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https://www.readbyqxmd.com/read/29777509/improving-the-oral-bioavailability-of-tapentadol-via-a-carbamate-prodrug-approach-synthesis-bioactivation-and-pharmacokinetics
#1
Yingchao Li, Yongjun Wang, Ran Zhang, Cuiru Liu, Yue Wei, Jin Sun, Zhonggui He, Youjun Xu, Tianhong Zhang
Tapentadol suffers from rapid clearance due to extensive metabolism in vivo, which results in low oral bioavailability. In the present study, three novel prodrugs of tapentadol (WWJ01, WWJ02, and WWJ03) were synthesized to improve its metabolic stability and thereby improve its oral bioavailability. They all exhibited good stability in phosphate buffers, simulated gastrointestinal fluids, rat plasma, and intestinal and liver homogenates. Disappointingly, the N,N-diethylcarbamate prodrug of tapentadol (WWJ02) and the N,N-diisopropylcarbamate prodrug of tapentadol (WWJ03) were metabolized into inactive metabolites when incubated with liver microsomes...
May 17, 2018: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29760569/concomitant-use-of-opioid-medications-with-triptans-or-serotonergic-antidepressants-in-us-office-based-physician-visits
#2
Kyle C Molina, Kathleen A Fairman, David A Sclar
Background: Opioids are not recommended for routine treatment of migraine because their benefits are outweighed by risks of medication overuse headache and abuse/dependence. A March 2016 US Food and Drug Administration (FDA) safety communication warned of the risk of serotonin syndrome from using opioids concomitantly with 5-hydroxytryptamine receptor agonists (triptans) or serotonergic antidepressants: selective serotonin reuptake inhibitors (SSRIs) or serotonin-norepinephrine reuptake inhibitors (SNRIs)...
2018: Drug, Healthcare and Patient Safety
https://www.readbyqxmd.com/read/29705271/effects-of-human-sult1a3-sult1a4-genetic-polymorphisms-on-the-sulfation-of-acetaminophen-and-opioid-drugs-by-the-cytosolic-sulfotransferase-sult1a3
#3
Ahsan F Bairam, Mohammed I Rasool, Fatemah A Alherz, Maryam S Abunnaja, Amal A El Daibani, Katsuhisa Kurogi, Ming-Cheh Liu
Sulfoconjugation has been shown to be critically involved in the metabolism of acetaminophen (APAP), morphine, tapentadol and O-desmethyl tramadol (O-DMT). The objective of this study was to investigate the effects of single nucleotide polymorphisms (SNPs) of human SULT1A3 and SULT1A4 genes on the sulfating activity of SULT1A3 allozymes toward these analgesic compounds. Twelve non-synonymous coding SNPs (cSNPs) of SULT1A3/SULT1A4 were investigated, and the corresponding cDNAs were generated by site-directed mutagenesis...
April 26, 2018: Archives of Biochemistry and Biophysics
https://www.readbyqxmd.com/read/29675431/tapentadol-prolonged-release-reduces-the-severe-chronic-ischaemic-pain-and-improves-the-quality-of-life-in-patients-with-type-2-diabetes
#4
Anna Tedeschi, Alessandra De Bellis, Piergiorgio Francia, Arianna Bernini, Marco Perini, Elisabetta Salutini, Roberto Anichini
This study has been performed in diabetic type 2 patients with pain due to peripheral artery disease (PAD) in order to evaluate the efficacy and tolerability of tapentadol prolonged release (PR). Methods . 25 patients with type 2 diabetes (13 F and 12 M) were admitted in the study. The evaluation of the analgesic efficacy of tapentadol PR was based on both the assessment of the intensity of the pain (NRS scale from 0 to 10) and the nature of the pain (DN4 questionnaire) and on assessment of the patient's quality of life and state of health (SF-12 Health Survey)...
