Mechanistic and functional differentiation of tapentadol and tramadol

@article{Raffa2012MechanisticAF,
  title={Mechanistic and functional differentiation of tapentadol and tramadol},
  author={Robert B Raffa and Helmut Heinrich Buschmann and Thomas Christoph and Gary M. Eichenbaum and Werner Englberger and Christopher M. Flores and Torsten Hertrampf and Babette Y. K{\"o}gel and Klaus Schiene and Wolfgang Werner A Strassburger and Rolf Dr Terlinden and Thomas M Tzschentke},
  journal={Expert Opinion on Pharmacotherapy},
  year={2012},
  volume={13},
  pages={1437 - 1449}
}
Introduction: Many opioid analgesics share common structural elements; however, minor differences in structure can result in major differences in pharmacological activity, pharmacokinetic profile, and clinical efficacy and tolerability. Areas covered: This review compares and contrasts the chemistry, pharmacodynamics, pharmacokinetics, and CNS ‘functional activity' of tapentadol and tramadol, responsible for their individual clinical utilities. Expert opinion: The distinct properties of… 
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  • 2016
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Does ‘Strong Analgesic’ Equal ‘Strong Opioid’? Tapentadol and the Concept of ‘µ-Load’
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This work applied standard drug–receptor theory and novel techniques to in vitro and in vivo data to estimate the μ-load of tapentadol (the % contribution of the opioid component to the adverse effect magnitude relative to a pure/classical µ-opioid at equianalgesia) in respiratory depression and constipation, and compared the results to clinical evidence.
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