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Oxymorphone

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https://www.readbyqxmd.com/read/29582394/comparative-rates-of-mortality-and-serious-adverse-effects-among-commonly-prescribed-opioid-analgesics
#1
David L Murphy, Jacob A Lebin, Stevan G Severtson, Heather A Olsen, Nabarun Dasgupta, Richard C Dart
INTRODUCTION: The epidemic of prescription opioid overdose and mortality parallels the dispensing rates of prescription opioids, and the availability of increasingly potent opioid analgesics. OBJECTIVE: The common assumption that more potent opioid analgesics are associated with higher rates of adverse outcomes has not been adequately substantiated. We compared the rate of serious adverse events among commonly prescribed opioid analgesics of varying potency. METHODS: Serious adverse events (SAEs; defined as death, major medical effect, or hospitalization) resulting from exposure to tablets containing seven opioid analgesics (oxycodone, hydrocodone, morphine, hydromorphone, oxymorphone, tapentadol, and tramadol) captured by the Researched Abuse, Diversion and Addiction-Related Surveillance (RADARS® ) System Poison Center Program were evaluated from 2010 through 2016...
March 26, 2018: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/29563006/opioid-rotation-in-cancer-pain-treatment
#2
Michael Schuster, Oliver Bayer, Florian Heid, Rita Laufenberg-Feldmann
BACKGROUND: Rotating several different WHO level III opioid drugs is a therapeutic option for patients with chronic cancer-related pain who suffer from inadequate analgesia and/or intolerable side effects. The evidence favoring opioid rotation is controversial, and the current guidelines in Germany and other countries contain only weak recommendations for it. METHODS: This review is based on pertinent publications retrieved by a systematic review of the literature on opioid rotation for adult patients with chronic cancerrelated pain who are regularly taking WHO level III opioids by the oral or trans - dermal route...
March 2, 2018: Deutsches Ärzteblatt International
https://www.readbyqxmd.com/read/29554298/development-of-a-quantitative-lc-ms-ms-assay-for-codeine-morphine-6-acetylmorphine-hydrocodone-hydromorphone-oxycodone-and-oxymorphone-in-neat-oral-fluid
#3
Megan Grabenauer, Katherine N Moore, Nichole D Bynum, Robert M White, John M Mitchell, Eugene D Hayes, Ronald Flegel
Recent advances in analytical capabilities allowing for the identification and quantification of drugs and metabolites in small volumes at low concentrations have made oral fluid a viable matrix for drug testing. Oral fluid is an attractive matrix option due to its relative ease of collection, reduced privacy concerns for observed collections and difficulty to adulterate. The work presented here details the development and validation of a liquid chromatography tandem mass spectrometry (LC-MS-MS) method for the quantification of codeine, morphine, 6-acetylmorphine, hydrocodone, hydromorphone, oxycodone and oxymorphone in neat oral fluid...
March 15, 2018: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29551331/trends-in-medical-use-of-opioids-in-the-u-s-2006-2016
#4
Brian J Piper, Dipam T Shah, Olapeju M Simoyan, Kenneth L McCall, Stephanie D Nichols
INTRODUCTION: The U.S. is experiencing an opioid epidemic which is at least partially iatrogenic and fueled by both prescription and illicit misuse. This study provides a nationwide examination of opioid distribution patterns during the last decade. METHODS: Data were obtained from the U.S. Drug Enforcement Administration's Automation of Reports and Consolidated Orders System for 2006-2016. Analyses include quantities of ten opioids legally dispensed nationwide by weight and converted to Morphine Milligram Equivalents...
March 9, 2018: American Journal of Preventive Medicine
https://www.readbyqxmd.com/read/29499200/monitoring-opioid-and-benzodiazepine-use-and-abuse-is-oral-fluid-or-urine-the-preferred-specimen-type
#5
Athena K Petrides, Stacy E F Melanson, Michalis Kantartjis, Rachel D Le, Christiana A Demetriou, James G Flood
BACKGROUND: Oral fluid (OF) has become an increasingly popular matrix to assess compliance in pain management and addiction settings as it reduces the likelihood of adulteration. However, drug concentrations and windows of detection are not as well studied in OF as in urine (UR). We compared the clinical utility and analytical performance of OF and UR as matrices for detecting common benzodiazepines and opioids. METHODS: OF and UR concentrations of 5 benzodiazepines and 7 opioids were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS) in 263 paired OF and UR specimens...
