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Tapentadol in Pain Management

A μ-Opioid Receptor Agonist and Noradrenaline Reuptake Inhibitor

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Abstract

Several mechanisms can be proposed to explain an apparent synergistic analgesic action between μ-opioid and α2-adrenergic receptor agonists. Combining both effects in a single molecule eliminates the potential for drug-drug interactions inherent in multiple drug therapy. Tapentadol is the first US FDA-approved centrally acting analgesic having both μ-opioid receptor agonist and noradrenaline (norepinephrine) reuptake inhibition activity with minimal serotonin reuptake inhibition. This dual mode of action may make tapentadol particularly useful in the treatment of neuropathic pain. Having limited protein binding, no active metabolites and no significant microsomal enzyme induction or inhibition, tapentadol has a limited potential for drug-drug interactions. Clinical trial evidence in acute and chronic non-cancer pain and neuropathic pain supports an opioid-sparing effect that reduces some of the typical opioid-related adverse effects. Specifically, the reduction in treatment-emergent gastrointestinal adverse effects for tapentadol compared with equianalgesic pure μ-opioid receptor agonists results in improved tolerability and adherence to therapy for both the immediate- and extended-release formulations of tapentadol.

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Acknowledgements

Dr Hartrick has received research funding from Ortho-McNeil and Johnson & Johnson. Dr Rozek has no potential conflicts of interest that are directly relevant to the content of this article. No funds or other assistance were sought or received for the preparation of this article.

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Authors and Affiliations

  1. Department of Health Sciences, Oakland University, Rochester, Michigan, USA

    Craig T. Hartrick (Professor) & Richard J. Rozek

  2. Biomedical Sciences and Anesthesiology, Oakland University William Beaumont School of Medicine, 525 O’Dowd Hall, Rochester, Michigan, 48309, USA

    Craig T. Hartrick (Professor) & Richard J. Rozek

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  1. Craig T. Hartrick
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Correspondence to Craig T. Hartrick.

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Hartrick, C.T., Rozek, R.J. Tapentadol in Pain Management. CNS Drugs 25, 359–370 (2011). https://doi.org/10.2165/11589080-000000000-00000

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