A-Z Drug Facts > Oxymorphone Hydrochloride

Oxymorphone Hydrochloride

Pronouncation: (OX-i-MOR-fone HYE-droe-KLOR-ide)
Class: Opioid analgesic

Trade Names:
Numorphan
- Injection 1 mg/mL

Trade Names:
Opana
- Tablets 5 mg
- Tablets 10 mg
- Injection 1 mg/mL

Trade Names:
Opana ER
- Tablets, extended-release 5 mg
- Tablets, extended-release 10 mg
- Tablets, extended-release 20 mg
- Tablets, extended-release 40 mg

Pharmacology

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Relieves pain by stimulating opiate receptors in the CNS.

Pharmacokinetics

Absorption

Bioavailability of oral oxymorphone is about 10%.

Distribution

Vd is 3.08 L/kg. Steady-state levels are achieved after 3 days of multiple-dose oral administration. Protein binding is 10% to 12%.

Metabolism

Undergoes extensive hepatic metabolism.

Elimination

Mean terminal t _½ is 1.3 h. Following a 10 mg oral dose, 49% is excreted in the urine over a 5-day period.

Onset

After parenteral administration, effects are seen within 5 to 10 min.

Duration

Duration of effect is 3 to 6 h.

Special Populations

Renal Function Impairment

There is an increase of 26%, 57%, and 65% in bioavailability in patients with mild, moderate, and severe renal function impairment, respectively.

Hepatic Function Impairment

Bioavailability of orally administered oxymorphone may be markedly increased in patients with moderate to severe liver disease.

Indications and Usage

Relief of moderate to severe acute pain; relief of moderate to severe pain in patients requiring, around-the-clock opioid treatment for an extended period of time ( Opana ER extended-release tablets).

Contraindications

Hypersensitivity to morphine analogs; hypersensitivity to any component of the product; moderate and severe hepatic function impairment; respiratory depression, except in monitored settings and in the presence of resuscitative equipment; in patients with acute or severe bronchial asthma or hypercarbia; patients who have or are suspected of having paralytic ileus; concomitant alcohol ingestion; in the immediate postoperative period (first 12 to 24 h following surgery) for patients not previously taking opioids or if pain is mild or not expected to persist for an extended period of time ( Opana ER ).

Dosage and Administration

Adults

IM/Subcutaneous Initially, 1 to 1.5 mg, repeated every 4 to 6 h as needed.

IV Initially, 0.5 mg. In nondebilitated patients, the dose may be cautiously increased until satisfactory pain relief is achieved.

PO Opana : Initiate patients who have not been receiving opioid analgesics at 10 to 20 mg every 4 to 6 h, depending on the initial pain. Titrate the dose based on the patient's response to the initial dose, taking into account the pain intensity and adverse reactions. Opana ER : Start with 5 mg every 12 h, then titrate the dosage in increments of 5 to 10 mg every 12 h every 3 to 7 days.

Conversion from Parenteral Oxymorphone to Opana or Opana ER
Adults

PO Administer a dose that is 10 times the patient's total daily parenteral oxymorphone dose as Opana in 4 to 6 equally divided doses or as Opana ER in 2 equally divided doses. Then titrate to optimal pain relief, taking into account pain intensity and adverse reactions.

Conversion from Other Oral Opioids to Opana or Opana ER
Adults

PO It is safest to start therapy by administering half of the calculated total daily dose of Opana in 4 to 6 equally divided doses, every 4 to 6 h, or as Opana ER in 2 equally divided doses, every 12 h. Then adjust the dose gradually, taking into account pain intensity and adverse reactions.

Conversion from Opana to Opana ER
Adults

PO Start therapy by administering half of the calculated total daily dose of Opana as Opana ER every 12 h. Then adjust the dose gradually, taking into account pain intensity and adverse reactions.

Use with CNS Depressants
Adults

PO Initiate therapy at one third to one half of the usual dose in patients receiving other CNS depressants, including sedative or hypnotics, general anesthetics, phenothiazine, tranquilizers, and alcohol, because respiratory depression, hypotension, and profound sedation or coma may occur.

