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Generic Name: Oxymorphone Hydrochloride
Class: Opiate Agonists
VA Class: CN101
CAS Number: 357-07-3

Warning(s)

Special Alerts:

[Posted 08/31/2016]

AUDIENCE: Pharmacy, Internal Medicine, Psychiatry, Neurology, Family Practice

ISSUE: FDA review has found that the growing combined use of opioid medicines with benzodiazepines or other drugs that depress the central nervous system (CNS) has resulted in serious side effects, including slowed or difficult breathing and deaths. Opioids are used to treat pain and cough; benzodiazepines are used to treat anxiety, insomnia, and seizures. In an effort to decrease the use of opioids and benzodiazepines, or opioids and other CNS depressants, together, FDA is adding Boxed Warnings, our strongest warnings, to the drug labeling of prescription opioid pain and prescription opioid cough medicines, and benzodiazepines. See the Drug Safety Communication, available at: , for a listing of all approved prescription opioid pain and cough medicines, and benzodiazepines and other CNS depressants.

FDA conducted and reviewed several studies showing that serious risks are associated with the combined use of opioids and benzodiazepines, other drugs that depress the CNS, or alcohol (see the FDA Drug Safety Communication, available at: , for a Data Summary). Based on these data, FDA is requiring several changes to reflect these risks in the opioid and benzodiazepine labeling, and new or revised patient Medication Guides. These changes include the new Boxed Warnings and revisions to the Warnings and Precautions, Drug Interactions, and Patient Counseling Information sections of the labeling.

FDA is continuing to evaluate the evidence regarding combined use of benzodiazepines or other CNS depressants with medication-assisted therapy (MAT) drugs used to treat opioid addiction and dependence. FDA is also evaluating whether labeling changes are needed for other CNS depressants, and will update the public when more information is available.

BACKGROUND: Opioids are powerful prescription medicines that can help manage pain when other treatments and medicines cannot be taken or are not able to provide enough pain relief. Benzodiazepines are a class of medicines that are widely used to treat conditions including anxiety, insomnia, and seizures.

RECOMMENDATION: Health care professionalsshould limit prescribing opioid pain medicines with benzodiazepines or other CNS depressants only to patients for whom alternative treatment options are inadequate. If these medicines are prescribed together, limit the dosages and duration of each drug to the minimum possible while achieving the desired clinical effect. Warn patients and caregivers about the risks of slowed or difficult breathing and/or sedation, and the associated signs and symptoms. Avoid prescribing prescription opioid cough medicines for patients taking benzodiazepines or other CNS depressants, including alcohol.

Patients taking opioids with benzodiazepines, other CNS depressant medicines, or alcohol, and caregivers of these patients, should seek medical attention immediately if they or someone they are caring for experiences symptoms of unusual dizziness or lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness.

REMS:

FDA approved a REMS for oxymorphone to ensure that the benefits outweigh the risk. The REMS may apply to one or more preparations of oxymorphone and consists of the following: medication guide and elements to assure safe use. See the FDA REMS page () or the ASHP REMS Resource Center ().

Warning(s)

  • Abuse Potential
  • Schedule II controlled substance with abuse liability similar to morphine.501

  • Potential for abuse in a manner similar to other legal or illicit opiates.501 Consider abuse potential when prescribing or dispensing oxymorphone extended-release tablets in situations where the clinician or pharmacist is concerned about increased risk of misuse, abuse, or diversion.501

  • Intended Uses of Extended-release Tablets
  • Oxymorphone hydrochloride extended-release tablets are indicated for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time.501

  • Oxymorphone hydrochloride extended-release tablets are not intended for use as a prn analgesic.501

  • Overdose Risk with Improper Administration of Extended-release Tablets
  • Oxymorphone hydrochloride extended-release tablets are to be swallowed whole and are not to be broken, chewed, dissolved, or crushed.501

  • Chewing, crushing, or dissolving the extended-release tablets could result in rapid release and absorption of a potentially fatal dose of oxymorphone.501

