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Tapentadol for pain

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 allows 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 2...
September 9, 2016: Pain Practice: the Official Journal of World Institute of Pain
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
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
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...
August 11, 2016: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
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...
August 11, 2016: European Journal of Pain: EJP
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
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
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
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
M Förster, S Helfert, R Dierschke, M Großkopf, P Hüllemann, T Keller, R Baron, A Binder
OBJECTIVE: Tapentadol is effective in the treatment of neuropathic and nociceptive pain and in acute and chronic pain conditions; two mechanisms combining opioid µ-receptor agonism and noradrenergic reuptake inhibition underlie its analgesic effect. RESEARCH DESIGN AND METHODS: With this single-center, placebo-controlled, double-blind, cross-over pilot-study, we investigated the antihyperalgesic effect of a single oral dose of 100 mg immediate-release tapentadol on thermal and mechanical hyperalgesia in two human models (i...
September 2016: Expert Opinion on Pharmacotherapy
Lorenzo Di Cesare Mannelli, Laura Micheli, Letizia Crocetti, Maria Paola Giovannoni, Claudia Vergelli, Carla Ghelardini
Neuropathic pain is originated from different alterations of the nervous system. The difficulty of treatment strongly impairs quality of life of affected people. It is associated with severe, chronic sensory disturbances characterized by spontaneous pain, increased responsiveness to painful stimuli and pain perceived in response to normally non-noxious stimuli. The underlying mechanisms are complex and involve both peripheral and central nervous components.The noradrenergic system plays a pivotal role in the control of pain since its widespread distribution in the "pain matrix" representing a valuable therapeutic target...
June 8, 2016: Mini Reviews in Medicinal Chemistry
Y Tominaga, H Koga, N Uchida, M Wanibe, K Hirose, T Matsumura, A Okamoto, U Richarz, M Etropolski
BACKGROUND: The efficacy of tapentadol extended release (ER) for managing chronic pain has been demonstrated in large-scale, randomized, controlled, phase 3 studies (N=318-1,030) in patients with chronic osteoarthritis (OA) pain, low back pain (LBP), and pain related to diabetic peripheral neuropathy (DPN), which led to registration in many regions, including the United States and Europe. 2 pilot 12-week, randomized, double-blind, placebo-controlled phase 2 studies of tapentadol ER for chronic pain (OA knee pain or LBP, n=91; DPN or peripheral herpetic neuralgia [PHN] pain; n=91) were conducted in Japan...
July 2016: Drug Research
H G Kress, E D Koch, H Kosturski, A Steup, K Karcher, C Dogan, M Etropolski, M Eerdekens
BACKGROUND: A recent randomized-withdrawal, active- and placebo-controlled, double-blind phase 3 study showed that tapentadol prolonged release (PR) was effective and well tolerated for managing moderate to severe, chronic malignant tumour-related pain in patients who were opioid naive or dissatisfied with current treatment (Pain Physician, 2014, 17, 329-343). This post hoc, subgroup analysis evaluated the efficacy and tolerability of tapentadol PR in patients who previously received and were dissatisfied with tramadol for any reason and who had a pain intensity ≥5 (11-point numerical rating scale) before converting directly to tapentadol PR...
October 2016: European Journal of Pain: EJP
Gregorio A Brunetti, Giovanna Palumbo, Giacomo S Morano, Erminia Baldacci, Ida Carmosino, Giorgia Annechini, Romina Talone, Sara Kiflom, Giada Mastrogiacomo, Sara Grammatico, Marta Chisini, Adriana Costa, Andrea Tendas, Laura Scaramucci, Marco Giovannini, Pasquale Niscola, Maria T Petrucci, Claudio Cartoni
BACKGROUND: More than 50% of oncohematological patients suffer from pain syndrome, mostly originating from the bone, which often include nociceptive and neuropathic complaints. Tapentadol, a recently available treatment option for cancer pain, exerts a dual analgesic mechanisms (opioid and noradrenergic), allowing for a high clinical efficacy as well as for a reduction in adverse events compared to traditional opioids. AIM: To explore the safety and efficacy of tapentadol as a suitable agent for the pain management in the setting of oncohematology...
