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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
Sonia Torres-Sanchez, Gisela Borges, Juan A Mico, Esther Berrocoso
Tapentadol is an analgesic that acts as an agonist of mu-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
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...
March 1, 2018: Japanese Journal of Clinical Oncology
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
Robert L Barkin, Stacy J Barkin
No abstract text is available yet for this article.
May 2017: Journal of Opioid Management
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
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
J Faria, J Barbosa, R Moreira, O Queirós, F Carvalho, R J Dinis-Oliveira
BACKGROUND AND OBJECTIVE: Moderate to severe pain represent 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. DATABASES AND DATA TREATMENT: We compared data on the pharmacological and toxicological profiles of tramadol and tapentadol, after an extensive literature search in the U...
January 25, 2018: European Journal of Pain: EJP
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
Laura E Gressler, Drayton A Hammond, Jacob T Painter
The potential association between serotonin syndrome and tapentadol is not well described in the literature. This study aimed to review the literature and identify methodological issues that could lead to inaccurately reported rates of serotonin syndrome associated with tapentadol use. A systematic review of English articles using MEDLINE, Cochrane Controlled Trials Register, and Scopus was performed. Additional studies were identified by cross-referencing article bibliographies. Original research that examined the safety of tapentadol in patients with nonconfounding indications were examined...
January 16, 2018: Journal of Pain & Palliative Care Pharmacotherapy
Juan R Zapata-Morales, Ángel J Alonso-Castro, Vinicio Granado-Soto, Sergio Sánchez-Enriquez, Mario A Isiordia-Espinoza
Preclinical Research & Development The objective of the present study was to evaluate the tapentadol-diclofenac combination in three dose-ratios in the mouse acetic acid-induced visceral pain and their ulcerogenic activity on the stomachal mucous. Dose-response curves were generated for tapentadol, diclofenac, and their combination in the acetic acid-induced writhing test in mice. Moreover, the stomachs of animals were surgically removal and gastrointestinal ulcerogenic action of the combination was assessed...
January 3, 2018: Drug Development Research
Valentina Malafoglia, Monica Celi, Carolina Muscoli, Sara Ilari, Filomena Lauro, Luigino Antonio Giancotti, Chiara Morabito, Maurizio Feola, Umberto Tarantino, William Raffaeli
BACKGROUND: The incidence of post-surgical chronic pain ranges between 20% and 40% in Europe. Osteoarthritis pain after prosthesis implantation is one of the most severe secondary syndromes, depending not only on surgery but also on organic changes before and after joints replacement. No data are available about risk factors. An excessive inflammatory response plays a central role but a best therapy is not defined yet. It is not clear whether opioid administration could influence post-surgical pain and lead to tolerance or addiction...
December 19, 2017: Trials
Maria Beatrice Passavanti, Marco Fiore, Pasquale Sansone, Caterina Aurilio, Vincenzo Pota, Manlio Barbarisi, Daniela Fierro, Maria Caterina Pace
BACKGROUND: This pilot study was designed to compare the efficacy of ultramicronized palmitoylethanolamide (um-PEA) as add-on therapy to tapentadol (TP) with TP therapy only in patients suffering from chronic low back pain (LBP). METHODS: This pilot observational study consists in two arms: the prospective arm and the retrospective one. In the prospective arm patients consecutively selected received um-PEA as add-on therapy to TP for 6 months; in the retrospective arm patients were treated with TP only for 6 months...
December 19, 2017: BMC Anesthesiology
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
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
Alex Mu, Erica Weinberg, Dwight E Moulin, Hance Clarke
OBJECTIVE: To provide family physicians with a practical clinical summary of the Canadian Pain Society (CPS) revised consensus statement on the pharmacologic management of neuropathic pain. QUALITY OF EVIDENCE: A multidisciplinary interest group within the CPS conducted a systematic review of the literature on the current treatments of neuropathic pain in drafting the revised consensus statement. MAIN MESSAGE: Gabapentinoids, tricyclic antidepressants, and serotonin-norepinephrine reuptake inhibitors are the first-line agents for treating neuropathic pain...
November 2017: Canadian Family Physician Médecin de Famille Canadien
Carlos A Guillén-Astete, César Cardona-Carballo, Cristina de la Casa-Resino
Nontraumatic musculoskeletal disorders are the main reason for presentation to the emergency department (ED), with rachialgia (back pain) being the most common reason to request medical assessment among them. This also generates the highest demand for reassessments due to poor pain control or onset of adverse reactions to the treatment prescribed in the initial assessment.A retrospective observational study based on usual clinical practice was conducted in patients attending the ED due to low back pain during a period of 24 months...
November 2017: Medicine (Baltimore)
V De Vito, H Owen, M Marzoni, T Won Kim, A Poapolathep, M Giorgi
1. The aim of the study was to evaluate the pharmacokinetics of Tapentadol (TAP), a novel opioid analgesic, in laying hens after intravenous (IV) and oral (PO) administration and to quantify the concentrations of TAP residues in eggs. 2. Twenty healthy laying hens were divided into three groups: A (n=6), B (n=6) and C (n=8). The study was conducted in 2 phases. Groups A and B received TAP by IV and PO routes at the dose of 1 and 5 mg/kg, respectively. 3. No visible adverse effects were observed after administration of the drug...
November 8, 2017: British Poultry Science
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
R van der Schrier, K Jonkman, M van Velzen, E Olofsen, A M Drewes, A Dahan, M Niesters
Background: There is a clinical need for potent opioids that produce little or no respiratory depression. In the current study we compared the respiratory effects of tapentadol, a mu-opioid receptor agonist and noradrenaline reuptake inhibitor, and oxycodone, a selective mu-opioid receptor agonist. We hypothesize that tapentadol 100 mg has a lesser effect on the control of breathing than oxycodone 20 mg. Methods: Fifteen healthy volunteers were randomized to receive oral tapentadol (100 and 150 mg), oxycodone 20 mg or placebo immediate release tablets in a crossover double-blind randomized design...
December 1, 2017: British Journal of Anaesthesia
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