The U.S. Food and Drug Administration approved oliceridine for the management of moderate to severe acute pain in adults on 7 August, 2020, where the pain is acute enough to need an opioid intravenously (IV) and for whom other therapies are ineffective. This opioid agonist is indicated for short-term IV use in hospitals or other controlled clinical settings, for example during inpatient and outpatient procedures. It is not indicated for at-home use.

This approval was based on controlled and open-label trials comprising of 1,535 patients with moderate to severe acute pain on oliceridine therapy. A comparison of oliceridine to placebo was used to establish its efficacy and safety in randomized, controlled studies of patients underwent bunion surgery or abdominal surgery. Patients administered oliceridine reported pain relief at the suggested doses. Oliceridine has a similar safety profile like other opioids with the most common side effects of Oliceridine being headache, nausea, vomiting, dizziness and constipation.

Also, this opioid agonist should not be given to patients with substantial respiratory depression; acute or severe bronchial asthma in an unmonitored setting or in the lack of resuscitative apparatus; known or alleged gastrointestinal obstruction; or known hypersensitivity to drug. In pregnancy, its sustained use can result in neonatal opioid withdrawal syndrome.

A boxed warning about addiction, abuse and misuse; life-threatening respiratory depression; neonatal opioid withdrawal syndrome; and risks from concomitant use with benzodiazepines or other central nervous system depressants has been mentioned. Oliceridine has a maximum suggested daily dose limit of 27 mgs, not like other opioids for IV use.