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比较静脉注射纳布啡和吗啡对健康志愿者的主观、精神运动和生理影响。

Comparing the subjective, psychomotor and physiological effects of intravenous nalbuphine and morphine in healthy volunteers.

作者信息

Zacny J P, Conley K, Marks S

机构信息

Department of Anesthesia and Critical Care, The Pritzker School of Medicine, The University of Chicago, Illinois 60637, USA.

出版信息

J Pharmacol Exp Ther. 1997 Mar;280(3):1159-69.

PMID:9067299
Abstract

The purposes of this study were to characterize the subjective, psychomotor and physiological effects of nalbuphine in healthy non-drug abusing volunteers and to compare and contrast the effects of equianalgesic doses of nalbuphine and morphine. Subjects (12 males, 4 females) without histories of opiate dependence were injected in an upper extremity vein with 0, 2.5, 5.0 or 10 mg/70 kg nalbuphine, or with 10 mg/70 kg morphine, using a randomized, double-blind, crossover design. The 10-mg doses of nalbuphine and morphine are considered equianalgesic and are doses commonly given for relief of postoperative pain. Subjective effects of nalbuphine included increased scores on the Pentobarbital-Chlorpromazine-Alcohol Group scale and the Lysergic Acid Diethylamide scale of the Addiction Research Center Inventory; increased adjective checklist ratings of "nodding," "numb" and "sweating"; increased visual analog scale ratings of "coasting or spaced out," "high" and "sleepy" and increased "feel drug effect" and drug-liking ratings. Ten milligrams of nalbuphine had subjective effects similar, and similar in magnitude, to those of 10 mg of morphine. Nalbuphine produced exophoria and impairment on the Digit Symbol Substitution Test in a dose-related fashion. Ten milligrams of morphine produced exophoria but did not affect performance on the Digit Symbol Substitution Test. Both nalbuphine and morphine induced miosis and decreases in respiration rate. The results of the present study demonstrate that 2.5 to 10 mg nalbuphine had orderly, dose-related effects on subjective, psychomotor and physiological variables. The results also indicate that 10 mg of nalbuphine produces a profile of subjective, psychomotor and physiological effects similar to that of an equianalgesic dose of morphine (10 mg). The similarity in profiles between drugs at this dose is consistent with both infrahuman studies, which suggests that nalbuphine is a mu agonist, and studies with nondependent opioid abusers, in which relatively low doses of nalbuphine (such as 10 mg) produce morphine-like effects.

摘要

本研究的目的是描述纳布啡在健康、不滥用药物的志愿者身上产生的主观、精神运动和生理效应,并比较和对比等效镇痛剂量的纳布啡和吗啡的效应。采用随机、双盲、交叉设计,对16名无阿片类药物依赖史的受试者(12名男性,4名女性)在上肢静脉注射0、2.5、5.0或10mg/70kg的纳布啡,或10mg/70kg的吗啡。10mg剂量的纳布啡和吗啡被认为具有等效镇痛作用,是常用于缓解术后疼痛的剂量。纳布啡的主观效应包括成瘾研究中心量表中戊巴比妥-氯丙嗪-酒精组量表和麦角酸二乙胺量表得分增加;“点头”“麻木”和“出汗”的形容词检查表评分增加;视觉模拟量表中“滑行或恍惚”“兴奋”和“困倦”的评分增加,以及“感觉有药物作用”和对药物喜爱程度的评分增加。10mg纳布啡产生的主观效应与10mg吗啡相似,且程度相当。纳布啡以剂量相关的方式导致外隐斜和数字符号替换测试成绩受损。10mg吗啡导致外隐斜,但不影响数字符号替换测试的成绩。纳布啡和吗啡均引起瞳孔缩小和呼吸频率降低。本研究结果表明,2.5至10mg纳布啡对主观、精神运动和生理变量具有有序的、剂量相关的效应。结果还表明,10mg纳布啡产生的主观、精神运动和生理效应与等效镇痛剂量的吗啡(10mg)相似。该剂量下两种药物效应的相似性与非人类研究一致,后者表明纳布啡是μ激动剂,也与对非依赖阿片类药物滥用者的研究一致,在这些研究中,相对低剂量的纳布啡(如10mg)产生类似吗啡的效应。

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