Tapentadol extended release in the management of peripheral diabetic neuropathic pain

Vadivelu, Nalini; Kai, Alice M.; Maslin, Benjamin; Kodumudi, Gopal; Legler, Aron; Berger, Jennifer

doi:10.2147/tcrm.s32193

Cited by 43 publications

(20 citation statements)

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“…The effect of repeated dosing with tapentadol matches very well many chronic pain conditions (Riemsma et al, 2011) with impaired CPM such as OA pain (Steigerwald et al, 2012b), LBP (Buynak et al, 2010;Steigerwald et al, 2012a;Baron et al, 2016), painful peripheral diabetic neuropathy (Schwartz et al, 2015;Vadivelu et al, 2015), and cancer pain (Kress et al, 2014).…”

Section: Targeting Descending Pathwaysmentioning

confidence: 76%

Assessment and manifestation of central sensitisation across different chronic pain conditions

Arendt-Nielsen

Morlion

Perrot

et al. 2017

European Journal of Pain

492

494

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Different neuroplastic processes can occur along the nociceptive pathways and may be important in the transition from acute to chronic pain and for diagnosis and development of optimal management strategies. The neuroplastic processes may result in gain (sensitisation) or loss (desensitisation) of function in relation to the incoming nociceptive signals. Such processes play important roles in chronic pain, and although the clinical manifestations differ across condition processes, they share some common mechanistic features. The fundamental understanding and quantitative assessment of particularly some of the central sensitisation mechanisms can be translated from preclinical studies into the clinic. The clinical perspectives are implementation of such novel information into diagnostics, mechanistic phenotyping, prevention, personalised treatment, and drug development. The aims of this paper are to introduce and discuss (1) some common fundamental central pain mechanisms, (2) how they may translate into the clinical signs and symptoms across different chronic pain conditions, (3) how to evaluate gain and loss of function using quantitative pain assessment tools, and (4) the implications for optimising prevention and management of pain. The chronic pain conditions selected for the paper are neuropathic pain in general, musculoskeletal pain (chronic low back pain and osteoarthritic pain in particular), and visceral pain (irritable bowel syndrome in particular). The translational mechanisms addressed are local and widespread sensitisation, central summation, and descending pain modulation. Significance Central sensitisation is an important manifestation involved in many different chronic pain conditions. Central sensitisation can be different to assess and evaluate as the manifestations vary from pain condition to pain condition. Understanding central sensitisation may promote better profiling and diagnosis of pain patients and development of new regimes for mechanism based therapy. Some of the mechanisms underlying central sensitisation can be translated from animals to humans providing new options in development of therapies and profiling drugs under development.

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Section: Targeting Descending Pathwaysmentioning

confidence: 76%

Assessment and manifestation of central sensitisation across different chronic pain conditions

Arendt-Nielsen

Morlion

Perrot

et al. 2017

European Journal of Pain

492

494

View full text Add to dashboard Cite

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“…Recently, tapentadol has been demonstrated to be effective in the management of both diabetic‐ and chemotherapy‐induced neuropathic pain (Vadivelu et al, , Galiè, Villani, Terrenato, & Pace, ). Similarly, Schwartz et al () evaluating the efficacy and tolerability of tapentadol extended its release for diabetic peripheral neuropathy.…”

Section: α2‐adrenoceptors As a Target For Neuropathic Pain Treatment;mentioning

confidence: 99%

Spinal α₂‐adrenoceptors and neuropathic pain modulation; therapeutic target

Bahari

Meftahi

2019

British J Pharmacology

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Neuropathic pain can arise from disease or damage to the nervous system. The most common symptoms of neuropathic pain include spontaneous pain, allodynia, and hyperalgesia. There is still limited knowledge about the factors that initiate and maintain neuropathic pain. However, ample evidence has proved the antinociceptive role of spinal α‐adrenoceptors following nerve injury. It is well‐documented that https://www.sciencedirect.com/topics/neuroscience/norepinephrine descending pathways from supraspinal loci exert an inhibitory influence on the spinal cord nociceptive neurons, mostly through the activation of spinal α2‐adrenoceptors. This, in turn, suppresses transmission of pain input and the hyperexcitability of spinal dorsal horn neurons. There is considerable evidence demonstrating that spinal application of α2‐adrenoceptor https://www.sciencedirect.com/topics/neuroscience/agonists leads to analgesic effects in animal models of neuropathic pain. Today, despite the recent rapid development of neuroscience and drug discovery, effective drugs with clear basic mechanisms have remained a mystery. Here, we give an overview of the cellular mechanisms through which brainstem adrenergic descending inhibitory processing can alter spinal pain transmission to the higher centres, and how these pathways change in neuropathic pain conditions focusing on the role of spinal α2‐adrenoceptors in the spinal dorsal horn. We then suggest that α2‐adrenoceptor agonist may be useful to treat neuropathic pain. Linked Articles This article is part of a themed section on Adrenoceptors—New Roles for Old Players. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v176.14/issuetoc

