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Journal of Pain and Symptom Management May 2005Oxycodone has been in clinical use since 1917. Parenteral oxycodone was used mainly for the treatment of acute postoperative pain whereas combinations, for example,... (Review)
Review
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. Controlled studies have been performed in postoperative pain, cancer pain, osteoarthritis-related pain, and neuropathic pain due to postherpetic neuralgia and diabetic neuropathy. 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.
Topics: Analgesics, Opioid; Animals; Biological Availability; Drug Interactions; History, 20th Century; Humans; Liver Failure; Neoplasms; Oxycodone; Pain; Pain, Postoperative; Renal Insufficiency
PubMed: 15907646
DOI: 10.1016/j.jpainsymman.2005.01.010 -
Pharmacogenomics Apr 2021Oxycodone is a semisynthetic μ- and κ-opioid receptor with agonist with a broad scope of use including postoperative analgesia as well as control of neuropathic and... (Review)
Review
Oxycodone is a semisynthetic μ- and κ-opioid receptor with agonist with a broad scope of use including postoperative analgesia as well as control of neuropathic and cancer pain. Advantages over other opioids include prolonged duration of action, greater potency than morphine and lack of histamine release or ceiling effect. Individual responses to oxycodone can vary due to genetic differences. This review article aims to summarize the oxycodone literature and provide context on its pharmacogenomics and pharmacokinetics. The evidence for clinical effect of genetic polymorphisms on oxycodone is conflicting. There is stronger evidence linking polymorphic genetic enzymes CYP2D6 and CYP3A with therapeutic outcomes. Further, research is needed to discern all of oxycodone's metabolites and their contribution to the overall analgesic effect.
Topics: Analgesics, Opioid; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Humans; Morphine; Oxycodone; Pharmacogenetics; Polymorphism, Genetic
PubMed: 33728947
DOI: 10.2217/pgs-2020-0143 -
Journal of Pain & Palliative Care... 2004Oxycodone is among the most commonly used opioid analgesics for the relief of moderate-to-severe pain and is pharmacodynamically comparable to morphine. Oxycodone is... (Review)
Review
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. The pharmacokinetics of oral oxycodone differs from oral morphine in that it has a higher bioavailability, a slightly longer half-life, and is hepatically metabolized by cytochrome P450 rather than undergoing glucuronidation. Understanding oxycodone pharmacokinetics favors safe and effective use of this analgesic in a wide variety of patients with different levels of organ function. 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.
Topics: Administration, Oral; Aged; Analgesics, Opioid; Biological Availability; Chemistry, Pharmaceutical; Child; Cytochrome P-450 CYP2D6; Drug Interactions; Female; Half-Life; Humans; Intestinal Absorption; Male; Metabolic Clearance Rate; Oxycodone; Tissue Distribution
PubMed: 15760805
DOI: 10.1300/j354v18n04_03 -
Anesthesiology Clinics Jun 2017Oxycodone, a semisynthetic opioid analgesic, is widely used in clinical practice. Oxycodone and morphine seem to be equally effective and equipotent; however, morphine... (Review)
Review
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.
Topics: Abdominal Pain; Analgesia; Analgesia, Patient-Controlled; Analgesics, Opioid; Cancer Pain; Humans; Morphine; Oxycodone; Pain; Pain Measurement
PubMed: 28526158
DOI: 10.1016/j.anclin.2017.01.022 -
Current Opinion in Anaesthesiology Aug 2009Since the introduction of oral immediate release and controlled-release oxycodone preparations to the market in the 1990s, the clinical use and scientific interest in... (Review)
Review
PURPOSE OF REVIEW
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.
