Relative potency of intravenous oxymorphone compared to other µ opioid agonists in humans - pilot study outcomes.
Relative potency of intravenous oxymorphone compared to other µ opioid agonists in humans - pilot study outcomes.
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静脉注射羟吗啡酮与其他μ阿片激动剂在人体中的相对效力-初步研究结果
DOI：
10.1007/s00213-021-05872-1
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发表时间：
2021-09
影响因子：
3.4
通讯作者：
Walsh SL
中科院分区：
文献类型：
--
作者：
Babalonis S;Comer SD;Jones JD;Nuzzo P;Lofwall MR;Manubay J;Hatton KW;Whittington RA;Walsh SL
静脉注射 (IV) 滥用μ阿片类镇痛药羟吗啡酮已造成重大公共健康危害；然而，没有关于其静脉注射滥用可能性的受控数据。该初步研究的主要目的是根据药物喜好的主观测量直接比较静脉注射羟吗啡酮与静脉注射羟考酮、吗啡和氢吗啡酮并评估相对效力。患有阿片类药物使用障碍、身体依赖和目前静脉注射使用的参与者 (n=6) 完成了这项两中心、受试者内、双盲、安慰剂对照、住院试点研究。在每次治疗期间，给予一次静脉注射剂量（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。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。所有活性测试药物均产生典型的、剂量相关的μ阿片激动剂作用（例如瞳孔缩小）。羟吗啡酮在多项指标上比对照阿片类药物更有效，包括药物喜好和呼吸抑制（p <0.05）。在与滥用相关的主观结果中，羟吗啡酮的效力比氢吗啡酮强 2.3 - 2.8 倍，比羟考酮强 12.5 - 14 倍（p<0.05）。尽管样本量相对较小，但这项初步研究检测到了强大的羟吗啡酮效应。羟吗啡酮比对照阿片类药物更有效，特别是在滥用的潜在后果方面。总体而言，这些发现可能有助于解释监测报告，这些报告表明，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。
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 aim of this pilot study was to directly compare IV oxymorphone to IV oxycodone, morphine and hydromorphone on a subjective measure of drug liking and to assess relative potency. 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. 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). 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.
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