Labor
Adults

IM 0.5 to 1 mg is recommended.

General Advice

• Injection
• For subcutaneous, IM, or IV administration. Not for intradermal or intraarterial administration.
• Do not administer if particulate matter or discoloration is noted.
• Discard any unused medication per institutional policy and procedure for Schedule II controlled substances.

• Tablets
• Take tablets 1 h before or 2 h after eating.
• Extended-release tablets are to be swallowed whole and not broken, chewed, dissolved, or crushed, which may lead to rapid release and absorption of a potentially fatal dose.
• Dosage adjustments are needed when switching from IM or subcutaneous to oral therapy.
• When discontinuing therapy, taper the dose gradually to prevent signs and symptoms of withdrawal.

Storage/Stability

Store injection at controlled room temperature (59° to 86°F). Protect from light. Store tablets at 59° to 86°F. Dispense in a tight container with a child-proof closure.

Drug Interactions

Anticholinergics or drugs with anticholinergic activity

Increased risk of urinary retention and severe constipation, possibly leading to paralytic ileus.

Cimetidine

Action of oxymorphone may be enhanced, resulting in increased pharmacologic and adverse reactions.

CNS depressants (eg, alcohol, hypnotics, sedatives, tranquilizers)

Additive CNS depressant effects. Respiratory depression, hypotension, profound sedation, or coma may occur.

Mixed agonist/antagonist opioid analgesics (buprenorphine, butorphanol, nalbuphine, pentazocine)

Action of oxymorphone may be reduced, possibly precipitating withdrawal symptoms.

Propofol

Increased risk of bradycardia.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Bradycardia; flushing; hypertension; hypotension; orthostatic hypotension; palpitations; tachycardia.

CNS

Anxiety; confusion; disorientation; dizziness; drowsiness; dysphoria; euphoria; fatigue; hallucinations; headache; lethargy; light-headedness; mental clouding; mental depression; nervousness; paradoxical CNS stimulation; pyrexia; restlessness; trouble sleeping; unusual tiredness or weakness.

Dermatologic

Allergic reaction (eg, hives, skin rash, swelling of the face); injection site reaction; itching; sweating.

EENT

Blurred vision; diplopia; miosis.

GI

Abdominal distention and pain; biliary tract spasm; constipation; cramps or pain; diarrhea; dry mouth; dyspepsia; flatulence; loss of appetite; nausea; paralytic ileus or toxic megacolon in patients with inflammatory bowel disease; vomiting.

Genitourinary

Antidiuretic effect; ureteral spasm; urinary hesitancy or retention.

Metabolic

Decreased weight; dehydration.

Respiratory

Allergic bronchospastic reaction; allergic laryngeal edema; allergic laryngospasm; atelectasis; dyspnea; hypoxia; respiratory depression.

Miscellaneous

Edema.

Precautions

Warnings Oxymorphone is a Schedule II controlled substance with abuse liability similar to other opioid analgesics. Oxymorphone extended-release tablets are indicated for management of moderate to severe pain when continuous, around-the-clock opioid treatment is needed for an extended period of time and they are not intended for as-needed use. Oxymorphone extended-release tablets are to be swallowed whole and not broken, chewed, dissolved, or crushed, which may lead to rapid release and absorption of a potentially fatal dose. Alcoholic beverages, or prescription or nonprescription medications containing alcohol, should not be consumed with oxymorphone extended-release tablets because increased plasma levels and a potentially fatal overdose of oxymorphone may result.

Monitor Because oxymorphone may decrease bowel motility and ileus is a common postoperative complication, monitor for decreased bowel motility in postoperative patients. Opana ER is not indicated in the immediate postoperative period (first 12 to 24 h following surgery) for patients not previously taking opioids or if pain is mild or not expected to persist for an extended period of time.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in patients younger than 18 yr of age.

