Oliceridine

Oliceridine is a full opioid agonist and is relatively selective for the mu-opioid receptor. The principal therapeutic action of oliceridine is analgesia.

• OLINVYK is indicated in adults for the management of acute pain severe enough to require an intravenous opioid analgesic and for whom alternative treatments are inadequate. Limitations of Use Because of the risks of addiction, abuse, misuse, overdose, and death, which can occur at any dosage or duration [see Warnings and Precautions ( 5.1 )] , and persist over the course of therapy, reserve opioid analgesics, including OLINVYK, for use in patients for whom alternative treatment options are ineffective, not management of pain.

• OLINVYK is contraindicated in patients with: Significant respiratory depression [see Warnings and Precautions ( 5.2 )] Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment [see Warnings and Precautions ( 5.8 )] Known or suspected gastrointestinal obstruction, including paralytic ileus [see Warnings and Precautions ( 5.12 )] Known hypersensitivity to oliceridine (e.g., anaphylaxis) Significant respiratory depression ( 4 ) Acute or severe bronchial asthma in an unmonitored setting or in absence of resuscitative equipment ( 4 ) Known or suspected gastrointestinal obstruction, including paralytic ileus ( 4 ) Known hypersensitivity to oliceridine ( 4 )contraindicated

For intravenous administration only. OLINVYK should be prescribed only by healthcare professionals who are knowledgeable about the use of opioids and how to mitigate the associated risks. ( 2.1 ) Use the lowest effective dosage for the shortest duration consistent with individual patient treatment goals. Reserve titration to higher doses of OLINVYK for patients in whom lower doses are insufficiently effective and in whom the expected benefits of using a higher dose opioid clearly outweigh the substantial risks. ( 2.1 , 5 ) Initiate the dosing regimen for each patient individually, taking into account the patient’s underlying cause and severity of pain, prior analgesic treatment and response, and risk factors for addiction, abuse and misuse. ( 2.1 , 5.1 ) Respiratory depression can occur at any time during opioid therapy, especially when initiating and following dosage increases with OLINVYK. Consider this risk when selecting an initial dose and when making dose adjustments. ( 2.1 , 5.2 ) Initiate treatment with a 1.5 mg dose. ( 2.2 ) For patient controlled analgesia (PCA), recommended demand dose is 0.35 mg, with a 6-minute lock-out. A demand dose of 0.5 mg may be considered. ( 2.2 ) Supplemental doses of 0.75 mg can be administered, beginning 1 hour after the initial dose, and hourly thereafter, as needed. ( 2.2 ) Periodically reassess patients receiving OLINVYK to evaluate the continued need for opioid analgesics to maintain pain control, for the signs or symptoms of adverse reactions, and for the development of addiction, abuse, or misuse.

Opioid-Induced Hyperalgesia and Allodynia: Opioid-Induced Hyperalgesia (OIH) occurs when an opioid analgesic paradoxically causes an increase in pain, or an increase in sensitivity to pain. If OIH is suspected, carefully consider appropriately decreasing the dose of the current opioid analgesic or opioid rotation. ( 5.7 ) Potential for QT Prolongation with Daily Doses Exceeding 27 mg : May increase risk for QT interval prolongation. Do not exceed a cumulative daily dose of 27 mg. ( 5.5 ) Life-Threatening Respiratory Depression in Patients with Chronic Pulmonary Disease or in Elderly, Cachectic, or Debilitated Patients : Monitor closely, particularly during initiation and titration. ( 5.8 ) Adrenal Insufficiency : If diagnosed, treat with physiologic replacement corticosteroids and wean the patient off the opioid. ( 5.9 ) Severe Hypotension : Monitor patients during initiation or titration. Avoid use of OLINVYK in patients with circulatory shock. ( 5.10 ) Risks of Use in Patients with Increased Intracranial Pressure, Brain Tumors, Head Injury, or Impaired Consciousness : Monitor for signs of sedation and respiratory depression. Avoid the use of OLINVYK in patients with impaired consciousness or coma. ( 5.11 ) 5.1 Addiction, Abuse, and Misuse OLINVYK contains oliceridine, a Schedule II controlled substance. As an opioid, OLINVYK exposes users to the risks of addiction, abuse, and misuse [see Drug Abuse and Dependence ( 9 )] . Although the risk of addiction in any individual is unknown, it can occur in patients appropriately prescribed OLINVYK.

