Drug information of Oxymorphone


Drug group:

Oxymorphone is an opioid medication used to treat moderate to severe pain.

The extended-release form of oxymorphone is for around-the-clock treatment of pain and should not be used on an as-needed basis for pain.

Mechanism of effect

Oxymorphone is a potent opioid analgesic with uses similar to those of morphine. The drug is a semisynthetic derivative of morphine (phenanthrene derivative) and is closely related to hydromorphone chemically (Dilaudid).

Oxymorphone interacts predominantly with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and certain cortical areas. They are also found on the terminal axons of primary afferents within laminae I and II (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve. Also, it has been shown that oxymorphone binds to and inhibits GABA inhibitory interneurons via mu-receptors. These interneurons normally inhibit the descending pain inhibition pathway. So, without the inhibitory signals, pain modulation can proceed downstream.




Vd: IV: 1.94 to 4.22 L/kg


Hepatic via glucuronidation to active and inactive metabolites


Urine (<1% as unchanged drug); feces

Onset of Action

Parenteral: 5 to 10 minutes

Duration of Action

Analgesic: Parenteral: 3 to 6 hours

Half-Life Elimination

Oral: Immediate release: 7 to 9 hours; Extended release: 9 to 11 hours

Protein Binding

10% to 12%

Drug indications

Pain management



Usual Adult Dose for Pain

The following dosing recommendations can only be considered suggested approaches to what is actually a series of clinical decisions over time; each patient should be managed individually.

Use as first Opioid Analgesic:
-Initial dose: 10 to 20 mg orally every 4 to 6 hours as needed for pain
Maximum initial dose: 20 mg

Conversion from Other Oral Opioids to Oral Oxymorphone:
-Determine equipotent dose using published potency tables; it is safest to start therapy by administering one-half the calculated total daily oxymorphone requirement in 4 to 6 equally divided oral doses every 4 to 6 hours and gradually adjust dose as needed.

-Dose conversion should be done carefully and with close monitoring due to large patient variability in regards to opioid analgesic response.
-Use the lowest effective dosage for the shortest duration consistent with individual patient treatment goals.
-Monitor closely for respiratory depression, especially within the first 24 to 72 hours of initiating therapy and with each dose increase.
-Due to risks of addiction, abuse, and misuse, even at recommended doses, reserve use for patients for whom alternative treatment options (e.g., non-opioid analgesics or opioid combination products) have not been tolerated, or are not expected to be tolerated, or have not provided adequate analgesia, or are not expected to provide adequate analgesia.

Use: For the management of acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate.

Usual Adult Dose for Chronic Pain

The following dosing recommendations can only be considered suggested approaches to what is actually a series of clinical decisions over time; each patient should be managed individually.

Use as the First Opioid Analgesic or for those who are NOT Opioid Tolerant:
Initial dose: Extended-release tablets: 5 mg orally every 12 hours

Immediate-Release Oxymorphone to Extended-Release Oxymorphone Tablets: Administer same total daily dose
-Initial dose: One-half total daily immediate-release requirement as extended-release tablet orally every 12 hours


Maintenance Dose: Individually titrate to a dose that provides adequate analgesia and minimizes adverse reactions; dose adjustments may be made in 5 to 10 mg increments every 12 hours, every 3 to 7 days.

Breakthrough Pain: If the level of pain increases after dose stabilization, attempt to identify the source before increasing dose; rescue medication with appropriate immediate-release analgesia may be helpful.

Drug contraindications

Hypersensitivity (eg, anaphylaxis, angioedema) to oxymorphone or any component of the formulation; significant respiratory depression; acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment; GI obstruction, including paralytic ileus (known or suspected); moderate and severe hepatic impairment.

