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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
Nebojsa Nick Knezevic, Tatiana Tverdohleb, Ivana Knezevic, Kenneth D Candido
INTRODUCTION: Even though pain is a complex process involving many different mediators, enzymes, receptors and ion channels, pain medications usually address only individual targets. Nucynta, which addresses multiple pain targets, was the first new centrally acting analgesic to be approved by the FDA in 2008. AREAS COVERED: Pharmacology: Tapentadol is a centrally acting opioid with two mechanisms of action, including agonism at the μ-opioid receptor (MOR) and inhibition of norepinephrine reuptake (NRI), producing analgesia individually and via a combination of both acts synergistically at the spinal and supraspinal levels...
2015: Expert Opinion on Drug Metabolism & Toxicology
Gary Eichenbaum, Karin Göhler, Mila Etropolski, Ilona Steigerwald, Joseph Pergolizzi, Myoung Kim, Gary Vorsanger
OBJECTIVES: Opioid-induced androgen deficiency (OPIAD) affects patients treated with opioid analgesics. The norepinephrine reuptake inhibitor (NRI) and µ-opioid receptor (MOR) agonist activities of tapentadol may result in tapentadol having less effect on serum androgen concentrations than analgesics acting through the MOR alone, such as morphine and oxycodone. The objectives of this publication are to 1) evaluate the effects of tapentadol (NUCYNTA and NUCYNTA extended release [ER]) on sex hormone concentrations in healthy male volunteers (vs placebo and morphine) and patients with osteoarthritis (vs placebo and oxycodone), and 2) present a mechanistic hypothesis explaining how the combined MOR agonist and NRI activities of tapentadol may result in less impact on androgen concentrations...
May 2015: Journal of Opioid Management
Douglas Borys, Matthew Stanton, David Gummin, Tracy Drott
BACKGROUND: Tapentadol (Nucynta) is indicated for the treatment of moderate to severe pain in adults. Tapentadol's mechanism of action consists of acting as an agonist on the μ-opioid receptor and by inhibiting the reuptake of norepinephrine. There are no published reports on the toxicity of tapentadol in pediatric patients. The goals of this study are to describe the incidence, medical outcomes, clinical effects, and treatment secondary to tapentadol exposure. METHODS: This retrospective observational study used data from the National Poison Data System...
February 2015: Pediatrics
Dori M Franco, Zabiullah Ali, Barry Levine, Robert A Middleberg, David R Fowler
Tapentadol (Nucynta) is a centrally acting opioid analgesic prescribed for the treatment of moderate to severe acute pain. Its efficacy is believed to be due to μ-opioid receptor agonist activity and inhibition of norepinephrine reuptake resulting in increased norepinephrine concentrations. There is only one other case in the literature relating to the toxicity of this agent or report of a fatality. This case report documents a case in which tapentadol was identified as the cause of death. The tapentadol concentration found in the heart blood submitted in this case was more than 20 times the upper limit of the therapeutic range...
December 2014: American Journal of Forensic Medicine and Pathology
Louis Alexander, Richard O Mannion, Brianne Weingarten, Richard J Fanelli, Gary L Stiles
BACKGROUND: Millions of patients are treated with opioid analgesics (OpAs) to relieve pain. Unfortunately, these medications are subject to abuse and/or unintended misuse. Abuse deterrent formulations (ADFs) represent an intervention strategy to decrease abuse/misuse without affecting patient access. The Food and Drug Administration (FDA) has issued Draft Guidance "Abuse deterrent opioids, Evaluation and Labeling" and is currently actively pursuing scientific input on this issue. METHODS: The development of ADF technologies was reviewed using peer reviewed journals describing OpA post marketing studies, web sites containing FDA announcements on product approvals and manufacturer product use profiles...
May 1, 2014: Drug and Alcohol Dependence
Mana Saraghi, Elliot V Hersh
Abstract Since 2008, three new analgesic entities, tapentadol immediate release (Nucynta) diclofenac potassium soft gelatin capsules (Zipsor), and bupivacaine liposome injectable suspension (EXPAREL) were granted US Food and Drug Administration (FDA) approval to treat acute pain. Tapentadol immediate-release is a both a mu-opioid agonist and a norepinephrine reuptake inhibitor, and is indicated for the treatment of moderate to severe pain. Diclofenac potassium soft gelatin capsules are a novel formulation of diclofenac potassium, which is a nonsteroidal anti-inflammatory drug (NSAID), and its putative mechanism of action is through inhibition of cyclooxygenase enzymes...
