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Oxymorphone

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https://www.readbyqxmd.com/read/28192197/characterization-of-3-h-oxymorphone-binding-sites-in-mouse-brain-quantitative-autoradiography-in-opioid-receptor-knockout-mice
#1
Ji Hoon Yoo, Anna Borsodi, Géza Tóth, Sándor Benyhe, Robert Gaspar, Audrey Matifas, Brigitte L Kieffer, Athanasios Metaxas, Ian Kitchen, Alexis Bailey
Oxymorphone, one of oxycodone's metabolic products, is a potent opioid receptor agonist which is thought to contribute to the analgesic effect of its parent compound and may have high potential abuse liability. Nonetheless, the in vivo pharmacological binding profile of this drug is still unclear. This study uses mice lacking mu (MOP), kappa (KOP) or delta (DOP) opioid receptors as well as mice lacking all three opioid receptors to provide full characterisation of oxymorphone binding sites in the brain. Saturation binding studies using [(3)H]oxymorphone revealed high affinity binding sites in mouse brain displaying Kd of 1...
February 9, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28162690/-443-evaluation-of-the-clinical-abuse-potential-of-opana-er-versus-oxymorphone-hcl-powder
#2
N Shusterman, F Diana, C Ciliberto, Q Xiang, J Jobes, D Kelsh, B Vince
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28156677/insurer-pre-authorization-and-copayment-for-palliative-patients-with-cancer-receiving-opioids-other-than-morphine
#3
Akhila Sunkepally Reddy, Eden Mae Rodriguez, Eduardo Bruera
: 217 Background: Uncontrolled pain is one of the main fears for patients with cancer and their families. Opioid analgesics are highly effective agents, but the choice of type, route, and dose needs to be personalized. The highly cost of some of them can make it difficult for patients to received adequate pain control without appropriate insurance coverage. There is a lack of information regarding the frequency of denials or heavy copayments by insurers. METHODS: We evaluated 143 continuous opioid test claims for prescriptions by our palliative care providers for opioids other than morphine, including transdermal fentanyl, extended release oxycodone, hydromorphone and oxymorphone...
October 9, 2016: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28119266/drugs-in-hair-part-i-metabolisms-of-major-drug-classes
#4
REVIEW
R M White
Currently, hair can be reliably tested for the presence of drugs. However, one major drawback to the use of parent drugs is the question of potential external or environmental contamination. The analysis of metabolites to confirm the use of the parent drugs was proposed in this short review. The development of hair as a test matrix and the incorporation of xenobiotics, in general, into the hair matrix were discussed. What constitutes an appropriate metabolite for drug testing to mirror the use of a parent drug was proposed and discussed...
January 2017: Forensic Science Review
https://www.readbyqxmd.com/read/28080998/determination-of-oxycodone-and-its-major-metabolites-noroxycodone-and-oxymorphone-by-ultra-high-performance-liquid-chromatography-tandem-mass-spectrometry-in-plasma-and-urine-application-to-real-cases
#5
Flaminia Pantano, Stefano Brauneis, Alexandre Forneris, Roberta Pacifici, Enrico Marinelli, Chrystalla Kyriakou, Simona Pichini, Francesco Paolo Busardò
BACKGROUND: Oxycodone is a narcotic drug widely used to alleviate moderate and severe acute and chronic pain. Variability in analgesic efficacy could be explained by inter-subject variations in plasma concentrations of parent drug and its active metabolite, oxymorphone. To evaluate patient compliance and to set up therapeutic drug monitoring (TDM), an ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) assay was developed and validated for the parent drug and its major metabolites noroxycodone and oxymorphone...
January 12, 2017: Clinical Chemistry and Laboratory Medicine: CCLM
https://www.readbyqxmd.com/read/27922764/comparison-of-abuse-suspected-suicidal-intent-and-fatalities-related-to-the-7-day-buprenorphine-transdermal-patch-versus-other-opioid-analgesics-in-the-national-poison-data-system
#6
COMPARATIVE STUDY
Paul M Coplan, Nelson E Sessler, Venkatesh Harikrishnan, Richa Singh, Charles Perkel
OBJECTIVE: Prescription opioid related abuse, suicide and death are significant public health problems. This study compares rates of poison center calls categorized as intentional abuse, suspected suicidal intent or fatality for the 7-day buprenorphine transdermal system/patch (BTDS) with other extended-release and long-acting (ER/LA) opioids indicated for chronic pain. METHODS: Retrospective 24-month cohort study using National Poison Data System data from July 2012 through June 2014...
