oliceridine (Rx)

Brand and Other Names:Olinvyk
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Dosing & Uses


Dosage Forms & Strengths

injection, solution: Schedule II

  • 1mg/mL (single-dose vial of 1mg/mL and 2mg/2mL)
  • 30mg/30mL (single-patient-use vial for PCA)

Acute Pain

Indicated for management of moderate-to-severe acute pain that is severe enough to require an IV opioid and for which alternative treatments are inadequate

Use lowest effect dose for shortest duration consistent with individual patient treatment goals

Initial: 1.5 mg/dose IV

Patient-controlled analgesia (PCA): 0.35 mg on demand with 6-minute lockout; may consider 0.5-mg on-demand dose; supplemental doses of 0.75 mg IV may be administered by clinicians

Individual single doses >3 mg not evaluated

Not to exceed cumulative dose of 27 mg/day; dose >27 mg/day may increase risk of QTc prolongation

If 27-mg cumulative daily dose reached and analgesia is still required, administer an alternative analgesic regimen until oliceridine can be resumed the next day

Safety beyond 48 hr use was not evaluated in controlled clinical trials

Conversion between morphine IV and oliceridine

  • Individuals differ in response to opioid drugs; use comparison only as a guide
  • Oliceridine 1-mg initial dose is approximately equipotent to morphine 5 mg

Dosage Modifications

Renal impairment

  • Any stage: No dosage adjustment required

Hepatic impairment

  • Mild-to-moderate: No adjustment of initial dose required; however, these patients may require less frequent dosing
  • Severe: Consider reducing initial dose; administer subsequent doses only after careful review of pain severity and overall clinical status

Dosing Considerations

Indicated for short-term IV use in hospitals or other controlled clinical settings (eg, inpatient and outpatient procedures)

Not indicated for at-home use

Limitations of use

  • Owing to the risks of addiction, abuse, and misuse with opioids, even at recommended doses, reserve use for patients without alternative treatment options (other analgesics not tolerated or have not provided adequate pain relief)

Safety and efficacy not established

Controlled clinical studies did not include sufficient numbers of patients aged ≥65 yr to determine whether they respond differently from younger individuals

In general, dose selection for geriatric patients should be cautious, starting at low end of dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy

The main risk for geriatric patients is respiratory; this has occurred after large initial doses were administered to patients not opioid-tolerant or when administered with other agents that depress respiration

Titrate dosage slowly and monitor for CNS and respiratory depression



Interaction Checker

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            Adverse Effects


            Nausea (56-75%)

            Vomiting (22-43%)

            Dizziness (9-35%)

            Hypoxia (5-20%

            Somnolence (5-19%)

            Pruritus (11-17%)

            Constipation (11-17%)

            Sedation (9-14%)

            Back pain (11-13%)


            Decreased oxygen saturation (4-5%)



            Black Box Warnings

            Addiction, abuse, and misuse

            • Risk of opioid addiction, abuse, and misuse, which can lead to overdose and death
            • Assess each patient’s risk before prescribing, and monitor regularly for development of these behaviors or conditions

            Life-threatening respiratory depression

            • Serious, life-threatening, or fatal respiratory depression may occur
            • Monitor for respiratory depression, especially during initiation or following dosage increase

            Neonatal opioid withdrawal syndrome

            • Prolonged use during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated, and requires management according to protocols developed by neonatology experts
            • Syndrome presents as irritability, hyperactivity and abnormal sleep pattern, high-pitched cry, tremor, vomiting, diarrhea, and failure to gain weight
            • Onset, duration, and severity of neonatal opioid withdrawal syndrome vary based on the specific opioid used, duration of use, timing and amount of last maternal use, and rate of elimination of the drug by the newborn
            • If opioid use required for prolonged period in pregnant females, advise patients of risk for neonatal opioid withdrawal syndrome and ensure availability of appropriate treatment

            CNS depressants

            • Coadministration with benzodiazepines or other CNS depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death
            • Reserve concomitant use in patients for whom alternative treatment options are inadequate
            • Limit dosages and durations to the minimum required
            • Monitor for signs and symptoms of respiratory depression and sedation


