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https://www.readbyqxmd.com/read/28526158/revisiting-oxycodone-analgesia-a-review-and-hypothesis
#1
REVIEW
Xiulu Ruan, Ken F Mancuso, Alan D Kaye
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...
June 2017: Anesthesiology Clinics
https://www.readbyqxmd.com/read/28523735/variability-in-prescription-opioid-intake-and-reinforcement-amongst-129-substrains
#2
Susan M Jimenez, Aiden F Healy, Michal A Coelho, Chelsea N Brown, Tod E Kippin, Karen K Szumlinski
Opioid abuse in the United States has reached epidemic proportions, with treatment admissions and deaths associated with prescription opioid abuse quadrupling over the past 10 years. Although genetics are theorized to contribute substantially to inter-individual variability in the development, severity, and treatment outcomes of opioid abuse/addiction, little direct preclinical study has focused on the behavioral genetics of prescription opioid reinforcement and drug-taking. Herein, we employed different 129 substrains of mice currently available from The Jackson Laboratory (129S1/SvlmJ, 129X1/SvJ, 129S4/SvJaeJ and 129P3/J) as a model system of genetic variation and assayed mice for oral opioid intake and reinforcement, as well as behavioral and somatic signs of dependence...
May 19, 2017: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/28516342/pharmacokinetic-bioequivalence-studies-of-an-extended-release-oxycodone-hydrochloride-tablet-in-healthy-japanese-subjects-under-fasting-and-fed-conditions-without-an-opioid-antagonist
#3
Kaoru Toyama, Hidetoshi Furuie, Kana Kuroda, Hitoshi Ishizuka
Oxycodone is a semisynthetic opioid used for the treatment of moderate to severe pain. Two separate studies were conducted to assess the pharmacokinetic bioequivalence of a newly formulated oxycodone hydrochloride extended-release tablet to a marketed oxycodone product in Japan under fasting and fed conditions. Each study was a randomized, open-label, single-dose, single-center, two-period, two-way crossover study. Healthy male Japanese subjects received the oxycodone 10-mg products under fasting and fed conditions...
May 17, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28515426/tolerability-of-opioid-analgesia-for-chronic-pain-a-network-meta-analysis
#4
Zengdong Meng, Jing Yu, Michael Acuff, Chong Luo, Sanrong Wang, Lehua Yu, Rongzhong Huang
Aim of this study was to study the tolerability of opioid analgesia by performing a network meta-analysis (NMA) of randomized-controlled trials (RCTs) which investigated effectiveness of opioids for the management of chronic pain. Research articles reporting outcomes of RCT/s comparing 2 or more opioid analgesics for the management of chronic pain were obtained by database search. Bayesian NMAs were performed to combine direct comparisons between treatments with that of indirect simulated evidence. Study endpoints were: incidence of adverse events, incidence of constipation, trial withdrawal rate, and patient satisfaction with treatment...
May 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28496358/analgesic-efficacy-adverse-effects-and-safety-of-oxycodone-administered-as-continuous-intravenous-infusion-in-patients-after-total-hip-arthroplasty
#5
Bogumił Olczak, Grzegorz Kowalski, Wojciech Leppert, Iwona Zaporowska-Stachowiak, Katarzyna Wieczorowska-Tobis
BACKGROUND: Total hip arthroplasty (THA) causes extensive tissue damage and severe pain. This study aimed to assess the analgesic efficacy, adverse effects (AEs), and safety of continuous intravenous (iv) oxycodone infusion with ketoprofen (injected into the iv line) in patients after THA, and to assay serum oxycodone levels. PATIENTS AND METHODS: Fourteen patients, aged 59‒82 years with American Society of Anesthesiologists (ASA) classification I or III, underwent THA with intrathecal analgesia and sedation induced by iv propofol...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28485763/dynamiken-i-f%C3%A3-rskrivningen-av-opioider-i-sverige-2000%C3%A2-2015-markanta-omf%C3%A3-rdelningar-inom-opioidgruppen-men-ingen-%C3%A2-epidemi%C3%A2
#6
Emmanuel Bäckryd, Markus Heilig, Mikael Hoffmann
Opioid prescription changes in Sweden 2000-2015 In contrast to the well-established »opioid epidemic« in the US, very little is known about how the prescription of opioids in Sweden has developed during the last decade. Aggregated data from the open Statistical database of the Swedish Board of Health and Welfare were analyzed descriptively. The yearly prevalence of opioid prescription did not change 2006-2015, but there were dramatic shifts in the choice of opioids. During this period, dextropropoxyphene was pulled off the market...
