What are the properties of intravenous (IV) Oxycodone (oxycodone hydrochloride)?

Properties of Intravenous (IV) Oxycodone

IV oxycodone is a strong opioid analgesic with rapid onset of action, high bioavailability (60-87%), and a half-life of 3-5 hours, making it an effective alternative to IV morphine for managing moderate to severe pain with potentially fewer side effects. 1, 2

Pharmacokinetic Properties

• Absorption and Bioavailability:

  • IV administration provides 100% bioavailability (compared to 60-87% with oral route) 1
  • Faster onset of pain relief compared to oral administration 3
  • More predictable pharmacokinetics than other routes 3

• Distribution:

  • Volume of distribution: 2.6 L/kg following IV administration 1
  • Plasma protein binding: approximately 45% 1, 2
  • Can be found in breast milk (important consideration for nursing mothers) 1

• Metabolism:

  • Primarily metabolized in the liver 1, 2
  • Major metabolic pathways:
    • N-dealkylation to noroxycodone (catalyzed by CYP3A4)
    • O-demethylation to oxymorphone (catalyzed by CYP2D6) 1
  • More predictable metabolism than morphine, making titration easier 2

• Elimination:

  • Half-life: 3-5 hours (shorter than morphine) 1, 2
  • Primarily excreted via kidneys 1
  • Stable plasma levels reached within 24 hours (vs. 2-7 days for morphine) 2

Pharmacodynamic Properties

• Receptor Activity:

  • Primary action at μ-opioid receptors
  • Also acts on κ- and δ-opioid receptors 2, 4
  • The κ-receptor activity may contribute to its efficacy in visceral pain 4

• Analgesic Potency:

  • Comparable to morphine with IV potency ratio of approximately 1:1 2, 5
  • For oral conversion, the ratio is approximately 1:2 (oral oxycodone:oral morphine) 2

• Onset and Duration:

  • Rapid onset of action when administered IV 3
  • Duration depends on dosing regimen and patient factors

Clinical Applications

• Indications:

  • Moderate to severe acute pain 6
  • Postoperative pain management 3
  • Cancer pain 6
  • Alternative to morphine in patients with poor morphine tolerance 6

• Dosing Considerations:

  • For IV titration in severe pain, can be used similarly to IV hydromorphone 6
  • When converting from other opioids, equianalgesic dosing tables should be used 6
  • For IV to transdermal fentanyl conversion: 25 mcg/h transdermal fentanyl ≈ 1.5 mg/d IV oxycodone 6

Advantages Over Other IV Opioids

• More predictable metabolism than morphine 2
• Potentially fewer side effects than morphine (less nausea, hallucinations, and pruritus) 2
• May provide better pain control in certain pain types, particularly visceral pain 4
• Can be easily converted to oral formulation when transitioning from IV to oral therapy 3

Side Effects and Safety Considerations

• Common Side Effects:

  • Similar to other opioids: nausea, constipation, drowsiness 2
  • Less common: vomiting, pruritus, dizziness 2
  • Side effects typically decrease over time 2

• Special Populations:

  • Renal Impairment: Use with caution as drug is substantially excreted by kidneys 1
  • Hepatic Impairment: Clearance may decrease; dose adjustment may be required 1
  • Elderly: No specific dose adjustment needed based on age alone, but consider starting at lower doses due to potential comorbidities 1

• Contraindications and Precautions:

  • Similar precautions as with other strong opioids 5
  • Risk of respiratory depression increases with higher doses 1
  • Potential for abuse similar to morphine 5

Practical Considerations for IV Administration

• IV oxycodone provides faster pain relief than oral administration, with similar efficacy to IV morphine after 30 minutes 7
• When IV access is difficult or delayed, oral oxycodone solution (0.125 mg/kg) can be considered as an alternative to IV morphine (0.1 mg/kg) 7
• For patients requiring rapid pain control in the emergency department, IV oxycodone can be used as part of a suggested approach to acute pain management 6

IV oxycodone represents an important option in the arsenal of pain management, particularly when rapid onset, predictable pharmacokinetics, and potentially fewer side effects than morphine are desired.