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Comparative pharmacology and toxicology of tramadol and tapentadol

Faria, J. ; Barbosa, J. ; Moreira, R. ; Queirós, O. ; Carvalho, F. ; Dinis‐Oliveira, R.J.

European journal of pain, 2018-05, Vol.22 (5), p.827-844 [Periódico revisado por pares]

England

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  • Título:
    Comparative pharmacology and toxicology of tramadol and tapentadol
  • Autor: Faria, J. ; Barbosa, J. ; Moreira, R. ; Queirós, O. ; Carvalho, F. ; Dinis‐Oliveira, R.J.
  • Assuntos: Analgesics, Opioid - pharmacology ; Analgesics, Opioid - therapeutic use ; Analgesics, Opioid - toxicity ; Humans ; Pain - drug therapy ; Quality of Life ; Tapentadol - pharmacology ; Tapentadol - therapeutic use ; Tapentadol - toxicity ; Tramadol - pharmacology ; Tramadol - therapeutic use ; Tramadol - toxicity
  • É parte de: European journal of pain, 2018-05, Vol.22 (5), p.827-844
  • Notas: Funding sources
    This work was supported by grants from CESPU TramTap‐CESPU‐2016 and ChronicTramTap_CESPU_2017 and project NORTE‐01‐0145‐FEDER‐000024, supported by Norte Portugal Regional Operational Programme NORTE 2020, under the PORTUGAL 2020 Partnership Agreement, through the European Regional Development Fund (ERDF). Juliana Faria is a PhD fellowship holder from FCT (SFRH/BD/104795/2014). Ricardo Dinis‐Oliveira acknowledges Fundação para a Ciência e a Tecnologia (FCT) for his Investigator Grant (IF/01147/2013).
    Conflict of interest
    None declared.
  • Descrição: Moderate‐to‐severe pain represents a heavy burden in patients’ quality of life, and ultimately in the society and in healthcare costs. The aim of this review was to summarize data on tramadol and tapentadol adverse effects, toxicity, potential advantages and limitations according to the context of clinical use. We compared data on the pharmacological and toxicological profiles of tramadol and tapentadol, after an extensive literature search in the US National Library of Medicine (PubMed). Tramadol is a prodrug that acts through noradrenaline and serotonin reuptake inhibition, with a weak opioid component added by its metabolite O‐desmethyltramadol. Tapentadol does not require metabolic activation and acts mainly through noradrenaline reuptake inhibition and has a strong opioid activity. Such features confer tapentadol potential advantages, namely lower serotonergic, dependence and abuse potential, more linear pharmacokinetics, greater gastrointestinal tolerability and applicability in the treatment of chronic and neuropathic pain. Although more studies are needed to provide clear guidance on the opioid of choice, tapentadol shows some advantages, as it does not require CYP450 system activation and has minimal serotonergic effects. In addition, it leads to less side effects and lower abuse liability. However, in vivo and in vitro studies have shown that tramadol and tapentadol cause similar toxicological damage. In this context, it is important to underline that the choice of opioid should be individually balanced and a tailored decision, based on previous experience and on the patient's profile, type of pain and context of treatment. Significance This review underlines the need for a careful prescription of tramadol and tapentadol. Although both are widely prescribed synthetic opioid analgesics, their toxic effects and potential dependence are not completely understood yet. In particular, concerning tapentadol, further research is needed to better assess its toxic effects.
  • Editor: England
  • Idioma: Inglês

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