February 27, 2018: Clinica Chimica Acta; International Journal of Clinical Chemistry
https://www.readbyqxmd.com/read/29435466/opana-er-oxymorphone-induced-thrombotic-microangiopathy-an-atypical-presentation-in-a-patient-with-hepatitis-c
#6
Hassan Mehmood, Muzammil Khan, Asghar Marwat, Medha Joshi, Varun Malhotra
Oxymorphone is a semisynthetic extended release opiate used to treat moderate to severe chronic pain. The Food and Drug Administration approved the oral form of oxymorphone available as Opana and Opana ER (extended release) since 2006. The Food and Drug Administration and the Centers for Disease Control and Prevention issued warning against intravenous use of Opana ER. We are presenting a case report of a 37-year-old female with a history of active intravenous drug abuse who presented to our hospital with acute kidney injury...
January 2018: Journal of Investigative Medicine High Impact Case Reports
https://www.readbyqxmd.com/read/29414014/determination-of-oxycodone-and-its-major-metabolites-in-haematic-and-urinary-matrices-comparison-of-traditional-and-miniaturised-sampling-approaches
#7
Michele Protti, Maria Carmen Catapano, Boaz Gedaliahu Samolsky Dekel, James Rudge, Gilberto Gerra, Lorenzo Somaini, Roberto Mandrioli, Laura Mercolini
Oxycodone is a widely prescribed, full agonist opioid analgesic. As such, it is used clinically to treat different kinds of painful conditions, with a relatively high potential for doping practices in athletes. In this paper, different classic and innovative miniaturised matrices from blood and urine have been studied and compared, to evaluate their relative merits and drawbacks within therapeutic drug monitoring (TDM) and to implement new protocols for anti-doping analysis. Plasma, dried blood spots (DBS) and dried plasma spots (DPS) have been studied for TDM purposes, while urine, dried urine spots (DUS) and volumetric absorptive microsamples (VAMS) from urine for anti-doping...
April 15, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29278838/multiple-injections-per-injection-episode-high-risk-injection-practice-among-people-who-injected-pills-during-the-2015-hiv-outbreak-in-indiana
#8
Dita Broz, Jon Zibbell, Carrie Foote, Jeremy C Roseberry, Monita R Patel, Caitlin Conrad, Erika Chapman, Philip J Peters, Richard Needle, Cameron McAlister, Joan M Duwve
BACKGROUND: Misuse of prescription opioid analgesics (POA) has increased dramatically in the US, particularly in non-urban areas. We examined injection practices among persons who inject POA in a rural area that experienced a large HIV outbreak in 2015. METHODS: Between August-September 2015, 25 persons who injected drugs within the past 12 months were recruited in Scott County, Indiana for a qualitative study. Data from in-depth, semi-structured interviews were analyzed...
February 2018: International Journal on Drug Policy
https://www.readbyqxmd.com/read/29274731/simultaneous-analysis-of-opioid-analgesics-and-their-metabolites-in-municipal-wastewaters-and-river-water-by-liquid-chromatography-tandem-mass-spectrometry
#9
Ivona Krizman-Matasic, Petra Kostanjevecki, Marijan Ahel, Senka Terzic
Although published literature provides a clear demonstration of widespread occurrence of opioid analgesics (OAs) in the aquatic environment, analytical methods suitable for a systematic study of this pharmaceutical class, which would include a broad spectrum of opioid analgesics and their metabolites, are still missing. In this work, a comprehensive multiresidue method for quantitative analysis of 27 opioid analgesics and their metabolites, including 2 morphine glucuronide conjugates, was developed and validated for three matrices: raw wastewater (RW), secondary effluent (SE) and river water...
January 19, 2018: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29236495/a-stable-heroin-analog-that-can-serve-as-a-vaccine-hapten-to-induce-antibodies-that-block-the-effects-of-heroin-and-its-metabolites-in-rodents-and-that-cross-react-immunologically-with-related-drugs-of-abuse
#10
Agnieszka Sulima, Rashmi Jalah, Joshua F G Antoline, Oscar B Torres, Gregory H Imler, Jeffrey R Deschamps, Zoltan Beck, Carl R Alving, Arthur E Jacobson, Kenner C Rice, Gary R Matyas
An improved synthesis of a haptenic heroin surrogate 1 (6-AmHap) is reported. The intermediate needed for the preparation of 1 was described in the route in the synthesis of 2 (DiAmHap). A scalable procedure was developed to install the C-3 amido group. Using the Boc protectng group in 18 allowed preparation of 1 in an overall yield of 53% from 4 and eliminated the necessity of preparing the diamide 13. Hapten 1 was conjugated to tetanus toxoid and mixed with liposomes containing monophosphoryl lipid A as an adjuvant...
