Oliceridine

Oliceridine is a prescription medication used to manage acute pain severe enough to require an intravenous opioid analgesic and for whom alternative treatments are inadequate.

• Oliceridine is available under the following different brand names: Olinvyk

Common side effects of Oliceridine include:

• nausea
• vomiting
• dizziness
• headache
• constipation
• itching
• low blood oxygen (hypoxia)

Serious side effects of Oliceridine include:

• seizures
• agitation 
• hallucinations (seeing things or hearing voices that do not exist) 
• fever
• sweating 
• confusion 
• fast heartbeat 
• shivering
• severe muscle stiffness or twitching 
• loss of coordination
• nausea
• vomiting, or diarrhea
• inability to get or keep an erection
• decreased sexual desire
• irregular menstruation
• rash
• hives
• swelling of the eyes, face, lips, tongue, mouth, or throat
• difficulty breathing or swallowing
• fainting

Rare side effects of Oliceridine include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, light-headedness, or passing out

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Injection, solution: Schedule II

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

Acute pain

Adult dosage

• Use the lowest effect dose for the shortest duration consistent with individual patient treatment goals
• Initial: 1.5 mg/dose IV
• 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 above 3 mg were not evaluated
• Not to exceed the cumulative dose of 27 mg/day; dose more than 27 mg/day may increase the risk for QTc prolongation
• If a 27-mg cumulative daily dose is reached and analgesia is still required, administer an alternative analgesic regimen until oliceridine can be resumed the next day
• Safety beyond 48-hour 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 Considerations – Should be Given as Follows:

• See "Dosages"

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Oliceridine has severe interactions with no other drugs.
• Oliceridine has serious interactions with the following drugs:
  • belladonna and opium
  • benzhydrocodone/acetaminophen
  • bremelanotide
  • buprenorphine
  • buprenorphine buccal
  • buprenorphine subdermal implant
  • buprenorphine transdermal
  • buprenorphine, long-acting injection
  • butorphanol
  • diazepam intranasal
  • fexinidazole
  • nalbuphine
  • olopatadine intranasal
  • ozanimod
  • pentazocine
  • selinexor
  • sufentanil SL
• Oliceridine has moderate interactions with at least 302 other drugs.
• Oliceridine has minor interactions with the following drug:
  • haloperidol

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Significant respiratory depression
• Acute or severe bronchial asthma in an unmonitored setting or the absence of resuscitative equipment
• Known or suspected gastrointestinal (GI) obstruction, including paralytic ileus
• Known hypersensitivity (eg, anaphylaxis)

Effects of drug abuse

• Overdose
• Death

Short-Term Effects

• See “What Are Side Effects Associated with Using Oliceridine?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Oliceridine?”

Cautions

• Opioids expose users to risks for addiction, abuse, and misuse; assess patient risk; risks for 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 was 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 a 27-mg cumulative daily dose is 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 above 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 intracranial pressure, brain tumors, head injury, impaired consciousness, coma); oliceridine may reduce respiratory drive
• May increase seizure frequency in patients with seizure disorders or other clinical settings associated with seizures
• Do not abruptly discontinue in a 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 spasms 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 the efficacy of diuretics by inducing the release of antidiuretic hormone
  • Anticholinergic drugs may increase the risk for 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 the neuromuscular blocking action of skeletal muscle relaxants and produce increased respiratory depression
  • Benzodiazepines or other central nervous system (CNS) depressants
  • Additive pharmacologic effect; increases the risk for hypotension, respiratory depression, profound sedation, coma, and death
  • Reserve coadministration for patients for whose alternative treatment options are inadequate; limit dosages and durations to the minimum required
  • If the decision is made to prescribe a benzodiazepine or other CNS depressant concomitantly with an opioid analgesic, prescribe the lowest effective dosages and minimum duration of concomitant use
  • If an opioid analgesic is initiated in a patient already taking a benzodiazepine or other CNS depressant, prescribe a lower initial dose of opioid analgesic, and titrate based on clinical response
  • Coadministration with benzodiazepines or other CNS depressants (including alcohol) increases the risk for 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 the 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 the 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 and Lactation

• Prolonged use of opioid analgesics during pregnancy may result in neonatal opioid withdrawal syndrome
• Clinical considerations
  • Opioids cross the placenta and may produce respiratory depression and psychophysiological effects in neonates
  • Not recommended for use in pregnant women during and immediately before labor, when other analgesic techniques are more appropriate
• Infertility
  • Long-term opioid use may cause reduced fertility in women and males of reproductive potential
  • Unknown whether these effects on fertility are reversible
• Lactation
  • 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