Journey of Oliceridine

Abstract

Opioid analgesics play a crucial role in the management of acute pain, but its use is often limited by various adverse effects, especially nausea, vomiting, and respiratory depression. There has always been an attempt to develop analgesics that are equi-efficacious to opioids but carry less risk of respiratory depression. Oliceridine has been the first among such biased/selective molecules approved by the United States Food and Drug Administration. Oliceridine is proposed to act selectively on mu-opioid receptors producing analgesia but does not propagate β-arrestin mediated mechanism postulated to be responsible for respiratory depression of other opioids, especially morphine. Oliceridine has favorable pharmacokinetics for intravenous administration and no significant drug interactions have been proposed.