RECENT FINDINGS
Recent studies have shown that the pharmacokinetics of oxycodone are dependent on age of the patient and therefore individual titration of the dose is necessary, especially in the elderly. Oxycodone has good oral bioavailability and it produces more predictable plasma concentrations than morphine, which has a poor and more variable bioavailability. Oxycodone has clinically significant drug interactions with drugs affecting cytochrome P450 3A enzymes. Clinical studies have demonstrated that oxycodone is a useful opioid analgesic in acute postoperative pain, cancer pain, visceral pain and chronic nonmalignant pain.
SUMMARY
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.
Topics: Analgesics, Opioid; Animals; Drug Interactions; Humans; Kidney Diseases; Liver Diseases; Oxycodone
PubMed: 19369865
DOI: 10.1097/ACO.0b013e32832bc818 -
Expert Opinion on Pharmacotherapy May 2012Pain is a likely outcome of any surgical procedure. In several countries the use of oxycodone has surpassed that of morphine in postoperative pain management. (Review)
Review
INTRODUCTION
Pain is a likely outcome of any surgical procedure. In several countries the use of oxycodone has surpassed that of morphine in postoperative pain management.
AREAS COVERED
This review summarizes the recent pharmacological and clinical data on oxycodone use for postoperative pain management. The benefits and the impact oxycodone may have on outcome in different patient groups is addressed. As oxycodone is available on different pharmaceutical formulations and as a new combination product with naloxone, the different approaches that may be used with oxycodone in postoperative pain management are also reviewed.
EXPERT OPINION
The recent interest in oxycodone is based on its favorable pharmacokinetics and pharmacodynamics, especially in the central nervous system. Moreover, relatively high enteral bioavailability allows an easy switch from one drug formulation to another during the course of pain management. Oxycodone is highly effective and well tolerated in different types of surgical procedures and patient groups, from preterm to aged patients. In the future, the use of transmucosal administration and enteral oxycodone-naloxone controlled-release tablets is likely to increase, and an appropriate concurrent use of different enteral drug formulations will decrease the need for more complex administration techniques, such as intravenous patient-controlled analgesia.
Topics: Analgesics, Opioid; Chemistry, Pharmaceutical; Humans; Oxycodone; Pain, Postoperative
PubMed: 22519769
DOI: 10.1517/14656566.2012.677823 -
Pain Physician Feb 2017Opioids are the mainstay of pain management for acute postsurgical pain. Oral oxycodone is an opioid that can provide effective acute postoperative pain relief. (Review)
Review
BACKGROUND
Opioids are the mainstay of pain management for acute postsurgical pain. Oral oxycodone is an opioid that can provide effective acute postoperative pain relief.
OBJECTIVES
To evaluate the use of oral oxycodone for acute postoperative pain management.
STUDY DESIGN
This is a narrative review based on published articles searched in PubMed and Medline from 2003 to 2015 on oral oxycodone for acute postoperative pain management.
METHODS
Clinical trials related to the use of oral oxycodone for acute postoperative pain management were searched via PubMed and Medline from 2003 to 2015. The search terms used were "oral strong opioids," "postsurgical," "postoperative," "post-surgical," and "post-operative." Treatment interventions were compared for analgesic efficacy, rescue medication use, side effects, recovery, length of hospital stay, and patient satisfaction.
RESULTS
There were 26 clinical trials included in the review. Oral oxycodone showed superior postoperative analgesic efficacy compared with placebo in patients undergoing laparoscopic cholecystectomy, abdominal or pelvic surgery, bunionectomy, breast surgery, and spine surgery. When compared with intravenous opioids, oral oxycodone provided better or comparable pain relief following knee arthroplasty, spine surgery, caesarean section, laparoscopic colorectal surgery, and cardiac surgery. One study of dental postsurgery pain reported inferior pain control with oral oxycodone versus rofecoxib. (withdrawn from the US market due to cardiac safety concerns). In many studies, the demand for rescue analgesia and total opioid consumption were reduced in the oxycodone treatment arm. Patients receiving oral oxycodone experienced fewer opioid-related side effects than those on other opioids, and had a similar occurrence of postoperative nausea and vomiting as patients on placebo. Furthermore, oral oxycodone did not prolong hospital stay and was associated with lower drug costs compared with epidural and intravenous analgesics. Oxycodone administered as part of a multimodal analgesic regimen produced superior pain relief with fewer side effects and a reduced hospital stay.
