oxymorphone (Rx)

Brand and Other Names:Opana
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injectable solution: Schedule II

  • 1mg/mL

tablet, immediate-release: Schedule II

  • 5mg
  • 10mg

tablet, extended-release: Schedule II

  • 5mg
  • 7.5mg
  • 10mg
  • 15mg
  • 20mg
  • 30mg
  • 40mg

reformulated extended-release tablet (Opana ER)

  • Opana ER was discontinued from market at the request of FDA owing to a significant shift in route of abuse from nasal to injection following the product’s reformulation Injection abuse of reformulated
  • Opana ER has been associated with a serious outbreak of HIV, hepatitis C, and thrombotic microangiopathy
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Parenteral Administration for Anesthesia/Analgesia/Dyspnea

Injection is indicated for management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate

It is also indicated for preoperative medication, for support of anesthesia, for obstetrical analgesia, and for relief of anxiety in patients with dyspnea associated with pulmonary edema secondary to acute left ventricular dysfunction

Initial dose

  • IM/SC: 1-1.5 mg IM/SC q4-6hr PRN
  • IV: 0.5 mg; in non-debilitated patients the dose can be cautiously increased PRN
  • Analgesia during labor: 0.5-1 mg IM

Moderate-to-Severe Pain

Acute pain

  • Immediate-release tablets are indicated for acute moderate-to-severe pain where pain is severe enough to require an opioid analgesic and for which alternative therapies are inadequate
  • Opioid-naive patients (immediate-release): 10-20 mg PO q4-6 hr PRN initially, then titrated as warranted (may start with 5-mg increments)
  • Conversion from IV oxymorphone to PO: The absolute bioavailability of PO is ~10%, therefore conversion from 1 mg IV q4-6hr is approximately equipotent to 10 mg PO q4-6hr

Chronic Severe Pain

Extended-release oxymorphone is indicated for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate

Extended-release tablet initial dosing

  • Patients who are opioid-naive or not opioid-tolerant
    • 5 mg PO q12hr initially, then titrated in increments of 5-10 mg q12hr every 3-7 days to level that provides adequate analgesia and minimizes side effects
    • Conversion from IV oxymorphone to extended-release PO: The absolute oral bioavailability of Opana ER is ~10%, therefore convertion from 1 mg IV q6hr (4 mg/day) is equipotent to 20 mg PO q12hr (40 mg/day)

Patients who are opioid-tolerant

  • Opioid-tolerant definition: Patients who are receiving, for 1 week or longer, at least 60 mg/day PO morphine, 25 mcg/hr transdermal fentanyl, 30 mg/day PO oxycodone, 8 mg/day PO hydromorphone, 25 mg/day PO oxymorphone, or an equianalgesic dose of another opioid
  • Conversion from immediate-release to extended-release oxymorphone: Administer one-half of total immediate-release daily dose as extended-release q12hr
  • Conversion from parenteral oxymorphone to extended-release oxymorphone: The absolute bioavailability of PO is ~10%, therefore conversion from 1 mg IV is approximately equipotent to 10 mg PO
  • Conversion from other opioids: Refer to equianalgesic recommendations within the prescribing information

Dosage Modifications

Renal impairment

  • Immediate-release tablet; CrCl <50 mL/min: Initiate therapy at lowest dose (eg, 5 mg); titrate to effect slowly; monitor
  • Injection; CrCl <50 mL/min: Administer cautiously and in reduced dosage
  • Extended-release tablet
    • CrCl <50 mL/min (opioid-naïve): Initiate with 5 mg PO q12hr
    • CrCl <50 mL/min (prior opioid therapy): Initiate at 50% lower than the starting dose for a patient with normal hepatic function and titrate slowly

Hepatic impairment

  • Mild; immediate-release or injection: Initiate therapy at lowest dose; titrate to effect slowly; monitor
  • Moderate to severe: Contraindicated
  • Extended-release
    • Mild (opioid-naïve): Initiate with 5 mg PO q12hr
    • Mild (prior opioid therapy): Initiate at 50% lower than the starting dose for a patient with normal hepatic function and titrate slowly
    • Moderate or severe: Contraindicated

Dosing Considerations

Extended-release tablets

  • Because of risks of addiction, abuse, and misuse with opioids, even at recommended doses, and because the greater risks of overdose and death with extended-release formulations, reserve for use in patients for whom alternative treatment options (eg, nonopioid analgesics or immediate-release opioids) are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient pain management
  • Extended-release formulations are not indicated as an as-needed (prn) analgesic