Side effects

Side effects requiring immediate medical attention

Along with its needed effects, oxymorphone may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking oxymorphone:

Less common

  • Blurred vision
  • confusion
  • decreased urination
  • difficult or labored breathing
  • dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
  • dry mouth
  • fast, pounding, racing, or irregular heartbeat or pulse
  • headache
  • nervousness
  • pounding in the ears
  • rapid breathing
  • sunken eyes
  • sweating
  • swelling of the hands, ankles, or feet
  • thirst
  • tightness in the chest
  • unusual tiredness or weakness
  • wrinkled skin


  • Chest pain or discomfort
  • chills
  • cold sweats
  • confusion about identity, place, and time
  • cough
  • decrease in consciousness
  • deep or fast breathing with dizziness
  • difficulty in passing urine (dribbling)
  • difficulty with sleeping
  • difficulty with swallowing
  • drowsiness to profound loss of consciousness
  • fever
  • hives, itching, or skin rash
  • hoarseness
  • irregular, slow, or shallow breathing
  • irritability
  • irritation
  • joint pain, stiffness, or swelling
  • numbness of the feet, hands, and around the mouth
  • painful urination
  • pale or blue lips, fingernails, or skin
  • puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
  • redness of the skin
  • restlessness
  • seeing, hearing, or feeling things that are not there
  • severe constipation
  • severe vomiting
  • stomach pain
  • shaking
  • trouble in holding or releasing urine
  • unusual drowsiness, dullness, or feeling of sluggishness

Incidence not known

  • Agitation
  • darkening of the skin
  • diarrhea
  • large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or genitals
  • loss of appetite
  • mental depression
  • nausea
  • overactive reflexes
  • poor coordination
  • seizures
  • shivering
  • talking or acting with excitement you cannot control
  • twitching
  • vomiting

Get emergency help immediately if any of the following symptoms of overdose occur while taking oxymorphone:

Symptoms of overdose

  • Cold and clammy skin
  • constricted, pinpoint, or small pupils (black part of the eye)
  • decreased awareness or responsiveness
  • difficult or troubled breathing
  • irregular, fast, slow, or shallow breathing
  • low blood pressure or pulse
  • muscle weakness
  • pale or blue lips, fingernails, or skin
  • severe sleepiness or unusual drowsiness
  • very slow breathing

Side effects not requiring immediate medical attention

Some side effects of oxymorphone may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects.

Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Difficulty having a bowel movement
  • feeling of constant movement of self or surroundings
  • relaxed and calm
  • sensation of spinning
  • sleepiness

Less common

  • Belching
  • decreased weight
  • discouragement
  • excess air or gas in the stomach or bowels
  • feeling of warmth
  • feeling sad or empty
  • full or bloated feeling
  • heartburn
  • indigestion
  • lack of appetite
  • loss of interest or pleasure
  • passing gas
  • pressure in the stomach
  • redness of the face, neck, arms, and occasionally, upper chest
  • stomach discomfort or upset
  • swelling of the abdominal or stomach area
  • tiredness
  • trouble concentrating


  • Blistering, crusting, irritation, itching, or reddening of the skin
  • cracked, dry, scaly skin
  • difficulty with thinking or concentrating
  • disturbed color perception
  • double vision
  • false or unusual sense of well-being
  • feeling jittery
  • halos around lights
  • loss of vision
  • night blindness
  • nightmares or unusually vivid dreams
  • overbright appearance of lights
  • sudden sweating
  • tunnel vision
  • welts

Incidence not known

  • Forgetfulness
  • loss of memory
  • problems with memory

heroin , morphine liposomal 


Addiction, abuse, and misuse:

Oxymorphone exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death. Assess each patient's risk prior to prescribing oxymorphone, and monitor all patients regularly for the development of these behaviors and conditions.

Opioid analgesic risk evaluation and mitigation strategy (REMS)

To ensure that the benefits of opioid analgesics outweigh the risks of addiction, abuse, and misuse, the FDA has required a REMS for these products. Under the requirements of the REMS, drug companies with approved opioid analgesic products must make REMS-compliant education programs available to health care providers. Health care providers are strongly encouraged to complete a REMS-compliant education program and 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, and consider other tools to improve patient, household, and community safety.

Life-threatening respiratory depression:

Serious, life-threatening, or fatal respiratory depression may occur with use of oxymorphone. Monitor for respiratory depression, especially during initiation of oxymorphone or following a dose increase. Instruct patients to swallow oxymorphone extended-release (ER) tablets whole; crushing, chewing, or dissolving oxymorphone ER tablets can cause rapid release and absorption of a potentially fatal dose of oxymorphone.