May 2, 2017: Läkartidningen
https://www.readbyqxmd.com/read/28481682/acute-impairing-effects-of-morphine-related-to-driving-a-systematic-review-of-experimental-studies-to-define-blood-morphine-concentrations-related-to-impairment-in-opioid-na%C3%A3-ve-subjects
#7
Maren Cecilie Strand, Marianne Arnestad, Bente Fjeld, Jørg Mørland
OBJECTIVE: To look for dose- and concentration-effect relationships in experimental studies on single-dose administration of morphine on traffic relevant behavioral tests by a systematic literature review, and possibly to see if a dose/concentration could be defined, below which few or no tests would be affected. METHODS: Searches for corresponding literature were conducted using MEDLINE, EMBASE, and PsycINFO, throughout March of 2016. The search strategy consisted of words colligated to cognitive- and psychomotor functions of relevance to driving, in relation to morphine administration...
May 8, 2017: Traffic Injury Prevention
https://www.readbyqxmd.com/read/28474563/opioids-and-the-blood-brain-barrier-a-dynamic-interaction-with-consequences-on-drug-disposition-in-brain
#8
Catarina Chaves, Fernando Remião, Salvatore Cisterninoa, Xavier Declèves
Opioids are widely used in pain management whose effects are due to binding to classical opioid receptors and/or Toll-like receptors (TLR) present at the central nervous system (CNS). At the blood-brain barrier (BBB), several influx and/or efflux transporters are expressed, such as the ATP-binding cassette (ABC) P-glycoprotein (P-gp, ABCB1), Breast Cancer Resistance Protein (BCRP, ABCG2) and multidrug resistance-associated proteins (MRP, ABCC) transporters, and solute carrier transporters (SLC), and are responsible for the transport of many xenobiotics from the brain into the bloodstream or vice versa...
May 3, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28474460/long-term-efficacy-and-safety-of-oxycodone-naloxone-prolonged-release-formulation-up-to-180-90-mg-daily-results-of-the-open-label-extension-phase-of-a-phase-iii-multicenter-multiple-dose-randomized-controlled-study
#9
D Dupoiron, A Stachowiak, O Loewenstein, A Ellery, W Kremers, B Bosse, M Hopp
BACKGROUND: The inclusion of naloxone with oxycodone in a fixed combination prolonged-release formulation (OXN PR) improves bowel function compared with oxycodone (Oxy) alone without compromising analgesic efficacy. In a recent 5-week, randomized, double-blind comparative trial of OXN PR and OxyPR, it could be shown that the beneficial properties of OXN PR extend to doses up to 160/80 mg. METHODS: Bowel function, pain, quality of life (QoL) and safety of OXN PR up to 180/90 mg daily were evaluated in a 24-week open-label extension phase of the 5-week randomized comparative study in patients with non-malignant or malignant pain requiring opioids and suffering from opioid-induced constipation...
May 4, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28474345/impact-of-pharmacists-assisting-with-prescribing-and-undertaking-medication-review-on-oxycodone-prescribing-and-supply-for-patients-discharged-from-surgical-wards
#10
T Tran, S E Taylor, A Hardidge, D Findakly, P Aminian, R A Elliott
WHAT IS KNOWN AND OBJECTIVES: Overprescribing of oxycodone is a contributor to the epidemic of prescription opioid misuse and deaths. Practice models to optimize oxycodone prescribing and supply need to be evaluated. We explored the impact of pharmacist-assisted discharge prescribing and medication review on oxycodone prescribing and supply for patients discharged from surgical wards. METHODS: A retrospective audit was conducted on two surgical inpatient wards following a 16-week prospective pre- and post-intervention study...
