Preston K L, Bigelow G E, Liebson I A
J Pharmacol Exp Ther. 1987 Mar;240(3):900-10.
The subjective, physiological and behavioral effects of morphine, pentazocine and ciramadol, an opioid agonist/antagonist, were studied in adult male nondependent opioid abusers living on a clinical research ward. Fifteen subjects were assigned randomly to one of three groups. Each group received, by i.m. injection, placebo and three doses of one active drug, twice in randomized block order under double-blind conditions in 4.5-hr experimental sessions. Physiological measures did not differentiate between the three drugs. All three drugs decreased respiratory rate and pupil diameter and increased blood pressure. However, morphine, ciramadol and pentazocine produced different profiles on the subjective effect measures. All three drugs increased "liking," "good effects," "any effects" and "high" subjective effect scales. Pentazocine increased subjective "bad effects" scale scores and scales measuring dysphoria and sedation. Observers reported significant behavioral changes after administration of morphine and pentazocine, but not after ciramadol. Overall, the effects of morphine (7.5, 15 and 30 mg) and pentazocine (22.5, 45 and 90 mg) were dose-related. Although pentazocine produced increases in scales that indicated negative subjective effects, it also produced significant changes in most self-report measures that were increased by morphine, including liking and good effects scales. The effects of ciramadol were not dose-related, with all three doses (30, 60 and 120 mg) producing effects approximately equivalent to morphine 15 mg. Thus, ciramadol exhibited a ceiling effect typical of the opioid agonist/antagonist.
在临床研究病房中，对成年男性非依赖型阿片类药物滥用者研究了吗啡、喷他佐辛和环拉马朵（一种阿片类激动剂/拮抗剂）的主观、生理和行为效应。15名受试者被随机分配到三组中的一组。在4.5小时的实验时段内，每组在双盲条件下，通过肌肉注射接受安慰剂和三种剂量的一种活性药物，按随机区组顺序给药两次。生理指标未能区分这三种药物。所有三种药物均降低呼吸频率和瞳孔直径，并升高血压。然而，吗啡、环拉马朵和喷他佐辛在主观效应指标上呈现出不同的特征。所有三种药物均提高了“喜欢”“良好效应”“任何效应”和“兴奋”等主观效应量表得分。喷他佐辛提高了主观“不良效应”量表得分以及测量烦躁不安和镇静程度的量表得分。观察者报告称，给予吗啡和喷他佐辛后出现了显著的行为变化，但给予环拉马朵后未出现。总体而言，吗啡（7.5、15和30毫克）和喷他佐辛（22.5、45和90毫克）的效应与剂量相关。尽管喷他佐辛使表明负面主观效应的量表得分升高，但它在大多数自我报告指标上也产生了显著变化，这些指标在吗啡作用下也会升高，包括喜欢和良好效应量表。环拉马朵的效应与剂量无关，其所有三个剂量（30、60和120毫克）产生的效应大致相当于15毫克吗啡的效应。因此，环拉马朵表现出阿片类激动剂/拮抗剂典型的天花板效应。