December 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29224919/assessment-of-tapentadol-api-abuse-liability-with-the-researched-abuse-diversion-and-addiction-related-surveillance-radars-system
#11
Suzanne K Vosburg, S Geoffrey Severtson, Richard C Dart, Theodore J Cicero, Steven P Kurtz, Mark W Parrino, Jody L Green
Tapentadol, a Schedule II opioid with a combination of µ-opioid activity and norepinephrine reuptake inhibition, is used for the management of moderate to severe acute and chronic pain. Its dual-mechanism of action is thought to reduce opioid-related side effects that can complicate pain management. Since approval, tapentadol has been tracked across multiple outcomes suggesting abuse liability, and a pattern of relatively low, although not absent, abuse liability has been found. This retrospective cohort study further details the abuse liability of tapentadol as an Active Pharmaceutical Ingredient (API) when both immediate-release and extended-release formulations were on the market together (4Q2011 to 2Q2016)...
December 7, 2017: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/29210063/opioid-induced-inhibition-of-the-human-5-ht-and-noradrenaline-transporters-in-vitro-link-to-clinical-reports-of-serotonin-syndrome
#12
Anna Rickli, Evangelia Liakoni, Marius C Hoener, Matthias E Liechti
BACKGROUND AND PURPOSE: Opioids may inhibit the 5-HT transporter (SERT) and the noradrenaline transporter (NET). NET inhibition may contribute to analgesia, and SERT inhibition or interactions with 5-HT receptors may cause serotonergic toxicity. However, the effects of different opioids on the human SERT, NET and 5-HT receptors have not been sufficiently studied. EXPERIMENTAL APPROACH: We determined the potencies of different opioids to inhibit the SERT and NET in vitro using human transporter-transfected HEK293 cells...
February 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29186453/detection-and-quantification-of-codeine-6-glucuronide-hydromorphone-3-glucuronide-oxymorphone-3-glucuronide-morphine-3-glucuronide-and-morphine-6-glucuronide-in-human-hair-from-opioid-users-by-lc-ms-ms
#13
Megan Grabenauer, Nichole D Bynum, Katherine N Moore, Robert M White, John M Mitchell, Eugene D Hayes, Ronald Flegel
Current hair testing methods that rely solely on quantification of parent drug compounds are unable to definitively distinguish between drug use and external contamination. One possible solution to this problem is to confirm the presence of unique drug metabolites that cannot be present through contamination, such as phase II glucuronide conjugates. This work demonstrates for the first time that codeine-6-glucuronide, hydromorphone-3-glucuronide, oxymorphone-3-glucuronide, morphine-3-glucuronide and morphine-6-glucuronide are present at sufficient concentrations to be quantifiable in hair of opioid users and that their concentrations generally increase as the concentrations of the corresponding parent compounds increase...
November 24, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29084357/adverse-events-associated-with-medium-and-long-term-use-of-opioids-for-chronic-non-cancer-pain-an-overview-of-cochrane-reviews
#14
REVIEW
Charl Els, Tanya D Jackson, Diane Kunyk, Vernon G Lappi, Barend Sonnenberg, Reidar Hagtvedt, Sangita Sharma, Fariba Kolahdooz, Sebastian Straube
BACKGROUND: Chronic pain is common and can be challenging to manage. Despite increased utilisation of opioids, the safety and efficacy of long-term use of these compounds for chronic non-cancer pain (CNCP) remains controversial. This overview of Cochrane Reviews complements the overview entitled 'High-dose opioids for chronic non-cancer pain: an overview of Cochrane Reviews'. OBJECTIVES: To provide an overview of the occurrence and nature of adverse events associated with any opioid agent (any dose, frequency, or route of administration) used on a medium- or long-term basis for the treatment of CNCP in adults...
October 30, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29016905/relative-abuse-of-crush-resistant-prescription-opioid-tablets-via-alternative-oral-modes-of-administration
#15
Stephen F Butler, Ryan A Black, Alison B Fleming
Objective: Some crush-resistant tablet formulations (CRTs) reduce prescription opioid abuse by nonoral routes of administration (ROAs), especially insufflation and injection, while oral abuse increases. Oral abuse involving product manipulation vs swallowing whole for CRTs and comparators was examined. Methods: Abuse by oral modes of administration (e.g., swallowing whole, chewing, dissolving in the mouth), was examined using the ASI-MV, a computerized, clinical interview for adults in substance abuse treatment from January 2009 to March 2015...
