Ihmsen H, Jeleazcov C, Schüttler J, Schwilden H, Bremer F
Anästhesiologische Klinik, Friedrich-Alexander-Universität Erlangen-Nürnberg, Krankenhausstrasse 12, 91054 Erlangen.
Anaesthesist. 2006 Jun;55(6):635-42. doi: 10.1007/s00101-006-0987-6.
Propofol is nowadays available in various lipid formulations. We compared two different propofol formulations with respect to pharmacodynamics, using the EEG and clinical signs.
Ten volunteers received Diprivan 1% and Propofol 1% MCT Fresenius as a computer controlled infusion with increasing propofol target concentrations. A sigmoid E(max) model with effect compartment was estimated for the median frequency of the EEG power spectrum, based on measured arterial propofol plasma concentrations. Clinical pharmacodynamics were assessed by reaction on acoustic stimuli, eyelid reflex and corneal reflex.
The drugs did not differ in pharmacodynamics with respect to EEG (EC(50) 2.1+/-0.6 for Diprivan and 2.1+/-0.5 microg/ml for Propofol Fresenius) and clinical signs. The pharmacodynamic model was characterized by a steep concentration effect relationship and a distinct hysteresis between propofol plasma concentration and effect (k(e0) 0.12+/-0.04 and 0.12+/-0.5 min(-1)).
The investigated lipid formulations have no influence on the pharmacodynamics of propofol.
丙泊酚目前有多种脂质制剂。我们使用脑电图（EEG）和临床体征，比较了两种不同丙泊酚制剂的药效学。
10名志愿者接受了1%得普利麻和费森尤斯1%丙泊酚中/长链脂肪乳剂，通过计算机控制输注，使丙泊酚目标浓度逐渐增加。基于测得的动脉丙泊酚血浆浓度，为EEG功率谱的中位频率估计了带有效应室的S形E(max)模型。通过对声刺激、眼睑反射和角膜反射的反应来评估临床药效学。
两种药物在EEG方面（得普利麻的半数效应浓度（EC(50)）为2.1±0.6，费森尤斯丙泊酚为2.1±0.5微克/毫升）和临床体征方面的药效学无差异。药效学模型的特点是浓度-效应关系陡峭，丙泊酚血浆浓度与效应之间存在明显的滞后现象（效应室药物消除速率常数（k(e0)）分别为0.12±0.04和0.12±0.5分钟-1）。
所研究的脂质制剂对丙泊酚的药效学无影响。