  • Do not consume alcoholic beverages or prescription or nonprescription preparations containing alcohol during therapy with extended-release tablets.501 Consuming alcohol while receiving extended-release tablets could result in increased plasma concentrations of oxymorphone and a potentially fatal dose of the drug.501

Introduction

Opiate agonist; phenanthrene derivative.500 501 502 a e

Uses for Opana

Acute and Chronic Pain

Relief of moderate to severe pain.500 501 502

Symptomatic relief of moderate to moderately severe pain such as that associated with acute and some chronic medical disorders including renal or biliary colic, acute trauma, postoperative pain, and cancer.e

In the management of chronic pain associated with a terminal illness such as cancer, the principal goal of analgesic therapy is to make the patient relatively pain-free while maintaining as good a quality of life as possible.e

Analgesic therapy must be individualized and titrated according to patient response and tolerance.500 501 502 e

Extended-release tablets (Opana ER) are used orally for management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time.501 The extended-release tablets are not intended for use on an as-needed (“prn”) basis, for preoperative administration to control postoperative pain, for pain in the immediate postoperative period (12–24 hours after surgery) in patients not previously exposed to opiates, or for postoperative pain that is expected to be mild or of short duration.501 Patients who were receiving this preparation prior to surgery may reinitiate such use after they are able to resume oral therapy.501 Extended-release tablets may be used postoperatively if pain is expected to be moderate to severe and persist for an extended period of time.501

Surgery

Used parenterally as a supplement to anesthesia.502 a

Analgesia During Labor

Used parenterally for analgesia during labor.502

Acute Pulmonary Edema

Used in patients with acute pulmonary edema for its cardiovascular effects and to allay anxiety.502 a e Should not be used in the treatment of pulmonary edema resulting from a chemical respiratory irritant.502

Opana Dosage and Administration

Administration

Administer orally,500 501 or by sub-Q, IM, or IV injection.502 a

Oral Administration

Administer orally as conventional tablets or extended-release tablets.500 501

Administer conventional and extended-release tablets on an empty stomach, at least 1 hour before or 2 hours after food.500 501 Food affects oral absorption.500 501 (See Food under Pharmacokinetics.)

Extended-release tablets: Swallow tablets whole; do not divide, crush, or chew.501 Do not administer with alcohol.501 (See Boxed Warning.)

IV Administration

Administer by direct IV injection.e

When administered IV, an opiate antagonist and facilities for administration of oxygen and control of respiration should be available.a e

Dosage

Available as oxymorphone hydrochloride; dosage expressed in terms of the salt.500 501

Give the smallest effective dose as infrequently as possible to minimize the development of tolerance and physical dependence.a

Individualize dosage according to clinical status of the patient, desired therapeutic effect, degree of existing opiate tolerance, and age and weight; assess dosage at periodic intervals.500 501 502

Reduce dosage in poor-risk patients, in geriatric patients, and in patients receiving other CNS depressants.a (See Specific Drugs under Interactions)

Avoid abrupt withdrawal from relatively high dosages (e.g., in chronic pain patients) since precipitation of severe abstinence syndrome is likely.500 501 502

Extended-release tablets usually are administered twice daily in 2 equally divided doses; an asymmetric daily dosing regimen (i.e., different dose in the morning than in the evening) may be appropriate in some patients, depending on the pain pattern.501

Adults

Pain (Oral Treatment)
Conventional Tablets
Oral

Opiate-naive patients: Usually, initiate with 10–20 mg every 4–6 hours as needed.500 Alternatively, use 5 mg every 4–6 hours.500 Do not initiate with doses >20 mg.500 Adjust according to response and tolerance.500

Switching from Parenteral Oxymorphone to Conventional Tablets
Oral

Calculate the total daily dosage of the parenteral preparation, multiply by a factor of 10 and administer as conventional tablets in 4 or 6 equally divided doses.500 For example, 10 mg of oral oxymorphone hydrochloride given every 6 hours as conventional tablets can be substituted for a total daily IM oxymorphone hydrochloride dosage of 4 mg.500

