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

Abstract

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...

Tapentadol, an opioid as a strategy for the treatment of chronic pain? A narrative review

“…The extended-release version has been used since 2011 for the treatment of moderate to severe chronic pain. [6][7][8] In Europe, the commercialization of immediate and extended-release formulations was approved in 2010 by the EMA (European Medicines Agency). 6 The extendedrelease formulation is indicated for patients with chronic pain who require long-term analgesic treatment, as it allows a frequent dose with better pain management.…”

“…[6][7][8] In Europe, the commercialization of immediate and extended-release formulations was approved in 2010 by the EMA (European Medicines Agency). 6 The extendedrelease formulation is indicated for patients with chronic pain who require long-term analgesic treatment, as it allows a frequent dose with better pain management. 2 This opioid analgesic is structurally similar to tramadol, but more potent and better tolerated.…”

“…Therefore, its intensity increases, so that pain does not depend only on an injury to organs or tissues, but on a complex change in the sensory processing of the nervous system. 5,6 In addition, pain is perceived by brain circuits linked to emotions, so it may be related to depression and be the cause and consequence of it. Thus, some myalgias improve with the use of antidepressant medications, or with measures that act on the emotional state and response to stress.…”

“…2,3 Tapentadol is an opioid analgesic similar to tramadol and has been used effectively to treat pain. [6][7][8] This drug has a high affinity for opioid receptors, in addition to acting to inhibit the reuptake of NA (nor epinephrine). 2,6,9,10 The Tapentadol therapeutic profile allows for a more potent action, with greater tolerability by the patient, reducing the emergence of respiratory, gastrointestinal and endocrine disorders 11,12 , being mainly nausea and vomiting, which have higher incidences with opioids such as Tramadol or Oxycodone.…”

“…[6][7][8] This drug has a high affinity for opioid receptors, in addition to acting to inhibit the reuptake of NA (nor epinephrine). 2,6,9,10 The Tapentadol therapeutic profile allows for a more potent action, with greater tolerability by the patient, reducing the emergence of respiratory, gastrointestinal and endocrine disorders 11,12 , being mainly nausea and vomiting, which have higher incidences with opioids such as Tramadol or Oxycodone. [13][14][15][16] In contrast, studies indicate that Tapentadol can imbalance the antioxidant system, leading to an increase in reactive oxygen species (ROS), which can favor the emergence of various pathologies or even increased pain.…”