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Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
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Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
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Oxycodone: new 'old' drug.

Klaus T Olkkola1, Nora M Hagelberg

  • 1Department of Anaesthesiology, Intensive Care, Emergency Care and Pain Medicine, University of Turku and Turku University Hospital, Turku, Finland. klaus.olkkola@utu.fi

Current Opinion in Anaesthesiology
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Oxycodone is a widely used opioid analgesic with predictable plasma concentrations and significant drug interactions. Individual dose titration is essential, particularly in the elderly, due to age-dependent pharmacokinetics.

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Area of Science:

  • Pharmacology
  • Pain Management
  • Drug Development

Background:

  • Oral oxycodone preparations (immediate and controlled-release) introduced in the 1990s have significantly increased clinical use and scientific interest.
  • Oxycodone is an opioid analgesic with growing importance in pain management.

Purpose of the Study:

  • To review the clinical use and scientific understanding of oxycodone.
  • To highlight recent findings on oxycodone's pharmacokinetics, bioavailability, drug interactions, and efficacy in various pain conditions.

Main Methods:

  • Review of recent clinical studies and scientific literature on oxycodone.

Main Results:

  • Oxycodone pharmacokinetics are age-dependent, necessitating individual dose titration, especially in the elderly.
  • Oxycodone exhibits good oral bioavailability with more predictable plasma concentrations compared to morphine.
  • Clinically significant drug interactions occur with agents affecting cytochrome P450 3A enzymes.
  • Oxycodone is effective for acute postoperative, cancer, visceral, and chronic nonmalignant pain.

Conclusions:

  • The clinical use of oxycodone has expanded significantly over the past decade.
  • Further research is required to fully elucidate its clinical pharmacology and potential.
  • Oxycodone remains a critical, yet not fully understood, therapeutic agent.