May 5, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28470980/aprepitant-and-fosaprepitant-drug-interactions-a-systematic-review
#11
Priya Patel, J Steven Leeder, Micheline Piquette-Miller, L Lee Dupuis
AIMS: Aprepitant and fosaprepitant, commonly used for the prevention of chemotherapy-induced nausea and vomiting, alter cytochrome P450 activity. This systematic review evaluates clinically significant pharmacokinetic drug interactions with aprepitant and fosaprepitant and describes adverse events ascribed to drug interactions with aprepitant or fosaprepitant. METHODS: We systematically reviewed the literature to September 11, 2016 to identify articles evaluating drug interactions involving aprepitant/fosaprepitant...
May 4, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28470370/high-dosage-of-a-fixed-combination-oxycodone-naloxone-prolonged-release-efficacy-and-tolerability-in-patients-with-chronic-cancer-pain
#12
Francesco Amato, Silvia Ceniti, Sergio Mameli, Giovanni M Pisanu, Renato Vellucci, Vincenzo Palmieri, Leonardo Consoletti, Dorotea Magaldi, Paolo Notaro, Claudio Marcassa
PURPOSE: Opioids are associated with side effects in the treatment of moderate-to-severe chronic cancer pain. Oral combination of opioid agonist-antagonist oxycodone-naloxone (OXN-PR) attenuates gastrointestinal side effects; however, evidence on high-dose OXN-PR treatment is scant. This study evaluates the efficacy and tolerability of high-dose OXN-PR in chronic cancer pain. PATIENTS AND METHODS: This was a multicenter, prospective 60-day observation on consecutive cancer patients with uncontrolled moderate-severe chronic pain or intolerant to other analgesics, who were switched at entry visit (T0) to OXN-PR ≥80 mg daily...
May 3, 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/28467891/combined-pet-and-microdialysis-for-in-vivo-estimation-of-drug-blood-brain-barrier-transport-and-brain-unbound-concentrations
#13
Sofia Gustafsson, Jonas Eriksson, Stina Syvänen, Olof Eriksson, Margareta Hammarlund-Udenaes, Gunnar Antoni
Methods to investigate blood-brain barrier transport and pharmacologically active drug concentrations in the human brain are limited and data translation between species is challenging. Hence, there is a need to further develop the read-out of techniques like positron emission tomography (PET) for studying neuropharmacokinetics. PET has a high translational applicability from rodents to man and measures total drug concentrations in vivo. The aim of the present study was to investigate the possibility of translating total drug concentrations, acquired through PET, to unbound concentrations, resembling those measured in the interstitial fluid by microdialysis sampling...
April 30, 2017: NeuroImage
https://www.readbyqxmd.com/read/28455085/randomized-controlled-trial-of-intravenous-acetaminophen-for-postcesarean-delivery-pain-control
#14
Brie Altenau, Catrina C Crisp, C Ganga Devaiah, Donna S Lambers
BACKGROUND: Cesarean delivery is a common surgery in the United States, with 1.3 million performed during 2009.(1) Obstetricians must balance the growing concern with opioid abuse, dependence, and side effects with optimal postoperative pain control. Intravenous acetaminophen may represent an additional method to decrease the reliance on opioid medications and improve postoperative pain following cesarean delivery. OBJECTIVE: The objective of the study was to determine whether the administration of intravenous acetaminophen following routine scheduled cesarean delivery would decrease the need for narcotic medications to control postoperative pain...
April 25, 2017: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28448398/intrathecal-morphine-versus-extended-release-epidural-morphine-for-postoperative-pain-control-in-pediatric-patients-undergoing-posterior-spinal-fusion
#15
Mindy Cohen, Jeannie Zuk, Nancy McKay, Mark Erickson, Zhaoxing Pan, Jeffrey Galinkin
BACKGROUND: Posterior spinal fusion for scoliosis is one of the most painful elective pediatric surgeries. Good postoperative pain control allows early ambulation and return of ability to tolerate oral intake. Options for analgesia in this patient population are suboptimal. We hypothesized that extended-release epidural morphine (EREM) would provide better pain control and less adverse effects compared to intrathecal (IT) morphine. METHODS: The primary outcome was total IV morphine consumption during 0-48 hours postoperatively...