Extended-release Tablets
Oral

Opiate-naive patients: Initiate with 5 mg every 12 hours.501 Adjust according to response and tolerance.501 Titrate in increments of 5–10 mg every 12 hours every 3–7 days to provide adequate analgesia.501

Switching from Conventional Oxymorphone Tablets to Extended-release Tablets
Oral

Calculate the total daily dosage of the conventional preparation and give as extended-release tablets in 2 divided doses at 12-hour intervals.501

Switching from Parenteral Oxymorphone to Extended-release Tablets
Oral

Calculate the total daily dosage of the parenteral preparation, multiply by a factor of 10 and administer as extended-release tablets in 2 equally divided doses.501 For example, 20 mg of oral oxymorphone hydrochloride given every 12 hours as extended-release tablets can be substituted for a total daily IM oxymorphone hydrochloride dosage of 4 mg.501

Monitor closely to ensure adequate analgesia and to minimize side effects.501

Switching from Other Oral Opiates to Extended-release Tablets
Oral

The equivalent total daily dosage of oxymorphone hydrochloride should be calculated based on standard conversion factors suggested by the manufacturer (table below); initiate therapy with oxymorphone hydrochloride extended-release tablets by administering half the calculated dose in 2 divided doses at 12-hour intervals.501 Titrate dosage to provide adequate analgesia.501

If patients are on a regimen of several opiates, calculate the approximate oral oxymorphone dose for each opiate and add the totals to estimate the total daily oxymorphone hydrochloride dosage.501

Converting Daily Opiate Dosages to Oxymorphone Hydrochloride Extended-release Tablets (mg/day prior opiate × factor = approximate mg/day oral oxymorphone hydrochloride)501

Prior Opiate

Approximate Oral Equivalent Dose

Factor Oral

Oxymorphone

10 mg

1

Hydrocodone

20 mg

0.5

Oxycodone

20 mg

0.5

Methadone

20 mg

0.5

Morphine

30 mg

0.333

Table to be used only for conversion to oxymorphone extended-release tablets.501

Refer to published relative potency information, keeping in mind that conversion ratios are only approximate.501

When converting from methadone to oxymorphone, monitor patients closely.501

Pain (Parenteral Routes)
IV

Initially, 0.5 mg.502 Adjust according to response and tolerance.502

Sub-Q or IM

1–1.5 mg every 4 to 6 hours as necessary.502

Analgesia During Labor
IM

0.5–1 mg.502

Prescribing Limits

Adults

Oral

Conventional tablet: Maximum initial dose is 20 mg.500

Special Populations

Hepatic Impairment

In patients with mild hepatic impairment, initiate with lowest dosage and increase dose slowly.500 501 502 (See Contraindications.)

Renal Impairment

In patients with Clcr <50 mL/minute, reduce dosage.500 501 502 (See Special Populations under Pharmacokinetics.)

Geriatric Patients

Select dosage with caution; use lower than usual initial dosages.500 501 502 (See Geriatric Use under Cautions and see Special Populations under Pharmacokinetics.)

Cautions for Opana

Contraindications

  • Known hypersensitivity to oxymorphone, morphine analogs such as codeine, or any ingredient in the formulation.500 501 502

  • Respiratory depression in the absence of resuscitative equipment.500 501 502

  • Acute or severe asthma or hypercarbia.500 501 502

  • Known or suspected paralytic ileus.500 501 502

  • Moderate or severe hepatic impairment.500 501 502

  • Extended-release preparation contraindicated in the management of immediate postoperative pain (first 12–24 hours following surgery), in patients with mild pain, and in those who are expected to require analgesia for a short period of time.501

  • Parenteral use contraindicated in the treatment of pulmonary edema resulting from a chemical respiratory irritant.502

Warnings/Precautions

Warnings

Dependence and Abuse

Possible tolerance, psychologic dependence, and physical dependence following prolonged administration.500 501 Use only with careful surveillance in patients with a history of drug or alcohol dependence or abuse.500 501 Clinicians should consider abuse potential when prescribing or dispensing oxymorphone in situations where they are concerned about an increased risk of misuse, abuse, or diversion.502 However, concerns about abuse, addiction, and diversion should not prevent the proper management of pain.501 502

Oxymorphone tablets can be abused by crushing, chewing, “snorting” the powder, or dissolving the contents in water and injecting.501 502

Breaking, chewing, or crushing of extended-release tablets results in immediate release of the opiate and the risk of a potentially fatal overdose.501 (See Boxed Warning.)