Accidental ingestion (oral only):

Accidental ingestion of even 1 dose of oxymorphone, especially by children, can result in a fatal overdose of oxymorphone.

Neonatal opioid withdrawal syndrome:

Prolonged use of oxymorphone 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. 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 (oral only):

Instruct patients not to consume alcoholic beverages or use prescription or nonprescription products that contain alcohol while taking oxymorphone. The coingestion of alcohol with oxymorphone may result in increased plasma levels and a potentially fatal overdose of oxymorphone

Risks from concomitant use with benzodiazepines or other CNS depressants:

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

Concerns related to adverse effects:

  • CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
  • Constipation: May cause constipation which may be problematic in patients with unstable angina and patients post-myocardial infarction. Consider preventive measures (eg, stool softener, increased fiber) to reduce the potential for constipation.


  • Hypotension: May cause severe hypotension (including orthostatic hypotension and syncope); use with caution in patients with hypovolemia, cardiovascular disease (including acute MI), or with drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics). Monitor for symptoms of hypotension following initiation or dose titration. Avoid use in patients with circulatory shock.
  • Phenanthrene hypersensitivity: Use with caution in patients with hypersensitivity reactions to other phenanthrene-derivative opioid agonists (codeine, hydrocodone, hydromorphone, levorphanol, oxycodone).
  • Respiratory depression: [US Boxed Warning]: Serious, life-threatening, or fatal respiratory depression may occur. Monitor closely for respiratory depression, especially during initiation or dose escalation. Swallow ER tablets whole; crushing, chewing, or dissolving can cause rapid release and a potentially fatal dose. Carbon dioxide retention from opioid-induced respiratory depression can exacerbate the sedating effects of opioids.
  • Thrombotic thrombocytopenic purpura (TTP): Cases of TTP resulting in kidney failure (requiring dialysis) and death have been reported as a result of misuse by drug abusers injecting the extended-release tablets intravenously. Tablets are intended for oral administration only.

Points of recommendation

MISUSE OF OPIOID MEDICINE CAN CAUSE ADDICTION, OVERDOSE, OR DEATH. Keep the medication in a place where others cannot get to it.

Taking opioid medicine during pregnancy may cause life-threatening withdrawal symptoms in the newborn.

Fatal side effects can occur if you use opioid medicine with alcohol, or with other drugs that cause drowsiness or slow your breathing.

Before taking this medicine

You should not take oxymorphone if you are allergic to oxymorphone, or if you have:

  • severe asthma or breathing problems; or
  • a blockage in your stomach or intestines.

Tell your doctor if you have ever had:

  • a head injury or seizures;
  • breathing problems, sleep apnea;
  • drug or alcohol addiction, or mental illness;
  • urination problems;
  • liver or kidney problems; or
  • problems with your gallbladder, pancreas, or thyroid.

If you use opioid medicine while you are pregnant, your baby could become dependent on the drug. This can cause life-threatening withdrawal symptoms in the baby after it is born. Babies born dependent on opioids may need medical treatment for several weeks.

Do not breast-feed while taking oxymorphone.

Overdose symptoms may include extreme drowsiness, muscle weakness, confusion, cold and clammy skin, pinpoint pupils, slow heart rate, very slow breathing, or coma.

 avoid while using oxymorphone  drink alcohol. Dangerous side effects or death could occur.

Avoid driving or hazardous activity until you know how oxymorphone will affect you. Dizziness or drowsiness can cause falls, accidents, or severe injuries.


Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect injection from light.

Pregnancy level


Benefit should outweigh risk

US FDA pregnancy category: Not assigned

Risk Summary: Based on animal data, may cause fetal harm; prolonged maternal use of opioids during pregnancy may cause neonatal opioid withdrawal syndrome.

Breast feeding warning

Benefit should outweigh risk

Excreted into human milk: Unknown
Excreted into animal milk: Data not available

-Monitor breastfed infants for excess sedation and respiratory depression; withdrawal symptoms can occur when maternal administration of this drug is stopped.
-Because of the potential for serious adverse reactions, including excess sedation and respiratory depression, breastfeeding is not recommended with use of the extended-release tablets.

Drug forms


Ask a Pharmacist

User's questions
    No comments yet.