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Created February 8, 2021, last updated almost 4 years ago.
Collection: 138, Score: 1010, Trend score: 0, Read count: 1434, Articles count: 9, Created: 2021-02-08 09:40:06 UTC. Updated: 2021-02-08 10:10:54 UTC.Notes
Oxycodone is a semi-synthetic opioid commonly used as an oral, rectal or intravenous analgesic (subcutaneous, intramuscular & intranasal also possible). Trade names include Endone™, OxyContin™ and OxyNorm™.
A. Physiochemistry
- Semi-synthetic opioid; thebaine derivative. First synthesised in 1916.
B. Pharmacokinetics
- Dose
- Oxycodone po conversion from morphine IV 2:1 (oxycodone:morph).
- (NB: oral to IV morphine 3:1)
- 10 mg of oral oxycodone is equivalent to 20 mg of oral morphine.
- 10 mg of oral oxycodone is equivalent to 5 mg of IV/IM morphine.
- 10-15 mg of parenteral oxycodone (IV/IM) is equivalent to 10-15 mg parenteral morphine (ie. morphine up to 50% more potent)
- Absorption - orally up to 87%
- Distribution - 2.6 L/kg
- Protein binding
- Onset - within 10-15 min orally, peak 45-60 minutes; Offset ~2-3h.
- Metabolism - ß1/2 ~3-4hrs, metabolised principally to noroxycodone, noroxymorphone and oxymorphone (p450 system). Oxymorphone has some activity
- Clearance - 0.8 L/min; predominately renally excreted.
C. Pharmacodynamics
- Oxycodone is a full opioid agonist with no antagonist properties whose principal therapeutic action is analgesia.
- It has affinity for kappa, mu and delta opiate receptors in the brain and spinal cord.
- Oxycodone is similar to morphine in its action. Other pharmacological actions of oxycodone are in the central nervous system (respiratory depression, antitussive, anxiolytic, sedative and miosis), smooth muscle (constipation, reduction in gastric, biliary and pancreatic secretions, spasm of sphincter of Oddi and transient elevations in serum amylase) and cardiovascular system (release of histamine and/or peripheral vasodilation, possibly causing pruritus, flushing, red eyes, sweating and/or orthostatic hypotension).
- Strong potentially for tolerance, dependence and abuse.
Daniel Jolley
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Collected Articles
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Oxycodone is among the most commonly used opioid analgesics for the relief of moderate-to-severe pain and is pharmacodynamically comparable to morphine. Oxycodone is available in the United States in oral dosage forms and controlled-release tablets. Studies have demonstrated marked interindividual variation in the pharmacokinetics of oxycodone. ⋯ A MEDLINE search was conducted to identify literature published between 1966 and May 2004 relevant to the pharmacokinetics of oxycodone. These publications were reviewed and the literature summarized regarding unique and clinically important elements of oxycodone disposition including its absorption profile (immediate release, controlled release, rectal administration, and intranasal administration), distribution, and its metabolism/excretion. Special populations, including children and those with liver/renal failure, have a unique oxycodone pharmacokinetic profile that must be taken into account in order to maximize analgesic efficacy and reduce the risk of adverse events.
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Since the introduction of oral immediate release and controlled-release oxycodone preparations to the market in the 1990s, the clinical use and scientific interest in oxycodone has increased greatly. ⋯ The availability of oxycodone preparations has increased its clinical use exponentially during the last decade. Further clinical studies are still needed to fully understand its clinical pharmacology. Oxycodone is still a new 'old' drug whose pharmacology and clinical potential is not yet fully understood.
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Oxycodone has been in clinical use since 1917. Parenteral oxycodone was used mainly for the treatment of acute postoperative pain whereas combinations, for example, oxycodone and acetaminophen, were used for moderate pain. Since the introduction of controlled-release oxycodone, it has been used to manage cancer-related pain and chronic non-cancer-related pain problems. ⋯ The pharmacodynamic effects of oxycodone are typical of a mu-opioid agonist. Oxycodone closely resembles morphine but it has some distinct differences, particularly in its pharmacokinetic profile. Being an old drug, the basic pharmacology of oxycodone has been a neglected field of research.