Abrupt cessation of therapy or sudden reduction in dosage after prolonged use may result in withdrawal symptoms.500 501 502 After prolonged exposure to opiate analgesics, if withdrawal is necessary, it must be undertaken gradually.500 501 502

Health-care professionals should contact the professional licensing board or controlled substance authority in their states for information about prevention and detection of abuse or diversion.501 502

Respiratory Depression

The major toxicity associated with oxymorphone.501 502 e

Occurs most frequently in geriatric or debilitated patients and in those with conditions accompanied by hypoxia or hypercapnia when even moderate therapeutic opiate dosages may dangerously decrease pulmonary ventilation.501 502 e

Use with extreme caution in patients with hypoxia, hypercapnia, or substantially decreased respiratory reserve (e.g., asthma, COPD, cor pulmonale, severe obesity, sleep apnea syndrome, myxedema, kyphoscoliosis, CNS depression, coma).501 502 e In such patients, even therapeutic oxymorphone doses may decrease respiratory drive while simultaneously increasing airway resistance to the point of apnea.501 502 e Consider use of non-opiate analgesics.501 502 e Use oxymorphone only with careful medical supervision and at lowest effective dosage.501 502 e

Interactions with Other CNS Depressants

Additive depressant effects may occur with concomitant use of other CNS depressants including other opiates, sedatives or hypnotics, general anesthetics, phenothiazines, tranquilizers, illicit drugs associated with CNS depression, and alcohol.501 502 e (See Specific Drugs under Interactions.)

Hypoventilation, hypotension, and profound sedation or coma may occur.501 502 e

Adrenal Insufficiency

Adrenal insufficiency reported in patients receiving opiate agonists or opiate partial agonists.400 Manifestations are nonspecific and may include nausea, vomiting, anorexia, fatigue, weakness, dizziness, and hypotension.400

If adrenal insufficiency is suspected, perform appropriate laboratory testing promptly and provide physiologic (replacement) dosages of corticosteroids; taper and discontinue the opiate agonist or partial agonist to allow recovery of adrenal function.400 If the opiate agonist or partial agonist can be discontinued, perform follow-up assessment of adrenal function to determine if corticosteroid replacement therapy can be discontinued.400 In some patients, switching to a different opiate improved symptoms.400

Head Injury and Increased Intracranial Pressure

Respiratory depressant effects of oxymorphone (with CO2 retention and secondary elevation of CSF pressure) may be markedly exaggerated in the presence of head injury, other intracranial lesions, or preexisting increase in intracranial pressure.501 502 e

Opiates produce effects (e.g., pupillary changes) that may obscure neurologic signs of further increase in pressure in patients with head injuries.501 502 e

Hypotensive Effects

Possible severe hypotension in individuals whose ability to maintain their BP is compromised by depleted blood volume or concomitant drugs that compromise vasculature tone (e.g., phenothiazines, general anesthetics).500 501 502 e

Use with caution in patients in circulatory shock, because vasodilation produced by the drug may further reduce cardiac output and BP.500 501 502

General Precautions

Acute Abdominal Conditions

Administration may complicate assessment of patients with acute abdominal conditions.500 501 502 (See GI Effects under Cautions.)

Seizures

May aggravate preexisting seizures in patients with seizure disorders.501 502 e May induce seizures.500 501 502

Debilitated and Special-Risk Patients.

