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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136 Citations

Comparative pharmacology and toxicology of tramadol and tapentadol
TLDR
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, which leads to less side effects and lower abuse liability.
Comparative metabolism of tramadol and tapentadol: a toxicological perspective
TLDR
A thorough knowledge about tramadol and tapentadol metabolomics is expected to provide additional insights to better understand the interindividual variability in their pharmacokinetics and dose-responsiveness, and contribute to the establishment of personalized therapeutic approaches, minimizing side effects and optimizing analgesic efficacy.
Tapentadol Versus Tramadol: A Narrative and Comparative Review of Their Pharmacological, Efficacy and Safety Profiles in Adult Patients
TLDR
Tapentadol is not a first-line opioid but represents an additional analgesic in the therapeutic choices, which some patients may benefit from after careful examination of their clinical situation, co-morbidities and co-medications.
Is tapentadol different from classical opioids? A review of the evidence
TLDR
The clinical studies and subsequent practice experience and surveillance support the concept of opioid and non-opioid mechanisms of action, and the reduced incidence of some of the typical opioid-induced side effects, supports the hypothesis that tapentadol analgesia is only partially mediated by opioid agonist mechanisms.
Tapentadol: an analgesic that differs from classic opioids due to its noradrenergic mechanism of action.
TLDR
Tapentadol represents a great innovation in chronic pain therapy with a unique analgesic profile different form classical opioids, therefore, thanks to its synergistic MOR-NRI action, it may be a good option for the treatment of chronic, neuropathic and mixed pain.
The switch from buprenorphine to tapentadol: is it worth?
  • A. Miclescu
  • Medicine, Biology
    Romanian journal of anaesthesia and intensive care
  • 2016
TLDR
The evidence to support the method used for transdermal buprenorphine rotation to tapentadol is weak and both drugs show particular pharmacodynamic and pharmacokinetic properties which reduce the risks of development of tolerance, opioid abuse, diversion and determine fewer hormone changes than the "classical opioids" making these opioids more attractive than other opioids in long term opioid treatment.
The Mu-Opioid Receptor Agonist/Noradrenaline Reuptake Inhibition (MOR–NRI) Concept in Analgesia: The Case of Tapentadol
TLDR
It is suggested that tapentadol is the first representative of a proposed new class of analgesics, MOR–NRI, such that relatively moderate activity at the two target sites (MOR and noradrenaline reuptake transporter) is sufficient to produce strong analgesic effects.
Does ‘Strong Analgesic’ Equal ‘Strong Opioid’? Tapentadol and the Concept of ‘µ-Load’
TLDR
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.
Comparative study of the neurotoxicological effects of tramadol and tapentadol in SH-SY5Y cells.
The anaesthetist, opioid analgesic drugs, and serotonin toxicity: a mechanistic and clinical review.
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