Fink M, Irwin P, Gastpar M, DeRidder J J
Psychopharmacology (Berl). 1977 Nov 15;54(3):249-54. doi: 10.1007/BF00426572.
A pharmacokinetic analysis of a new antidepressant drug, mianserin (ORG GB-94), was undertaken in 4 male volunteers, each of whom received 15 mg mianserin on two occasions. Plasma levels peak at 2 h with a median level of 11.0 ng/ml, a median beta-phase half-life of 10.0 h, and a median apparent volume of distribution of 3.3 X 10(3) 1. EEG profile analysis shows mianserin to increase frequencies below 6 Hz, decrease those from 7.5 to 15 Hz, and increase frequencies above 18 Hz, a pattern similar to amitriptyline. Peak EEG effects range from 2 to 5 h with a pattern of measured changes that parallels plasma levels with varying latency. Decreases in vigilance measures and in critical flicker-fusion frequency show a similar time course. Mianserin is a putative thymoleptic on EEG profile analysis with high cerebral penetrance.
对一种新型抗抑郁药物米安色林(ORG GB - 94)进行了药代动力学分析,4名男性志愿者参与其中,每人分两次服用15毫克米安色林。血浆浓度在2小时达到峰值,中位数水平为11.0纳克/毫升,β相半衰期中位数为10.0小时,表观分布容积中位数为3.3×10³升。脑电图图谱分析显示,米安色林会增加6赫兹以下的频率,降低7.5至15赫兹的频率,并增加18赫兹以上的频率,这一模式与阿米替林相似。脑电图效应峰值出现在2至5小时,测量到的变化模式与血浆浓度相似,但有不同的延迟。警觉性测量和临界闪烁融合频率的降低显示出相似的时间进程。在脑电图图谱分析中,米安色林被认为是一种具有高脑渗透率的精神安定剂。