Norberg L, Wahlström G
Department of Pharmacology, University of Umeå, Sweden.
Arch Int Pharmacodyn Ther. 1988 Mar-Apr;292:45-57.
The anaesthetic effects of a benzodiazepine derivate, flurazepam, and the anaesthetic interaction between flurazepam and 2 barbiturates, thiopental and hexobarbital, were studied in male rats using an EEG-threshold method. The criterion of anaesthesia was defined by a burst suppression in the EEG of 1 sec or more (the "silent second"). The dose needed to induce the criterion was used as the threshold. The data on the interaction were evaluated with the isobolographic method. Flurazepam alone infused with different rates gave an almost V-shaped dose-rate curve. Convulsive activity was seen in all rats in connection with the EEG-criterion. The mortality during anaesthesia increased with increased infusion rates of flurazepam. The anaesthetic interaction between thiopental-flurazepam and hexobarbital-flurazepam was with low admixture of flurazepam, a pronounced potentiation. With increased admixture of flurazepam, an additive interaction with thiopental and flurazepam was obtained, whereas an antagonistic interaction was obtained with hexobarbital and flurazepam. Convulsive activity and mortality during anaesthesia in the interaction studies were only observed in tests where high admixtures of flurazepam were used.
采用脑电图阈值法,在雄性大鼠中研究了苯二氮䓬衍生物氟西泮的麻醉作用以及氟西泮与两种巴比妥类药物(硫喷妥钠和己巴比妥)之间的麻醉相互作用。麻醉标准定义为脑电图出现持续1秒或更长时间的爆发抑制(“沉默秒”)。诱导该标准所需的剂量用作阈值。用等效应线图法评估相互作用的数据。以不同速率输注单独的氟西泮可得到近似V形的剂量-速率曲线。与脑电图标准相关的惊厥活动在所有大鼠中均可见。麻醉期间的死亡率随氟西泮输注速率的增加而升高。硫喷妥钠-氟西泮和己巴比妥-氟西泮之间的麻醉相互作用在氟西泮低混合比例时表现为明显的增强作用。随着氟西泮混合比例的增加,与硫喷妥钠呈现相加相互作用,而与己巴比妥呈现拮抗相互作用。相互作用研究中麻醉期间的惊厥活动和死亡率仅在使用高混合比例氟西泮的试验中观察到。