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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 -
Cellular and Molecular Neurobiology Jul 2021It is estimated that nearly a third of people who abuse drugs started with prescription opioid medicines. Approximately, 11.5 million Americans used prescription drugs... (Review)
Review
It is estimated that nearly a third of people who abuse drugs started with prescription opioid medicines. Approximately, 11.5 million Americans used prescription drugs recreationally in 2016, and in 2018, 46,802 Americans died as the result of an opioid overdose, including prescription opioids, heroin, and illicitly manufactured fentanyl (National Institutes on Drug Abuse (2020) Opioid Overdose Crisis. https://www.drugabuse.gov/drugs-abuse/opioids/opioid-overdose-crisis . Accessed 06 June 2020). Yet physicians will continue to prescribe oral opioids for moderate-to-severe pain in the absence of alternative therapeutics, underscoring the importance in understanding how drug choice can influence detrimental outcomes. One of the opioid prescription medications that led to this crisis is oxycodone, where misuse of this drug has been rampant. Being one of the most highly prescribed opioid medications for treating moderate-to-severe pain as reflected in the skyrocketed increase in retail sales of 866% between 1997 and 2007, oxycodone was initially suggested to be less addictive than morphine. The false-claimed non-addictive formulation of oxycodone, OxyContin, further contributed to the opioid crisis. Abuse was often carried out by crushing the pills for immediate burst release, typically by nasal insufflation, or by liquefying the pills for intravenous injection. Here, we review oxycodone pharmacology and abuse liability as well as present the hypothesis that oxycodone may exhibit a unique pharmacology that contributes to its high likability and abuse susceptibility. We will discuss various mechanisms that likely contribute to the high abuse rate of oxycodone including clinical drug likability, pharmacokinetics, pharmacodynamics, differences in its actions within mesolimbic reward circuity compared to other opioids, and the possibility of differential molecular and cellular receptor interactions that contribute to its selective effects. We will also discuss marketing strategies and drug difference that likely contributes to the oxycodone opioid use disorders and addiction.
Topics: Analgesics, Opioid; Animals; Behavior, Addictive; Humans; Opioid Epidemic; Opioid-Related Disorders; Oxycodone; Pain; Reward
PubMed: 33245509
DOI: 10.1007/s10571-020-01013-y -
Tidsskrift For Den Norske Laegeforening... May 2020Inadequate pain relief after caesarean section is a topic of international concern. At Oslo University Hospital, Ullevål, patients receive bupivacaine infiltration...
BACKGROUND
Inadequate pain relief after caesarean section is a topic of international concern. At Oslo University Hospital, Ullevål, patients receive bupivacaine infiltration local anaesthesia as well as oral paracetamol, ibuprofen and oxycodone for pain management during the first 24 hours post-surgery. The aim of this study was to survey pain after acute and elective caesarean sections in our department.
MATERIAL AND METHOD
The study included 50 patients who had undergone acute or elective caesarean section. Pain intensity on an 11-point numerical scale, pain duration, degree of mobilisation, and use of analgesia on postoperative day one were obtained from patient interviews and medical records.
RESULTS
Inadequate pain relief was defined as an average pain intensity of ≥ 4 and was reported by 34 patients (68 %). Total opioid consumption on postoperative day one exceeded 40 mg oral oxycodone equivalents in 28 patients. Of these, seven patients received more than 60 mg oral oxycodone equivalents.
INTERPRETATION
A large proportion of patients had high pain intensity and opioid requirement in the first 24 hours after caesarean section.
Topics: Analgesics, Opioid; Cesarean Section; Female; Humans; Oxycodone; Pain Management; Pain, Postoperative; Pregnancy
PubMed: 32378860
DOI: 10.4045/tidsskr.19.0506 -
Current Opinion in Nephrology and... Nov 2020This review evaluates current recommendations for pain management in chronic kidney disease (CKD) and end-stage kidney disease (ESKD) with a specific focus on evidence...
PURPOSE OF REVIEW
This review evaluates current recommendations for pain management in chronic kidney disease (CKD) and end-stage kidney disease (ESKD) with a specific focus on evidence for opioid analgesia, including the partial agonist, buprenorphine.
RECENT FINDINGS
Recent evidence supports the use of physical activity and other nonpharmacologic therapies, either alone or with pharmacological therapies, for pain management. Nonopioid analgesics, including acetaminophen, topical analgesics, gabapentinoids, serotonin-norepinephrine reuptake inhibitors, and TCA may be considered based on pain cause and type, with careful dose considerations in kidney disease. NSAIDs may be used in CKD and ESKD for short durations with careful monitoring. Opioid use should be minimized and reserved for patients who have failed other therapies. Opioids have been associated with increased adverse events in this population, and thus should be used cautiously after risk/benefit discussion with the patient. Opioids that are safer to use in kidney disease include oxycodone, hydromorphone, fentanyl, methadone, and buprenorphine. Buprenorphine appears to be a promising and safer option due to its partial agonism at the mu opioid receptor.
SUMMARY
Pain is poorly managed in patients with kidney disease. Nonpharmacological and nonopioid analgesics should be first-line approaches for pain management. Opioid use should be minimized with careful monitoring and dose adjustment.
Topics: Analgesics, Opioid; Buprenorphine; Fentanyl; Humans; Hydromorphone; Kidney Failure, Chronic; Oxycodone; Pain; Pain Management; Receptors, Opioid, mu; Renal Insufficiency, Chronic
PubMed: 32941189
DOI: 10.1097/MNH.0000000000000646 -
Ugeskrift For Laeger Sep 2023This review summarises the current knowledge of the effects of morphine and oxycodone. The analgesic effect is estimated to be equal. However, the relative potency of...
This review summarises the current knowledge of the effects of morphine and oxycodone. The analgesic effect is estimated to be equal. However, the relative potency of oxycodone is variably higher which increases the risk of over- and underdosing. The time to onset of analgesia following intravenous or oral administration of oxycodone is shorter than the one of morphine. This, among other factors, may lead to a higher risk of addictive behaviour.
PubMed: 37772499
DOI: No ID Found -
CMAJ : Canadian Medical Association... Nov 2021
Topics: Accidents, Traffic; Acetaminophen; Analgesics, Opioid; Anxiety; Drug Combinations; Family Relations; Female; Humans; Musculoskeletal Pain; Opioid-Related Disorders; Oxycodone; Professional-Patient Relations; Self Concept
PubMed: 34782383
DOI: 10.1503/cmaj.211817