2018: Journal of Diabetes Research
https://www.readbyqxmd.com/read/29650881/-combination-therapy-of-oxycodone-and-tapentadol-was-effective-for-intractable-pain-caused-by-breast-cancer-bone-metastasis-a-case-report
#5
Tetsuya Matsuura, Akihiko Kusakabe, Takaomi Kessoku, Yasushi Honda, Asuka Yoshimi, Ayumu Goto, Haruhisa Yoshida, Akiko Sukegawa, Atsushi Nakajima, Yasushi Ichikawa
A 52-year-old woman had been prescribed oral medication of acetaminophen, non-steroidal anti-inflammatory drugs (NSAIDs), and oxycodone for intractable pain associated with thoracic metastasis of breast cancer. However, the pain control was poor. Although pregabalin and gabapentin were used as supplementary analgesics, they could not be continued because of their side effects. Based on the noradrenalin reincorporation-inhibiting action of tapentadol, a combination therapy of tapentadol and oxycodone was introduced and satisfactory pain control was achieved...
March 2018: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/29623654/tapentadol-extended-release-in-the-treatment-of-severe-chronic-low-back-pain-and-osteoarthritis-pain
#6
REVIEW
Joseph V Pergolizzi, Robert Taylor, Jo Ann LeQuang, Robert B Raffa, John Bisney
Tapentadol is a novel pain reliever with apparently synergistic dual mechanisms of action, capable of addressing both nociceptive and neuropathic components of chronic pain. As an effective analgesic with good tolerability, tapentadol may be appropriate for patients suffering from severe chronic pain associated with low back pain (LBP) or osteoarthritis (OA). Efficacy studies of tapentadol in populations of patients with severe chronic LBP or OA pain suggest that tapentadol is non-inferior to oxycodone. Its tolerability, especially with respect to gastrointestinal (GI) side effects, may be better than that of other strong opioids in clinical trials and analyses of multiple trials...
April 5, 2018: Pain and Therapy
https://www.readbyqxmd.com/read/29623185/spontaneously-reported-adverse-drug-events-related-to-tapentadol-and-oxycodone-naloxone-in-australia
#7
Carmen Abeyaratne, Samanta Lalic, J Simon Bell, Jenni Ilomäki
Background: The rapid increase in prescribing and use of opioids for noncancer pain has coincided with an increase in opioid-related adverse drug events (ADEs). The objective of our study was to describe ADEs related to tapentadol and oxycodone/naloxone spontaneously reported to the Australian Therapeutic Goods Administration (TGA). Methods: Public case detail reports for tapentadol (September 2013-March 2017) and oxycodone/naloxone (April 2011-March 2017) were sourced from the TGA...
April 2018: Therapeutic Advances in Drug Safety
https://www.readbyqxmd.com/read/29616344/novel-pharmacological-nonopioid-therapies-in-chronic-pain
#8
REVIEW
Alan David Kaye, Elyse M Cornett, Brendon Hart, Shilpadevi Patil, Andrew Pham, Matthew Spalitta, Kenneth F Mancuso
PURPOSE OF REVIEW: Opioid use and abuse has led to a worldwide opioid epidemic. And while opioids are clinically useful when appropriately indicated, they are associated with a wide range of dangerous side effects and whether they are effective at treating or eliminating chronic pain is controversial. There has long been a need for the development of nonopioid alternative treatments for patients that live in pain, and until recently, only a few effective treatments were available. Today, there are a wide range of nonopioid treatments available including NSAIDs, acetaminophen, corticosteroids, nerve blocks, SSRIs, neurostimulators, and anticonvulsants...
April 3, 2018: Current Pain and Headache Reports
https://www.readbyqxmd.com/read/29583048/pharmacokinetics-and-pharmacodynamics-after-oral-administration-of-tapentadol-hydrochloride-in-dogs
#9
James Howard, Turi K Aarnes, Jonathan Dyce, Phillip Lerche, Larry W Wulf, Johann F Coetzee, Jeffrey Lakritz
OBJECTIVE To evaluate pharmacokinetic and pharmacodynamic characteristics of 3 doses of tapentadol hydrochloride orally administered in dogs. ANIMALS 6 healthy adult mixed-breed dogs. PROCEDURES In a prospective, randomized crossover study, dogs were assigned to receive each of 3 doses of tapentadol (10, 20, and 30 mg/kg, PO); there was a 1-week washout period between subsequent administrations. Plasma concentrations and physiologic variables were measured for 24 hours. Samples were analyzed by use of high-performance liquid chromatography-tandem mass spectrometry...
