Oliceridine in the treatment of moderate to severe acute pain

• Published in: Pain management (London) 2021-05, Vol.11 (3), p.237-248
• Main Authors: Eleswarpu, Sarada S, Habib, Ashraf S
• Format: Article
• Language: English
• Subjects: analgesia; analgesia-mu receptor; analgesia-opioid; G-protein biased ligand; g-protein ligand; G-protein selective ligand; oliceridine; parenteral opioid administration; side effects – opioids; TRV130
• ISSN: 1758-1869; 1758-1877
• DOI: 10.2217/pmt-2020-0087

Intravenous opioids are a mainstay for the management of moderate to severe acute pain. Opioid administration provides effective pain control at the cost of significant side effects. Commonly used opioids like morphine are nonselective μ-receptor agonists, which stimulate both the G-protein pathway, associated with the analgesic effect, and the β-arrestin pathway, associated with the side effects. Oliceridine is a G-protein selective ligand at the μ-receptor with less activation of the β-arrestin pathway. The drug has recently been US FDA approved. This review will focus on the efficacy and safety of intravenous oliceridine in the treatment of moderate to severe acute pain. Opioids provide effective pain control for the management of moderate to severe acute pain. However, there are significant side effects associated with these pain control medications, including shallower and slower breathing, nausea and vomiting, constipation, itchiness and drowsiness. Commonly used opioids like morphine work by activating two signaling pathways; one pathway leads to the pain relief effect and the other pathway is associated with the development of the side effects. Oliceridine is a novel opioid medication that is designed to activate the side effect pathway to a lesser extent. The drug has recently been US FDA approved. This review article will focus on the efficacy and safety of intravenous oliceridine in the treatment of moderate to severe acute pain.