What is the drug Oliceridine used for? A Comprehensive Guide

October 11, 2025 •

3 min read

Oliceridine (brand name Olinvyk), an intravenous opioid analgesic approved in 2020, was developed with a unique mechanism intended to provide powerful pain relief with a potentially improved safety profile compared to traditional opioids. This medication is specifically used in hospital and controlled clinical settings for managing acute pain.

Quick Summary

Oliceridine, marketed as Olinvyk, is an intravenous opioid used for short-term management of acute, severe pain, typically in hospital settings. Its unique mechanism offers analgesia with potentially fewer gastrointestinal side effects than morphine.

Key Points

Acute, Severe Pain: Oliceridine (Olinvyk) is primarily used for the short-term, intravenous management of acute, severe pain in adults, particularly in a hospital setting for post-surgical pain.
G-Protein Biased Agonist: Its unique mechanism aims to preferentially activate the G-protein pathway for pain relief while minimizing the beta-arrestin pathway responsible for many opioid side effects.
Intravenous Administration: It is administered via intravenous injection, either through intermittent bolus doses or a patient-controlled analgesia (PCA) pump, under medical supervision.
Significant Risks: The drug carries serious risks, including life-threatening respiratory depression, addiction, abuse, misuse, and neonatal opioid withdrawal syndrome.
Comparison to Morphine: While initial development aimed for a superior safety profile, clinical studies have shown mixed results; it may cause less nausea and vomiting but respiratory depression risk remains comparable to morphine at equipotent doses.
Schedule II Controlled Substance: The U.S. Drug Enforcement Administration (DEA) has classified oliceridine as a Schedule II controlled substance due to its high potential for abuse.

What is Oliceridine Used For?

Oliceridine (Olinvyk) is an intravenous opioid analgesic indicated for the management of acute pain in adults. It is reserved for pain that is severe enough to require an intravenous opioid and for whom alternative treatments, such as non-opioid analgesics or combination products, are inadequate or not tolerated. The medication is administered in a controlled clinical environment, such as a hospital. It is primarily used in the post-surgical period, with clinical trials showing its effectiveness for moderate-to-severe postoperative pain after procedures like bunionectomies and abdominoplasties.

Mechanism of Action: G-Protein Bias

Oliceridine is a G-protein biased mu-opioid receptor (MOR) agonist. Unlike non-biased opioids like morphine, which activate both G-protein and β-arrestin pathways, oliceridine preferentially activates the G-protein pathway responsible for analgesia while having less effect on the β-arrestin pathway, which is linked to side effects like respiratory depression and constipation. This was intended to offer potent pain relief with fewer opioid-related adverse events. While animal studies supported this, clinical trial results have been mixed, showing potential for reduced gastrointestinal side effects but similar respiratory safety outcomes to morphine at effective doses.

Administration

Oliceridine is administered intravenously in a clinical setting using two primary methods:

Intermittent Bolus Dosing: Single injections administered by a healthcare provider at specific intervals as needed, with limits on the total daily dose.
Patient-Controlled Analgesia (PCA): Allows patients to self-administer set doses using a pump with programmed dose limits and lockout periods to prevent overdose.

Potential Risks and Side Effects

Oliceridine carries significant risks and side effects, similar to other opioid analgesics, and includes a boxed warning concerning addiction, abuse, misuse, and life-threatening respiratory depression.

Common Side Effects

Nausea and vomiting
Dizziness and headache
Constipation
Hypoxia (low blood oxygen)
Flushing and itching

Serious Risks

Respiratory Depression: Serious, life-threatening, or fatal respiratory depression is a risk, particularly within the first 24-48 hours and after dose increases.
Abuse Potential: As a Schedule II controlled substance, oliceridine has a high potential for abuse.
Neonatal Opioid Withdrawal Syndrome: Prolonged use during pregnancy can cause severe withdrawal in newborns.
QT Prolongation: High doses may cause a heart rhythm abnormality (QTc interval prolongation).
Interactions with CNS Depressants: Combining oliceridine with central nervous system depressants like benzodiazepines or alcohol can cause profound sedation, respiratory depression, or coma.
Gastrointestinal Obstruction: The drug is contraindicated in patients with known or suspected gastrointestinal obstruction.

Oliceridine vs. Morphine Comparison

Oliceridine was developed as an alternative to conventional opioids like morphine. The table below compares the two based on available clinical data:


Feature	Oliceridine (Olinvyk)	Morphine
Primary Indication	Short-term management of acute, severe intravenous opioid pain in adults.	Management of acute and chronic moderate-to-severe pain.
Mechanism of Action	G-protein biased mu-opioid receptor (MOR) agonist.	Non-biased MOR agonist.
Gastrointestinal Effects	May have lower rates of nausea, vomiting, and constipation.	Higher incidence of nausea, vomiting, and constipation.
Respiratory Depression	Dose-related risk, potentially similar to morphine at equipotent doses.	Well-known, dose-related risk.
Onset of Action	Rapid onset (2-5 minutes IV).	Slower onset compared to oliceridine.
Dependence and Addiction	High potential for abuse and dependence (Schedule II).	High potential for abuse and dependence.
Adverse Event Profile	Nausea, vomiting, dizziness, headache, risk of QT prolongation.	Nausea, vomiting, dizziness, constipation.

Conclusion

Oliceridine is an intravenous opioid analgesic used for the short-term treatment of acute, severe pain, typically in hospital settings for post-surgical pain. Its G-protein biased mechanism was designed to potentially reduce common opioid side effects. However, while some studies show a potential reduction in gastrointestinal issues, findings regarding respiratory safety compared to morphine are mixed, with similar risks at effective analgesic doses. Oliceridine carries significant risks, including addiction, abuse, and misuse, and is a Schedule II controlled substance. Its use is managed under close medical supervision, with clinicians needing to balance its rapid onset and efficacy against its risks compared to other opioids.

For more information on opioids, consult the National Institutes of Health: [https://www.ncbi.nlm.nih.gov/books/NBK605806/].

Frequently Asked Questions

The brand name for oliceridine is Olinvyk.

No, oliceridine is specifically indicated for the short-term management of acute pain and has not been studied or approved for use in chronic pain conditions.

Oliceridine is a G-protein biased agonist, meaning it selectively activates the analgesic pathway of the mu-opioid receptor while having a lesser effect on the pathway associated with side effects. In contrast, morphine activates both pathways more indiscriminately.

No, oliceridine is only approved for use in a controlled clinical setting, such as a hospital, for intravenous administration under direct medical supervision.

Yes, oliceridine can cause serious and life-threatening respiratory depression, and patients must be closely monitored for this risk, especially during treatment initiation or dose increases.

Yes, the Drug Enforcement Administration (DEA) has placed oliceridine in Schedule II of the Controlled Substances Act due to its high potential for abuse and dependence.

At higher dose levels, oliceridine has been associated with a risk of QTc interval prolongation, a condition that can potentially affect heart rhythm.