April 2018: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/29582394/comparative-rates-of-mortality-and-serious-adverse-effects-among-commonly-prescribed-opioid-analgesics
#10
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/29574444/opioid-use-and-harms-associated-with-a-sustained-release-tapentadol-formulation-a-postmarketing-study-protocol
#11
Amy Peacock, Briony Larance, Michael Farrell, Rose Cairns, Nicholas Buckley, Louisa Degenhardt
INTRODUCTION: It has been argued that tapentadol may pharmacologically have lower abuse potential than other pharmaceutical opioids currently available. However, there has been no comprehensive triangulation of data regarding use and harms associated with this formulation. A sustained-release formulation (SRF) of tapentadol (Palexia) was released in Australia in 2011 and listed for public subsidy in 2013. We summarise here the methods of a postmarketing study which will measure postintroduction: (1) population level availability, (2) extramedical use and diversion, (3) attractiveness for extramedical use and (4) associated harms, of tapentadol compared against other pharmaceutical opioids...
March 23, 2018: BMJ Open
https://www.readbyqxmd.com/read/29563006/opioid-rotation-in-cancer-pain-treatment
#12
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/29551688/opioid-and-noradrenergic-contributions-of-tapentadol-to-the-inhibition-of-locus-coeruleus-neurons-in-the-streptozotocin-rat-model-of-polyneuropathic-pain
#13
Sonia Torres-Sanchez, Gisela Da Silva Borges, Juan A Mico, Esther Berrocoso
Tapentadol is an analgesic that acts as an agonist of µ opioid receptors (MOR) and that inhibits noradrenaline reuptake. Data from healthy rats show that tapentadol inhibits neuronal activity in the locus coeruleus (LC), a nucleus regulated by both the noradrenergic and opioid systems. Thus, we set out to investigate the effect of tapentadol on LC activity in streptozotocin (STZ)-induced diabetic rats, a model of diabetic polyneuropathy, by analyzing single-unit extracellular recordings of LC neurons. Four weeks after inducing diabetes, tapentadol dose-response curves were obtained from animals pre-treated with RX821002 or naloxone (alpha2-adrenoceptors and opioid receptors antagonists, respectively)...
March 15, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29506199/efficacy-of-tapentadol-for-first-line-opioid-resistant-neuropathic-pain-in-japan
#14
Yosuke Sugiyama, Tomoya Kataoka, Yoshihiko Tasaki, Yuki Kondo, Noriko Sato, Taku Naiki, Nobuhiro Sakamoto, Tatsuo Akechi, Kazunori Kimura
Background: Cancer-related neuropathic pain is sometimes unresponsive to multidrug treatment. Novel drugs are required to treat such severe pain without necessitating the use of adjuvant analgesics. Tapentadol is a new drug that has a dual mechanism as both an opioid agonist and noradrenalin reuptake inhibitor. The study objective was to investigate the effectiveness of oral tapentadol for relieving cancer-related neuropathic pain. Methods: A retrospective, single-center, open, non-randomized study was conducted at the Nagoya City University Hospital...
April 1, 2018: Japanese Journal of Clinical Oncology
https://www.readbyqxmd.com/read/29483406/-new-opioid-options-in-japan-methadone-tapentadol-and-hydromorphone
#15
Yusuke Takagi, Etsuko Aruga
In 2010s, several opioids became available in Japan, including methadone, tapentadol and hydromorphone. Methadone was approved in September 2012 by Japanese regulatory authority. Since methadone is positioned as so-called "step 4 opioid" in Japan, it must be prescribed as alternative opioid switched from another of 60mg/day or greater equivalent dose of oral morphine. Diversity of pharmacokinetics among individuals and various drug interactions require close monitoring of adverse events. In spite of these cautions, unique characteristics such as inhibiting N-methyl-D-aspartate(NMDA)and in- ducing internalization/degradation of mu-delta opioid receptor heterodimers underline the value of methadone in opioid switching...