LIMITATIONS
There is a limited number of randomized double blinded studies in individual surgical operations, thus making it more difficult to come up with definitive conclusions.
CONCLUSION
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.
Topics: Analgesia; Analgesics, Opioid; Clinical Trials as Topic; Female; Humans; Oxycodone; Pain Measurement; Pain, Postoperative; Pregnancy
PubMed: 28226340
DOI: No ID Found -
Journal of Opioid Management 2018The role of analgesia is crucial in the management of postoperative pain. Different combinations of oral analgesics have been proposed in the past. The... (Review)
Review
BACKGROUND
The role of analgesia is crucial in the management of postoperative pain. Different combinations of oral analgesics have been proposed in the past. The oxycodone/naloxone (OXN) combination is a recent addition and is being used by different surgical specialties. The aim of our study was to clarify the possible role, advantages, and disadvantages of OXN in the pain management of surgical patients.
METHOD
The authors retrieved the included studies after performing a systematic search in PubMed and Scopus.
RESULTS
Ten studies (six randomized controlled trials, three retrospective studies, and a prospective study) were eligible for inclusion in this review. In total, 1,996 patients were included. Six studies reported on orthopedic procedures while four studies referred to colorectal, gynecologic, cardiac, and thoracic surgery procedures, respectively. The analgesic effect of OXN was evaluated in nine out of 10 studies, where OXN showed superiority only in two out of nine studies. Postoperative bowel function was evaluated in seven out of 10 studies. Patients treated with OXN did not show any significant differences in bowel function when compared to control groups. No superiority was found regarding the possible adverse events.
CONCLUSION
Analgesia is crucial to postoperative recovery. Pain control can be achieved a combination of different analgesics, including OXN. This oral analgesic combination can have the potential to minimize side effects, such as opioid-induced constipation and optimize the recovery period.
Topics: Drug Combinations; Humans; Naloxone; Oxycodone; Pain, Postoperative
PubMed: 29508896
DOI: 10.5055/jom.2018.0429 -
The Cochrane Database of Systematic... Feb 2015Many patients with cancer experience moderate to severe pain that requires treatment with strong opioids, of which oxycodone and morphine are examples. Strong opioids... (Meta-Analysis)
Meta-Analysis Review
BACKGROUND
Many patients with cancer experience moderate to severe pain that requires treatment with strong opioids, of which oxycodone and morphine are examples. Strong opioids are, however, not effective for pain in all patients, nor are they well-tolerated by all patients. The aim of this review was to assess whether oxycodone is associated with better pain relief and tolerability than other analgesic options for patients with cancer pain.
OBJECTIVES
To assess the effectiveness and tolerability of oxycodone for pain in adults with cancer.
SEARCH METHODS
We searched the Cochrane Central Register of Controlled Trials (CENTRAL) in the Cochrane Library, MEDLINE and MEDLINE In-Process (Ovid), EMBASE (Ovid), Science Citation Index, Conference Proceedings Citation Index - Science (ISI Web of Science), BIOSIS (ISI), PsycINFO (Ovid) and PubMed to March 2014. We also searched Clinicaltrials.gov, metaRegister of Controlled Trials (mRCT), EU Clinical Trials Register and World Health Organization International Clinical Trials Registry Platform (ICTRP). We checked the bibliographic references of relevant identified studies and contacted the authors of the included studies to find additional trials not identified by the electronic searches. No language, date or publication status restrictions were applied to the search.
SELECTION CRITERIA
We included randomised controlled trials (parallel-group or cross-over) comparing oxycodone (any formulation or route of administration) with placebo or an active drug (including oxycodone) for cancer background pain in adults.
