Linyi Central Hospital, Shandong, China.
Ann Pharmacother. 2021 Oct;55(10):1283-1289. doi: 10.1177/1060028020987679. Epub 2021 Jan 11.
To review the pharmacological characteristics, clinical evidence, and place in the management of acute postoperative pain severe enough to require an intravenous opioid.
A comprehensive literature search was conducted in PubMed (January 2000 to December 1, 2020). Key search terms included or . Other sources were derived from product labeling and ClinicalTrials.gov.
All English-language articles identified from the data sources were reviewed and evaluated. Phase I, II, and III clinical trials were included.
Oliceridine is a novel selective µ-receptor G-protein pathway modulator. It has the property of activating G-protein signaling while causing low β-arrestin recruitment to the µ-receptor. Intravenous oliceridine showed statistically superior analgesia than placebo in patients with moderate or severe pain after surgery, with a favorable safety and tolerability profile regarding respiratory and gastrointestinal adverse effects, compared with morphine.
The analgesic capacity of oliceridine is at least comparable to that of morphine at clinically relevant dosages, with a rapid onset of action. Also, it may be associated with a lower incidence of adverse events at dosing regimens associated with comparable analgesia. These data suggest that oliceridine may provide an important new treatment option for the management of moderate to severe postoperative pain where an intravenous opioid is warranted.
Oliceridine has obvious analgesic effects in patients with moderate or severe pain after surgery; additionally, it has a favorable safety and tolerability profile.
综述足以需要静脉使用阿片类药物的急性术后疼痛的药理学特征、临床证据及在疼痛管理中的地位。
在 PubMed 中进行了全面的文献检索(2000 年 1 月至 2020 年 12 月 1 日)。关键检索词包括 或 。其他来源来自产品标签和 ClinicalTrials.gov。
从资料来源中识别出的所有英文文章都进行了审查和评估。纳入了 I、II 和 III 期临床试验。
奥立利定是一种新型选择性 μ 受体 G 蛋白途径调节剂。它具有激活 G 蛋白信号的特性,同时导致 μ 受体与 β-抑制蛋白的募集减少。与吗啡相比,奥立利定在术后中重度疼痛患者中显示出比安慰剂统计学上更好的镇痛效果,且在呼吸和胃肠道不良反应方面具有良好的安全性和耐受性。
奥立利定的镇痛能力至少与临床相关剂量的吗啡相当,起效迅速。此外,在与相当的镇痛作用相关的剂量方案中,它可能与不良事件的发生率较低相关。这些数据表明,奥立利定可能为需要静脉使用阿片类药物的中重度术后疼痛的管理提供一种重要的新治疗选择。
奥立利定对术后中重度疼痛患者具有明显的镇痛作用;此外,它具有良好的安全性和耐受性。