January 2017: Postgraduate Medicine
https://www.readbyqxmd.com/read/27881622/stability-of-21-cocaine-opioid-and-benzodiazepine-drug-analytes-in-spiked-meconium-at-three-temperatures
#7
Fang Wu, Stephanie J Marin, Gwendolyn A McMillin
In this study, the stability of 21 cocaine, opioid and benzodiazepine analytes in spiked meconium was investigated at three storage temperatures: 4°C, room temperature (RT), and 37°C (body temperature). The drugs/metabolites included were hydrocodone, hydromorphone, codeine, morphine, 6-acetylmorphine (6-AM), oxycodone, oxymorphone, cocaine, cocaethylene, benzoylecgonine, m-hydroxybenzoylecgonine, diazepam, oxazepam, temazepam, nordiazepam, chlordiazepoxide, lorazepam, alprazolam, alpha-hydroxyalprazolam, clonazepam, 7-aminoclonazepam, midazolam, alpha-hydroxymidazolam and zolpidem...
November 22, 2016: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/27864296/a-mechanistic-investigation-of-thrombotic-microangiopathy-associated-with-intravenous-abuse-of-opana-er
#8
Ryan Hunt, Ayla Yalamanoglu, James Tumlin, Tal Schiller, Jin Hyen Baek, Andrew Wu, Agnes B Fogo, Haichun Yang, Edward Wong, Peter Miller, Paul W Buehler, Chava Kimchi-Sarfaty
Since 2012, a number of case reports have described the occurrence of thrombotic microangiopathy (TMA) following intravenous abuse of extended release oxymorphone hydrochloride (Opana ER), an oral opioid for long-term treatment of chronic pain. Here, we present unique clinical features of three patients and investigate intravenous exposure to the tablet's inert ingredients as a possible causal mechanism. Guinea pigs were used as an animal model to understand the hematopathologic and nephrotoxic potential of the inert ingredient mixture (termed here as PEO+) which primarily contains high molecular weight polyethylene oxide (HMW PEO)...
November 18, 2016: Blood
https://www.readbyqxmd.com/read/27802072/prevalence-of-prescription-opioid-misuse-abuse-as-determined-by-international-classification-of-diseases-codes-a-systematic-review
#9
Carl L Roland, Joanita Lake, Gary M Oderda
We conducted a systematic review to evaluate worldwide human English published literature from 2009 to 2014 on prevalence of opioid misuse/abuse in retrospective databases where International Classification of Diseases (ICD) codes were used. Inclusion criteria for the studies were use of a retrospective database, measured abuse, dependence, and/or poisoning using ICD codes, stated prevalence or it could be derived, and documented time frame. A meta-analysis was not performed. A qualitative narrative synthesis was used, and 16 studies were included for data abstraction...
December 2016: Journal of Pain & Palliative Care Pharmacotherapy
https://www.readbyqxmd.com/read/27780305/maturation-of-oxycodone-pharmacokinetics-in-neonates-and-infants-oxycodone-and-its-metabolites-in-plasma-and-urine
#10
Merja Kokki, Marja Heikkinen, Pyry Välitalo, Heidi Hautajärvi, Juho Hokkanen, Hanna Pitkänen, Ulla Sankilampi, Veli-Pekka Ranta, Hannu Kokki
AIMS: This study aimed to characterize the pharmacokinetics of oxycodone and its major metabolites in infants and covered the age range between extremely preterm neonates and 2-year-old infants. METHODS: Seventy-nine infants (gestational age 23-42 weeks; postnatal age 0-650 days) received intravenous oxycodone hydrochloride trihydrate at a dose of 0.1 mg kg(-1) during or after surgery. Three to seven blood samples were taken from each infant, and plasma concentrations of oxycodone, noroxycodone, oxymorphone, and noroxymorphone were quantified...
October 25, 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27764026/suitability-of-the-dri-hydrocodone-hydromorphone-immunoassay-in-the-clinical-environment-at-a-lower-cutoff-validation-with-lc-ms-ms-analysis
#11
Robert B Dixon, Amitava Dasgupta
BACKGROUND: We evaluated the analytical performance of the DRI hydrocodone/hydromorphone assay by comparing semiquantitative values obtained by this assay with values obtained by a liquid chromatography combined with tandem mass spectrometry (LC-MS/MS) method. We also evaluated the possibility of lowering the cutoff of the DRI assay from 300 to 100 ng/mL. METHODS: We compared semiquantitative values obtained by the DRI assay in 97 specimens with values obtained by the LC-MS/MS method including 10 specimens containing hydrocodone and/or hydromorphone concentrations between 105...
