Piletta P, Porchet H C, Dayer P
Department of Medicine, University Hospital, Geneva, Switzerland.
Clin Pharmacol Ther. 1991 Apr;49(4):350-4. doi: 10.1038/clpt.1991.40.
The central nervous system effect of acetaminophen (paracetamol) and acetylsalicylic acid was investigated in healthy volunteers according to a crossover, double-blind, and placebo-controlled design. Ten subjects received, by intravenous route, a placebo, 1 gm acetaminophen, and 1 gm acetylsalicylic acid. Analgesia was assessed by measurement of the subjective pain threshold and the objective nociceptive flexion reflex threshold in response to selective transcutaneous electrical stimulations. A close correlation was observed between subjective and objective pain thresholds. Acetaminophen increased both thresholds for more than 4 hours (24% and 23% of baseline value at 120 minutes, respectively; p less than 0.001, ANOVA). In contrast, acetylsalicylic acid had no noticeable effect on either threshold. These findings show that acetaminophen-induced analgesia is centrally mediated, in contrast to aspirin. The time delay between plasma concentration kinetics and acetaminophen analgesic effect is another argument in favor of its direct action on the central nervous system.
按照交叉、双盲和安慰剂对照设计,在健康志愿者中研究了对乙酰氨基酚(扑热息痛)和阿司匹林的中枢神经系统效应。10名受试者通过静脉途径接受了安慰剂、1克对乙酰氨基酚和1克阿司匹林。通过测量主观疼痛阈值和对选择性经皮电刺激的客观伤害性屈曲反射阈值来评估镇痛效果。主观和客观疼痛阈值之间观察到密切相关性。对乙酰氨基酚使两个阈值升高超过4小时(120分钟时分别为基线值的24%和23%;方差分析,p小于0.001)。相比之下,阿司匹林对任何一个阈值均无明显影响。这些发现表明,与阿司匹林不同,对乙酰氨基酚诱导的镇痛是由中枢介导的。血浆浓度动力学与对乙酰氨基酚镇痛效果之间的时间延迟是支持其对中枢神经系统直接作用的另一个论据。