June 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28442580/ethanol-reversal-of-tolerance-to-the-antinociceptive-effects-of-oxycodone-and-hydrocodone
#16
Joanna C Jacob, Justin L Poklis, Hamid I Akbarali, Graeme Henderson, William L Dewey
This study compared the development of tolerance and its reversal by ethanol of two orally-bioavailable prescription opioids, oxycodone and hydrocodone, to that of morphine. Oxycodone (s.c) was significantly more potent in the mouse tail withdrawal assay than either morphine or hydrocodone. Oxycodone was also significantly more potent in this assay than hydrocodone when administered orally. Tolerance was seen following chronic subcutaneous administration of each of the three drugs and by the chronic administration of oral oxycodone, but not following the chronic oral administration of hydrocodone...
April 25, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28421874/pharmacokinetics-safety-and-tolerability-of-a-novel-tocopheryl-phosphate-mixture-oxycodone-transdermal-patch-system-a-phase-i-study
#17
Paul D Gavin, Lee S Simon, Thomas Schlagheck, Alisha J Smith, Sepehr Shakib
AIM: To characterize the pharmacokinetic profile and evaluate the safety and tolerability of a transdermal oxycodone patch containing tocopheryl phosphate mixture (TPM). PATIENTS & METHODS: Eleven healthy subjects received a single application of three TPM/oxycodone patches applied to the torso for 72 h. RESULTS: Oxycodone was detected 8.0 ± 2.7-h postpatch administration, reaching a mean maximum plasma concentration of 3.41 ± 1.34 ng/ml at 49...
April 19, 2017: Pain Management
https://www.readbyqxmd.com/read/28415907/transdermal-oxycodone-patch-for-the-treatment-of-postherpetic-neuralgia-a-randomized-double-blind-controlled-trial
#18
Paul D Gavin, Louise Tremper, Alisha Smith, Gemma Williams, Charles Brooker
AIM: To evaluate the efficacy, systemic exposure, safety and tolerability of a transdermal oxycodone patch containing tocopheryl phosphate mixture (TPM) in patients with postherpetic neuralgia (PHN). PATIENTS & METHODS: The study was a Phase IIa, multicenter, randomized, double-blind, vehicle-controlled crossover study. RESULTS: While the TPM/oxycodone patch did not significantly improve 'average' Numeric Pain Rating Scale scores versus vehicle patch, patients reporting high levels of paresthesia (n = 9) showed a trend toward improved pain reduction...
April 18, 2017: Pain Management
https://www.readbyqxmd.com/read/28410920/potential-drug-interaction-with-opioid-agonist-in-the-setting-of-chronic-low-dose-opioid-antagonist-use
#19
James B Leonard, Vidya Nair, Christopher J Diaz, Jonathan B Penoyar, Penelope A Goode
Low dose naltrexone (LDN) has been evaluated in several small studies for the treatment of inflammatory conditions. It is thought to work through modulation of inflammatory mediators and upregulation of endogenous opioid receptors. This may hypersensitize patients to exogenous opioids. Drug-drug interaction screening tools built into electronic health records and other services identify the interaction as risk of opioid withdrawal rather than hypersensitivity. We present a case of a drug-drug interaction in a patient who was receiving LDN treatment of multiple sclerosis...
April 6, 2017: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/28405945/the-comparative-risk-of-delirium-with-different-opioids-a-systematic-review
#20
REVIEW
Lieke M Swart, Vera van der Zanden, Petra E Spies, Sophia E de Rooij, Barbara C van Munster
OBJECTIVE: There is substantial evidence that the use of opioids increases the risk of adverse outcomes such as delirium, but whether this risk differs between the various opioids remains controversial. In this systematic review, we evaluate and discuss possible differences in the risk of delirium from the use of various types of opioids in older patients. METHODS: We performed a search in MEDLINE by combining search terms on delirium and opioids. A specific search filter for use in geriatric medicine was used...
April 12, 2017: Drugs & Aging
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