Bogaert M G, Rosseel M T, Deberdt R, Vranckx C
Arzneimittelforschung. 1981;31(1):113-5.
In depressed patients treated with doxepin (Sinequan), a 15:85% mixture of cis- and trans-isomers, plasma levels of the cis- and trans-forms of doxepin and desmethyldoxepin were measured using a GLC-method with a capillary column and a nitrogen detector. A gradual increase of the concentration of the products in the plasma is seen in the first days of administration. There is a remarkable variation from patient to patient in the steady-state concentrations of trans-doxepin and of cis- and trans-desmethyldoxepin. cis-Doxepin levels are always very low. It is suggested that for studies of correlation between plasma levels and therapeutic and toxic effects of doxepin, the isomers of the parent compound and its metabolite should be measured separately.
在用多塞平（多虑平）治疗的抑郁症患者中，多塞平是顺式和反式异构体的15:85%混合物，采用带有毛细管柱和氮检测器的气相色谱法测定血浆中多塞平及其去甲基多塞平的顺式和反式异构体的水平。给药后的头几天，血浆中产物的浓度逐渐升高。反式多塞平以及顺式和反式去甲基多塞平的稳态浓度在患者之间存在显著差异。顺式多塞平的水平始终非常低。建议在研究血浆水平与多塞平的治疗及毒性作用之间的相关性时，应分别测定母体化合物及其代谢物的异构体。
