OLINVYK
Clinical safety rating
cautionComprehensive clinical and safety monograph for OLINVYK (OLINVYK).
Oliceridine is a G protein-biased μ-opioid receptor agonist. It preferentially activates the G protein pathway (associated with analgesia) over β-arrestin recruitment (associated with opioid-related adverse effects like respiratory depression and gastrointestinal dysfunction).
| Metabolism | Primarily metabolized by CYP3A4 and CYP2D6 to inactive metabolites; also undergoes glucuronidation. |
| Excretion | Primarily renal (approximately 90% as unchanged drug and metabolites); biliary/fecal excretion accounts for <5% |
| Half-life | Terminal elimination half-life is approximately 26–29 hours, supporting once-daily dosing in chronic pain |
| Protein binding | Approximately 93–95% bound to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | Approximately 3.5–4.5 L/kg, indicating extensive tissue distribution |
| Bioavailability | Oral: approximately 70% for extended-release formulation; intravenous: 100% |
| Onset of Action | Intravenous: within 2–5 minutes; oral: approximately 30–60 minutes |
| Duration of Action | Intravenous: 3–6 hours; oral: 12–24 hours with extended-release formulation |
| Molecular Weight | 449.5 |
Initial adult dose: 1.5 mg intravenously (IV) every 3 to 6 hours as needed. May be titrated in increments of 0.75 mg to 1.5 mg every 3 to 6 hours. Maximum single dose: 4.5 mg. Maximum daily dose: 27 mg.
| Dosage form | SOLUTION |
| Renal impairment | For GFR 15 to 29 mL/min: reduce dose by 50% and monitor for respiratory depression. For GFR <15 mL/min: not recommended. For dialysis: not recommended. |
| Liver impairment | Child-Pugh Class A: no adjustment needed. Child-Pugh Class B: reduce dose by 50%; consider reducing dose frequency. Child-Pugh Class C: avoid use. |
| Pediatric use | Not approved for use in pediatric patients under 18 years of age; safety and efficacy not established. |
| Geriatric use | Initial dose: 1.5 mg IV every 3 to 6 hours; consider dose reduction to 0.75 mg in patients aged 65 years or older due to increased sensitivity and risk of respiratory depression. |
| 1st trimester | Insufficient human data; animal studies show embryo-fetal toxicity at high doses. Use only if potential benefit justifies risk. |
| 2nd trimester | Insufficient human data; use only if clearly needed. |
| 3rd trimester | Prolonged use may cause neonatal opioid withdrawal syndrome. Avoid or use lowest effective dose for shortest duration. |
Clinical note
Comprehensive clinical and safety monograph for OLINVYK (OLINVYK).
| Placental transfer | Oliceridine crosses the placenta; fetal exposure is expected due to molecular weight and lipophilicity. |
| Breastfeeding | Oliceridine is present in breast milk; due to risk of infant sedation and respiratory depression, breastfeeding is not recommended during treatment. If used, monitor infant for signs of opioid toxicity. |
| Lactation Rating | L5 (Contraindicated) |
| Teratogenic Risk | Prolonged use of opioids during pregnancy can result in neonatal opioid withdrawal syndrome. First trimester: Limited data, but opioids as a class are not major teratogens. Second/third trimester: Chronic use may lead to fetal dependence and withdrawal postnatally. Use only if benefit outweighs risk, especially near term. |
| Fetal Monitoring | Monitor maternal respiratory status, level of consciousness, and bowel function. Assess for signs of misuse or abuse. In fetus/neonate, monitor for neonatal opioid withdrawal syndrome if used chronically near term. |
| Fertility Effects | Opioid use may cause reversible hypothalamic-pituitary-gonadal axis disruption, leading to decreased fertility in both sexes. Specific data for oliceridine lacking; class effect presumed. |
■ FDA Black Box Warning
Risk of addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion; risks from concomitant use with benzodiazepines or CNS depressants; neonatal opioid withdrawal syndrome; and risks associated with use in patients with compromised respiratory function, especially in elderly, cachectic, or debilitated patients.
| Serious Effects |
Significant respiratory depressionAcute or severe bronchial asthma in an unmonitored setting or without resuscitative equipmentKnown or suspected gastrointestinal obstruction (e.g., paralytic ileus)Hypersensitivity to oliceridine or any component of the formulation
| Precautions | Life-threatening respiratory depression; addiction, abuse, and misuse; neonatal opioid withdrawal syndrome; risks from concomitant use with benzodiazepines or CNS depressants; severe hypotension; adrenal insufficiency; seizure; and withdrawal. |
| Food/Dietary | No specific food interactions. Grapefruit juice has no known interaction. Avoid alcohol consumption due to additive CNS depression. |
| Clinical Pearls | OLINVYK (oliceridine) is a mu-opioid receptor agonist with reduced beta-arrestin recruitment, potentially offering a therapeutic window with less respiratory depression at equianalgesic doses. Requires ECG monitoring due to QTc prolongation; avoid in patients with history of long QT syndrome or concurrent QT-prolonging drugs. Do not use more than 27 mg in a 24-hour period due to hepatic metabolite accumulation. Administer only in a hospital setting for short-term intravenous use (≤48 hours). |
| Patient Advice | OLINVYK is a strong pain medicine that can cause serious side effects like slowed breathing, low blood pressure, and heart rhythm changes. · Tell your healthcare provider right away if you feel dizzy, lightheaded, or faint, or if you have a fast or irregular heartbeat. · Do not stop taking this medicine suddenly, as withdrawal symptoms may occur. · Do not drive or operate heavy machinery while receiving this medication. · This drug may cause constipation; increase fluid intake and request stool softeners if needed. |
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