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Tapentadol for pain

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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/28280384/tapentadol-extended-release-for-the-management-of-chronic-neck-pain
#4
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/28096581/role-of-preemptive-tapentadol-in-reduction-of-postoperative-analgesic-requirements-after-laparoscopic-cholecystectomy
#5
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/27997452/effect-of-tapentadol-on-splenic-cytokine-production-in-mice
#6
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/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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
https://www.readbyqxmd.com/read/27580162/comparative-metabolism-of-tramadol-and-tapentadol-a-toxicological-perspective
#13
Joana Barbosa, Juliana Faria, Odília Queirós, Roxana Moreira, Félix Carvalho, Ricardo Jorge Dinis-Oliveira
Tramadol and tapentadol are centrally acting, synthetic opioid analgesics used in the treatment of moderate to severe pain. Main metabolic patterns for these drugs in humans are well characterized. Tramadol is mainly metabolized by cytochrome P450 CYP2D6 to O-desmethyltramadol (M1), its main active metabolite. M1 and tapentadol undergo mainly glucuronidation reactions. On the other hand, the pharmacokinetics of tramadol and tapentadol are dependent on multiple factors, such as the route of administration, genetic variability in pharmacokinetic components and concurrent consumption of other drugs...
November 2016: Drug Metabolism Reviews
https://www.readbyqxmd.com/read/27568082/a-tapentadol-related-fatality-case-report-with-postmortem-concentrations
#14
F Lee Cantrell, Phyllis Mallett, Lenore Aldridge, Kimi Verilhac, Iain M McIntyre
Tapentadol (TAP) is an analgesic agent indicated for the management of different types of pain. It has a novel mechanism of action in that it induces analgesia via both μ-opioid receptor agonism and norepinephrine reuptake inhibition. Although deaths associated with TAP use have been reported, there is a paucity of published literature regarding TAP concentrations in biological samples obtained from TAP-associated fatalities. We report a case of TAP toxicity resulting in death with postmortem peripheral and central blood concentrations, liver, vitreous, urine, and gastric contents...
September 2016: Forensic Science International
https://www.readbyqxmd.com/read/27516366/efficacy-and-safety-of-tapentadol-immediate-release-assessment-in-treatment-of-moderate-to-severe-pain-a-systematic-review-and-meta-analysis
#15
Jing-Ping Xiao, Ai-Ling Li, Bi-Min Feng, Yun Ye, Guo-Jun Wang
Objective.: To assess the efficacy and safety of tapentadol IR for moderate to severe pain compared to oxycodone IR. Methods.: A search was carried out up to July 2015 for randomized controlled trials (RCTs) of tapentadol IR compared to placebo or oxycodone HCL IR 10 mg for moderate to severe pain. Studies were pooled by risk ratio (RR) and weighted mean differences (WMD) with 95% confidence interval (CI). Results.: Nine RCTs (n = 3,961) were analyzed...
January 1, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/27510567/prediction-of-response-to-tapentadol-in-chronic-low-back-pain
#16
M Reimer, P Hüllemann, M Hukauf, T Keller, A Binder, J Gierthmühlen, R Baron
BACKGROUND: Many chronic low back pain (cLBP) patients do not satisfactorily respond to treatment. The knowledge of responders and non-responders before initiating treatment would improve decision making and reduce health care costs. The aims of this exploratory prediction study in cLBP patients treated with tapentadol were to identify predictors of treatment outcome based on baseline characteristics, to evaluate quality-of-life and functionality as alternative outcome parameters and to develop nomograms to calculate the individual probability of response...
February 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/27479625/treating-painful-diabetic-peripheral-neuropathy-an-update
#17
REVIEW
Matthew J Snyder, Lawrence M Gibbs, Tammy J Lindsay
Painful diabetic peripheral neuropathy occurs in approximately 25% of patients with diabetes mellitus who are treated in the office setting and significantly affects quality of life. It typically causes burning pain, paresthesias, and numbness in a stocking-glove pattern that progresses proximally from the feet and hands. Clinicians should carefully consider the patient's goals and functional status and potential adverse effects of medication when choosing a treatment for painful diabetic peripheral neuropathy...
August 1, 2016: American Family Physician
https://www.readbyqxmd.com/read/27448104/effectiveness-of-tapentadol-prolonged-release-for-the-management-of-painful-mucositis-in-head-and-neck-cancers-during-intensity-modulated-radiation-therapy
#18
Mazzola Rosario, Ricchetti Francesco, Fersino Sergio, Giaj Levra Niccolò, Fiorentino Alba, Nicodemo Maurizio, Albanese Sergio, Gori Stefania, Alongi Filippo
PURPOSE: To evaluate the effectiveness and tolerability profile of tapentadol prolonged release (PR) in a cohort of head and neck cancer (HNC) patients affected by background pain due to painful mucositis during intensity modulated radiation therapy with or without cisplatin with definitive and adjuvant intent. MATERIALS AND METHODS: Tapentadol PR was administered at the moment of pain onset in opioid-naive patients at the dosage of 50 mg BID. The dosage was increased 50 mg twice a day until the optimal dose of no more than 500 mg/day of tapentadol PR...
October 2016: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/27435439/effectiveness-and-tolerability-of-tapentadol-sustained-release-in-the-australian-setting
#19
Marc A Russo, Danielle M Santarelli
OBJECTIVE: To assess the effectiveness and tolerability of tapentadol sustained release (SR) following its introduction to the Australian private market. DESIGN: A retrospective audit of routine clinical practice with data collection beginning 2 months after the first tapentadol SR prescription. SETTING: A multidisciplinary Australian pain clinic. PATIENTS: Fifty patients who were prescribed tapentadol SR as part of routine clinical management at the pain clinic...
May 2016: Journal of Opioid Management
https://www.readbyqxmd.com/read/27413479/tapentadol-can-it-kill-two-birds-with-one-stone-without-breaking-windows
#20
REVIEW
Eun Jung Chang, Eun Ji Choi, Kyung Hoon Kim
Tapentadol is a novel oral analgesic with a dual mode of action as an agonist of the µ-opioid receptor (MOR), and as a norepinephrine reuptake inhibitor (NRI) all in a single molecule. Immediate release (IR) tapentadol shows its analgesic effect quickly, at around 30 minutes. Its MOR agonistic action produces acute nociceptive pain relief; its role as an NRI brings about chronic neuropathic pain relief. Absorption is rapid, with a mean maximal serum concentration at 1.25-1.5 h after oral intake. It is present primarily in the form of conjugated metabolites after glucuronidation, and excretes rapidly and completely via the kidneys...
July 2016: Korean Journal of Pain
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