Oxymorphone

Oxymorphone is a narcotic pain reliever used to treat moderate to severe pain. The extended-release form is for around-the-clock treatment of pain.

Oxymorphone is available under the following different brand names: Opana, and Opana ER.

Dosage Forms and Strengths

Injectable solution: Schedule II

• 1 mg/mL

Tablet: Schedule II

• 5 mg
• 10 mg

Tablet, extended release: Schedule II

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

Tablet, extended release: abuse deterrent Schedule II

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

Dosage Considerations – Should be Given as Follows:

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

Preoperative Anesthesia/Analgesia

Also effective for relief of anxiety in patients with shortness of breath (dyspnea) associated with pulmonary edema secondary to acute left ventricular dysfunction

• 1-1.5 mg intramuscularly/subcutaneously (IM/SC) every 4-6 hours as needed
• Analgesia during labor: 0.5-1 mg IM
• Intravenously (IV): 0.5 mg, increased as needed

Moderate-to-Severe Pain

Acute

• Immediate-release tablets indicated for acute moderate-to-severe pain where opioid use is appropriate
• Opioid-naive patients (immediate-release): 10-20 mg orally every 4-6 hours as needed initially, then titrated as warranted (may start with 5-mg increments)
• Conversion from intravenous (IV) oxymorphone to oral: The absolute bioavailability of orally is approximately 10%, therefore conversion from 1 mg IV every 4-6 hours is equipotent to 10 mg orally every 4-6 hours
• Elderly patients or those with renal or hepatic impairment: 5 mg orally every 4-6 hours initially

Chronic Severe Pain

Extended-release 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

Opioid-naive patients (extended-release): 5 mg orally every 12 hours initially, then titrated in increments of 5-10 mg every 12 hours every 3-7 days to level that provides adequate analgesia and minimizes side effects

Conversion from intravenous (IV) oxymorphone to extended-release oral: The absolute oral bioavailability of Opana ER is approximately 10%, therefore conversion from 1 mg IV every 6 hours (4 mg/day) is equipotent to 20 mg orally every 12 hours (40 mg/day)

Conversion from orally opioids to Opana ER: See prescribing information

Opioid-tolerant definition

• Use of higher starting doses in patients who are not opioid tolerant may cause fatal respiratory depression
• Patients who are opioid tolerant are those receiving, for 1 week or longer, at least 60 mg/day orally morphine, 25 mcg/hour transdermal fentanyl, 30 mg/day orally oxycodone, 8 mg/day orally hydromorphone, 25 mg/day orally oxymorphone, or an equianalgesic dose of another opioid

Dosing limitations

• Because of the risks of addiction, abuse, and misuse with opioids, even at recommended doses, and because of the greater risks of overdose and death with extended-release opioid formulations, reserve for patients whom alternative treatment options (e.g., non-opioid analgesics or immediate-release opioids) are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain
• Not indicated as a as needed analgesic

Bipolar Mania

Renal Impairment

• CrCl less than 50 mL/min: Initiate therapy at lowest dose; titrate to effect slowly; monitor

Hepatic impairment

• Mild: Initiate therapy at lowest dose; titrate to effect slowly; monitor
• Moderate to severe: Do not administer

Administration

• Do not stop abruptly; taper gradually to stop treatment
• Extended-release tablets must be taken on empty stomach (i.e., at least 1 hour before or 2 hours after eating)
• Opana ER tablets are designed to be crush-resistant; must not be broken, chewed, dissolved, or crushed; too-rapid release and absorption may potentially cause fatal overdose
• Not recommended for pediatric use.