February 2018: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/29441514/treating-postoperative-pain-in-the-patient-who-is-in-recovery-or-remission-from-opioid-abuse-focus-on-tapentadol
#16
LETTER
Robert L Barkin, Stacy J Barkin
No abstract text is available yet for this article.
May 2017: Journal of Opioid Management
https://www.readbyqxmd.com/read/29436434/updates-in-palliative-care-overview-and-recent-advancements-in-the-pharmacological-management-of-cancer-pain
#17
Helen Wood, Andrew Dickman, Angela Star, Jason W Boland
Pain is a common symptom in many types of cancer. Interdisciplinary team management, including pain assessment, explanation to the patient/family, treating the reversible, non-pharmacological treatments and reassessment are essential. This article focuses on the pharmacological management of cancer pain, and overviews and updates on the recent advances in this field. Both non-opioid and opioid analgesia as well as coanalgesics (adjuvants) are reviewed. Within non-opioid analgesia the risks of non-steroidal anti-inflammatory drugs (NSAIDs) are considered and recommendations for NSAIDs in patients at risk of gastrointestinal and cardiovascular toxicity are made...
February 2018: Clinical Medicine: Journal of the Royal College of Physicians of London
https://www.readbyqxmd.com/read/29434240/improved-therapeutic-potential-of-tapentadol-employing-cationic-exchange-resins-as-carriers-in-neuropathic-pain-evidence-from-pharmacokinetic-and-pharmacodynamics-study
#18
Manu Sharma, Ranju Soni
Current investigation was endeavoured to overcome problem of poor palatability and bioavailability of centrally acting analgesic, tapentadol (TAP) by formulating controlled release drug-resin complexes (DRCs). The technology encompassed in preparation of DRCs involved chemisorption of TAP to weak cationic resins (KyronT-134 and Tulsion335) by batch method. Various formulation variables like drug-resin ratio, pH, resin activation and swelling time were optimized to achieve maximum drug loading in DRCs. FT-IR, DSC, pXRD, in vitro release study under bio-relevant condition of mouth and in vivo sensory taste evaluation established formation of taste masked DRC whereas dissolution study assured prolonged drug release behaviour of optimized DRC...
February 12, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29369473/comparative-pharmacology-and-toxicology-of-tramadol-and-tapentadol
#19
REVIEW
J Faria, J Barbosa, R Moreira, O Queirós, F Carvalho, R J Dinis-Oliveira
Moderate-to-severe pain represents a heavy burden in patients' quality of life, and ultimately in the society and in healthcare costs. The aim of this review was to summarize data on tramadol and tapentadol adverse effects, toxicity, potential advantages and limitations according to the context of clinical use. We compared data on the pharmacological and toxicological profiles of tramadol and tapentadol, after an extensive literature search in the US National Library of Medicine (PubMed). Tramadol is a prodrug that acts through noradrenaline and serotonin reuptake inhibition, with a weak opioid component added by its metabolite O-desmethyltramadol...
May 2018: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/29367870/epstein-barr-virus-related-cutaneous-necrotizing-vasculitis-in-a-girl-heterozygous-for-factor-v-leiden
#20
Cristina Guerriero, Gaia Moretta, Giulia Bersani, Piero Valentini, Antonio Gatto, Donato Rigante
Background: Necrotizing vasculitides are basically characterized by vessel wall neutrophil infiltration and necrosis and they can occur as a primary process or secondary to an underlying disease. Although Henoch-Schönlein purpura (HSp) is the more frequent primary vasculitis in childhood, sometimes it has to be distinguished from other secondary vasculitides induced by infections, drugs, vaccines, or immune-mediated disorders. Main observations: We report a case of a 14-year-old girl with cutaneous necrotizing vasculitis, appearing in the course of acute Epstein-Barr virus infection...
December 1, 2017: Journal of Dermatological Case Reports
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