Aims

Intravenous (IV) misuse of the µ opioid analgesic oxymorphone has caused significant public health harms; however, no controlled data on its IV abuse potential are available. The primary aims of this pilot study were to directly compare IV oxymorphone to IV oxycodone, morphine, and hydromorphone on a subjective measure of drug liking and to assess relative potency.

Methods

Participants (n = 6) with opioid use disorder, physical dependence, and current IV use completed this two-site, within-subject, double-blind, placebo-controlled, inpatient pilot study. During each session, one IV dose (mg/70 kg) was administered: oxymorphone (1.8, 3.2, 5.6, 10, 18, 32), hydromorphone (1.8, 3.2, 5.6, 10, 18), oxycodone (18, 32, 56), morphine (18, 32), and placebo. Data were collected before and for 6 h after dosing. Primary outcomes included safety/physiological effects, subjective reports of drug liking, and relative potency estimates.

Results

All active test drugs produced prototypical, dose-related µ opioid agonist effects (e.g., miosis). Oxymorphone was more potent than the comparator opioids on several measures, including drug liking and respiratory depression (p < 0.05). Across abuse-related subjective outcomes, oxymorphone was 2.3–2.8-fold more potent than hydromorphone and 12.5–14-fold more potent than oxycodone (p < 0.05).

Conclusions

Despite the relatively small sample size, this pilot study detected robust oxymorphone effects. Oxymorphone was far more potent than the comparator opioids, particularly on abuse potential outcomes. Overall, these findings may help explain surveillance reports that demonstrate, after adjusting for prescription availability, oxymorphone is injected at the highest frequency, relative to other prescription opioids.

中文翻译：

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与其他 µ 阿片受体激动剂相比，静脉内羟吗啡酮在人体中的相对效力——初步研究结果

目标

静脉内 (IV) 滥用 µ 阿片类镇痛药羟吗啡酮已对公众健康造成重大危害；然而，没有关于其 IV 滥用潜力的受控数据可用。这项试点研究的主要目的是直接比较静脉注射羟吗啡酮与静脉注射羟考酮、吗啡和氢吗啡酮对药物喜好的主观测量，并评估相对效力。

方法

患有阿片类药物使用障碍、身体依赖和目前使用静脉注射的参与者 ( n  = 6) 完成了这项两点、受试者内、双盲、安慰剂对照、住院试验研究。在每个疗程中，静脉注射一剂（mg/70 kg）：羟吗啡酮（1.8, 3.2, 5.6, 10, 18, 32），氢吗啡酮（1.8, 3.2, 5.6, 10, 18），羟考酮（18, 32, 56)、吗啡 (18, 32) 和安慰剂。在给药前和给药后 6 小时收集数据。主要结果包括安全性/生理效应、药物喜好的主观报告和相对效力估计。

结果

所有活性试验药物都产生了典型的、剂量相关的μ阿片激动剂作用（例如瞳孔缩小）。羟吗啡酮在几个指标上比对照阿片类药物更有效，包括药物嗜好和呼吸抑制（p  < 0.05）。在与滥用相关的主观结果中，羟吗啡酮的效力是氢吗啡酮的 2.3-2.8 倍，是羟考酮的 12.5-14 倍（p  < 0.05）。

结论

尽管样本量相对较小，但这项试点研究检测到了强有力的羟吗啡酮效应。羟吗啡酮比对照阿片类药物更有效，特别是在滥用潜在结果方面。总体而言，这些发现可能有助于解释监测报告显示，在调整处方可用性后，相对于其他处方阿片类药物，羟吗啡酮的注射频率最高。