Chronic pain treatment represents one of the most complex clinical challenges and even though
opioids exhibit particular efficacy on
nociceptive pain, their use must be controlled to avoid the risk of adverse reactions. A useful approach, aimed at maintaining
analgesia and mitigating side effects, is represented by the use of a new class of
analgesics endowed of µ-
opioid (MOR) receptor agonism and
noradrenaline reuptake inhibition (NRI) mechanisms.
Tapentadol is the progenitor of this new class of drugs called MOP-NRI. A literature review has been conducted to gain information about the efficacy and the tolerability profile of
tapentadol shifting from MOR agonism (
acute pain) to NRI activity (
chronic pain). The tolerability and therapeutic safety of
tapentadol in
neuropathic pain models, as well as in clinical settings, has been analyzed showing a good gastrointestinal tolerability profile, a moderate effect on
hormone levels (in healthy volunteers and in patients) and on cognitive performance, a lack of significant alteration of the electrocardiogram recording and no changes of the QT/QTc interval, a minimal effect on
serotonin reuptake in vivo with a low risk of
serotonin syndrome, a longer time for the onset of
analgesic tolerance and a less occurrence of abuse liability compared to formulations containing other comparator compounds.
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.