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10.1177/2049463716657363

http://scihub22266oqcxt.onion/10.1177/2049463716657363
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C5102094!5102094!27867511
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suck abstract from ncbi


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pmid27867511      Br+J+Pain 2016 ; 10 (4): 217-21
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  • Is tapentadol different from classical opioids? A review of the evidence #MMPMID27867511
  • Langford RM; Knaggs R; Farquhar-Smith P; Dickenson AH
  • Br J Pain 2016[Nov]; 10 (4): 217-21 PMID27867511show ga
  • Tapentadol is a single molecule able to deliver analgesia by two distinct mechanisms, a feature which differentiates it from many other analgesics. Pre-clinical data demonstrate two mechanisms of action: mu-opioid receptor agonist activity and noradrenaline re-uptake inhibition. From these, one may predict that tapentadol would be applicable across a broad spectrum of pain from nociceptive to neuropathic. The evidence in animal models suggests that norepinephrine re-uptake inhibition (NRI) is a key mechanism and may even predominate over opioid actions in chronic (and especially neuropathic) pain states, reinforcing that tapentadol is different to classical opioids and may, therefore, be an a priori choice for the treatment of neuropathic and mixed pain. The clinical studies and subsequent practice experience and surveillance support the concept of opioid and non-opioid mechanisms of action. The reduced incidence of some of the typical opioid-induced side effects, compared to equianalgesic doses of classical opioids, supports the hypothesis that tapentadol analgesia is only partially mediated by opioid agonist mechanisms. Both the pre-clinical and clinical profiles appear to be differentiated from those of classical opioids.
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