2013: Anesthesia Progress
Gina Games, Amber Hutchison
With the prevalence of diabetes mellitus (DM) increasing, pathologic complications such as diabetic peripheral neuropathy (DPN) are also becoming more common. Of those diagnosed with DM, 10% to 20% of patients suffer from painful DPN. Until recently, only pregabalin and duloxetine possessed Food and Drug Administration (FDA) approval for this condition. However, FDA recently approved tapentadol-ER [extended release] (Nucynta ER) for painful DPN. Tapentadol-ER is an opioid analgesic commonly used for the treatment of moderate-to-severe chronic pain that contains a unique dual mechanism acting as both a weak mu-opiod receptor agonist and norepinephine-reuptake inhibitor...
October 2013: Consultant Pharmacist: the Journal of the American Society of Consultant Pharmacists
Nalini Vadivelu, Yili Huang, Brian Mirante, Michael Jacoby, Ferne R Braveman, Roberta L Hines, Raymond Sinatra
Poorly controlled acute and chronic pain can increase morbidity, impair quality of life and prolong disability. Over 80 percent of post surgical patients report moderate to severe uncontrolled postoperative pain. Over-reliance on potent opioid agonists can lead to several opioid related side effects such as gastrointestinal intolerability, respiratory depression and cognitive impairment. A recently approved dual acting central analgesic tapentadol may offer improved tolerability over traditional opioid agonists while having multimodal opioid and nonopioid analgesic benefits...
2013: Drug, Healthcare and Patient Safety
Deborah R Erlich, Warren Bodine
No abstract text is available yet for this article.
May 1, 2012: American Family Physician
Scott J Larson, Joseph Pestaner, Sunil K Prashar, Ciena Bayard, Lucas W Zarwell, Marie Pierre-Louis
Postmortem distribution concentrations of the pain medication tapentadol and its metabolite N-desmethyltapentadol are reported. Tapentadol (Nucynta®) is a synthetic mu-opioid receptor agonist that also has norepinephrine reuptake inhibitor action. The laboratory received two cases. Case 1: a 19-year-old, morbidly obese male with sudden unexpected death. Toxicology results revealed tapentadol (femoral blood: 0.77 mg/L, liver: 1.65 mg/kg), N-desmethyltapentadol (femoral blood: 0.07 mg/L, liver: 0.19 mg/kg), diazepam (femoral blood: 0...
July 2012: Journal of Analytical Toxicology
Rob Riemsma, Carol Forbes, Julie Harker, Gill Worthy, Kate Misso, Michael Schäfer, Jos Kleijnen, Steffen Stürzebecher
AIM: A systematic review of chronic pain treatment with strong opioids (step 3 WHO pain ladder) and a comparison to a new drug recently approved for the treatment of severe chronic pain in Europe, tapentadol (Palexia, Nucynta*), were performed. METHODS: Thirteen electronic databases were searched as well as a number of other sources from 1980 up to November 2010 for relevant randomized controlled clinical trials in chronic moderate and severe pain investigating at least one step 3 opioid...
October 2011: Current Medical Research and Opinion
James A Bourland, Ayodele A Collins, Scot A Chester, Sumankalai Ramachandran, Ronald C Backer
Urine specimens from pain management patients dosed with Nucynta (Tapentadol) were confirmed for the presence of tapentadol and N-desmethyltapentadol using ultra-performance liquid chromatography-tandem mass spectrometry to minimize sample preparation and urine volume requirements. The linearity of the method for both tapentadol and N-desmethyltapentadol demonstrated correlation coefficients (R²) above 0.99 and linear ranges from 50 to 500,000 ng/mL for tapentadol and 100 to 500,000 ng/mL for N-desmethyltapentadol...
October 2010: Journal of Analytical Toxicology
James E Frampton
Tapentadol (Nucynta) is an orally active, centrally acting synthetic analgesic that is thought to exert its analgesic effects via two mechanisms of action (mu-opioid receptor agonism and norepinephrine reuptake inhibition). In the US, the immediate-release (IR) formulation of the drug is approved for the relief of moderate to severe acute pain in patients aged > or =18 years. In the EU, the drug is currently in the marketing authorization process. In clinical trials in patients with moderate to severe acute (postorthopaedic surgical or musculoskeletal) pain, recommended regimens of tapentadol IR (50-100 mg every 4-6 hours) provided an analgesic effect that was superior to that of placebo, and noninferior or similar to that of oxycodone IR (10 or 15 mg every 4-6 hours)...
September 10, 2010: Drugs
(no author information available yet)
The FDA has approved tapentadol hydrochloride (Nucynta--Ortho-McNeil Janssen) for oral treatment of moderate to severe acute pain in patients >18 years old. It has been classified as a Schedule II controlled substance. Tapentadol (Nucynta) is a centrally acting oral analgesic with opioid and adrenergic activity. In studies published to date, it was as effective as oxycodone or morphine with a lower incidence of gastrointestinal adverse effects, but until more data become available, older analgesics are preferred...
August 10, 2009: Medical Letter on Drugs and Therapeutics
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