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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 -
Pain Research & Management 2020Radiotherapy is commonly used to treat cancer patients. Besides the curable effect, radiotherapy also could relieve the pain of cancer patients. However, cancer pain is... (Review)
Review
Radiotherapy is commonly used to treat cancer patients. Besides the curable effect, radiotherapy also could relieve the pain of cancer patients. However, cancer pain is gradually alleviated about two weeks after radiotherapy. In addition, cancer patients who receive radiotherapy may also suffer from pain flare or radiotherapy-induced side effects such as radiation esophagitis, enteritis, and mucositis. Pain control is reported to be inadequate during the whole course of radiotherapy (before, during, and after radiotherapy), and quality of life is seriously affected. Hence, radiotherapy is suggested to be combined with analgesic drugs in clinical guidelines. Previous studies have shown that radiotherapy combined with oxycodone hydrochloride can effectively alleviate cancer pain. In this review, we firstly presented the necessity of analgesia during the whole course of radiotherapy. We also sketched the role of oxycodone hydrochloride in radiotherapy of bone metastases and radiotherapy-induced oral mucositis. Finally, we concluded that oxycodone hydrochloride shows good efficacy and tolerance and could be used for pain management before, during, and after radiotherapy.
Topics: Analgesics, Opioid; Female; Humans; Male; Oxycodone; Pain; Pain Management; Quality of Life; Radiation Injuries
PubMed: 32089760
DOI: 10.1155/2020/7565962 -
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 -
Clinical Nurse Specialist CNS Sep 2001
Review
Topics: Administration, Inhalation; Analgesics, Opioid; Delayed-Action Preparations; Humans; Injections, Intravenous; Nursing Care; Oxycodone; Pain; Patient Compliance; Patient Education as Topic; Pharmaceutical Services; Substance-Related Disorders; Tablets
PubMed: 11855610
DOI: 10.1097/00002800-200109000-00010 -
Acta Crystallographica. Section C,... Nov 2012The title compound, (5R,9R,13S,14S,17R)-14-hydroxy-3-methoxy-17-methyl-4,5-epoxymorphinan-6-one N-oxide, C(18)H(21)NO(5), has been prepared in a diastereomerically pure...
The title compound, (5R,9R,13S,14S,17R)-14-hydroxy-3-methoxy-17-methyl-4,5-epoxymorphinan-6-one N-oxide, C(18)H(21)NO(5), has been prepared in a diastereomerically pure form by the reaction of oxycodone with 3-chloroperbenzoic acid and subsequent crystallization of the product from chloroform. The crystal packing shows that the molecule exhibits intramolecular O-H···O [D···A = 2.482 (2) Å] hydrogen bonding. In addition, there are weak intermolecular C-H...O interactions which, along with van der Waals forces, stabilize the structure. The new chiral center at the 17-position is demonstrated to be R.
Topics: Chlorobenzoates; Crystallography, X-Ray; Hydrogen Bonding; Molecular Structure; Oxycodone
PubMed: 23124457
DOI: 10.1107/S0108270112040188 -
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 -
Zhongguo Yi Xue Ke Xue Yuan Xue Bao.... Feb 2020To evaluate the value of oxycodone hydrochloride for postoperative pain management in patients undergoing patient-controlled intravenous analgesia(PCIA). The medical...
To evaluate the value of oxycodone hydrochloride for postoperative pain management in patients undergoing patient-controlled intravenous analgesia(PCIA). The medical records on postoperative pain management in our department from January 1 to June 30,2018,were retrospectively analyzed.Totally 136 patients were assigned into oxycodone,sufentanil,or morphine groups according to the opioid used in the PCIA.Patients were assessed for postoperative pain severity(scored with NRS)and adverse reactions 24,36,and 48 hours after surgery.The area under curve(AUC)was calculated. The score of pain at exercise was significantly lower in the oxycodone group(2.2±2.4)than in the sufentanil group(3.4±2.1)(=0.305,=0.0126)or the morphine group(3.4±1.7)(=0.104,=0.0277)36 hours after surgery.AUC at rest was significantly lower in the oxycodone and morphine groups than in the sufentanil group(29.00,27.00,and 40.01,respectively);in contrast,AUC at exercise was significantly lower in the oxycodone group(63.17)than in the sufentanil and morphine groups(82.00 and 80.93,respectively).The consumption of opioids was significantly higher in the sufentanil group[(37.2±16.1),(46.1±24.3),(64.4±33.4)mg]than in the oxycodone group[(20.4±14.8)(=3.571,=0.001),(24.2±16.1)(=4.63,<0.0001),(34.4±25.1)mg(=6.409,<0.0001)]or the morphine group[(16.6±11.7)(=4.233,<0.0001),(20.5±14.1)(=5.250,<0.0001),(28.8±19.0)mg(=7.354,<0.0001)]24,36,48 hours after surgery.The oxycodone group experienced less vomiting(=11.360,=0.003)and early termination of PCIA(=7.914,=0.019)compared with the other two groups. Oxycodone can be used for postoperative PCIA.It can alleviate a variety of postoperative pain,with superior analgesic efficiency and safety to sufentanil and morphine.
Topics: Analgesia, Patient-Controlled; Humans; Morphine; Oxycodone; Pain, Postoperative; Retrospective Studies; Sufentanil; Surgical Procedures, Operative
PubMed: 32131946
DOI: 10.3881/j.issn.1000-503X.11141 -
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 -
Organic Letters Dec 2014Our novel synthetic route to (-)-oxycodone, a semisynthetic opioid analgesic, features a palladium-catalyzed direct intramolecular arylation of an aryl bromide,...
Our novel synthetic route to (-)-oxycodone, a semisynthetic opioid analgesic, features a palladium-catalyzed direct intramolecular arylation of an aryl bromide, oxidative dearomatization of a dihydrophenanthrenol, formation of a benzylic quaternary carbon by an intramolecular Michael addition of a malonate moiety, and construction of the morphinan skeleton via a Hofmann rearrangement/lactamization cascade.
Topics: Analgesics, Opioid; Catalysis; Hydrocarbons, Brominated; Molecular Structure; Oxycodone; Palladium; Stereoisomerism
PubMed: 25423610
DOI: 10.1021/ol503175n -
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