2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
R Baron, A Binder, N Attal, R Casale, A H Dickenson, R-D Treede
BACKGROUND AND OBJECTIVE: Low back pain (LBP) is one of the most common chronic pain conditions. This paper reviews the available literature on the role of neuropathic mechanisms in chronic LBP and discusses implications for its clinical management, with a particular focus on pharmacological treatments. DATABASES AND DATA TREATMENT: Literature searches were performed in PubMed, key pain congresses and ProQuest Dialog to identify published evidence on neuropathic back pain and its management...
July 2016: European Journal of Pain: EJP
Antonio Alcántara-Montero, Clara I Sánchez-Carnerero
INTRODUCTION: Most of the clinical practice guidelines consulted agree that tricyclics, dual (venlafaxine/duloxetine) antidepressants, gabapentin/pregabalin antiepileptic drugs, lidocaine 5% patches and capsaicin 8% patches are the first-line drugs in the treatment of peripheral neuropathic pain, being tramadol and some strong opioids (morphine, oxycodone and tapentadol) second-line drugs treatment. Moreover, the prevalence of neuropathic pain refractory to treatment is about 1.5% of the population, so that an estimated 50% of patients not responding to prescribed treatment...
March 1, 2016: Revista de Neurologia
Richard C Dart, Hilary L Surratt, Marie-Claire Le Lait, Yami Stivers, Vikhyat S Bebarta, Clark C Freifeld, John S Brownstein, John J Burke, Steven P Kurtz, Nabarun Dasgupta
OBJECTIVE:   Prescription opioid analgesics are commonly prescribed for moderate to severe pain. An unintended consequence of prescribing opioid analgesics is the abuse and diversion of these medications. Tapentadol ER is a recently approved centrally acting analgesic with synergistic mechanisms of action: μ-opioid receptor agonism and inhibition of norepinephrine reuptake. We assessed the amount of diversion and related cost of obtaining tapentadol IR (Nucynta®) and tapentadol ER (Nucynta ER®) as well as other Schedule II opioid medications in street transactions in the United States using the Researched Abuse, Diversion and Addiction-Related Surveillance (RADARS®) System...
August 2016: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
Kunihito Kanazawa, Akitaka Yoshizawa, Hiroyuki Ishigure, Atsuko Shimoda, Rie Hiratsuka, Hiroyoshi Ikeda, Takayuki Yoshizawa
Tapentadol(TP)is a new strong opioid analgesicthat has both m-opioid receptor(MOR)effects and norepinephrine reuptake inhibitor(NRI)effects. In comparison with the existing strong opioid analgesics, the mechanism of action suitable for palliation of neuropathic pain is expected to be better for TP. The analgesic effect and side effects of this drug were tested in 10 cases of exacerbation of neuropathic pain at our hospital, and the sedative response rate was 70%. The main side effects were somnolence 44.4%, nausea 33...
December 2015: Gan to Kagaku Ryoho. Cancer & Chemotherapy
Dymphy R Huntjens, Lia C Liefaard, Partha Nandy, Henk-Jan Drenth, An Vermeulen
BACKGROUND AND OBJECTIVE: Tapentadol is a centrally acting analgesic with two mechanisms of action, µ-opioid receptor agonism and noradrenaline reuptake inhibition. The objectives were to describe the pharmacokinetic behavior of tapentadol after oral administration of an extended-release (ER) formulation in healthy subjects and patients with chronic pain and to evaluate covariate effects. METHODS: Data were obtained from 2276 subjects enrolled in five phase I and nine phase II and III studies...
March 2016: Clinical Drug Investigation
Yoshika Takahashi, Masako Iseki
Opioid analgesics are widely used for managing moderate to severe pain. In cancer pain management sustained-release opioids are used for continuous pain as well as immediate-release opioids for breakthrough pain. Sustained-release drugs have the advantage of stabilizing the blood concentration, although it takes some time to exert their effects. In Japan, the currently available oral sustained-release opioids include six types of sustained-release morphine (three are once-a-day formulations, while the rest are twice-a-day), one type of oxycodone and tapentadol...
November 2015: Masui. the Japanese Journal of Anesthesiology
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