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Oxymorphone Hydrochloride

Pronunciation

Pronunciation: OX-i-MOR-fone HYE-droe-KLOR-ide
Class: Opioid analgesic

Trade Names

Opana
- Tablets 5 mg
- Tablets 10 mg
- Injection 1 mg/mL

Opana ER
- Tablets, ER 5 mg
- Tablets, ER 10 mg
- Tablets, ER 20 mg
- Tablets, ER 30 mg
- Tablets, ER 40 mg

Oxymorphone
- Tablets, ER 7.5 mg
- Tablets, ER 15 mg

Pharmacology

Relieves pain by stimulating opiate receptors in the CNS.

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Pharmacokinetics

Absorption

Bioavailability of oral oxymorphone is about 10%.

Distribution

After an IV dose, 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 half-life 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

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 hepatic function impairment.

Elderly

On average, patients older than 65 years of age experience 1.4- and 1.5-fold increases in oxymorphone AUC and C max , respectively.

Gender

No differences in pharmacokinetics are observed between men and women when AUC and C max are adjusted for body weight.

Indications and Usage

PO Relief of moderate to severe acute pain (immediate-release); relief of moderate to severe pain in patients requiring around-the-clock opioid treatment for an extended period of time (ER). Parenteral Relief of moderate to severe pain; preoperative medication; support of anesthesia; obstetrical analgesia; relief of anxiety in patients with dyspnea associated with pulmonary edema secondary to acute left ventricular dysfunction.

Contraindications

PO Hypersensitivity to morphine analogs; hypersensitivity to any component of the product; moderate or severe hepatic function impairment; respiratory depression, except in monitored settings and in the presence of resuscitative equipment; acute or severe bronchial asthma or hypercarbia; patients who have or are suspected of having paralytic ileus; concomitant alcohol ingestion (ER); 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 (ER). Parenteral Treatment of pulmonary edema secondary to a chemical respiratory irritant.

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, cautiously increase the dose until satisfactory pain relief is achieved.

PO Immediate release: Initiate patients who have not been receiving opioid analgesics at 10 to 20 mg every 4 to 6 h, depending on initial pain. Titrate the dose based on the patient's response to the initial dose, taking into account pain intensity and adverse reactions. 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 immediate release to ER
Adults

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

Conversion from Opana to Opana Injection
Adults

Because oral bioavailability of oxymorphone is approximately 10%, convert patients receiving oral oxymorphone to parenteral oxymorphone by giving one-tenth of the oral oxymorphone daily dose as parenteral oxymorphone in 4 to 6 equally divided doses.

Conversion from Other Oral Opioids to Oxymorphone or Oxymorphone ER
Adults

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

Conversion from Parenteral Oxymorphone to Oxymorphone or Oxymorphone ER
Adults

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

Labor
Adults

IM 0.5 to 1 mg is recommended.

Maintenance Therapy
Adults

The intent of the titration period is to establish a patient-specific, 12-h dose that will maintain adequate analgesia with acceptable adverse reactions for as long as pain relief is necessary. During titration and before a stable dose is achieved, use immediate-release medications to supplement analgesia between doses. If pain recurs, incrementally increase the dose to reestablish pain control.

Use With CNS Depressants
Adults

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

Hepatic Function Impairment

Contraindicated in moderate to severe hepatic function impairment. Use lowest dose and titrate slowly with careful monitoring of adverse reactions in mild hepatic function impairment.

Renal Function Impairment

Administer with caution and reduced doses in patients with CrCl less than 50 mL/min.

Elderly Patients

Initiate therapy at the low end of the dosing range.

General Advice

  • When discontinuing therapy, taper the dose gradually to prevent signs and symptoms of withdrawal.
  • 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
  • Administer tablets 1 h before or 2 h after eating.
  • Advise patients to swallow ER tablets whole and not break, chew, dissolve, or crush, which may lead to rapid release and absorption of a potentially fatal dose.
  • Make appropriate dosage adjustments when switching from IM or subcutaneous to oral therapy.

Storage/Stability

Store at 59° to 86°F. Protect injection from light.

