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https://www.readbyqxmd.com/read/28434283/considering-tapentadol-as-a-first-line-analgesic-14-questions
#1
Joseph V Pergolizzi, Frank Breve, Robert Taylor, Robert B Raffa, Stephani E Strasburger, Jo Ann LeQuang
Tapentadol is the newest centrally acting analgesic to be approved by the US FDA and regulatory bodies in other countries. It has been called the first-in-class of a novel-acting analgesic mechanism of action that combines µ-opioid receptor agonist activity with neuronal norepinephrine-reuptake inhibition in a single molecule. This duality of action should combine inhibition of ascending (afferent) pain-transmitting signals with activation of descending (efferent) pain-attenuating systems (e.g., diffuse noxious inhibitory controls)...
April 24, 2017: Pain Management
https://www.readbyqxmd.com/read/28429337/from-acute-to-chronic-pain-tapentadol-in-the-progressive-stages-of-this-disease-entity
#2
F Coluzzi, D Fornasari, J Pergolizzi, P Romualdi
OBJECTIVE: Chronic pain is now recognized as a neural disease, which results from a maladaptive functional and structural transformation process occurring over time. In its chronic phase, pain is not just a symptom but also a disease entity. Therefore, pain must be properly addressed, as many patients still report unsatisfactory pain control despite on-going treatment. The selection of the therapy - taking into account the pathophysiological mechanisms of pain - and the right timing can result in a successful analgesic outcome...
April 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28412373/mechanistic-evaluation-of-tapentadol-in-reducing-the-pain-perception-using-in-vivo-brain-and-spinal-cord-microdialysis-in-rats
#3
Vijay Benade, Ramakrishna Nirogi, Gopinadh Bhyrapuneni, Saivishal Daripelli, Ganesh Ayyanki, Shantaveer Irappanavar, Ranjithkumar Ponnamaneni, Arunkumar Manoharan
Role of monoamine neurotransmitters in the modulation of emotional and pain processing in spinal cord and brain regions is not well known. Tapentadol, a norepinephrine reuptake inhibitor with µ-opioid receptor agonistic activity has recently been introduced for the treatment of moderate to severe pain. The objective of the present study was to examine the effects of tapentadol on modulation of monoamines in the prefrontal cortex and dorsal horn using brain microdialysis. Tapentadol was administered intraperitoneally at 4...
April 12, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28378327/characterization-of-a-single-isomer-carboxymethyl-beta-cyclodextrin-in-chiral-capillary-electrophoresis
#4
Ida Fejős, Erzsébet Varga, Gábor Benkovics, Milo Malanga, Tamás Sohajda, Julianna Szemán, Szabolcs Beni, Szabolcs Béni
In this work, the synthesis, characterization and chiral capillary electrophoretic study of heptakis-(2,3-di-O-methyl-6-O-carboxymethyl)-β-cyclodextrin (HDMCM), a single-isomer carboxymethylated cyclodextrin are presented. The pH-dependent and selector concentration-dependent enantiorecognition properties of HDMCM were investigated and discussed herein. The enantioseparation was assessed applying a structurally diverse set of non-charged, basic, and zwitterionic racemates. The increase in the selector concentration and in the gross negative charge of HDMCM improved the enantioseparation that could be observed in the majority of the cases...
