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NERVOUS SYSTEM › ANALGESICS › OPIOIDS › Other opioids
oliceridine
N02AX07
Forms & Strengths
- Intravenous injection: 1 mg/mL in 1 mL single-dose vials
- Intravenous injection: 2 mg/2 mL (1 mg/mL) in 2 mL single-dose vials
- Intravenous injection: 30 mg/30 mL (1 mg/mL) in 30 mg single-dose pharmacy bulk package
Adult Dosing
- Initial loading dose: 1.5 mg IV; may give additional doses of 0.75 mg within 10 to 15 minutes if needed
- Patient-controlled analgesia (PCA): Demand dose of 0.35 mg, 0.5 mg, or 1 mg with a lockout interval of 6 minutes
- Max cumulative daily dose: 27 mg per day
- Transition to other opioids requires careful titration due to variable cross-tolerance
Pediatric Dosing
- Safety and effectiveness in pediatric patients below the age of 17 years have not been established
Indications
- Management of moderate-to-severe acute pain in adult patients requiring intravenous opioid therapy, typically in hospitals or controlled clinical settings
Mechanism of Action
- Full mu-opioid receptor agonist biased toward G-protein signaling over beta-arrestin recruitment
- Provides analgesia while theoretically exhibiting reduced opioid-related adverse effects associated with beta-arrestin pathways, such as respiratory depression and gastrointestinal dysfunction
Contraindications
- Significant respiratory depression
- Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment
- Known or suspected gastrointestinal obstruction, including paralytic ileus
- Hypersensitivity to oliceridine
Adverse Reactions
- Nausea
- Vomiting
- Dizziness
- Headache
- Constipation
- Pruritus
- Hypotension
- Somnolence
- Respiratory depression
Drug Interactions
- Concomitant use with central nervous system (CNS) depressants (e.g., alcohol, benzodiazepines, other opioids, sedatives) increases risk of profound sedation, respiratory depression, coma, and death
- Strong CYP3A4 inhibitors (e.g., ketoconazole) or CYP2D6 inhibitors may increase oliceridine exposure
- Strong CYP3A4 inducers (e.g., rifampin) may decrease oliceridine exposure
- Serotonergic drugs: Concomitant use with SSRIs, SNRIs, or MAO inhibitors increases risk of serotonin syndrome
Curated Content: Needs Vetting Before Put to Clinical Use