Piguet V, Desmeules J A, Collart L, Dayer P
Division de pharmacologie clinique, Hôpital cantonal universitaire de Genève.
Schweiz Med Wochenschr. 1994 Dec 3;124(48):2196-8.
The purpose of this study was to evaluate the dose-response of paracetamol and to assess its plasma concentration-effect relationship. According to a randomized, double-blind, and placebo controlled design healthy volunteers (n = 11) received 0.5, 1 and 2 g paracetamol (as propacetamol) intravenously (15 min). The extent of analgesic effect was measured over 8 hours by objective pain threshold (R-III) monitoring after selective transcutaneous electrical stimulation of the ipsilateral sural nerve. Maximal R-III threshold increase is at 2 hours after 0.5 g and 2.5 hours after 1 g and 2 g. The delayed peak effects, when compared to peak plasma concentrations, draw counter clockwise hysteresis. Duration of paracetamol antinociceptive effect increased concomitantly to dosage increment. Intravenous paracetamol exerts a dose-dependent central analgesia.
本研究的目的是评估对乙酰氨基酚的剂量反应,并评估其血浆浓度-效应关系。根据随机、双盲、安慰剂对照设计,健康志愿者(n = 11)静脉注射(15分钟)0.5、1和2克对乙酰氨基酚(以丙帕他莫形式)。通过对同侧腓肠神经进行选择性经皮电刺激后,用客观疼痛阈值(R-III)监测在8小时内测量镇痛效果的程度。最大R-III阈值增加分别在注射0.5克后2小时、1克和2克后2.5小时出现。与血浆浓度峰值相比,效应延迟出现,呈逆时针滞后现象。对乙酰氨基酚的抗伤害感受作用持续时间随剂量增加而延长。静脉注射对乙酰氨基酚发挥剂量依赖性的中枢镇痛作用。