April 5, 2017: Electrophoresis
https://www.readbyqxmd.com/read/28280384/tapentadol-extended-release-for-the-management-of-chronic-neck-pain
#5
Domenico Billeci, Flaminia Coluzzi
BACKGROUND: The role of opioids in the management of chronic neck pain is still poorly investigated. No data are available on tapentadol extended release (ER). In this article, we present 54 patients with moderate-to-severe chronic neck pain treated with tapentadol ER. PATIENTS AND METHODS: Patients received tapentadol ER 100 mg/day; dosage was then adjusted according to clinical needs. The following parameters were recorded: pain; Douleur Neuropathique 4 score; Neck Disability Index score; range of motion; pain-associated sleep interference; quality of life (Short Form [36] Health Survey); Patient Global Impression of Change (PGIC); Clinician GIC; opioid-related adverse effects; and need for other analgesics...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28242230/thermal-antinociception-following-oral-administration-of-tapentadol-in-conscious-cats
#6
Graeme M Doodnaught, Marina C Evangelista, Paulo V M Steagall
OBJECTIVE: To evaluate the onset, magnitude and duration of thermal antinociception after oral administration of two doses of tapentadol in cats. STUDY DESIGN: Prospective, randomized, blinded, experimental study. ANIMALS: Six healthy adult cats weighing 4.4 ± 0.4 kg. METHODS: Skin temperature (ST) and thermal threshold (TT) were evaluated using a wireless TT device up to 12 hours after treatment. Treatments included placebo (PBO, 50 mg dextrose anhydrase orally), buprenorphine (BUP, 0...
January 7, 2017: Veterinary Anaesthesia and Analgesia
https://www.readbyqxmd.com/read/28162692/-445-secondary-endpoints-in-the-phase-iii-pivotal-trials-of-tapentadol-er
#7
P Schmidt
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/28162369/-144-routes-of-administration-of-tapentadol-products-as-reported-to-poison-centers
#8
S Severtson, B Bucher Bartelson, J Green, R Dart
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/28156625/clinical-and-health-care-setting-of-patients-admitted-at-pain-control-center-hospice-of-solofra-a-feasibility-model-of-end-of-life-care-in-the-avellino-province-of-italy
#9
Carmela Fasano, Luisa M Rizzo, A M Strollo, Elena De Vinco, Vincenzo Landolfi, Elena Altieri, Mario Nicola Vittorio Ferrante, Sergio Canzanella, Giuseppe Servillo, Lucia Genua, Maddalena Zampi, Gaetano D'Onofrio
59 Background: The Pain Control Center Hospice of Solofra (Italy) is managed with a mixed public / private, the first experience in the Campania region.We have evaluated the treatment procedures and the clinical outcome to make a comparison by between 123 evaluable patients in palliative care in 2015 and 232 evaluable patients in the biennium 2012-2014. METHODS: The following characteristics: patient gender, mean hospitalization time, differentiation between cancer and non cancer patients, medical weapon use, venous access type, enteral and parenteral feeding, pain killer use,Karnofsky scale...
October 9, 2016: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28119437/metabolic-patterns-of-fentanyl-meperidine-methylphenidate-tapentadol-and-tramadol-observed-in-urine-serum-or-plasma
#10
Fang Wu, Matthew H Slawson, Kamisha L Johnson-Davis
Drug testing is a useful tool to identify drug use or monitor adherence to prescription drugs. The interpretation of drug results can be complicated based on the pattern and proportional concentrations of drugs and/or drug metabolite(s). The purpose of this retrospective study was to detect the positivity rates and metabolic patterns of five prescription drugs, including fentanyl, meperidine, methylphenidate, tapentadol and tramadol. Retrospective data were retrieved from the laboratory information system in a national reference laboratory...
May 1, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28096581/role-of-preemptive-tapentadol-in-reduction-of-postoperative-analgesic-requirements-after-laparoscopic-cholecystectomy
#11
Ghanshyam Yadav, Gaurav Jain, Abhishek Samprathi, Annavi Baghel, Dinesh Kumar Singh
BACKGROUND AND AIMS: Poorly managed acute postoperative pain may result in prolonged morbidity. Various pharmacotherapies have targeted this, but research on an ideal preemptive analgesic continues, taking into account drug-related side effects. Considering the better tolerability profile of tapentadol, we assessed its role as a preemptive analgesic in the reduction of postoperative analgesic requirements, after laparoscopic cholecystectomy. MATERIAL AND METHODS: In a prospective-double-blinded fashion, sixty patients posted for above surgery, were randomized to receive tablet tapentadol 75 mg (Group A) or starch tablets (Group B) orally, an hour before induction of general anesthesia...