December 2016: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/27723230/effect-of-morphine-methadone-hydromorphone-or-oxymorphone-on-the-thermal-threshold-following-intravenous-or-buccal-administration-to-cats
#12
Bruno H Pypendop, Yael Shilo-Benjamini, Jan E Ilkiw
OBJECTIVE: To determine the effects of morphine, methadone, hydromorphone or oxymorphone on the thermal threshold in cats, following buccal and intravenous (IV) administration. STUDY DESIGN: Randomized crossover study. ANIMALS: Six healthy adult female ovariohysterectomized cats weighing 4.5 ± 0.4 kg. METHODS: Morphine sulfate (0.2 mg kg(-1) IV or 0.5 mg kg(-1) buccal), methadone hydrochloride (0.3 mg kg(-1) IV or 0...
November 2016: Veterinary Anaesthesia and Analgesia
https://www.readbyqxmd.com/read/27702939/degradation-of-opioids-and-opiates-during-acid-hydrolysis-leads-to-reduced-recovery-compared-to-enzymatic-hydrolysis
#13
Pongkwan Sitasuwan, Cathleen Melendez, Margarita Marinova, Kaylee R Mastrianni, Alicia Darragh, Emily Ryan, L Andrew Lee
Drug monitoring laboratories utilize a hydrolysis process to liberate the opiates from their glucuronide conjugates to facilitate their detection by tandem mass spectrometry (MS). Both acid and enzyme hydrolysis have been reported as viable methods, with the former as a more effective process for recovering codeine-6-glucuronide and morphine-6-glucuronide. Here, we report concerns with acid-catalyzed hydrolysis of opioids, including a significant loss of analytes and conversions of oxycodone to oxymorphone, hydrocodone to hydromorphone and codeine to morphine...
October 2016: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/27692933/characterization-of-oxycodone-in-vitro-metabolism-by-human-cytochromes-p450-and-udp-glucuronosyltransferases
#14
Stéphanie Romand, Dany Spaggiari, Niloufar Marsousi, Caroline Samer, Jules Desmeules, Youssef Daali, Serge Rudaz
The hepatic metabolism of oxycodone by cytochromes P450 (CYP) and the UDP-glucuronosyltransferases (UGT), the main metabolic enzymes of phase I and phase II, respectively, was assessed in vitro. The N-demethylation by CYP3A4/5 and the O-demethylation by CYP2D6 in human liver microsomes (HLM) followed Michaelis-Menten kinetics, with intrinsic clearances of 1.46μL/min/mg and 0.35μL/min/mg, respectively. Although noroxycodone and oxymorphone mainly contribute to the elimination of oxycodone, the simulated total in vivo clearance using in vitro phase I metabolism was underestimated...
September 26, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27589376/dialyzability-of-oxycodone-and-its-metabolites-in-chronic-noncancer-pain-patients-with-end-stage-renal-disease
#15
Boaz Gedaliahu Samolsky Dekel, Gabriele Donati, Alessio Vasarri, Anna Laura Croci Chiocchini, Alberto Gori, Giuseppe Cavallari, Gianfranco Di Nino, Laura Mercolini, Michele Protti, Roberto Mandrioli, Rita Maria Melotti, Gaetano La Manna
OBJECTIVES: Opioids are the preferred analgesic drugs to treat severe chronic pain conditions among dialysis patients; however, knowledge about their dialyzability features is limited. Oxycodone is increasingly used for the treatment of chronic pain conditions as oral controlled release (CR) tablets; however, evidence about this drug and its metabolites' dialyzability is lacking. METHODS: We assessed, during 4-hour dialysis sessions, the effect of standard hemodialysis (HD) and online hemodiafiltration (HDF) methods on the plasma concentration of oxycodone and its metabolites in n = 20 chronic pain patients with end-stage renal disease who were stably treated with oral CR oxycodone...
