed on the Hamilton Rating Scale (HRS). Eleven of 12 patients who responded satisfactorily to the treatment (HRS post-treatment score less than 8) had plasma concentration of imipramine greater than or equal to 45 mug/L, and desipramine greater than 75 mug/L, whereas the 12 patients not responding satisfactorily (post-treatment score on HRS greater than or equal to 8) all had concentrations of imipramine or desipramine or both below these limits.
在24例内源性抑郁症患者中研究了丙咪嗪的抗抑郁作用与丙咪嗪及活性代谢产物去甲丙咪嗪血浆浓度之间的关系。经过7天的安慰剂期后，患者服用丙咪嗪，每日3次，每次75毫克。有明显副作用的患者减少剂量。在最后一次服药15小时后的早晨采集血样进行药物测定。采用定量原位薄层色谱法测定血浆中的丙咪嗪和去甲丙咪嗪。丙咪嗪和去甲丙咪嗪的血浆浓度个体差异均为20至30倍。采用汉密尔顿评定量表（HRS）评估抑郁严重程度。对治疗反应良好（治疗后HRS评分小于8）的12例患者中有11例丙咪嗪血浆浓度大于或等于45微克/升，去甲丙咪嗪大于75微克/升，而12例反应不佳（治疗后HRS评分大于或等于8）的患者丙咪嗪或去甲丙咪嗪或两者浓度均低于这些限值。