October 2016: Journal of Anaesthesiology, Clinical Pharmacology
https://www.readbyqxmd.com/read/28070880/on-the-molecular-basis-underlying-the-metabolism-of-tapentadol-through-sulfation
#12
Ahsan F Bairam, Mohammed I Rasool, Katsuhisa Kurogi, Ming-Cheh Liu
BACKGROUND AND OBJECTIVES: Previous studies reported that tapentadol-sulfate represented one of the major metabolites of tapentadol excreted in urine. The current study aimed to identify the human cytosolic sulfotransferases (SULTs) that is(are) capable of sulfating tapentadol and to examine whether human cells and human organ specimens are capable of sulfating tapentadol. METHODS: Thirteen human SULTs, previously expressed and purified, as well as human organ cytosols, were analyzed for tapentadol-sulfating activity using an established sulfotransferase assay...
January 10, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27997452/effect-of-tapentadol-on-splenic-cytokine-production-in-mice
#13
Silvia Franchi, Giada Amodeo, Marta Gandolla, Giorgia Moschetti, Alberto Emilio Panerai, Paola Sacerdote
BACKGROUND: Opioid drugs affect immunity, but not all opioid drugs share the same immunomodulatory properties. Tapentadol is an analgesic drug with a dual synergistic mechanism of action: µ-opioid receptor agonism and noradrenaline reuptake inhibition. Weaker µ-opioid receptor agonism combined with noradrenaline reuptake inhibition results in potent analgesia with reduced opioid side effects. We evaluated the impact of tapentadol on splenic cytokine in normal and in hyperalgesia/allodynia mice, comparing it with morphine and reboxetine, a noradrenaline reuptake inhibitor...
March 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/27987222/the-antinociceptive-effect-of-a-tapentadol-ketorolac-combination-in-a-mouse-model-of-trigeminal-pain-is-mediated-by-opioid-receptors-and-atp-sensitive-k-channels
#14
Israel Barreras-Espinoza, José Alberto Soto-Zambrano, Nicolás Serafín-Higuera, Ramón Zapata-Morales, Ángel Alonso-Castro, Ronell Bologna-Molina, Vinicio Granados-Soto, Mario A Isiordia-Espinoza
Preclinical Research The aim of the present study was to evaluate the antinoceptive interaction between the opioid analgesic, tapentadol, and the NSAID, ketorolac, in the mouse orofacial formalin test. Tapentadol or ketorolac were administered ip 15 min before orofacial formalin injection. The effect of the individual drugs was used to calculate their ED50 values and different proportions (tapentadol-ketorolac in 1:1, 3:1, and 1:3) were assayed in the orofacial test using isobolographic analysis and interaction index to evaluate the interaction between the drugs...
December 16, 2016: Drug Development Research
https://www.readbyqxmd.com/read/27881925/efficacy-and-tolerability-balance-of-oxycodone-naloxone-and-tapentadol-in-chronic-low-back-pain-with-a-neuropathic-component-a-blinded-end-point-analysis-of-randomly-selected-routine-data-from-12-week-prospective-open-label-observations
#15
Michael A Ueberall, Gerhard H H Mueller-Schwefe
OBJECTIVE: To evaluate the benefit-risk profile (BRP) of oxycodone/naloxone (OXN) and tapentadol (TAP) in patients with chronic low back pain (cLBP) with a neuropathic component (NC) in routine clinical practice. METHODS: This was a blinded end point analysis of randomly selected 12-week routine/open-label data of the German Pain Registry on adult patients with cLBP-NC who initiated an index treatment in compliance with the current German prescribing information between 1st January and 31st October 2015 (OXN/TAP, n=128/133)...