September 2, 2016: Pain Practice: the Official Journal of World Institute of Pain
https://www.readbyqxmd.com/read/27496654/activation-of-delta-opioid-receptor-contributes-to-the-antinociceptive-effect-of-oxycodone-in-mice
#16
Pao-Pao Yang, Geng-Chang Yeh, Teng-Kuang Yeh, Jinghua Xi, Horace H Loh, Ping-Yee Law, Pao-Luh Tao
Oxycodone has been used clinically for over 90 years. While it is known that it exhibits low affinity for the multiple opioid receptors, whether its pharmacological activities are due to oxycodone activation of the opioid receptor type or due to its active metabolite (oxymorphone) that exhibits high affinity for the mu-opioid receptors remains unresolved. Ross and Smith (1997) reported the antinociceptive effects of oxycodone (171nmol, i.c.v.) are induced by putative kappa-opioid receptors in SD rat while others have reported oxycodone activities are due to activation of mu- and/or delta-opioid receptors...
September 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27478601/relapsing-thrombotic-microangiopathy-and-intravenous-sustained-release-oxycodone
#17
Melissa Nataatmadja, Dakshinamurthy Divi
Thrombotic microangiopathy (TMA) associated with injecting sustained-release oxymorphone, an opioid intended for oral use, has previously been reported. We report a case of TMA secondary to intravenous use of sustained-release oxycodone, and the first case to demonstrate relapsing disease due to persistent intravenous opioid use. In cases such as these, TMA is suspected to be due to a polyethylene oxide (PEO) coating found on these drugs, and the disease is likely due to a directly toxic effect of PEO to endothelial cells...
August 2016: Clinical Kidney Journal
https://www.readbyqxmd.com/read/27468059/hiv-infection-linked-to-injection-use-of-oxymorphone-in-indiana-2014-2015
#18
Philip J Peters, Pamela Pontones, Karen W Hoover, Monita R Patel, Romeo R Galang, Jessica Shields, Sara J Blosser, Michael W Spiller, Brittany Combs, William M Switzer, Caitlin Conrad, Jessica Gentry, Yury Khudyakov, Dorothy Waterhouse, S Michele Owen, Erika Chapman, Jeremy C Roseberry, Veronica McCants, Paul J Weidle, Dita Broz, Taraz Samandari, Jonathan Mermin, Jennifer Walthall, John T Brooks, Joan M Duwve
BACKGROUND: In January 2015, a total of 11 new diagnoses of human immunodeficiency virus (HIV) infection were reported in a small community in Indiana. We investigated the extent and cause of the outbreak and implemented control measures. METHODS: We identified an outbreak-related case as laboratory-confirmed HIV infection newly diagnosed after October 1, 2014, in a person who either resided in Scott County, Indiana, or was named by another case patient as a syringe-sharing or sexual partner...
July 21, 2016: New England Journal of Medicine
https://www.readbyqxmd.com/read/27405370/prescription-opioids-v-metabolism-and-excretion-of-oxymorphone-in-urine-following-controlled-single-dose-administration
#19
Anne Z DePriest, Rebecca Heltsley, David L Black, John M Mitchell, Charles LoDico, Ronald Flegel, Edward J Cone
Oxymorphone (OM), a prescription opioid and metabolite of oxycodone, was included in the recently published proposed revisions to the Mandatory Guidelines for Federal Workplace Drug Testing Programs. To facilitate toxicological interpretation, this study characterized the time course of OM and its metabolite, noroxymorphone (NOM), in hydrolyzed and non-hydrolyzed urine specimens. Twelve healthy subjects were administered a single 10 mg controlled-release OM dose, followed by a periodic collection of pooled urine specimens for 54 h following administration...
October 2016: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/27405363/case-report-of-methylone-oxymorphone-and-ethanol-in-a-fatality-case-with-tissue-distribution
#20
Eric T Shimomura, Alice J Briones, Wendy S Warren, Joseph W Addison, Jessica L Knittel, Sarah A Shoemaker, Taj D King, Thomas Z Bosy
It is reasonable to expect the presence of multiple drugs to present a complicated picture of toxicity. We report a fatal case involving a young man who purchased illicit drugs and knowingly consumed them. After consuming these drugs and going to sleep in his friend's car, he was found unresponsive the next morning with no signs of physical violence. Drugs found in the peripheral blood at autopsy were oxymorphone, methylone and ethanol at concentrations of 0.106, 0.50 and 130 mg/dL, respectively. The levels of oxymorphone and methylone in peripheral blood were comparable to those observed in other reported fatalities...
September 2016: Journal of Analytical Toxicology
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