Brazilian Journal of Pain
Brazilian Journal of Pain
Review Article

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

Tapentadol: o que todo médico precisa saber sobre esse novo fármaco

Bernardo De Marchi Mosele; Daniel Benzecry de Almeida; Válery Baggio Hess

Downloads: 0
Views: 230


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.


Dual mechanism of action, Opioids, Tapentadol


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.

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 tolerância, menos efeitos adversos e melhor resposta terapêutica na dor crônica neuropática quando comparado com agonistas receptores opioides tipo µ puros.


Duplo mecanismo de ação, Opioides, Tapentadol


Fornasari D. Pain pharmacology: focus on opioids. Clin Cases Miner Bone Metab. 2014;11(3):165-8.

Pergolizzi J, Alegre C, Blake D, Alén JC, Caporali R, Casser HR. Current considerations for the treatment of severe chronic pain: the potential for tapentadol. Pain Pract. 2012;12(4):290-6.

Hartrick CT, Rozek RJ. Tapentadol in pain management a µ-opioid receptor agonist and noradrenaline reuptake inhibitor. CNS Drugs. 2011;25(5):359-70.

Singh DR, Nag K, Shetti AN, Krishnaveni N. Tapentadol hydrochloride: a novel analgesic. Saudi J Anaesth. 2013;7(3):322-6.

Mercadante S, Porzio G, Gebbia V. New Opioids. J Clin Oncol. 2014;32(16):1671-6.

Hartrick CT, Rodríguez Hernandez JR. Tapentadol for pain: a treatment evaluation. Expert Opin Pharmacother. 2012;13(2):283-6.

Santos J, Alarcão J, Fareleira F, Vaz-Carneiro A, Costa J. Tapentadol for chronic musculoskeletal pain in adults. Cochrane Database Syst Rev. 2015:CD009923.

Vadivelu N, Kai A, Maslin B, Kodumudi G, Legler A, Berger JM. Tapentadol extended release in the management of peripheral diabetic neuropathic pain. Ther Clin Risk Manag. 2015;11:95-105.

Rodriguez MA. Tapentadol, una nueva opción terapêutica. Rev Col Anest. 2011;39(3):375-85.

Sánchez Del Águila MJ, Schenk M, Kern KU, Drost T, Steigerwald I. Practical considerations for the use of tapentadol prolonged release for the management of severe chronic pain. Clin Ther. 2015;37(1):94-113.

Wade WE, Spruill WJ. Tapentadol hydrochloride: a centrally acting oral analgesic. Clin Ther. 2009;31(12):2804-18.

Knezevic NN, Tverdohleb T, Knezevic I, Candido KD. Unique pharmacology of tapentadol for treating acute and chronic pain. Expert Opin Drug Metab Toxicol. 2015;11(9):1475-92.

Hartrick CT. Tapentadol immediate-release for acute pain. Expert Rev Neurother. 2010;10(6):861-9.

Frampton JE. Tapentadol immediate release: a review of its use in the treatment of moderate to severe acute pain. Drugs. 2010;70(13):1719-43.

Pierce DM, Shipstone E. Pharmacology update: tapentadol for neuropathic pain. Am J Hosp Palliat Care. 2012;29(8):663-6.

Taylor R, Pergolizzi JV, Raffa RB. Tapentadol extended release for chronic pain patients. Adv Ther. 2013;30(1):14-27.

Hoy SM. Tapentadol extended release: in adults with chronic pain. Drugs. 2012;72(3):375-93.

Afilalo M, Morlion B. Efficacy of tapentadol ER for managing moderate to severe chronic pain. Pain Physician. 2013;16(1):27-40.

Langford RM, Knaggs R, Farquhar-Smith P, Dickenson AH. Is tapentadol different from classical opioids? A review of the evidence. Br J Pain. 2016;10(4):217-21.

Tzschentke TM, Cristoph T, Kögel BY. The mu-opioid receptor agonist/noradrenaline reuptake inhibition (MOR-NRI) concept in analgesia: the case of tapentadol. CNS Drugs. 2014;28(4):319-29.

Hartrick CT. Tapentadol immediate release for the relief of moderate-to-severe acute pain. Expert Opin Pharmacother. 2009;10(16):2687-96.

Desai B, Freeman E, Huang E, Hung A, Knapp E, Breunig IM. Clinical value of tapentadol extended-release in painful diabetic peripheral neuropathy. Expert Rev Clin Pharmacol. 2014;7(2):203-9.

Veal FC, Peterson GM. Pain in the frail or elderly patient: does tapentadol have a role?. Drugs Aging. 2015;32(6):419-26.

Nossaman VE, Ramadhyani U, Kadowitz PJ, Nossaman BD. Advances in perioperative pain management: use of medications with dual analgesic mechanisms, tramadol & tapentadol. Anesthesiol Clin. 2010;28(4):647-66.

Riemsma R, Forbes C, Harker J, Worthy G, Misso K, Schafer M. Systematic review of tapentadol in chronic severe pain. Curr Med Res Opin. 2011;27(10):1907-30.

Vadivelu N, Timchenko A, Huang Y, Sinatra R. Tapentadol extended-release for treatment of chronic pain: a review. J Pain Res. 2011;4:211-8.

Tsutaoka BT, Ho RY, Fung SM, Kearney TE. Comparative toxicity of tapentadol and tramadol utilizing data reported to the national poison data system. Ann Pharmacother. 2015;49(12):1311-6.

Kemp W, Schlueter S, Smalley E. Death due to apparent intravenous injection of tapentadol. J Forensic Sci. 2013;58(1):288-91.

Borys D, Stanton M, Gummin D, Drott T. Tapentadol toxicity in children. Pediatrics. 2015;135(2):392-6.

Raffa RB, Buschmann H, Cristoph T, Eichenbaum G, Englberger W, Flores CM. Mechanistic and functional differentiation of tapentadol and tramadol. Expert Opin Pharmacother. 2012;13(10):1437-49.

Biondi D, Xiang J, Benson C, Etropolski M, Moskovitz B, Rauschkolb C. Tapentadol immediate release versus oxycodone immediate release for treatment of acute low back pain. Pain Physician. 2013;16(3):E237-46.

Submitted date:

Accepted date:

5f160ce50e88257e599517e3 brjp Articles


Share this page
Page Sections