2016: Journal of Pain Research
https://www.readbyqxmd.com/read/27867511/is-tapentadol-different-from-classical-opioids-a-review-of-the-evidence
#16
Richard M Langford, Roger Knaggs, Paul Farquhar-Smith, Anthony H Dickenson
Tapentadol is a single molecule able to deliver analgesia by two distinct mechanisms, a feature which differentiates it from many other analgesics. Pre-clinical data demonstrate two mechanisms of action: mu-opioid receptor agonist activity and noradrenaline re-uptake inhibition. From these, one may predict that tapentadol would be applicable across a broad spectrum of pain from nociceptive to neuropathic. The evidence in animal models suggests that norepinephrine re-uptake inhibition (NRI) is a key mechanism and may even predominate over opioid actions in chronic (and especially neuropathic) pain states, reinforcing that tapentadol is different to classical opioids and may, therefore, be an a priori choice for the treatment of neuropathic and mixed pain...
November 2016: British Journal of Pain
https://www.readbyqxmd.com/read/27853999/quantifying-the-exposure-of-tapentadol-extended-release-in-japanese-patients-with-cancer-pain-and-bridging-tapentadol-pharmacokinetics-across-populations-using-a-modeling-approach
#17
Liping Zhang, Xiaoyu Yan, Sayori Nobe, Peter Zannikos, Mila Etropolski, Partha Nandy
BACKGROUND AND OBJECTIVES: Tapentadol extended release (ER) is approved for the management of chronic and acute pain in adults. There has been no report of tapentadol ER pharmacokinetics in subjects with cancer pain. This analysis investigated tapentadol ER pharmacokinetics in Japanese patients with cancer pain and bridged it with the pharmacokinetics in Japanese healthy subjects and Caucasian patients with cancer pain. METHODS: Nonlinear mixed-effect pharmacokinetic modeling was conducted based on pooled tapentadol ER concentration data collected in five Phase 1 studies from 138 Japanese and Korean healthy subjects and in two Phase 3 studies from 215 Japanese and Korean subjects with cancer pain...
March 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/27844472/patient-relevant-outcomes-and-health-related-quality-of-life-in-patients-with-chronic-severe-noncancer-pain-treated-with-tapentadol-prolonged-release-using-criteria-of-health-technology-assessment
#18
Johannes Fx Hofmann, Arun Lal, Maike Steffens, Robert Boettger
OBJECTIVE: To perform a systematic comparison of tapentadol prolonged release (PR) and oxycodone controlled release (CR) using patient-relevant endpoints of efficacy, safety, and health-related quality of life (HRQoL) according to criteria used in health technology assessment. To derive a minimal important difference (MID) for the EQ-5D from three pivotal trials to measure patient-relevant changes in HRQoL. DESIGN: Randomized, double-blind, placebo and active controlled...
September 2016: Journal of Opioid Management
https://www.readbyqxmd.com/read/27807793/opioids-and-gi-motility-friend-or-foe
#19
REVIEW
Allen A Lee, William L Hasler
The use of opioids for the treatment of chronic non-cancer pain is growing at an alarming rate. Opioid-induced bowel dysfunction (OBD) is a common adverse effect of long-term opioid treatment manifesting as constipation, nausea, and vomiting. These effects are primarily mediated by peripheral μ-opioid receptors with resultant altered GI motility and function. As a result, patients may present with opioid-induced constipation (OIC), opioid-induced nausea and vomiting (OINV), and/or narcotic bowel syndrome (NBS)...
November 2, 2016: Current Treatment Options in Gastroenterology
https://www.readbyqxmd.com/read/27611642/tapentadol-prolonged-release-for-chronic-pain-a-review-of-clinical-trials-and-5-years-of-routine-clinical-practice-data
#20
REVIEW
Ralf Baron, Leopold Eberhart, Kai-Uwe Kern, Stefan Regner, Roman Rolke, Christian Simanski, Thomas Tölle
Tapentadol prolonged release (PR) for the treatment of moderate to severe chronic pain combines 2 modes of action. These are μ-opioid receptor agonism and noradrenaline reuptake inhibition in a single molecule that allow higher analgesic potency through modulation of different pharmacological targets within the pain transmitting systems. At the same time, this can also serve as a clue for modulation of different pain-generating mechanisms according to nociceptive, neuropathic, or mixed pain conditions. Tapentadol PR has now been on the market for 5 years, with over 4...
September 9, 2016: Pain Practice: the Official Journal of World Institute of Pain
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