Oxymorphone Hydrochloride

Oxymorphone Tablet is indicated for treatment of moderate to severe pain like chronic cancer, arthritis, postoperative & low back pain.

Oxymorphone Injection is indicated for the relief of moderate to severe pain. It is also indicated for pre-operative & post-operative medication for support of anesthesia, for obstetrical analgesia and for relief of anxiety in patients with dyspnea associated with pulmonary edema secondary to acute left ventricular dysfunction.

Oxymorphone is an opioid agonist whose principal therapeutic action is analgesia. Like all pure opioid agonist
analgesics, with increasing doses there is increasing analgesia, unlike with mixed agonist/antagonists or non opioid analgesics, where there is a limit to the analgesic effect with increasing doses. With pure opioid agonist analgesics, there is no defined maximum dose. Administered parenterally, 1 mg of Oxymorphone Hydrochloride injection is approximately equivalent in analgesic activity to 10 mg of Morphine sulfate.

Oxymorphone Tablet: This may be used as needed in the treatment of acute post-surgical pain with a dose of 5-10 mg every 4 hours. Administer Oxymorphone Tablet on an empty stomach at least one hour prior to or two hours after eating.

Oxymorphone Injection:

• Subcutaneous or Intramuscular Administration: Initially 1 mg to 1.5 mg, repeated every 4 to 6 hours as needed.
• Intravenous: 0.5 mg initially. For analgesia during labor 0.5 mg to 1 mg intramuscularly is recommended.

Conversion from Oral Oxymorphone to Oxymorphone Injection: Given the absolute oral bioavailability of approximately 10%, patients receiving oral Oxymorphone may be converted to Oxymorphone Hydrochloride injection by administering one-tenth the patient's total daily oral Oxymorphone dose as Oxymorphone Hydrochloride injectable in four or six equally divided doses (e.g., total daily oral dose/ [10X4]). For example, approximately 1 mg of Oxymorphone Hydrochloride injectable IM every 6 hours (4 mg total IM dose) may be required to provide pain relief equivalent to a total daily dose of 40 mg oral Oxymorphone. As with any opioid drug product, it is necessary to adjust the dosing regimen for each patient individually taking into account the patient's prior analgesic treatment experience.

Clinical drug interaction studies with Oxymorphone showed no induction of CYP450 3A4 or 2C9 enzyme activity indicating that no dose adjustment for CYP 3A4 or 2C9 mediated drug-drug interactions is required.

Oxymorphone Hydrochloride tablet and injection should not be administered to patients with a known hypersensitivity to Oxymorphone Hydrochloride or to any of the other ingredients in Oxymorphone Hydrochloride tablet and injection or with known hypersensitivity to morphine analogs such as codeine. Oxymorphone Hydrochloride is contraindicated in patients with respiratory depression, acute or severe bronchial asthma, paralytic ileus or moderate to severe hepatic impairment.

General Disorders: Respiratory depression, Fatigue, Asthenia.
Metabolism and Nutrition Disorders: Anorexia.
Cardiac Disorders: Tachycardia, Bradycardia, Palpitations.
Eye Disorders: Miosis, Diplopia, Blurred vision.
Gastrointestinal Disorders: Vomiting, Constipation.
Psychiatric Disorders: Dysphoria, Euphoric mood, Nervousness, Restlessness, Insomnia, Agitation, Hallucination, Depression.
Vascular Disorders: Hypotension & Flushing.

Pregnancy Category C. The safety of using Oxymorphone in pregnancy has not been established with regard to possible adverse effects on fetal development. The use of Oxymorphone in pregnancy, in nursing mothers, or in women of child-bearing potential requires that the possible benefits of the drug be weighed against the possible hazards to the mother and the child.

Opioid analgesics should be used with caution especially when combined with other drugs. Oxymorphone should be used with caution in elderly and debilitated patients and in patients who are known to be sensitive to central nervous system depressants such as those with cardiovascular, pulmonary, renal or hepatic disease. Oxymorphone should be used with caution in the following conditions: acute alcoholism, coma & delirium tremens. Administer Oxymorphone with extreme caution to patients with conditions accompanied by hypoxia, hypercapnia, or decreased respiratory reserve such as: asthma, chronic obstructive pulmonary disease or, severe obesity, sleep apnea syndrome, myxedema, kyphoscoliosis, CNS depression, or coma. Oxymorphone, like all opioid analgesics, should be started at 1/3 to 1/2 of the usual dose in patients who are concurrently receiving other central nervous system (CNS) depressants including sedatives or hypnotics, general anesthetics, phenothiazines, tranquilizers, and alcohol, because respiratory depression, hypotension and profound sedation, coma or death may result. Use Oxymorphone with caution in patients with mild hepatic impairment, starting with the lowest dose (e.g., 5 mg). The plasma levels of Oxymorphone administered as an extended-release tablet were about 40% higher in elderly (=65 years of age) than in younger subjects. So for geriatric patients may be started with Oxymorphone 5 mg. There are 57% and 65% increases in Oxymorphone bioavailability in patients with moderate and severe renal impairment, respectively. So for renal impaired patients may be started with Oxymorphone 5 mg. Use Oxymorphone with caution in the following conditions: adrenocortical insufficiency (e.g., Addison's disease), prostatic hypertrophy or urethral stricture, severe impairment of pulmonary or renal function, and toxic psychosis Opioid analgesics impair the mental and physical abilities needed to perform potentially hazardous activities such as driving a car or operating machinery.

Dependence: Oxymorphone should not be abruptly discontinued. When the patient no longer requires therapy
with Oxymorphone, doses should be tapered gradually to prevent signs and symptoms of withdrawal in the
physically dependent patient.

Pediatric use: Safety and effectiveness of Oxymorphone Hydrochloride tablet and injection in pediatric patients below the age of 18 years have not been established.

Geriatric use: Oxymorphone Hydrochloride tablet and injection should be used with caution in elderly patients. These adverse events included dizziness, somnolence, confusion and nausea.

Opioid analgesics

Tablet: Store in a cool and dry place, protect from light.
Injection: Store at 25°C, protect from light.