            Significant respiratory depression

            Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment

            Known or suspected GI obstruction, including paralytic ileus

            Known hypersensitivity (eg, anaphylaxis)


            Opioids expose users to risks of addiction, abuse, and misuse; assess patient risk; risks of addiction, abuse and misuse are increased in patients with a personal or family history of substance abuse (including drug or alcohol abuse or addiction) or mental illness (eg, major depression); the potential for these risks should not, however, prevent the proper management of pain in any given patient; patients at increased risk may be prescribed opioids, but use in such patients necessitates intensive counseling about the risks and proper use of the drug along with intensive monitoring for signs of addiction, abuse, and misuse

            Serious life-threatening respiratory depression reported, even when used as recommended

            Increased risk for life-threatening respiratory depression in patients with chronic pulmonary disease, geriatric patients, or those who are cachectic or debilitated

            Prolonged use of opioids during pregnancy can result in withdrawal in the neonate; observe newborns for signs of neonatal opioid withdrawal syndrome and manage accordingly

            QT prolongation may occur with doses exceeding 27 mg/day; if 27-mg cumulative daily dose reached and analgesia is still required, an alternative analgesic regimen should be administered until oliceridine can be resumed the next day

            Cases of adrenal insufficiency reported with opioid use, more often following >1 month of use; symptoms may include nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure; if adrenal insufficiency is diagnosed, treat with physiologic replacement doses of corticosteroids; wean patient off opioid to allow adrenal function to recover and continue corticosteroid treatment until adrenal function recovers; other opioids may be tried as some cases reported use of a different opioid without recurrence of adrenal insufficiency

            Avoid use in patients susceptible to carbon dioxide retention (eg, increased ICP, brain tumors, head injury, impaired consciousness, coma); oliceridine may reduce respiratory drive

            May increase seizure frequency in patients with seizure disorders or in other clinical settings associated with seizures

            Do not abruptly discontinue in patient physically dependent on opioids; abrupt discontinuation following prolonged therapy may lead to withdrawal symptoms; taper gradually

            May impair mental or physical abilities to perform potentially hazardous actives (eg, driving, operating machinery)

            Monitor patients on PCA for episodes of respiratory depression

            GI conditions

            • Contraindicated with known or suspected GI obstruction, including paralytic ileus
            • Opioids may cause spasm of the sphincter of Oddi and may increase serum amylase
            • Monitor patients with biliary tract disease, including acute pancreatitis, for worsening symptoms

            Drug interaction overview

            Opioids may reduce efficacy of diuretics by inducing release of antidiuretic hormone

            Anticholinergic drugs may increase risk of urinary retention and/or severe constipation, which may lead to paralytic ileus; monitor for signs of urinary retention or reduced gastric motility if oliceridine is coadministered with anticholinergics

            Oliceridine may enhance neuromuscular blocking action of skeletal muscle relaxants and produce increased respiratory depression

            • Benzodiazepines or other CNS depressants
              • Additive pharmacologic effect; increases risk of hypotension, respiratory depression, profound sedation, coma, and death
              • Reserve coadministration for patients whom alternative treatment options are inadequate; limit dosages and durations to minimum required
              • If decision is made to prescribe a benzodiazepine or other CNS depressant concomitantly with an opioid analgesic, prescribe lowest effective dosages and minimum duration of concomitant use
              • If opioid analgesic initiated in a patient already taking a benzodiazepine or other CNS depressant, prescribe lower initial dose of opioid analgesic, and titrate based on clinical response
              • Coadministration with benzodiazepines or other CNS depressants (including alcohol) increases risk of adverse reactions, including overdose and death
            • Moderate-to-strong CYP2D6 and/or CYP3A4 inhibitors
              • Caution; monitor closely for respiratory depression and sedation
              • If administered with both a CYP2D6 and CYP3A4 inhibitor, may require less frequent oliceridine dosing
              • Coadministration with moderate-to-strong CYP2D6 and/or CYP3A4 inhibitors can increase oliceridine plasma concentration, resulting in increased or prolonged opioid adverse reactions
            • CYP3A4 inducers
              • Monitor for signs of opioid withdrawal
              • If coadministration with a CYP3A4 inducer is necessary, consider increasing oliceridine dose until stable drug effects are achieved
              • If a CYP3A4 inducer is discontinued, consider oliceridine dosage reduction and monitor for signs of respiratory depression
            • Serotonergic drugs
              • Monitor if concomitant use is warranted; discontinue oliceridine if serotonin syndrome suspected
              • Opioids may enhance serotonergic effect of drugs (eg, SSRIs, SNRIs, MAOIs, TCAs, triptans, 5-HT3 antagonists, linezolid, IV methylene blue) that affect the serotonergic neurotransmitter system
            • Mixed agonist/antagonist and partial agonist opioids
              • Avoid coadministration
              • May reduce oliceridine analgesic effects and/or precipitate withdrawal

