Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

North America

USA: Opana.


Japan: Numorphan, Opana.

Drug combinations


Oxymorphone Hydrochloride: C~17~H~19~NO~4~ HCl. Mw: 337.80. (1) Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-methyl-, hydrochloride, (5α)-; (2) 4,5α-Epoxy-3,14-dihydroxy-17-methylmorphinan-6-one hydrochloride. CAS-357-07-3; CAS-76-41-5 (oxymorphone).

Pharmacologic Category

Analgesics and Antipyretics; Opiate Agonists. (ATC-Code: N02A).

Mechanism of action

Narcotic analgesic with uses similar to those of morphine. A semisynthetic derivative of morphine (phenanthrene derivative) and chemically closely related to hydromorphone. Shares actions of opiate agonists. Precise mechanism of action not fully elucidated. Opiate agonists act at several CNS sites, involving several neurotransmitter systems to produce analgesia. Opiate agonists act at specific receptor binding sites in CNS and other tissues. Agonist activity at opiate μ- or κ-receptor can result in analgesia, miosis, and/or decreased body temperature. Agonist activity at μ-receptor can also result in suppression of opiate withdrawal (and antagonist activity can result in precipitation of withdrawal). Respiratory depression may be mediated by μ-receptors, possibly μ~2~-receptors (which may be distinct from μ~1~-receptors involved in analgesia). κ- and δ-receptors may also be involved in respiratory depression.

Therapeutic use

Moderate-to-severe pain and preoperatively as sedative and/or supplement to anesthesia.

Pregnancy and lactiation implications

Teratogenic effects not observed in animals; however, decreased fetal weight, decreased litter size, increased stillbirths, and increased neonatal death noted. Chronic opioid use during pregnancy may lead to physical dependency in infant and withdrawal syndrome in neonate. Administration during labor may cause neonatal respiratory depression. Use of oxymorphone tablets and extended-release tablets not recommended during or immediately prior to labor. Excretion in breast milk unknown (use caution).

Unlabeled use


Hypersensitivity to oxymorphone, other morphine analogs (phenanthrene derivatives), or any component of the formulation. Paralytic ileus (known or suspected). Increased intracranial pressure. Moderate-to-severe hepatic impairment. Severe respiratory depression (unless in monitored setting with resuscitative equipment). Acute/severe bronchial asthma. Hypercarbia. Pregnancy (prolonged use or high doses at term). Extended-release preparation contraindicated in management of immediate postoperative pain (first 12-24 hours following surgery), in mild pain, and in patients expected to require analgesia for short period of time. Parenteral use contraindicated in treatment of pulmonary edema resulting from chemical respiratory irritant.

Warnings and precautions

May cause CNS depression (caution in CNS depression or coma). Effects may be potentiated when used with other sedative drugs or ethanol. Use with caution in history of drug abuse or acute alcoholism (potential for drug dependency exists; tolerance, psychological and physical dependence may occur with prolonged use). Use with extreme caution with head injury, intracranial lesions, or elevated intracranial pressure (exaggerated elevation of intracranial pressure may occur). May cause hypotension (caution if hypovolemia, cardiovascular disease (including acute myocardial infarction), or drugs which may exaggerate hypotensive effects). Use with caution in hypersensitivity reactions to other phenanthrene-derivative opioid agonists (codeine, hydrocodone, hydromorphone, levorphanol, oxymorphone). May obscure diagnosis or clinical course of acute abdominal conditions. Use with caution in adrenal insufficiency, including Addison’s disease, and in biliary tract dysfunction; acute pancreatitis may cause constriction of sphincter of Oddi, in mild hepatic dysfunction (contraindicated in moderate-to-severe impairment). Use with caution in morbidly obese patients, in prostatic hyperplasia and/or urinary stricture, in renal impairment, and in pre-existing respiratory compromise (hypoxia and/or hypercapnia), chronic obstructive pulmonary disease or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function (critical respiratory depression may occur). Use with caution in thyroid dysfunction, in debilitated patients (higher risk for critical respiratory depression), and in the elderly (may be more sensitive to adverse effects). Extended release oral formulation not suitable for use as «as needed» analgesic. Tablets should not be broken, chewed, dissolved, or crushed (should be swallowed whole). Extended release formulation intended for use in long-term, continuous management of moderate-to-severe chronic pain; not indicated for use in immediate postoperative period (12-24 hours). Coingestion of ethanol or ethanol-containing medications with extended release formulation may result in accelerated release of drug from dosage form, abruptly increasing plasma levels, which may have fatal consequences. Concurrent use of agonist/antagonist analgesics may precipitate withdrawal symptoms and/or reduced analgesic efficacy in patients following prolonged therapy with μ-opioid agonists. Abrupt discontinuation following prolonged use may also lead to withdrawal symptoms. Some quinolones may produce false-positive urine screening result for opiates using commercially-available immunoassay kits. May cause elevation in amylase (due to constriction of sphincter of Oddi).



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