What it isMu-opioid agonist with G-protein-biased signaling; IV treatment of acute severe pain.
Why this oneIt was designed to separate analgesia from respiratory depression, but its clinical advantage over conventional mu agonists is modest.
What limits it⚑ It retains boxed warnings for respiratory depression, misuse, and benzodiazepines; QT prolongation limits cumulative exposure.
FDA-approved for
FDA label
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BOXED WARNING Opioid addiction, abuse, and misuse; life-threatening respiratory depression; risks from concomitant benzodiazepines/CNS depressants; neonatal opioid withdrawal syndrome
| FDA dosing | Population | Start | Target | Max |
| Acute pain severe enough to require an IV opioid | Adults | 1.5 mg IV | Demand 0.35 mg (6-min lockout) or supplemental 0.75 mg | 27 mg/day cumulative |
Renal No adjustment needed
Hepatic Mild-moderate: no initial-dose change but may need less frequent dosing; severe: reduce initial dose and space subsequent doses
PCA demand dose 0.35 mg with 6-min lockout (may consider 0.5 mg); supplemental 0.75 mg beginning 1 h after initial dose, then hourly PRN
Instructions
- For IV administration only
- Use lowest effective dose for shortest duration
- Do not exceed a cumulative 27 mg/day (QT prolongation risk)
- CYP2D6 poor metabolizers may require less frequent dosing
Contraindications
- Significant respiratory depression
- Acute or severe bronchial asthma in an unmonitored setting or without resuscitative equipment
- Known or suspected GI obstruction, including paralytic ileus
Cautions
- Opioid-induced hyperalgesia/allodynia
- QT prolongation at daily doses >27 mg
- Life-threatening respiratory depression in chronic pulmonary disease or elderly/cachectic/debilitated
- Adrenal insufficiency
- Severe hypotension; avoid in circulatory shock
- Risk with increased ICP/head injury/impaired consciousness
Adverse reactions
- Nausea
- Vomiting
- Dizziness
- Headache
- Constipation
- Pruritus
- Hypoxia
Pregnancy No human data; prolonged use in pregnancy can cause neonatal opioid withdrawal syndrome
Lactation Presence in human milk unknown; monitor breastfed infant for excess sedation and respiratory depression
⚠ BOXED WARNINGS
- Addiction, abuse and misuse
- Life-threatening respiratory depression
- Risk from concomitant use with benzodiazepines
Classes and tags
Clinical profile
Direct muscarinic antagonism0 / 4
Mechanism of action: Oliceridine ballicule
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