Use with caution in debilitated patients, those sensitive to CNS depressants, patients with Addison's disease, CNS depression or coma, kyphoscoliosis, myxedema or hypothyroidism, prostatic hypertrophy, urethral stricture, severe impairment of pulmonary function, toxic psychosis, acute alcoholism, delirium tremens, or following GI surgery.500 501 502

Pancreatic and Biliary Disease

May cause spasm of the sphincter of Oddi.500 501 502 Use with caution in patients with biliary tract disease, including acute pancreatitis, and patients undergoing biliary tract surgery.500 501 502

GI Effects

Monitor for decreased bowel motility in post-operative patients.500 501 502 (See Acute Abdominal Conditions under Cautions.)

Contraindicated in patients with known or suspected paralytic ileus.500 501 502

Hypogonadism

Hypogonadism or androgen deficiency reported in patients receiving long-term opiate agonist or opiate partial agonist therapy;400 401 402 403 404 causality not established.400 Manifestations may include decreased libido, impotence, erectile dysfunction, amenorrhea, or infertility.400 Perform appropriate laboratory testing in patients with manifestations of hypogonadism.400

Specific Populations

Pregnancy

Category C.500 501 502

Use parenteral preparation with caution during labor.502 Administration during labor may cause neonatal respiratory depression.502 An opiate antagonist and resuscitative equipment for reversal of opiate-induced respiratory depression should be readily available when opiates are administered during labor and delivery.502

Use of oxymorphone tablets and extended-release tablets not recommended during or immediately prior to labor.501

Infants born to women regularly taking opiates during pregnancy may be physically dependent.500 501 502

Lactation

Not known whether oxymorphone is distributed into human milk.500 501 502 Women receiving oxymorphone generally should not nurse.500 501 502

Pediatric Use

Safety and efficacy not established in pediatric patients <18 years of age.500 501 502

Geriatric Use

No substantial difference in efficacy of oral preparations in geriatric patients relative to younger adults.500 501 Dizziness, somnolence, confusion, nausea reported more frequently in geriatric adults than in younger adults.500 501

Following oral administration, plasma concentrations of oxymorphone are higher in geriatric patients ≥65 years of age than in younger patients.500 501 502 (See Special Populations under Pharmacokinetics.)

Parenteral preparation not systematically evaluated in geriatric adults.502

Select dose with caution, starting at the low end of the dosing range, because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy.500 501 502

Hepatic Impairment

Use with caution in patients with mild hepatic impairment.500 501 502 (See Hepatic Impairment under Dosage and Administration.)

Contraindicated in patients with moderate or severe hepatic impairment.500 501 502

Renal Impairment

Use with caution in patients with moderate or severe renal impairment.500 501 502 Dosage adjustment needed in these patients.500 501 502 (See Renal Impairment under Dosage and Administration and see Special Populations under Pharmacokinetics.)

Common Adverse Effects

Nausea, constipation, pyrexia, somnolence, vomiting, pruritus, headache, dizziness, confusion.500 501 502

Interactions for Opana

Drugs Associated with Serotonin Syndrome

Risk of serotonin syndrome when used with other serotonergic drugs.400 May occur at usual dosages.400 Symptom onset generally occurs within several hours to a few days of concomitant use, but may occur later, particularly after dosage increases.400 (See Advice to Patients.)

If concomitant use of other serotonergic drugs is warranted, monitor patients for serotonin syndrome, particularly during initiation of therapy and dosage increases.400

If serotonin syndrome is suspected, discontinue oxymorphone, other opiate therapy, and/or any concurrently administered serotonergic agents.400

Specific Drugs

Drug

Interaction

Comments

Alcohol

Additive CNS effects500 501 502

Oxymorphone extended-release tablets: Increased or decreased plasma oxymorphone concentrations reported501

Avoid concomitant use500 501

Anticholinergic agents

Increased risk of urinary retention and/or severe constipation, which may lead to paralytic ileus500 501 502

Antidepressants, SSRIs (e.g., citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline), SNRIs (e.g., desvenlafaxine, duloxetine, milnacipran, venlafaxine), tricyclic antidepressants (TCAs), mirtazapine, nefazodone, trazodone, vilazodone