Common side effects of oxymorphone include:

• Dizziness
• Headache
• Fever
• Drowsiness
• Itching
• Nausea
• Vomiting
• Constipation
• Agitation
• Chest pain (angina)
• Anticholinergic effects (dry mouth, palpitations, fast heart rate)
• Slow heart rate
• Cardiac arrest
• Coma
• Low blood pressure (hypotension)
• Flushing
• High blood pressure (hypertension)
• Swelling (edema)
• Sedation
• Nervousness
• Insomnia
• Confusion
• Depression
• Disorientation
• Lethargy
• Dehydration
• Gas (flatulence)
• Indigestion
• Diarrhea
• Decreased appetite
• Low blood oxygen levels
• Shortness of breath
• Increased sweating
• Lightheadedness
• Rash

Less common side effects of oxymorphone include:

• Agitation
• Dermatitis
• Bronchospasm
• Constricted pupils
• Temporary suspension of breathing, often while sleeping
• Urinary hesitancy
• Urinary retention
• Euphoric mood
• Urethral spasm
• Physical and psychological dependence
• Hot flashes

Serious side effects of oxymorphone include:

• Mental/mood changes
• Severe stomach or abdominal pain
• Changes in the amount of urine
• Vision changes
• Slow or fast heartbeat
• Difficulty urinating

This is not a complete list of side effects and other serious side effects may occur. Call your doctor for information and medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

If your doctor has directed you to use this medication for your condition, your doctor or pharmacist may already be aware of any possible drug interactions or side effects and may be monitoring you for them. Do not start, stop, or change the dosage of this medicine or any medicine before getting further information from your doctor, healthcare provider or pharmacist first.

Severe interactions of oxymorphone include:

• alvimopan

Oxymorphone has serious interactions with at least 28 different drugs.

Oxymorphone has moderate interactions with at least 210 different drugs.

Mild interactions of oxymorphone include:

• brimonidine
• dextroamphetamine
• eucalyptus
• lidocaine
• naloxone
• sage
• ziconotide

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Warnings

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 ingestion 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 varies 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 alcohol:

• Instruct patients not to consume alcoholic beverages or use prescription or nonprescription products that contain alcohol
• Co-ingestion 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

This medication contains oxymorphone. Do not take Opana or Opana ER if you are allergic to oxymorphone or any ingredients contained in this drug.

This medication contains oxymorphone. Do not take Risperdal, Risperdal Consta, or Risperdal M-Tab if you are allergic to oxymorphone or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Hypersensitivity
• Non-opioid-tolerant patient
• Paralytic ileus, toxin-mediated diarrhea
• Respiratory depression, acute or severe bronchial asthma, hypercapnia, upper airway obstruction
• Treatment of pulmonary edema secondary to chemical respiratory irritant
• Moderate-to-severe hepatic impairment (oral)

Effects of Drug Abuse

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

Short-Term Effects

• See "What Are Side Effects Associated with Using Oxymorphone?"

Long-Term Effects

• Prolactin elevations occur and persist during chronic administration.
• See "What Are Side Effects Associated with Using Oxymorphone?"

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.
• Avoid alcohol.
• Reduce dosage if drug is coadministered with other central nervous system (CNS) depressants.
• Thrombocytopenia purpura resulting in kidney failure or death has been reported when extended-release tablets are dissolved and injected intravenously (IV).
• May obscure diagnosis of abdominal conditions.
• Long-acting opioids:
  • 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 Warnings)
  • Addiction, abuse, and misuse risks are increased in patients with a personal or family history of substance abuse or mental illness (e.g. 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 Warnings)
  • Serious, life-threatening, or fatal respiratory depression reported (see Warnings)
  • Accidental exposure reported, including fatalities (see Warnings)
  • Neonatal opioid withdrawal syndrome reported with long-term use during pregnancy (see Warnings)
  • Interactions with central nervous system (CNS) depressants (e.g., alcohol, sedatives, anxiolytics, hypnotics, neuroleptics, other opioids) can cause additive effects and increase risk for respiratory depression, profound sedation, and hypotension
  • Life-threatening respiratory depression is more likely to occur in elderly, cachectic, or debilitated patients as they may have altered pharmacokinetics or altered clearance compared to younger, healthier patients

Pregnancy and Lactation

• Use oxymorphone with caution during pregnancy if benefits outweigh risks. Animal studies show risk and human studies are not available or neither animal nor human studies were done. Neonatal opioid withdrawal syndrome has been reported with long-term use of oxymorphone during pregnancy (see Warnings).
• It is unknown whether oxymorphone is excreted in breast milk; use caution if breastfeeding.