The following adverse reactions are described, or described in greater detail, in other sections: Addiction, Abuse, and Misuse [see Warnings and Precautions ( 5.1 )] Life-threatening Respiratory Depression [see Warnings and Precautions ( 5.2 )] Interactions with Benzodiazepines or Other CNS Depressants [see Warnings and Precautions ( 5.3 )] Neonatal Opioid Withdrawal Syndrome [see Warnings and Precautions ( 5.4 )] Opioid-Induced Hyperalgesia and Allodynia [see Warnings and Precautions ( 5.7 )] Adrenal Insufficiency [see Warnings and Precautions ( 5.9 )] Severe Hypotension [see Warnings and Precautions ( 5.10 )] Gastrointestinal Adverse Reactions [see Warnings and Precautions ( 5.12 )] Seizures [see Warnings and Precautions ( 5.13 )] Withdrawal [see Warnings and Precautions ( 5.14 )] The most common (incidence ≥10%) adverse reactions in controlled clinical trials (Studies 1 and 2) were nausea, vomiting, dizziness, headache, constipation, pruritus, and hypoxia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Trevena, Inc. at 1-844-465-4686 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Studies Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. A total of 1535 patients were treated with OLINVYK in controlled and open-label trials in patients with moderate to severe acute pain.

Pregnancy : May cause fetal harm ( 8.1 ) Decreased CYP2D6 function: Patients may require less frequent dosing. Monitor closely and administer subsequent doses based on severity of pain and patient response. ( 8.8 ) 8.1 Pregnancy Risk Summary Use of opioid analgesics for an extended period of time during pregnancy may result in neonatal opioid withdrawal syndrome [see Warnings and Precautions ( 5.4 )] . There are no available data on OLINVYK use in pregnant women to evaluate for a drug-associated risk of major birth defects and miscarriage or adverse maternal outcomes. There are adverse outcomes reported within detal exposure to opioid analgesics (see Clinical Considerations) . In animal reproductive studies, oliceridine reduced live litter size at birth and increased postnatal pup mortality between birth and Postnatal Day 4 when administered intravenously to rats from organogenesis through weaning at doses producing clinically relevant plasma exposure. Oliceridine had no effect on embryo-fetal development in rats and rabbits when administered intravenously during organogenesis at doses producing plasma exposures 7 and 8 times the estimated plasma exposure at the maximum recommended human dose (MRHD) on an AUC basis, respectively (see Data) . The background risk of major birth defects and miscarriage for the indicated population is unknown.

Metabolism

Distribution The mean steady-state volume of distribution of oliceridine ranges between 90-120 L indicating extensive tissue distribution. The plasma protein binding of oliceridine is 77%.

Clinical Presentation Acute overdose with OLINVYK can be manifested by respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, and, in some cases, pulmonary edema, bradycardia, hypotension, hypoglycemia, partial or complete airway obstruction, atypical snoring, and death. Marked mydriasis rather than miosis may be seen due to severe hypoxia in overdose situations [see Clinical Pharmacology ( 12.2 )] . Toxic leukoencephalopathy has been reported after opioid overdose and can present hours, days, or weeks after apparent recovery from the initial intoxication. Treatment of Overdose In case of overdose, priorities are the reestablishment of a patent and protected airway and institution of assisted or controlled ventilation, if needed. Employ other supportive measures (including oxygen and vasopressors) in the management of circulatory shock and pulmonary edema as indicated. Cardiac arrest or arrhythmias will require advanced life-support measures.