Risk of serotonin syndrome400

If concomitant use warranted, monitor for serotonin syndrome, particularly during initiation of therapy and dosage increases400

If serotonin syndrome suspected, discontinue oxymorphone, the antidepressant, and/or any concurrently administered opiates or serotonergic agents400

Antiemetics, 5-HT3 receptor antagonists (e.g., dolasetron, granisetron, ondansetron, palonosetron)

Risk of serotonin syndrome400

If concomitant use warranted, monitor for serotonin syndrome, particularly during initiation of therapy and dosage increases400

If serotonin syndrome suspected, discontinue oxymorphone, the 5-HT3 receptor antagonist, and/or any concurrently administered opiates or serotonergic agents400

Buspirone

Risk of serotonin syndrome400

If concomitant use warranted, monitor for serotonin syndrome, particularly during initiation of therapy and dosage increases400

If serotonin syndrome suspected, discontinue oxymorphone, buspirone, and/or any concurrently administered opiates or serotonergic agents400

Cimetidine

Adverse CNS effects (confusion, disorientation, respiratory depression, apnea, seizures) reported with opiates500 501 502

Caution500 501 502

CNS depressants (e.g., opiate agonists, general anesthetics, tranquilizers, phenothiazines, sedatives/hypnotics)

Additive CNS effects500 502

Reduce dosage of one or both agents; initiate oxymorphone therapy using (1/3) to ½ the usual dose500 501 502

Cyclobenzaprine

Risk of serotonin syndrome400

If concomitant use warranted, monitor for serotonin syndrome, particularly during initiation of therapy and dosage increases400

If serotonin syndrome suspected, discontinue oxymorphone, cyclobenzaprine, and/or any concurrently administered opiates or serotonergic agents400

Dextromethorphan

Risk of serotonin syndrome400

If concomitant use warranted, monitor for serotonin syndrome, particularly during initiation of therapy and dosage increases400

If serotonin syndrome suspected, discontinue oxymorphone, dextromethorphan, and/or any concurrently administered opiates or serotonergic agents400

5-HT1 receptor agonists (triptans; e.g., almotriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan)

Risk of serotonin syndrome400

If concomitant use warranted, monitor for serotonin syndrome, particularly during initiation of therapy and dosage increases400

If serotonin syndrome suspected, discontinue oxymorphone, the triptan, and/or any concurrently administered opiates or serotonergic agents400

Lithium

Risk of serotonin syndrome400

If concomitant use warranted, monitor for serotonin syndrome, particularly during initiation of therapy and dosage increases400

If serotonin syndrome suspected, discontinue oxymorphone, lithium, and/or any concurrently administered opiates or serotonergic agents400

MAO inhibitors (e.g., isocarboxazid, linezolid, methylene blue, phenelzine, selegiline, tranylcypromine)

Risk of serotonin syndrome400

If concomitant use warranted, monitor for serotonin syndrome, particularly during initiation of therapy and dosage increases400

If serotonin syndrome suspected, discontinue oxymorphone, the MAO inhibitor, and/or any concurrently administered opiates or serotonergic agents400

Opiate partial agonists (butorphanol, buprenorphine, nalbuphine, pentazocine)

Possible reduced analgesic effect and/or withdrawal symptoms500 501 502

Avoid concomitant use500 501 502

St. John’s wort (Hypericum perforatum)

Risk of serotonin syndrome400

If concomitant use warranted, monitor for serotonin syndrome, particularly during initiation of therapy and dosage increases400

If serotonin syndrome suspected, discontinue oxymorphone, St. John’s wort, and/or any concurrently administered opiates or serotonergic agents400

Tryptophan

Risk of serotonin syndrome400

If concomitant use warranted, monitor for serotonin syndrome, particularly during initiation of therapy and dosage increases400

If serotonin syndrome suspected, discontinue oxymorphone, tryptophan, and/or any concurrently administered opiates or serotonergic agents400