July 8, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28891868/bivalent-ligand-that-activates-mu-opioid-receptor-and-antagonizes-mglur5-receptor-reduces-neuropathic-pain-in-mice
#16
Cristina D Peterson, Kelley F Kitto, Eyup Akgün, Mary M Lunzer, Maureen S Riedl, Lucy Vulchanova, George L Wilcox, Philip S Portoghese, Carolyn A Fairbanks
The mu opioid receptor (MOR) and metabotropic glutamate receptor 5 (mGluR5) are well-established pharmacological targets in the management of chronic pain. Both receptors are expressed in the spinal cord. MMG22, a bivalent ligand containing 2 pharmacophores separated by 22 atoms, which simultaneously activates MOR and antagonizes mGluR5, has been shown to produce potent reversal of tactile hypersensitivity in rodent models of lipopolysaccharide (LPS)-and bone cancer-induced chronic pain. This study assessed whether intrathecal MMG22 also is effective in reducing pain of neuropathic origin...
December 2017: Pain
https://www.readbyqxmd.com/read/28864212/14-o-methylmorphine-a-novel-selective-mu-opioid-receptor-agonist-with-high-efficacy-and-affinity
#17
Ferenc Zádor, Mihály Balogh, András Váradi, Zoltán S Zádori, Kornél Király, Edina Szűcs, Bence Varga, Bernadette Lázár, Sándor Hosztafi, Pál Riba, Sándor Benyhe, Susanna Fürst, Mahmoud Al-Khrasani
14-O-methyl (14-O-Me) group in morphine-6-O-sulfate (M6SU) or oxymorphone has been reported to be essential for enhanced affinity, potency and antinociceptive effect of these opioids. Herein we report on the pharmacological properties (potency, affinity and efficacy) of the new compound, 14-O-methylmorphine (14-O-MeM) in in vitro. Additionally, we also investigated the antinociceptive effect of the novel compound, as well as its inhibitory action on gastrointestinal transit in in vivo. The potency and efficacy of test compound were measured by [ 35 S]GTPγS binding, isolated mouse vas deferens (MVD) and rat vas deferens (RVD) assays...
November 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28858693/trends-in-average-days-supply-of-opioid-medications-in-medicaid-and-commercial-insurance
#18
Ali Bonakdar Tehrani, Rachel Mosher Henke, Mir M Ali, Ryan Mutter, Tami L Mark
OBJECTIVES: To calculate trends in adult average days' supply for six commonly prescribed opioids: hydrocodone, hydromorphone, morphine, oxycodone, oxymorphone, and tapentadol to assess whether physicians changed prescribing practices at the time of the intensifying epidemic. METHODS: We used 2005-2015 Truven Health MarketScan Commercial Claims and Encounters data to measure trends in opioid average days' supply among commercially insured individuals and 2005-2014 MarketScan Multi-State Medicaid data to measure trends in opioid average days' supply among Medicaid beneficiaries...
January 2018: Addictive Behaviors
https://www.readbyqxmd.com/read/28814158/a-phase-i-study-of-the-pharmacokinetics-safety-and-tolerability-of-a-novel-tocopheryl-phosphate-mixture-oxymorphone-transdermal-patch-system
#19
Paul D Gavin, Lee S Simon, Thomas Schlagheck, Alisha J Smith, Janakan Krishnarajah
AIM: Characterize the pharmacokinetic profile and tolerability of two tocopheryl phosphate mixture/oxymorphone patch formulations in healthy subjects, and the active metabolite (6-OH-oxymorphone). MATERIALS & METHODS: Fifteen participants received a single application of oxymorphone patches +/- capsaicin for 72 h and were crossed-over for another 72 h. RESULTS: Plasma oxymorphone was detected approximately 7 h and 6-OH-oxymorphone after approximately 18-19 h postapplication of both formulations, respectively...
November 2017: Pain Management
https://www.readbyqxmd.com/read/28802086/acute-kidney-injury-is-common-with-intravenous-abuse-of-extended-release-oral-oxymorphone-and-delayed-renal-recovery-rates-are-associated-with-increased-kdigo-staging
#20
Alex K Bonnecaze, Matthew Whitaker Wilson, Ajay Dharod, Alison Fletcher, P J Miller
BACKGROUND: Prescription opioid abuse poses a serious problem in the United States, representing 615 per 100,000 deaths annually. Extended-release oxymorphone (Opana-ER) is an oral opioid pain medication that has recently been found to cause thrombotic microangiopathy when intravenously abused. In this retrospective study, prevalence and outcomes of AKI among patients intravenously abusing extended-release oral oxymorphone were analyzed. METHODS: A query of electronic medical records for "drug abuse" at an academic medical center during January 2012 to December 2015 was performed and yielded 2350 patients...
August 12, 2017: Nephrology
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