Safety and efficacy not established

Steady-state plasma concentrations are ~40% higher in elderly individuals

Initiate with lowest dose; consider less frequent dosing

Carefully monitor for respiratory or CNS depression

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Interactions

Interaction Checker

and oxymorphone

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Dizziness (7-18%)

            Headache (7-12%)

            Fever (1-14%)

            Somnolence (9-19%)

            Pruritus (8-15%)

            Nausea (19-33%)

            Vomiting (9-16%)

            Constipation (4-28%)

            Agitation 

            Angina pectoris

            Anticholinergic effects (dry mouth, palpitation, tachycardia) 

            Bradycardia 

            Cardiac arrest 

            Coma 

            Constipation 

            1-10%

            Hypotension (<10%)

            Flushing (<10%)

            Hypertension (<10%)

            Edema (<10%)

            Sedation (1-10%)

            Nervousness (<10%)

            Insomnia (<4%)

            Confusion (3%)

            Depression (<10%)

            Disorientation (<10%)

            Lethargy (<10%)

            Dehydration (<10%)

            Flatulence (1-10%)

            Dyspepsia (<10%)

            Diarrhea (<4%)

            Decreased appetite (<3%)

            Hypoxia (<10%)

            Dyspnea (<10%)

            Diaphoresis (1-10%)

            <1%

            Agitation

            Dermatitis

            Bronchospasm

            Miosis

            Oliguria

            Bradycardia

            Apnea

            M:icturition difficulty

            Palpitation

            Euphoric mood

            Urethral spasm

            Urinary retention

            Physical and psychological dependence

            Hot flashes

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            Warnings

            Black Box Warnings

            Opioid analgesic risk evaluation and mitigation strategy (REMS)

            • To ensure that benefits of opioid analgesics outweigh risks of addiction, abuse, and misuse, the Food and Drug Administration (FDA) has required a REMS for these products; under requirements of the REMS, drug companies with approved opioid analgesic products must make REMS-compliant education programs available to healthcare providers
            • Healthcare providers are strongly encouraged to
              • Complete a REMS-compliant education program
              • Counsel patients and/or their caregivers, with every prescription, on safe use, serious risks, storage, and disposal of these products
              • Emphasize to patients and their caregivers the importance of reading the Medication Guide every time it is provided by their pharmacist
              • Consider other tools to improve patient, household, and community safety

            Addiction, abuse, and misuse

            • Risk of opioid addiction, abuse, and misuse, which can lead to overdose and death
            • Assess each patient’s risk prior to prescribing and monitor all patients regularly for the 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 a dose increase
            • Instruct patients to swallow tablet/capsule whole; crushing, chewing, or dissolving can cause rapid release and absorption of a potentially fatal dose

            Accidental exposure

            • Accidental of even 1 dose, especially by children, can result in a fatal overdose

            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 is required for a prolonged period in a pregnant woman, advise the patient of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available

            Interaction with central nervous system (CNS) depressants

            • Coadministration with benzodiazepines or other CNS depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death
            • Reserve concomitant prescribing for use in patients for whom alternative treatment options are inadequate; limit dosages and durations to the minimum required; and follow patients for signs and symptoms of respiratory depression and sedation
            • Instruct patients not to consume alcoholic beverages or use alcohol-containing drug products while taking morphine due to risk of additive sedation and respiratory depression
            • Coingestion of alcohol may cause rapid release of opioid content from long-acting tablet/capsule and result in increased plasma levels and a potentially fatal overdose

            Contraindications

            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

            Hypersensitivity

            Moderate-to-severe hepatic impairment

            Cautions

            Use caution in patients with acute pancreatitis, Addison disease, benign prostatic hyperplasia, cardiac arrhythmias, central nervous system (CNS) depression, drug abuse or dependence, emotional lability, gallbladder disease, gastrointestinal (GI) disorder, pseudomembranous colitis, GI surgery, head injury, hypothyroidism or untreated myxedema, intracranial hypertension, brain tumor, toxic psychosis, urethral stricture, urinary tract surgery, seizures, acute alcoholism, delirium tremens, shock, cor pulmonale, chronic pulmonary disease, emphysema, kyphoscoliosis, severe obesity, renal or hepatic impairment, elderly or debilitated patients