DATA COLLECTION AND ANALYSIS
Two authors independently extracted study data (study design, participant details, interventions and outcomes) and independently assessed the quality of the included studies according to standard Cochrane methodology. Where possible, we meta-analysed the pain intensity data using the generic inverse variance method, otherwise these data were summarised narratively along with the adverse event and patient preference data. The overall quality of the evidence for each outcome was assessed according to the GRADE approach.
MAIN RESULTS
We included 17 studies which enrolled/randomised 1390 patients with 1110 of these analysed for efficacy and 1170 for safety. The studies examined a number of different drug comparisons. Four studies compared controlled release (CR) oxycodone to immediate release (IR) oxycodone and pooled analysis of three of these studies showed that the effects of CR and IR oxycodone on pain intensity after treatment were similar (standardised mean difference (SMD) 0.1, 95% confidence interval (CI) -0.06 to 0.26; low quality evidence). This was in line with the finding that none of the included studies reported differences in pain intensity between the treatment groups. Three of the four studies also found similar results for treatment acceptability and adverse events in the IR and CR groups; but one study reported that, compared to IR oxycodone, CR oxycodone was associated with significantly fewer adverse events.Six studies compared CR oxycodone to CR morphine and pooled analysis of five of these studies indicated that pain intensity did not differ significantly between the treatments (SMD 0.14, 95% CI -0.04 to 0.32; low quality evidence). There were no marked differences in adverse event rates, treatment acceptability or quality of life ratings.The remaining seven studies either compared oxycodone in various formulations or compared oxycodone to different alternative opioids. None of them found any clear superiority or inferiority of oxycodone for cancer pain, neither as an analgesic agent nor in terms of adverse event rates and treatment acceptability.The quality of this evidence base was limited by the risk of bias of the studies and by small sample sizes for many outcomes. Random sequence generation and allocation concealment were under-reported, and the results were substantially compromised by attrition with data missing from more than 20% of the enrolled/randomised patients for efficacy and from more than 15% for safety.
AUTHORS' CONCLUSIONS
Overall, the data included within this review suggest that oxycodone offers similar levels of pain relief and adverse events to other strong opioids including morphine, which is commonly considered the gold standard strong opioid. Our conclusions are consistent with other recent 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 will be justified. This means that for clinical purposes oxycodone or morphine can be used as first line oral opioids for relief of cancer pain.
Topics: Analgesics, Opioid; Delayed-Action Preparations; Drug Administration Schedule; Humans; Morphine; Neoplasms; Oxycodone; Pain; Pain Management; Randomized Controlled Trials as Topic
PubMed: 25723351
DOI: 10.1002/14651858.CD003870.pub5 -
Expert Review of Neurotherapeutics May 2017As a consequence of greater prescription opioid utilization, there has been the parallel increase in misuse, abuse, and overdose, which are serious risks. Associated new... (Review)
Review
As a consequence of greater prescription opioid utilization, there has been the parallel increase in misuse, abuse, and overdose, which are serious risks. Associated new formulations may be safer. Areas covered: The introduction of abuse-deterrent opioid formulations and continuous programs to improve opioid prescribing practices may limit the opioid abuse and its consequences. Oxycodone extended release capsules are an extended-release (ER), microsphere-in-capsule abuse-deterrent-formulation designed to retain its extended-release properties following tampering or misuse (e.g., chewing, crushing). Studies have reported that this preparation is efficacious in patients with low back pain, less attractive for illicit use, and an option for patients who have difficulty swallowing and erroneously crush their medication. Expert commentary: Preliminary data regarding oxycodone extended release capsules are encouraging. However, more data in different populations are necessary to confirm initial observations, and comparison should be performed with active substances.
Topics: Analgesics, Opioid; Capsules; Child; Chronic Pain; Delayed-Action Preparations; Humans; Oxycodone
PubMed: 28277802
DOI: 10.1080/14737175.2017.1302331