• Pharmacol Rep · Aug 2018

    Review

    Tapentadol - A representative of a new class of MOR-NRI analgesics.

    • Renata Zajączkowska, Barbara Przewłocka, Magdalena Kocot-Kępska, Joanna Mika, Wojciech Leppert, and Jerzy Wordliczek.
    • Department of Interdisciplinary Intensive Care, Jagiellonian University, College of Medicine, Kraków, Poland. Electronic address: renia356@poczta.onet.pl.
    • Pharmacol Rep. 2018 Aug 1; 70 (4): 812-820.

    AbstractTapentadol is a centrally acting analgesic with a dual mode of action as a μ-opioid receptor (MOR) agonist and a noradrenaline reuptake inhibitor (NRI). It was initially approved by the US Food and Drug Administration in November 2008 for the treatment of moderate-to-severe acute pain in adult patients, and in August 2011, for chronic pain in an prolonged release form in the same population. Due to its limited protein binding capacity, the absence of active metabolites and significant microsomal enzyme induction or inhibition, tapentadol has a limited potential for drug-drug interactions. It appears to be well-tolerated and effective in the treatment of moderate-to severe acute and chronic pain. Owing to its dual mechanism of action, it is hypothesized to be good option in the treatment of both nociceptive and neuropathic pain.Copyright © 2018 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier B.V. All rights reserved.

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