            Pregnancy & Lactation


            Prolonged use of opioid analgesics during pregnancy may result in neonatal opioid withdrawal syndrome

            Animal studies

            • Reduced live litter size at birth and increased postnatal pup mortality between birth and Postnatal Day 4 when oliceridine was administered IV to rats from organogenesis through weaning at doses producing clinically relevant plasma exposure
            • Oliceridine had no effect on embryofetal development in rats and rabbits when administered IV during organogenesis at doses producing plasma exposures 7 and 8 times the estimated plasma exposure at the maximum recommended human dose

            Clinical considerations

            • Opioids cross the placenta and may produce respiratory depression and psychophysiologic effects in neonates
            • Not recommended for use in pregnant females during and immediately prior to labor, when other analgesic techniques are more appropriate


            • Long-term opioid use may cause reduced fertility in females and males of reproductive potential
            • Unknown whether these effects on fertility are reversible


            • Unknown if present in human milk
            • Monitor infants exposed through breast milk for excess sedation and respiratory depression
            • Withdrawal symptoms can occur in breastfed infants when maternal administration of an opioid analgesic is stopped or when breastfeeding is stopped

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.



            Mechanism of Action

            Mu-opioid receptor agonist

            Precise mechanism of action unknown; however, specific CNS opioid receptors for endogenous compounds with opioidlike activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug


            Onset of analgesia: 2-5 minutes (after initial dose)


            Protein bound: 77%

            Vd: 90-120 L


            Primarily metabolized to inactive metabolites by CYP3A4 and CYP2D6; minor contributions from CYP2C9 and CYP2C19


            Half-life: 1.3-3 hr; ~44 hr (metabolites)

            Excretion: Urine ~70% (as metabolites), 0.97-6.75% (unchanged); remainder eliminated in feces


            CYP2D6 poor metabolizers

            • Approximately 3-10% of Whites, 2-7% of African Americans, and <2% of Asians generally lack the capacity to metabolize CYP2D6 substrates and are classified as poor metabolizers
            • In healthy individuals who are CYP2D6 poor metabolizers, AUC was ~2-fold higher than in nonpoor CYP2D6 metabolizers


            IV Preparation

            Visually inspect parenteral drug products for particulate matter and discoloration before administration

            Solution is a clear, colorless, preservative-free solution for IV use

            If visibly opaque particles, discoloration, or other foreign particles are observed, do not use

            IV Administration

            For short-term IV use only in hospital or healthcare facility

            Dose titration and maintenance

            • Individually titrate dose to provide adequate analgesia and minimizes adverse reactions; continually reevaluate to assess the maintenance of pain relief
            • If level of pain increases after dosage stabilization, attempt to identify the source of increased pain before increasing dosage
            • If unacceptable opioid-related adverse reactions observed, consider reducing the dosage
            • Adjust dosage to obtain appropriate balance between management of pain and opioid-related adverse reactions


            • Do not abruptly discontinue in physically dependent patient
            • If patient shows signs of physical dependence, raise dose to previous level and taper more slowly, either by increasing interval between decreases, decreasing amount of dosage change, or both


            Store at controlled room temperature 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

            Protect from freezing

            Protect from light





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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
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