Drug Interactions

Anticholinergics or drugs with anticholinergic activity

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

Cimetidine

May enhance action of oxymorphone, resulting in increased pharmacologic and adverse reactions.

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

Additive CNS depressant effects. Coma, hypotension, profound sedation, or respiratory depression may occur. Alcohol is contraindicated in patients receiving oxymorphone ER.

Food

Oxymorphone plasma concentrations may be increased. Oxymorphone should be taken 1 h before or 2 h after eating.

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

May reduce action of oxymorphone, possibly precipitating withdrawal symptoms.

Propofol

Increased risk of bradycardia.

Adverse Reactions

Cardiovascular

Flushing, hypertension, hypotension, tachycardia (1% to less than 10%); bradycardia, orthostatic hypotension, palpitations.

CNS

Somnolence (19%); dizziness (18%); pyrexia (14%); headache (12%); sedation (6%); fatigue, insomnia (4%); decreased appetite (3%); anxiety, confusion, disorientation, lethargy, nervousness, restlessness, weakness (1% to less than 10%); depression, drug dependence, dysphoria, euphoria, hallucination, light-headedness, unusual tiredness or weakness.

Dermatologic

Pruritus (15%); sweating (9%).

EENT

Blurred vision (1% to less than 10%); diplopia, miosis.

GI

Nausea (33%); constipation (28%); vomiting (16%); dry mouth (6%); diarrhea (4%); abdominal pain (3%); abdominal distention, dyspepsia, flatulence (1% to less than 10%); paralytic ileus.

Genitourinary

Ureteral spasm, urinary hesitation, urinary retention.

Hypersensitivity

Allergic dermatitis, pruritus, swelling face, urticaria.

Local

Injection-site reaction.

Metabolic-Nutritional

Decreased weight, dehydration (1% to less than 10%); anorexia.

Respiratory

Dyspnea, hypoxia (1% to less than 10%); apnea, atelectasis, bronchospasm, laryngeal edema, laryngospasm, respiratory depression.

Miscellaneous

Edema (1% to less than 10%).

Precautions

Warnings

Oxymorphone is a Schedule II controlled substance with abuse liability similar to other opioid analgesics. Oxymorphone ER tablets are indicated for management of moderate to severe pain when around-the-clock opioid treatment is needed for an extended period of time; they are not intended for as-needed use. Oxymorphone ER 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, must not be consumed with oxymorphone ER 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. Oxymorphone 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 are about 40% higher in patients 65 yr of age and older, use with caution in these patients. Start treatment with lower doses and adjust the dose cautiously, taking into account pain intensity and adverse reactions.

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 Addison disease, acute alcoholism, convulsive disorders, delirium tremens, diarrhea secondary to poisoning, gallbladder disease or gallstones, hypothyroidism, inflammatory bowel disease, prostatic hypertrophy or urethral stricture, recent GI or GU tract surgery, or toxic psychosis until toxin is eliminated.

Acute abdominal conditions

May obscure patient's diagnosis or clinical course.

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, abdominal pain, muscle cramps, piloerection, sweating). Be prepared to reinstitute previous dosing schedule and attempt a less rapid tapering regimen after patient has stabilized.

Drug abuse

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. Contraindicated in patients with moderate to severe hepatic function impairment.

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 doses, too frequently, or in full dosage to compromised patients. Use with caution in patients with impaired respiratory reserve or respiratory depression.

Tolerance and physical dependence

Both tolerance and physical dependence may occur.

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

  • Injection
  • Advise patient or caregiver that medication will be prepared and administered by health care provider in a health care setting.
  • 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 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, low BP, severe constipation, slow heart rate, slow or shallow breathing.
  • Instruct patient to get up slowly from lying or sitting positions 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 patient that oxymorphone ER tablets are to be swallowed whole and not broken, chewed, dissolved, or crushed, because this may lead to rapid release and absorption of a potentially fatal dose.
  • Advise patient that alcoholic beverages, or prescription or nonprescription medications containing alcohol, must not be consumed with oxymorphone ER tablets because increased plasma levels and a potentially fatal overdose of oxymorphone may result.
  • Caution patient to avoid other CNS depressant medications while using oxymorphone.

Copyright © 2009 Wolters Kluwer Health.

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