Nurses Compass
Drug Guide
Oliceridine
Classification
Therapeutic: Analgesic
Pharmacological: Selective G protein pathway opioid receptor agonist
FDA Approved Indications
- Management of moderate to severe acute pain requiring opioid analgesia in adults
Mechanism of Action
Oliceridine selectively activates the μ-opioid receptor (MOR), preferentially stimulating G protein pathways that mediate analgesia, while minimizing recruitment of β-arrestin pathways associated with adverse effects such as respiratory depression and constipation.
Dosage and Administration
Adult: Initial dose: 1.5 mg IV over 1 minute; repeat doses may be given every 4 to 6 hours as needed, with adjustments based on response and tolerability. Maximum dose varies based on clinical response.
Pediatric: Not FDA approved for pediatric use.
Geriatric: Start at lower end of dosing spectrum due to increased sensitivity and comorbidities.
Renal Impairment: No specific dosage adjustment required, but caution in severe impairment.
Hepatic Impairment: Not well studied; use with caution and monitor closely.
Pharmacokinetics
Absorption: Administered intravenously; bioavailability is 100%.
Distribution: Widely distributed with a volume of distribution approximately 134 L.
Metabolism: Primarily metabolized in the liver via glucuronidation and oxidation pathways.
Excretion: Excreted mainly via urine and feces.
Half Life: Approximately 1.2 hours.
Contraindications
- Known hypersensitivity to oliceridine or components of the formulation.
Precautions
- Use with caution in patients with respiratory impairment, head injury, or decreased consciousness. Monitor for adverse effects such as respiratory depression, hypotension, and sedation. Not recommended for use with CYP3A4 inhibitors due to potential increased exposure.
Adverse Reactions - Common
- Nausea (Frequent)
- Constipation (Frequent)
- Headache (Common)
- Dizziness (Common)
Adverse Reactions - Serious
- Respiratory depression (Uncommon)
- Hypotension (Uncommon)
- Serotonin syndrome (rare) (Rare)
- Addiction, abuse, misuse (Serious)
Drug-Drug Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase oliceridine levels; CYP3A4 inducers (e.g., rifampin) may decrease efficacy.
Drug-Food Interactions
- No significant interactions reported.
Drug-Herb Interactions
- Potential interactions with serotonergic herbs (e.g., St. John's Wort) due to risk of serotonin syndrome.
Nursing Implications
Assessment: Monitor respiratory status, sedation levels, and pain relief frequently.
Diagnoses:
- Acute pain related to surgical procedure or injury
- Risk for respiratory depression due to opioid use
Implementation: Administer IV as prescribed, observe for adverse reactions, and provide supportive care as needed.
Evaluation: Assess pain relief using appropriate scales and monitor for signs of adverse effects.
Patient/Family Teaching
- Do not exceed prescribed dose, and do not combine with alcohol or other CNS depressants.
- Report signs of respiratory depression, excessive sedation, or any adverse effects promptly.
- Use caution when operating machinery or driving after administration.
Special Considerations
Black Box Warnings:
- Risks of opioid overdose leading to respiratory depression and death.
- Use with caution in combination with serotonergic drugs due to serotonin syndrome risk.
Genetic Factors: Genetic variability in CYP3A4 enzymes can affect metabolism and response.
Lab Test Interference: No known significant effects on laboratory tests.
Overdose Management
Signs/Symptoms: Respiratory depression, sedation, coma.
Treatment: Discontinue oliceridine, provide supportive respiratory care, administer opioid antagonists such as naloxone if necessary.
Storage and Handling
Storage: Store at room temperature between 20°C to 25°C (68°F to 77°F).
Stability: Stable for 24 months when stored properly.