Trade Names:Opana- Tablets 5 mg- Tablets 10 mg- Injection 1 mg/mL
Trade Names:Opana ER- Tablets, ER 5 mg- Tablets, ER 7.5 mg- Tablets, ER 10 mg- Tablets, ER 15 mg- Tablets, ER 20 mg- Tablets, ER 30 mg- Tablets, ER 40 mg
Relieves pain by stimulating opiate receptors in the CNS.
Bioavailability of oral oxymorphone is about 10%.
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%.
Undergoes extensive hepatic metabolism.
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.
After parenteral administration, effects are seen within 5 to 10 min.
3 to 6 h.
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.
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 ( Opana 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.
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 ( Opana 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 ( Opana ER ). Parenteral Treatment of pulmonary edema secondary to a chemical respiratory irritant.
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 Opana : 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. 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 Opana to Opana ERAdults
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.Conversion from Opana to Opana InjectionAdults
Since 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 Opana or Opana ERAdults
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 Parenteral Oxymorphone to Opana or Opana ERAdults
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. Titrate to optimal pain relief, taking into account pain intensity and adverse reactions.LaborAdults
IM 0.5 to 1 mg is recommended.Maintenance TherapyAdults
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 DepressantsAdults
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.
Store injection and tablets at controlled room temperature (59° to 86°F). Protect injection from light. Dispense tablets in a tight container with a child-proof closure.
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 Opana 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.
None well documented.
Flushing, hypertension, hypotension, tachycardia (1% to less than 10%); bradycardia, orthostatic hypotension, palpitations.
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.
Pruritus (15%); sweating (9%).
Blurred vision (1% to less than 10%); diplopia, miosis.
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.
Ureteral spasm, urinary hesitation, urinary retention.
Allergic dermatitis, pruritus, swelling face, urticaria.
Decreased weight, dehydration (1% to less than 10%); anorexia.
Dyspnea, hypoxia (1% to less than 10%); apnea, atelectasis, bronchospasm, laryngeal edema, laryngospasm, respiratory depression.
Edema (1% to less than 10%).
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.
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.
Category C .
Safety and efficacy not established in patients younger than 18 yr of age.
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.
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.
May obscure patient's diagnosis or clinical course.
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.
Has abuse potential.
Respiratory depressant effects may be markedly exaggerated in the presence of head injury, intracranial lesions, or preexisting increased intracranial pressure.
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.
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.
Because oxymorphone can cause spasm of the Oddi sphincter, use with caution in patients with biliary tract disease, including acute pancreatitis.
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.
Both tolerance and physical dependence may occur.
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.
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