oxymorphone

Contraindicated in:

Hypersensitivity;
Concurrent alcohol;
Moderate or severe hepatic impairment;
Significant respiratory depression (unless monitoring and resuscitative equipment are readily available);
Acute or severe bronchial asthma (unless monitoring and resuscitative equipment are readily available);
Paralytic ileus.

Use Cautiously in:

Personal or family history of substance use disorder or mental illness;
Acute alcoholism or delirium tremens or other toxic psychoses;
Mild hepatic impairment;
Head injury/↑ intracranial pressure (may obscure neurologic signs and further ↑ pressure);
Volume depletion or drugs that may cause hypotension including diuretics and phenothiazines (↑ risk of severe hypotension);
Circulatory shock (may ↑ risk of severe hypotension);
Adrenocortical insufficiency;
Seizure disorders;
Hypothyroidism;
Prostatic hypertrophy or ureteral stricture;
Severe pulmonary impairment;
Renal impairment (CCr <50 mL/min);
Biliary tract disease or pancreatitis;
OB: Avoid chronic use; prolonged use of opioids during pregnancy can result in neonatal opioid withdrawal syndrome;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children;
Geri: ↑risk of respiratory depression in older adults; dose ↓ suggested.

Exercise Extreme Caution in:

Conditions association with hypoxia, hypercapnea, ↓ respiratory reserve (including asthma, COPD, cor pulmonale, morbid obesity, sleep apnea, myxedema, kyphoscoliosis, CNS depression, and coma).

Adv. Reactions/Side Effects ⬆ ⬇

CV: orthostatic hypotension

Derm: flushing, sweating

EENT: blurred vision, diplopia, miosis

Endo: adrenal insufficiency

GI: constipation, dry mouth, nausea, vomiting

GU: urinary retention

Neuro: confusion, sedation, dizziness, dysphoria, euphoria, floating feeling, hallucinations, headache, unusual dreams, confusion, sedation, dizziness, dysphoria, euphoria, floating feeling, hallucinations, headache, unusual dreams

Resp: RESPIRATORY DEPRESSION (INCLUDING CENTRAL SLEEP APNEA AND SLEEP-RELATED HYPOXEMIA)

Misc: allodynia, opioid-induced hyperalgesia, physical dependence, psychological dependence, tolerance

Interactions ⬆ ⬇

Drug-drug:

Use with caution in patients receiving MAO inhibitors (may result in unpredictable reactions; ↓ initial dose of oxymorphone to 25% of usual dose).
Use with benzodiazepines or other CNS depressants, including other opioids, nonbenzodiazepine sedative/hypnotics, anxiolytics, general anesthetics, muscle relaxants, antipsychotics, and alcohol, may cause profound sedation, respiratory depression, coma, and death; reserve concurrent use for when alternative treatment options are inadequate.
Alcohol may ↑ levels and ↑ the risk of toxicity.
Drugs that may cause volume depletion or hypotension, including diuretics and phenothiazines, may ↑ risk of severe hypotension.
Administration of partial-antagonist opioid analgesics may precipitate withdrawal in physically dependent patients.
Nalbuphine or buprenorphine↓ analgesia.
Drugs that affect serotonergic neurotransmitter systems, including tricyclic antidepressants, SSRIs, SNRIs, MAO inhibitors, TCAs, tramadol, trazodone, mirtazapine, 5-HT3 receptor antagonists, linezolid, methylene blue, and triptans, ↑ risk of serotonin syndrome.

Drug-Natural Products:

Concomitant use of kava-kava, valerian, or chamomile can ↑ CNS depression.