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Opioids are the mainstay of pain management for acute postsurgical pain. Oral oxycodone is an opioid that can provide effective acute postoperative pain relief. ⋯ Oral oxycodone appears to offer safe and effective postoperative analgesia, and is a well-accepted and reasonable alternative to standard intravenous opioid analgesics.Key words: Postoperative, pain, analgesia, oral oxycodone, opioid.
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Oxycodone, a semisynthetic opioid analgesic, is widely used in clinical practice. Oxycodone and morphine seem to be equally effective and equipotent; however, morphine is 10 times more potent than oxycodone when given epidurally. This article provides an updated review of the basic pharmacology of oxycodone with a special focus on pharmacokinetic/pharmacodynamics properties. The controversy regarding oxycodone-mediated effects for visceral pain via agonism and the possible role of peripheral opioid analgesia are discussed in the present investigation in an attempt to propose a plausible explanation to the perplexing question of oxycodone analgesia.
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Many people with cancer experience moderate to severe pain that requires treatment with strong opioids, such as oxycodone and morphine. Strong opioids are, however, not effective for pain in all people, neither are they well-tolerated by all people. The aim of this review was to assess whether oxycodone is associated with better pain relief and tolerability than other analgesic options for adults with cancer pain. This is an updated version of the original Cochrane review published in 2015, Issue 2 on oxycodone for cancer-related pain. ⋯ The conclusions have not changed since the previous version of this review. The data suggest that oxycodone offers similar levels of pain relief and overall adverse events to other strong opioids including morphine. Although we identified a clinically insignificant benefit on pain relief in favour of CR morphine over CR oxycodone, this did not persist following sensitivity analysis and so we do not consider this important. However, in this updated analysis, we found that hallucinations occurred less often with CR oxycodone than with CR morphine, but the quality of this evidence was very low so this finding should be treated with utmost caution. Our conclusions are consistent with other reviews and suggest that while the reliability of the evidence base is low, given the absence of important differences within this analysis it seems unlikely that larger head to head studies of oxycodone versus morphine are justified, although well-designed trials comparing oxycodone to other strong analgesics may well be useful. For clinical purposes, oxycodone or morphine can be used as first-line oral opioids for relief of cancer pain in adults.
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This is an update of an earlier review that considered both neuropathic pain and fibromyalgia (Issue 6, 2014), which has now been split into separate reviews for the two conditions. This review considers neuropathic pain only.Opioid drugs, including oxycodone, are commonly used to treat neuropathic pain, and are considered effective by some professionals. Most reviews have examined all opioids together. This review sought evidence specifically for oxycodone, at any dose, and by any route of administration. Separate reviews consider other opioids. ⋯ There was only very low quality evidence that oxycodone (as oxycodone MR) is of value in the treatment of painful diabetic neuropathy or postherpetic neuralgia. There was no evidence for other neuropathic pain conditions. Adverse events typical of opioids appeared to be common.
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The use of prescription opioid medications has increased greatly in the United States during the past two decades; in 2010, there were 16,651 opioid-related deaths. In response, hundreds of federal, state, and local interventions have been implemented. We describe trends in the diversion and abuse of prescription opioid analgesics using data through 2013. ⋯ Postmarketing surveillance indicates that the diversion and abuse of prescription opioid medications increased between 2002 and 2010 and plateaued or decreased between 2011 and 2013. These findings suggest that the United States may be making progress in controlling the abuse of opioid analgesics. (Funded by the Denver Health and Hospital Authority.).
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Curr Pain Headache Rep · Feb 2019
Oxycodone's Unparalleled Addictive Potential: Is it Time for a Moratorium?
Oxycodone possesses pharmacologic qualities that render it disproportionately liable to abuse and addiction compared to other commonly used opioids.
pearl