Opana Pharmacokinetics

Absorption

Bioavailability

Absolute oral bioavailability is 10%.500 501

Onset

5–10 minutes following IV administration.502 a

10–15 minutes following sub-Q or IM administration.a

Duration

3–6 hours following parenteral administration.502 a

Food

Conventional tablets with high-fat meal: Peak plasma concentration and AUC increase 38%.500

Extended-release tablets with food: Peak plasma concentrations increase 50%; time to peak plasma concentrations delayed; no change in AUC or small increase.501

Special Populations

Oxymorphone extended-release tablets: Bioavailability increased 26, 57, or 65% in patients with mild (Clcr 51–80 mL/minute), moderate (Clcr 30–50 mL/minute), or severe renal impairment (Clcr <30 mL/minute), respectively.501

Oxymorphone extended-release tablets: Based on information from a few individuals with hepatic impairment, bioavailability increased 1.6-, 3.7-, or 12.2-fold in patients with mild, moderate, or severe hepatic impairment, respectively.501

Oxymorphone extended-release tablets: Plasma concentrations increased 40% in geriatric individuals.501

Distribution

Plasma Protein Binding

10–12%.500 501

Elimination

Metabolism

Extensively metabolized in the liver; undergoes reduction or conjugation with glucuronic acid to form oxymorphone-3-glucuronide and 6-OH-oxymorphone.500 501 502

Elimination Route

33–38% excreted in the urine as oxymorphone-3-glucuronide, <1% excreted in urine as 6-OH-oxymorphone, <1% excreted unchanged in the urine.500 501 502

Half-life

Extended-release tablets: 9.4–11.3 hours.501

Stability

Storage

Oral

Conventional Tablets

Tight container at 25°C (may be exposed to 15–30°C).500

Extended-release Tablets

Tight container at 25°C (may be exposed to 15–30°C).501

Parenteral

Injection

25°C (may be exposed to 15°–30°C).502 Protect from light.502

Actions

  • A potent analgesic; shares the actions of the opiate agonists.500 501 502

  • Precise mechanism of action has not been fully elucidated; opiate agonists act at several CNS sites, involving several neurotransmitter systems to produce analgesia.e

  • Pain perception is altered in the spinal cord and higher CNS levels (e.g., substantia gelatinosa, spinal trigeminal nucleus, periaqueductal gray, periventricular gray, medullary raphe nuclei, hypothalamus).e

  • Opiate agonists do not alter the threshold or responsiveness of afferent nerve endings to noxious stimuli, nor peripheral nerve impulse conduction.e

  • Opiate agonists act at specific receptor binding sites in the CNS and other tissues; opiate receptors are concentrated in the limbic system, thalamus, striatum, hypothalamus, midbrain, and spinal cord.e

  • Agonist activity at the opiate μ- or κ-receptor can result in analgesia, miosis, and/or decreased body temperature.e

  • Agonist activity at the μ-receptor can also result in suppression of opiate withdrawal (and antagonist activity can result in precipitation of withdrawal).e

  • Respiratory depression may be mediated by μ-receptors, possibly μ2-receptors (which may be distinct from μ1-receptors involved in analgesia); κ- and δ-receptors may also be involved in respiratory depression.e

Advice to Patients

  • Importance of not breaking, crushing, or chewing extended-release tablets; potentially fatal overdose can occur.501

  • Conventional and extended-release tablets: Advise patients to take tablets on an empty stomach, at least 1 hour before or 2 hours after food.500 501

  • Importance of taking only as prescribed; do not increase dosage or abruptly discontinue without consulting a clinician.500 501 502

  • Advise patients to report any episodes of breakthrough pain or adverse experiences to their clinician.500 501 502

  • Importance of informing patients that this is a drug of potential abuse and should be protected from theft.500 501 502

  • Importance of informing patients that oxymorphone should never be given to anyone other than the individual for whom it was prescribed.500 501 502