• Aug 7, 2020NDANDA210730Trevena

1. 1Respiratory Depression1100%

The 10 most recently updated of 31 ClinicalTrials.gov registrations naming Oliceridine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Oliceridine on Postoperative Nausea and Vomiting in Gynecological Laparoscopic Surgery
  Completed · Phase 4 · Interventional · 96 enrolled · YanYing Xiao
  NCT07026162updated 2026-06-09
• Comparison of the Analgesic Effect of Oliceridine Versus Morphine or Sufentanil for Postoperative Analgesia in Lumbar Surgeries: a Randomized Control Trial
  Recruiting · Interventional · 90 enrolled · Anqing Municipal Hospital
  NCT06990893updated 2026-06-01
• Oliceridine Versus Sufentanil for Postoperative Nausea in Cerebellopontine Angle Surgery
  Recruiting · Interventional · 174 enrolled · Xuanwu Hospital, Beijing
  NCT07479446updated 2026-05-22
• Intravenous Oliceridine and Opioid-related Complications
  Completed · Phase 4 · Interventional · 204 enrolled · The Cleveland Clinic
  NCT04979247updated 2026-05-14
• Dexmedetomidine-Enhanced PCIA After Lobectomy in Nicotine-Dependent Patients
  Withdrawn · Phase 4 · Interventional · 0 enrolled · Shenyang Sixth People's Hospital
  NCT07306702updated 2026-04-13
• Effects and Safety of Oliceridine in Anesthesia Induction:A Randomised Controlled Trial
  Completed · Interventional · 120 enrolled · Tangshan Maternal and Child Health Hospital
  NCT07372209updated 2026-01-28
• The Effect of Oliceridine Patient-Controlled Intravenous Analgesia on Postoperative Chronic Pain After Video-Assisted Thoracoscopic Lobectomy
  Not yet recruiting · Phase 4 · Interventional · 320 enrolled · Tianjin Medical University General Hospital
  NCT07018375updated 2026-01-06
• Respiratory Safety of Oliceridine During Sedated Gastrointestinal Endoscopy
  Completed · Interventional · 508 enrolled · Shiyou Wei
  NCT07187765updated 2026-01-05
• Effect of Postoperative Analgesia of Oliceridine Fumarate for Gastrointestinal Function Recovery in Patients Undergoing Lumbar Spine Surgery
  Not yet recruiting · Interventional · 428 enrolled · Xijing Hospital
  NCT07307495updated 2025-12-29
• Oliceridine Dose for Tracheal Intubation Hemodynamic Elevation: Up-and-Down Trial
  Completed · Interventional · 58 enrolled · Shiyou Wei
  NCT07154979updated 2025-11-18

CPIC-curated drug–gene pairs for Oliceridine. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• CYP2D6CPIC A/B (provisional)FDA label: Actionable PGx

Frequently asked questions

How does Oliceridine work?

Oliceridine is a full opioid agonist and is relatively selective for the mu-opioid receptor. The principal therapeutic action of oliceridine is analgesia.

What is Oliceridine used for?

According to FDA labeling, Oliceridine carries indications including: OLINVYK is indicated in adults for the management of acute pain severe enough to require an intravenous opioid analgesic and for whom alternative treatments are inadequate. Limitations of Use Because of the risks of addiction, abuse, misuse, overdose, and death, which can occur at any dosage or duration [see Warnings and Precautions ( 5.1 )] , and persist over the course of therapy, reserve opioid analgesics, including OLINVYK, for use in patients for whom alternative treatment options are ineffective, not management of pain.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Oliceridine?

Oliceridine is classified as Other opioids, Opioid Agonists, Analgesia.

What are the brand names for Oliceridine?

Oliceridine is marketed under brand names including Olinvyk.

What are the contraindications for Oliceridine?

Oliceridine labeling lists contraindications including: OLINVYK is contraindicated in patients with: Significant respiratory depression [see Warnings and Precautions ( 5.2 )] Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment [see Warnings and Precautions ( 5.8 )] Known or suspected gastrointestinal obstruction, including paralytic ileus [see Warnings and Precautions ( 5.12 )] Known hypersensitivity to oliceridine (e.g., anaphylaxis) Significant respiratory depression ( 4 ) Acute or severe bronchial asthma in an unmonitored setting or in absence of resuscitative equipment ( 4 ) Known or suspected gastrointestinal obstruction, including paralytic ileus ( 4 ) Known hypersensitivity to oliceridine ( 4 ). Always consult the full prescribing information and a clinician.