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通过药物脑电图和心理测量法对新型抗缺氧药物长春乙酯的药效学进行分类和测定。

Classification and determination of pharmacodynamics of a new antihypoxidotic drug, vinconate, by pharmaco-EEG and psychometry.

作者信息

Saletu B, Grünberger J, Linzmayer L, Wittek R

出版信息

Arch Gerontol Geriatr. 1984 Jul;3(2):127-46. doi: 10.1016/0167-4943(84)90005-0.

DOI:10.1016/0167-4943(84)90005-0
PMID:6476974
Abstract

In a double-blind, placebo-controlled study the encephalotropic and psychotropic properties of both orally and intravenously administered doses of vinconate (OC 340)--a new vincamine analogue--were studied in 10 elderly subjects in their sixties by means of quantitative EEG and psychometric analyses. They received at weekly intervals randomized single oral doses of placebo, 40 mg, 80 mg and 160 mg vinconate orally as well as placebo and 30 mg vinconate intravenously. EEG recordings and the monitoring of blood pressure, heart rate and side effects were carried out at the hours 0, 1, 2, 4 and 6. Psychometric tests were performed at the hours 0, 2, 4 and 6. Computer-assisted spectral analysis of the EEG showed a significant CNS effect of vinconate as compared with placebo characterized by a decrease of delta activity, increase of alpha and specifically of alpha-adjacent slow beta activity as well as an acceleration of the centroid of the total activity. Such changes were described previously by us after several other antihypoxidotics and are indicative of improvement in vigilance in the sense of Head (Br. J. Psychol., 14, 125-147). The encephalotropic effect was most pronounced after 160 mg vinconate p.o. followed by 80 mg and 40 mg vinconate orally, which timewise could be observed best in the 6th hour after drug administration. Changes after the i.v. injection of vinconate peaked as early as the 2nd hour post-drug. Psychometric investigations demonstrated only small psychotropic effects, which rarely reached the level of statistical significance as compared with placebo. Generally, the orally administered vinconate induced a trend towards an improvement of psychomotor activity, complex reaction and cognitive function as well as a significant improvement in attention and concentration, while the von Zerssen score increased as compared with placebo. 30 mg vinconate i.v., however, induced an improvement in mood as well as a shortening of reaction time and activation in the after-effect as compared with placebo in addition to a trend towards improvement in psychomotor activity, complex reaction and Pauli test. Evaluation of pulse rate, blood pressure and side effects showed a good tolerance of the drug. The findings are discussed.

摘要

在一项双盲、安慰剂对照研究中,通过定量脑电图和心理测量分析,对10名60多岁的老年受试者研究了口服和静脉注射剂量的长春乙酯(OC 340)——一种新的长春胺类似物——的亲脑性和精神性特性。他们每隔一周随机接受单次口服安慰剂、40毫克、80毫克和160毫克长春乙酯,以及安慰剂和30毫克静脉注射长春乙酯。在0、1、2、4和6小时进行脑电图记录以及血压、心率和副作用监测。在0、2、4和6小时进行心理测量测试。脑电图的计算机辅助频谱分析显示,与安慰剂相比,长春乙酯具有显著的中枢神经系统效应,其特征为δ活动减少、α活动增加,特别是α相邻的慢β活动增加,以及总活动质心加速。我们之前在使用其他几种抗缺氧药物后也描述过这种变化,这表明在海德(《英国心理学杂志》,14,125 - 147)意义上的警觉性有所改善。亲脑效应在口服160毫克长春乙酯后最为明显,其次是口服80毫克和40毫克长春乙酯,在给药后第6小时在时间上观察得最为明显。静脉注射长春乙酯后的变化在给药后第2小时最早达到峰值。心理测量研究仅显示出较小的精神性效应,与安慰剂相比很少达到统计学显著水平。一般来说,口服长春乙酯会导致心理运动活动、复杂反应和认知功能有改善的趋势,以及注意力和专注力有显著改善,而与安慰剂相比,冯·泽尔森评分增加。然而,与安慰剂相比,静脉注射30毫克长春乙酯除了导致心理运动活动、复杂反应和保利测试有改善趋势外,还能改善情绪、缩短反应时间并在后续效应中产生激活作用。对脉搏率、血压和副作用的评估显示该药物耐受性良好。对研究结果进行了讨论。

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