CENTRAL NERVOUS-SYSTEM DEPRESSANT ACTIONS OF CLONIDINE AND UK-14,304 - PARTIAL DISSOCIATION OF EEG AND BEHAVIORAL-EFFECTS
CENTRAL NERVOUS-SYSTEM DEPRESSANT ACTIONS OF CLONIDINE AND UK-14,304 - PARTIAL DISSOCIATION OF EEG AND BEHAVIORAL-EFFECTS
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DOI：
10.1111/j.1365-2125.1978.tb01614.x
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发表时间：
1978-01-01
影响因子：
3.4
通讯作者：
RAWLINS, MD
中科院分区：
文献类型：
--
作者：
ASHTON, H;RAWLINS, MD
[1]采用双盲对照研究方法，比较了可乐定（300 μg）、UK-14，304（750 μg）和安慰剂单次给药对5名正常人6 h内警觉/嗜睡主观评分、关联负变（CNV）、反应时、血压和心率的影响。2两种药物治疗后，收缩压、舒张压和心率均下降。这些变化在2和4小时之间最大，可乐定后比UK-14，304后更大。3.两种药物治疗后，嗜睡的主观评分逐渐增加，从1小时开始，在2 - 4小时之间最大。可乐定的这种作用比UK-14，304更明显。两种药物治疗后，血压的下降和主观嗜睡评分的变化之间存在密切的相关性。两种药物后也出现了行为睡眠。4与安慰剂相比，两种药物后2小时和4小时CNV幅度降低，与反应时间延长相关，与主观和行为变化一致。可乐定治疗后CNV幅度的降低比UK-14，304治疗后更明显。5在一些受试者中，在两种药物后，CNV幅度在1.5 h时初始增加，与行为睡眠和主观嗜睡评级同时发生。CNV的幅度和主观和行为的药物在人的影响之间的这种分离以前没有报道。6结论是，UK-14，304在此剂量下引起的中枢神经系统抑制比可乐定少，但也具有不太明显的肿胀作用。
1 The effects in five normal subjects of a single dose of clonidine (300 μg), UK-14,304 (750 μg) and placebo on a subjective rating scale for alertness/sleepiness, the contingent negative variation (CNV), reaction time, blood pressure and heart rate were compared over 6 h in a double-blind study. 2 After both drugs there was a fall in systolic and diastolic blood pressure and in heart rate. These changes were maximal between 2 and 4 h and were greater after clonidine than after UK-14,304. 3 There was a progressive increase in subjective ratings of sleepiness after both drugs, commencing at 1 h and maximal between 2 and 4 h. This effect was more pronounced after clonidine than after UK-14,304. There was a close correlation between the fall in blood pressure and the change in subjective rating for sleepiness after both drugs. Behavioural sleep also occurred after both drugs. 4 Compared with placebo there was a decrease in CNV magnitude at 2 and 4 h after both drugs, associated with a lengthening of reaction time and consistent with the subjective and behavioural changes. Depression of CNV magnitude was more pronounced after clonidine than after UK-14,304. 5 In some subjects after both drugs there was an initial increase in CNV magnitude at 1.5 h, occurring at the same time as behavioural sleep and subjective ratings of sleepiness. Such a dissociation between CNV magnitude and subjective and behavioural effects of drugs in man has not previously been reported. 6 It was concluded that UK-14,304 causes less central nervous system depression than clonidine at this dosage, but also has a less marked hypotensive effect.