Oxymorphone Hydrochloride

• Moderate to severe acute pain:
• Short-term management when alternative treatments are inadequate
• Chronic pain management:
• Severe chronic pain requiring continuous, around-the-clock opioid analgesia
• Postoperative pain control:
• Particularly in hospital settings with injectable form
• Off-label uses:
• Cancer-related pain management
• Pain refractory to other opioids

Oral Immediate-Release (IR) Tablets:

• Adults: Initial dose typically 5 mg every 4 to 6 hours as needed for pain.
• Titrate carefully based on pain relief and tolerability.

Oral Extended-Release (ER) Tablets:

• Adults opioid-tolerant patients only.
• Starting dose varies; typically 10 mg every 12 hours.
• Dose adjustments individualized for efficacy and side effects.

Injectable Form:

• Adults: 1–4 mg every 4 to 6 hours as needed, administered IV, IM, or SC.
• Use caution with titration.

Special Populations:

• Elderly: Start at lower doses; monitor closely due to increased sensitivity.
• Renal impairment: Use cautiously; may require dose reduction.
• Hepatic impairment: Use with caution; metabolism may be affected.
• Pediatrics: Safety and efficacy not established.

Oxymorphone hydrochloride is a potent opioid agonist primarily acting on the mu-opioid receptors in the central nervous system. Activation of these receptors inhibits ascending pain pathways, alters the perception and response to pain, and produces generalized CNS depression. This action results in effective analgesia.

• Absorption: Oral bioavailability ~10-11% due to extensive first-pass metabolism.
• Distribution: Widely distributed; crosses blood-brain barrier.
• Metabolism: Mainly hepatic via glucuronidation to active and inactive metabolites.
• Elimination half-life: Approximately 7–8 hours (oral ER).
• Excretion: Primarily renal as metabolites and unchanged drug.
• Onset: Oral IR onset ~15–30 minutes; injectable onset within minutes.
• Duration: Oral ER lasts up to 12 hours; IR shorter duration (~3–6 hours).

• Pregnancy: Category C. Risk of fetal harm if used chronically or in high doses. Use only if benefits outweigh risks.
• Lactation: Excreted in breast milk; may cause sedation or respiratory depression in infant. Breastfeeding not recommended during treatment.

• Opioid analgesic
• Schedule II controlled substance

• Known hypersensitivity to oxymorphone or opioid analgesics
• Significant respiratory depression without resuscitative equipment
• Acute or severe bronchial asthma or hypercarbia
• Paralytic ileus or gastrointestinal obstruction
• Concurrent use with MAO inhibitors or within 14 days of use

• Risk of respiratory depression, especially in opioid-naïve patients
• Potential for addiction, abuse, and misuse
• Risk of accidental overdose and death
• CNS depression when combined with other CNS depressants (e.g., benzodiazepines)
• Use with caution in patients with head injury, increased intracranial pressure, or impaired hepatic/renal function
• Monitor for withdrawal symptoms upon discontinuation
• Not recommended in children under 18 years

Common:

• Nausea, vomiting
• Constipation
• Drowsiness, dizziness
• Headache
• Sweating

Serious:

• Respiratory depression
• Hypotension
• Bradycardia
• Seizures (rare)
• Anaphylaxis (rare)

• CNS depressants: Additive sedation and respiratory depression (e.g., benzodiazepines, alcohol)
• MAO inhibitors: Risk of severe reactions; contraindicated
• CYP3A4 inhibitors/inducers: May alter oxymorphone levels slightly, but primarily metabolized by glucuronidation, so less affected
• Other opioids: Additive effects increase risk of adverse events

• Updated opioid prescribing guidelines emphasize cautious initiation, lowest effective dose, and close monitoring for abuse and respiratory depression
• FDA boxed warning highlights risks of addiction, overdose, and concomitant use with benzodiazepines
• Emphasis on risk evaluation and mitigation strategies (REMS) for opioids

• Store at 20°C to 25°C (68°F to 77°F)
• Protect from moisture and light
• Keep out of reach of children
• Dispose of unused medication according to local regulations