Saletu B, Grünberger J, Linzmayer L
Int J Clin Pharmacol Ther Toxicol. 1986 Jul;24(7):362-73.
In a double-blind, placebo-controlled study the encephalotropic and psychotropic properties of gabapentin - a new gaba-analogue with anticonvulsant and antispastic properties penetrating the blood brain barrier easily - were studied in 10 normal subjects by means of quantitative pharmaco-EEG and psychometric analyses. They received randomized and in weekly intervals single oral doses of 50 mg, 100 mg, 200 mg and 400 mg gabapentin as well as placebo. EEG recordings and evaluation of pulse, blood pressure and side effects were carried out after 0, 1, 2, 4, 6 and 8 hours; psychometric tests were done at the same times except for the first hour. Computer-assisted spectral analysis of the EEG showed moderate though significant central effects of gabapentine in doses of 200-400 mg as compared with placebo, which were maximally pronounced in the 2nd hour post drug. These alterations were generally characterized by an attenuation of total power, augmentation of delta and theta activity and a decrease of alpha activity indicating CNS-inhibitory properties. Only at the late hours did the type of changes shift towards a vigilance-promoting one. Beta activity showed alternating changes. Psychometric and psychophysiological evaluations demonstrated subtle psychotropic effects as compared with placebo characterized mostly by an improvement in concentration, numerical memory, complex reaction and performance in the alphabetical reaction test while performance variability increased as well. Subjectively experienced well-being changed dose-dependently. CFF decreased after 100 mg as did pupil size after 50-200 mg. Evaluation of pulse, blood pressure and side effects demonstrated good tolerability of the drug.
在一项双盲、安慰剂对照研究中,对10名正常受试者采用定量药物脑电图和心理测量分析方法,研究了加巴喷丁(一种新型γ-氨基丁酸类似物,具有抗惊厥和抗痉挛特性,能轻松穿透血脑屏障)的亲脑性和精神性特性。他们随机且每周一次接受50毫克、100毫克、200毫克和400毫克加巴喷丁的单次口服剂量以及安慰剂。在0、1、2、4、6和8小时后进行脑电图记录以及脉搏、血压和副作用评估;除第一小时外,在相同时间进行心理测量测试。脑电图的计算机辅助频谱分析显示,与安慰剂相比,200 - 400毫克剂量的加巴喷丁具有适度但显著的中枢效应,在用药后第2小时最为明显。这些改变通常表现为总功率衰减、δ和θ活动增强以及α活动减少,表明具有中枢神经系统抑制特性。仅在较晚时间,变化类型才转向促进警觉的类型。β活动表现出交替变化。与安慰剂相比,心理测量和心理生理评估显示出细微的精神性效应,主要表现为注意力、数字记忆、复杂反应以及字母反应测试表现的改善,但表现变异性也增加。主观幸福感呈剂量依赖性变化。100毫克后临界闪光融合频率降低,50 - 200毫克后瞳孔大小减小。脉搏、血压和副作用评估表明该药物耐受性良好。