Availability ⬆ ⬇

(Generic available)

Immediate-release tablets : 5 mg; 10 mg
Extended-release tablets: 5 mg; 7.5 mg; 10 mg; 15 mg; 20 mg; 30 mg; 40 mg

Route/Dosage ⬆ ⬇

Larger doses may be required during chronic therapy
PO (Adults ): Opioid-naive patients: 10–20 mg (of immediate release [IR]) every 4–6 hr as needed; some patients may require initial dose of 5 mg, not to exceed 20 mg. For extended release (ER), give 5 mg every 12 hr; may titrate in increments of 5–10 mg every 12 hr every 3–7 days.

US Brand Names ⬆ ⬇

~~Opana,~~ ~~Opana ER~~

Action ⬆ ⬇

Binds to opiate receptors in the CNS.
Alters the perception of and response to painful stimuli while producing generalized CNS depression.

Therapeutic effects:

Decrease in pain.

Classifications ⬆ ⬇

Therapeutic Classification: opioid analgesics

Pharmacologic Classification: opioid agonists

Pharmacokinetics ⬆ ⬇

Absorption: 10% absorbed following oral administration. Food and alcohol significantly ↑ absorption (38%).

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Mostly metabolized by the liver; at least 2 metabolites are pharmacologically active, <1% excreted unchanged in urine.

Half-Life: 2.6–4 hr.

Contr. Subst. Schedule ⬆ ⬇

Time/Action Profile ⬆ ⬇

(analgesic effects)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	unknown	4–6 hr

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of oxymorphone to patient. Instruct them to take medication as directed and when to ask for pain medication. Do not share medication with others, even if they have similar symptoms; may be harmful and is against the law. Keep out of children's reach. Advise patient to read Patient Informationbefore starting and with each Rx refill in case of changes.
REMS: Instruct patient to take oxymorphone as directed and not to adjust dose without consulting health care professional. Take missed doses as soon as possible if on chronic therapy. If almost time for next dose, skip dose and return to regular schedule. Do not double doses unless advised by health care professional. Do not stop taking oxymorphone abruptly; may cause withdrawal symptoms. Discontinue gradually under supervision of health care professional. Discuss safe use, risks, and proper storage and disposal of opioid analgesics with patients and caregivers with each Rx. The Patient Counseling Guide is available at www.fda.gov/OpioidAnalgesicREMSPCG.
Advise patient that oxymorphone is a drug with known abuse potential. Protect it from theft, and never give to anyone other than the individual for whom it was prescribed. Store out of sight and reach of children, and in a location not accessible by others.
Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose. Inform patients and caregivers about various ways to obtain naloxone as permitted by individual state naloxone dispensing and prescribing requirements or guidelines (Rx, direct from pharmacist, or state programs). OTC naloxone nasal spray is available at pharmacies nationwide for overdose or accidental ingestion.
Advise patient to notify health care professional if pain control is not adequate or if severe or persistent side effects occur.
Medication may cause drowsiness or dizziness. Advise patient to call for assistance when ambulating and to avoid driving or other activities that require alertness until response to the medication is known.
Advise patient to make position changes slowly to minimize orthostatic hypotension.
Advise patient to avoid concurrent use of alcohol or other CNS depressants with this medication.
Emphasize the importance of aggressive prevention of constipation with the use of oxymorphone.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Encourage patient to turn, cough, and breathe deeply every 2 hr to prevent atelectasis.
Inform patients taking ER oxymorphone tablets that a soft mass resembling tablets may appear in stool; active medication was already absorbed.
Advise patient that good oral hygiene, frequent mouth rinses, and sugarless gum or candy may ↓ dry mouth.
Rep: Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Inform patient of potential for neonatal opioid withdrawal syndrome with prolonged use during pregnancy. Monitor neonate for signs and symptoms of withdrawal symptoms (irritability, hyperactivity and abnormal sleep pattern, high-pitched cry, tremor, vomiting, diarrhea, failure to gain weight); usually occur the first days after birth. Monitor infants exposed to oxymorphone through breast milk for excess sedation and respiratory depression. Chronic use may ↓ fertility in females and males.

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Indications ⬇

Contraind./Precautions ⬆ ⬇