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“…It is in available in the U.S. since 2008 for the treatment of moderate acute to severe pain, in its immediate release (IR) formulation, and since 2011 for the treatment of moderate chronic to severe pain in its extended release (ER) formulation, after approval by the Food and Drug Administration (FDA) 5,6 . In the European market, the IR and ER formulations of the drug were approved by the European Medicines Agency (EMA) in 2010 7,8 . Its central analgesic action occurs by means of two mechanisms: 1) as an agonist of the μ-opioid receptors (MOR), with the same affinity or 10 times higher on KOR receptors (k-opioid receptor) REVIEW ARTICLE DOI 10.5935/2595-0118.20180015 and DOR (delta opioid receptor) 4 ; 2) as a norepinephrine reuptake inhibitor (NRI).…”

Section: Contentsmentioning

confidence: 99%

“…The main metabolic pathway occurs through glucuronic acid binding, 97% due to phase 2 reactions. The main metabolite is tapentadol-O-glucuronide 4,8 , which does not exercise any activity on opioid receptors or reuptake systems of synapses or other junction 9 . Ninety seven percent of the drug delivered is transformed into inactive metabolites 4 .…”

Section: Contentsmentioning

confidence: 99%

“…During the first 24 months after the initial release and commercialization of tapentadol IR in the U.S., the abuse rates found were much lower than those for oxycodone or hydrocodone, through a system called RADARS 12 . A cohort study showed that the risk of abuse with tapentadol was lower when compared to oxycodone 8 . A study with rats and mice studied the acute toxicity by oral and venous administration.…”

Section: Contentsmentioning

confidence: 99%

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Tapentadol: what every doctor needs to know about this new drug

Mosele¹,

Almeida²,

Hess³

2018

Brazilian Journal of Pain

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BACKGROUND AND OBJECTIVES:Acute and chronic pain is a major problem with repercussion in our society, causing impairment in the quality of life of patients as well as socioeconomic losses, due to work absenteeism. This review aims to analyze the use of tapentadol, an analgesic not yet available in Brazil, with a dual mechanism of action, in the treatment of acute and chronic pain syndromes. CONTENTS: A review about this new drug was made on the Pubmed database using the keywords "tapentadol" and "opioids," evaluating its pharmacological and clinical aspects comparing with other current drugs in pain treatment, as well as its indications and contraindications in the management of patients with pain disorders. CONCLUSION: Tapentadol has been shown to be effective in the treatment of acute and chronic pain, with potency equivalent to the opioids currently used. In addition, it developed less tolerance, less adverse effects and better therapeutic response in chronic neuropathic pain when compared to pure μ-opioid receptors agonists. Keywords: Dual mechanism of action, Opioids, Tapentadol. RESUMO JUSTIFICATIVA E OBJETIVOS:A dor aguda e crônica consiste em um problema de grande repercussão em qualquer sociedade atual, causando degradação na qualidade de vida dos próprios pacientes e comprometimento socioeconômico pelo absenteísmo laboral. O objetivo deste estudo foi analisar o uso do tapentadol, um analgésico ainda não disponível no Brasil e com duplo mecanismo de ação, no tratamento das síndromes dolorosas agudas e crônicas. Tapentadol: what every doctor needs to know about this new drug CONTEÚDO:Foi realizada uma pesquisa na base de dados Pubmed utilizando os descritores "tapentadol" e "opioides" para revisão da literatura mundial sobre esse novo fármaco, avaliando as características farmacológicas e aspectos clínicos do seu uso na realidade atual, em comparação com os fármacos já existentes no mercado, assim como suas indicações e contraindicações no manuseio do paciente com dor. CONCLUSÃO: O tapentadol se mostrou eficaz no tratamento de dores agudas e crônicas, com potência equiparável aos opioides já comercializados. Além disso, desenvolveu menos tolerân-cia, menos efeitos adversos e melhor resposta terapêutica na dor crônica neuropática quando comparado com agonistas receptores opioides tipo μ puros. Descritores: Duplo mecanismo de ação, Opioides, Tapentadol. INTRODUCTIONPain is a problem of great proportion, involving 20 to 25% of the population with an increasing incidence. Despite the extraordinary advances in anatomy, physiology, diagnosis and pain management, more than 50% of patients report improper relief. This can be related to the neuroplasticity process of the pain pathways 1 , creating a persistent "memory" of the aggressive event and neuronal hiperexcitability 2,3 . Understanding chronic pain neurobiology is fundamental to target the treatment. Thus, the use of drugs that act on more than one pathophysiologic mechanism, as tapentadol, can be a new weapon in the therapeutic armamentarium aga...

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Tapentadol extended release in the management of peripheral diabetic neuropathic pain

Cited by 43 publications

References 87 publications

Assessment and manifestation of central sensitisation across different chronic pain conditions

Assessment and manifestation of central sensitisation across different chronic pain conditions

Spinal α₂‐adrenoceptors and neuropathic pain modulation; therapeutic target

Tapentadol: what every doctor needs to know about this new drug

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Tapentadol extended release in the management of peripheral diabetic neuropathic pain

Cited by 43 publications

References 87 publications

Assessment and manifestation of central sensitisation across different chronic pain conditions

Assessment and manifestation of central sensitisation across different chronic pain conditions

Spinal α2‐adrenoceptors and neuropathic pain modulation; therapeutic target

Tapentadol: what every doctor needs to know about this new drug

Contact Info

Product

Resources

About

Spinal α₂‐adrenoceptors and neuropathic pain modulation; therapeutic target