替利定与纳洛酮对人体脑电位及疼痛评分的拮抗作用。

Antagonism between tilidine and naloxone on cerebral potentials and pain ratings in man.

作者信息

Bromm B, Meier W, Scharein E

出版信息

Eur J Pharmacol. 1983 Mar 4;87(4):431-9. doi: 10.1016/0014-2999(83)90082-1.

PMID:6852098

Abstract

The effects of the opioid tilidine and the opiate antagonist naloxone on somatosensory evoked potentials (SSEP) and pain ratings (E), elicited by electrical skin stimuli with randomized intensities, were investigated for different, orally administered tilidine and naloxone combinations in a double-blind Latin square design in 15 healthy humans. A high correlation between SSEP amplitudes and E was found for all treatments investigated. Tilidine (100 mg) decreased both SSEP amplitudes and E by about 25% compared to the placebo. No significant differences were found between the analgesic effects of tilidine and TN8 (tilidine 100 mg; naloxone 8 mg). The effects of both treatments were significantly different from those of the naloxone, placebo and TN32 treatments (tilidine 100 mg; naloxone 32 mg), indicating a marked naloxone-induced reversal of tilidine analgesia. Naloxone (32 mg) increased the SSEP amplitudes. No naloxone-induced hyperalgesia was seen in the pain ratings.

摘要

在一项双盲拉丁方设计中，对15名健康受试者口服不同组合的蒂立定和纳洛酮后，研究了阿片类药物蒂立定和阿片拮抗剂纳洛酮对随机强度电刺激皮肤诱发的体感诱发电位（SSEP）和疼痛评分（E）的影响。在所有研究的治疗中，均发现SSEP波幅与E之间存在高度相关性。与安慰剂相比，蒂立定（100毫克）使SSEP波幅和E均降低约25%。蒂立定与TN8（蒂立定100毫克；纳洛酮8毫克）的镇痛效果之间未发现显著差异。两种治疗的效果与纳洛酮、安慰剂和TN32治疗（蒂立定100毫克；纳洛酮32毫克）的效果显著不同，表明纳洛酮可显著逆转蒂立定的镇痛作用。纳洛酮（32毫克）使SSEP波幅增加。在疼痛评分中未观察到纳洛酮诱发的痛觉过敏。