            Thrombocytopenia purpura resulting in kidney failure or death has been reported when extended-release tablets are dissolved and injected IV

            May obscure diagnosis of abdominal conditions

            Cases of serotonin syndrome, a potentially life-threatening condition, reported with concomitant use of serotonergic drugs; this may occur within the recommended dosage range; the onset of symptoms generally occur within several hours to a few days of concomitant use, but may occur later than that; discontinue therapy immediately if serotonin syndrome is suspected

            Therapy may cause severe hypotension including orthostatic hypotension and syncope in ambulatory patients; there is increased risk in patients whose ability to maintain blood pressure has already been compromised by a reduced blood volume or concurrent administration of certain CNS depressant drugs (e.g., phenothiazines or general anesthetics); monitor patients for signs of hypotension after initiating or titrating dosage; in patients with circulatory shock, therapy may cause vasodilation that can further reduce cardiac output and blood pressure; avoid therapy in patients with circulatory shock

            In patients who may be susceptible to intracranial effects of CO2 retention (e.g., those with evidence of increased intracranial pressure or brain tumors), therapy may reduce respiratory drive, and resultant CO2 retention can further increase intracranial pressure; monitor such patients for signs of sedation and respiratory depression, particularly when initiating therapy; opioids may obscure clinical course in a patient with a head injury; avoid the use in patients with impaired consciousness or coma

            Contraindicated in patients with known or suspected gastrointestinal obstruction, including paralytic ileus; may cause spasm of sphincter of Oddi; opioids may cause increases in serum amylase; monitor patients with biliary tract disease, including acute pancreatitis, for worsening symptoms

            Therapy may increase frequency of seizures in patients with seizure disorders and in other clinical settings associated with seizures; monitor patients for worsened seizure control during therapy

            Avoid use of mixed agonist/antagonist (e.g., pentazocine, nalbuphine, and butorphanol) or partial agonist (e.g., buprenorphine) analgesics in patients who are receiving a full opioid agonist analgesic; mixed agonist/antagonist and partial agonist analgesics may reduce analgesic effect and/or precipitate withdrawal symptoms; when discontinuing therapy in physically-dependent patient, gradually taper dosage; do not abruptly discontinue therapy in these patients

            Warn patients not to drive or operate dangerous machinery unless they are tolerant to effects of drug and know how they will react to medication

            While serious, life-threatening, or fatal respiratory depression can occur at any time during therapy, risk is greatest during initiation of therapy or following dosage increase; monitor patients closely for respiratory depression, especially within first 24 to 72 hr of initiating therapy with and following dosage increases; accidental ingestion of even one dose, especially by children, can result in respiratory depression and death due to overdose of opioid

            Profound sedation, respiratory depression, coma, and death may result from concomitant administration with benzodiazepines or other CNS depressants (e.g., non-benzodiazepine sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, other opioids, alcohol); because of these risks, reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate

            Use in patients with acute or severe bronchial asthma in an unmonitored setting or in absence of resuscitative equipment is contraindicated; patients with significant chronic obstructive pulmonary disease or cor pulmonale, and with substantially decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression are at increased risk of decreased respiratory drive including apnea, even at recommended dosages

            Life-threatening respiratory depression is more likely to occur in elderly, cachectic, or debilitated patients because they may have altered pharmacokinetics or altered clearance compared to younger, healthier patients; monitor closely

            Monoamine oxidase inhibitors (MAOIs) may potentiate effects of opioid, opioid’s active metabolite, including respiratory depression, coma, and confusion; therapy should not be administered within 14 days of initiating or stopping MAOIs

            Cases of adrenal insufficiency reported with opioid use, more often following greater than one 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 of 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

            Use caution when selecting dosage for an elderly patient, usually starting at low end of dosing range, reflecting greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy; because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and may be useful to monitor renal function

            Opioid pharmacokinetics may be altered in patients with renal failure; clearance may be decreased and metabolites may accumulate much higher plasma levels in patients with renal failure as compared to patients with normal renal function; start with a lower than normal dosage or with longer dosing intervals and titrate slowly while monitoring for signs of respiratory depression, sedation, and hypotension

            Schedule II opioid analgesics expose users to the risks of addiction, abuse, and misuse; there is a greater risk for overdose and death with extended-release opioids due to the larger amount of active opioid present (see Black Box Warnings)

