Nakano S, Hollister L E
Clin Pharmacol Ther. 1978 Feb;23(2):199-203. doi: 10.1002/cpt1978232199.
Kinetics of a single 100-mg dose of nortriptyline were studied in 10 normal men who took this dose at 9 A.M. in the morning and on another occasion at 9 P.M. Only minimal differences in kinetic parameters were observed, none enough to be of any clinical consequence. A rather high first-pass metabolism of the drug was evident by high plasma concentrations of 10-hydroxynortriptyline. It is thus unlikely that the recent custom of giving single daily doses of tricyclic antidepressants in the evening excludes regimens with more favorable drug kinetics.
对10名正常男性进行了研究,他们于上午9点服用单次100毫克剂量的去甲替林,另一次于晚上9点服用该剂量。观察到动力学参数仅有极小差异,均不足以产生任何临床影响。10-羟基去甲替林的血浆浓度较高,表明该药物存在相当高的首过代谢。因此,近期在晚上给予三环类抗抑郁药每日单次剂量的习惯,不太可能排除具有更有利药物动力学的给药方案。