Elderly

Because plasma levels may be elevated, use with caution in patients 65 yr of age and older.

Special Risk Patients

Use with caution in elderly and debilitated patients and in patients known to be sensitive to CNS depressants (eg, CV, pulmonary, renal, or hepatic disease); use with caution in patients with hypothyroidism, acute alcoholism, delirium tremens, convulsive disorders, Addison disease, gallbladder disease or gallstones, prostatic hypertrophy or urethral stricture, recent GI or GU tract surgery, inflammatory bowel disease, or diarrhea secondary to poisoning until toxin is eliminated.

Acute abdominal conditions

Diagnosis or clinical course of patient may be obscured.

Discontinuation

If treatment is to be discontinued or the dose reduced, gradually taper the dose and monitor patient for withdrawal symptoms. Note significant withdrawal symptoms (eg, sweating, muscle cramps, abdominal pain, piloerection). Be prepared to reinstitute previous dosing schedule and attempt a less rapid tapering regimen after patient has stabilized.

Drug dependence

Has abuse potential.

Head injury

Respiratory depressant effects may be markedly exaggerated in the presence of head injury, intracranial lesions, or preexisting increased intracranial pressure.

Hepatic/Renal function impairment

Use with caution in patients with mild hepatic function impairment or moderate to severe renal function impairment, starting with lowest dose and titrating slowly with careful monitoring.

Hypotension

May cause severe hypotension in postoperative patients or in individuals whose ability to maintain BP is compromised (eg, volume depletion). May cause orthostatic hypotension in ambulatory patients.

Pancreatic/Biliary tract disease

Because oxymorphone can cause spasm of the Oddi sphincter, use with caution in patients with biliary tract disease, including acute pancreatitis.

Respiratory depression

May cause serious or potentially fatal respiratory depression if given in excessive dose, too frequently, or in full dosage to compromised patients. Use with caution in patients with impaired respiratory reserve or respiratory depression.

Overdosage

Symptoms

Apnea, bradycardia, cardiac arrest, circulatory collapse, CNS depression, cold and clammy skin, constricted pupils, death, extreme somnolence progressing to stupor or coma, hypotension, respiratory depression, skeletal muscle flaccidity.

Patient Information

• Oral
• Instruct patient or caregiver that medication may be habit forming, and to use exactly as prescribed and not to change the dose or discontinue therapy unless advised by health care provider. Advise patient or caregiver to notify health care provider if medication does not adequately control pain.
• Advise patient, family, or caregiver that if medication needs to be discontinued after prolonged use, it usually will be slowly withdrawn unless safety concerns (eg, rash) require a more rapid withdrawal.
• Advise patient or caregiver to notify health care provider if any of the following occur: excessive sedation or drowsiness, slow or shallow breathing, low BP, slow heart rate, severe constipation.
• Instruct patient to get up slowly from lying or sitting position and to avoid sudden position changes to prevent postural hypotension. Advise patient to report dizziness with position changes to health care provider. Caution patient that hot tubs and hot showers or baths may make dizziness worse.
• Caution patient that drug may cause dizziness or drowsiness and to use caution while driving or performing other tasks requiring mental alertness or coordination until tolerance is determined.
• Advise patient to report episodes of breakthrough pain and adverse reactions to health care provider.
• Advise patient of the potential for severe constipation and to consider use of appropriate laxatives and stool softeners.
• Advise patient of the potential for drug abuse and to never give the medication to anyone.
• Caution patients that oxymorphone extended-release tablets are to be swallowed whole and not broken, chewed, dissolved, or crushed, which may lead to rapid release and absorption of a potentially fatal dose.
• Advise patients that alcoholic beverages, or prescription or nonprescription medications containing alcohol, should not be consumed with oxymorphone extended-release tablets because increased plasma levels and a potentially fatal overdose of oxymorphone may result.
• Caution patient to avoid alcohol and other CNS depressant medications while using this medication.

• Injection
• Advise patient or caregiver that medication will be prepared and administered by a health care provider in a health care setting.

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