  • Advise patients that oxymorphone should not be combined with alcohol or other CNS depressants (e.g., sleep medications, tranquilizers).500 501 502

  • Importance of informing patients that oxymorphone may impair mental and/or physical ability required for performance of potentially hazardous tasks; avoid driving or operating heavy machinery until effects on individual are known.500 501 502

  • Potential risk of serotonin syndrome with concurrent use of oxymorphone and other serotonergic agents.400 Importance of immediately contacting clinician if manifestations of serotonin syndrome (e.g., agitation, hallucinations, tachycardia, labile BP, fever, excessive sweating, shivering, shaking, muscle stiffness, twitching, loss of coordination, nausea, vomiting, diarrhea) develop.400

  • Potential risk of adrenal insufficiency.400 Importance of contacting clinician if manifestations of adrenal insufficiency (e.g., nausea, vomiting, loss of appetite, fatigue, weakness, dizziness, hypotension) develop.400

  • Potential for severe constipation.500 501 502 Counsel patients on appropriate laxatives and/or stool softeners and other therapeutic approaches.500 501 502

  • Risk of dizziness and other adverse events.500 501 502

  • Possible risk (although causality not established) of hypogonadism or androgen deficiency with long-term opiate agonist or partial agonist use.400 Importance of informing clinician if decreased libido, impotence, erectile dysfunction, amenorrhea, or infertility occurs.400

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.500 501 502

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.500 501 502

  • Importance of informing patients of other important precautionary information.500 501 502 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Oxymorphone hydrochloride is subject to control under the Federal Controlled Substances Act of 1970 as a schedule II (C-II) drug.

Oxymorphone Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

5 mg

Opana ( C-II)

Endo

10 mg

Opana ( C-II)

Endo

Tablet, extended-release

5 mg

Opana ER ( C-II)

Endo

10 mg

Opana ER ( C-II)

Endo

20 mg

Opana ER ( C-II)

Endo

40 mg

Opana ER ( C-II)

Endo

Parenteral

Injection

1 mg/mL

Opana ( C-II; preservative-free)

Endo

AHFS DI Essentials. © Copyright 2017, Selected Revisions December 1, 2016. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

400. US Food and Drug Administration. Drug safety communication: FDA warns about several safety issues with opioid pain medicines; requires label changes. Silver Spring, MD; 2016 Mar 22. From FDA website.

401. Katz N, Mazer NA. The impact of opioids on the endocrine system. Clin J Pain. 2009; 25:170-5. [PubMed 19333165]

402. Rajagopal A, Vassilopoulou-Sellin R, Palmer JL et al. Symptomatic hypogonadism in male survivors of cancer with chronic exposure to opioids. Cancer. 2004; 100:851-8. [PubMed 14770444]

403. Abs R, Verhelst J, Maeyaert J et al. Endocrine consequences of long-term intrathecal administration of opioids. J Clin Endocrinol Metab. 2000; 85:2215-22. [PubMed 10852454]

404. Fraser LA, Morrison D, Morley-Forster P et al. Oral opioids for chronic non-cancer pain: higher prevalence of hypogonadism in men than in women. Exp Clin Endocrinol Diabetes. 2009; 117:38-43. [PubMed 18523930]

500. Endo Pharmaceuticals Inc. Opana (oxymorphone hydrochloride) tablets prescribing information. Chadds Ford, PA; 2006 Jul.

501. Endo Pharmaceuticals Inc. Opana ER (oxymorphone hydrochloride) extended-release tablets prescribing information. Chadds Ford, PA; 2007 June.

502. Endo Pharmaceuticals Inc. Opana (oxymorphone hydrochloride) injection prescribing information. Chadds Ford, PA; 2006 Sept.

a. AHFS drug information 2007. McEvoy GK, ed. Oxymorphone. Bethesda, MD: American Society of Health-System Pharmacists; 2007: 2154-5.

e. AHFS drug information 2007. McEvoy GK, ed. Opioid Agonists General Statement. Bethesda, MD: American Society of Health-System Pharmacists; 2007:2123-8.

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