            Addiction, abuse, and misuse risks are increased in patients with a personal or family history of substance abuse or mental illness (eg, major depression); the potential for these risks should not, however, prevent the prescribing of proper pain management in any given patient; intensive monitoring is necessary (see Black Box Warnings)

            Opioid analgesic risk evaluation and mitigation strategy (REMS)

            • To ensure that benefits of opioid analgesics outweigh risks of addiction, abuse, and misuse, the Food and Drug Administration (FDA) has required a Risk Evaluation and Mitigation Strategy (REMS) for these products
            • Discuss the safe use, serious risks, and proper storage and disposal of opioid analgesics with patients and/or their caregivers every time these medicines are prescribed; use the following link to obtain the Patient Counseling Guide (PCG): www.fda.gov/OpioidAnalgesicREMSPCG
            • Emphasize to patients and their caregivers the importance of reading the Medication Guide that they will receive from their pharmacist every time an opioid analgesic is dispensed to them
            • Consider using other tools to improve patient, household, and community safety, such as patient-prescriber agreements that reinforce patient-prescriber responsibilities
            • To obtain further information on opioid analgesic REMS and for a list of accredited REMS CME/CE, call 1-800-503-0784, or log on to www.opioidanalgesicrems.com; the FDA Blueprint can be found at www.fda.gov/OpioidAnalgesicREMSBlueprint
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            Pregnancy & Lactation

            Pregnancy

            Prolonged use of opioid analgesics during pregnancy can cause neonatal opioid withdrawal syndrome; there are no available data in pregnant women to inform a drug associated risk for major birth defects and miscarriage; published studies with morphine use during pregnancy have not reported a clear association with morphine and major birth defects

            Prolonged use of opioid analgesics during pregnancy for medical or nonmedical purposes can result in physical dependence in the neonate and neonatal opioid withdrawal syndrome shortly after birth; the onset, duration, and severity of neonatal opioid withdrawal syndrome vary based on specific opioid used, duration of use, timing and amount of last maternal use, and rate of elimination of drug by newborn; observe newborns for symptoms of neonatal opioid withdrawal syndrome and manage accordingly

            Observe newborns for symptoms of neonatal opioid withdrawal syndrome (eg, poor feeding, diarrhea, irritability, tremor, rigidity, and seizures), and manage accordingly

            Labor or delivery

            • Opioids cross placenta and may produce respiratory depression and psycho-physiologic effects in neonates; an opioid antagonist, such as naloxone, must be available for reversal of opioid induced respiratory depression in neonate; drug is not recommended for use in women during and immediately prior to labor, when use of shorter-acting analgesics or other analgesic techniques are more appropriate; opioid analgesics can prolong labor through actions that temporarily reduce strength, duration, and frequency of uterine contractions; however, this effect is not consistent and may be offset by an increased rate of cervical dilatation, which tends to shorten labor; monitor neonates exposed to opioid analgesics during labor for signs of excess sedation and respiratory depression

            Infertility

            • Due to effects of androgen deficiency, chronic use of opioids may cause reduced fertility in females and males of reproductive potential; it is not known whether effects on fertility are reversible

            Lactation

            Unknown if excreted in breast milk; many drugs, including some opioids, are excreted in human milk

            If opioid must be used; monitor infant closely for excess sedation and respiratory depression; withdrawal symptoms can occur when breastfeeding or maternal opioid 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.

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            Pharmacology

            Mechanism of Action

            Opioid agonist; inhibits ascending pain pathways, thus altering response to pain; produces analgesia, respiratory depression, and sedation  

            Absorption

            Bioavailability: 10% (PO)

            Onset: 5-10 min

            Duration: 3-6 hr

            Distribution

            Protein bound: 10-12%

            Vd: IV, 1.94-4.22 L/kg

            Metabolism

            Metabolized in liver via conjugation

            Elimination

            Half-life: Immediate release, 7-9 hr; extended release, 9-11 hr

            Excretion: Urine, feces

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            Administration

            Oral Administration

            Take on empty stomach, at least 1 hr before or 2 hr after eating

            Do not stop abruptly if opioid tolerant; taper gradually to stop treatment

            Extended-release tablets

            • Swallow tablet whole; do not crush, chew, or dissolve
            • Altering tablet (ie, crushing, chewing, or dissolving) will result in uncontrolled delivery of oxymorphone and can lead to overdose or death
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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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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            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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