Tapentadol, is a novel opioid analgesic drug dual centrally acting agonist at the mu opioid receptor (MOR) and inhibitor of CNS norepinephrine reuptake (NRI) whose potency is between morphine and tramadol. The Food and Drug Administration (FDA) has approved it for the treatment of moderate to severe acute pain in the form of immediate release tablets and also for chronic pain in its extended release form (PR), last one with a half-life of 12 hours.
Its high efficacy has been demonstrated in a range of animal models of acute and chronic, nociceptive, inflammatory, and neuropathic pain as well as in clinical studies with moderate to severe pain arising from a number of different etiologies.
As you describe, tapentadol (Nucynta brand in USA) has dual acting agonist activity most similar to tramadol. Whereas tramadol also inhibits reuptake of serotonin, it behaves more as an SNRI. Potential interactions may have clinical consequences with triptans and other serotonergic agents, including both serotonergic syndrome and serotonin withdrawal symptoms. These are theoretically less likely with tapentadol. There is an ER formulation available in multiple doses would implying off label use for chronic malignant and non malignant pain.
The company got indication for DPN (on label approval for marketing purposes). The agent also has a sigma 2 agonist activity (controversial effects) that may make it, theoretically, help minimize some ADRs such as nausea, dizziness. In the FDA submitted post bunionectomy study comparing ibuprofen , tapentadol and morphine, there was less of those ADRs. No difference in vomiting or lethargy was found. However the limitation was 3 days of postop pain, not chronic pain. see: Vlessides, M. (September 2006). "Two New Analgesics May Help Patients After Bunionectomy". Anesthesiology News 32 (9). ID 5326 A REMS is required given the ER status for all long acting opioids. Severe knee OA studies and Dental extraction studies were also performed, but no long term studies in chronic pain, malignant or otherwise, have been published in peer -reviewed Journals.
As is typical in these types of issues, clinical judgement prevails when considering an individual patient. The drug is glucuronidated as a metabolite that would therefore accumulate in renal insufficiency, but it is unknown whether this is clinically significant. I usually counsel, in the absence of data, avoidance in low Cr Clearance patient or very cautious use until more data are available.
I sincerely hope some of this thoughts are helpful in Shared Decision Making with the patient.
in our country ( the netherlands) just recently available; still depending on patients willeing to pay a little extra for tapentadol
firtsd experrience is promising!
Most of the potential advantages over some other opioïds have been specified in this Q&A. I think that the fact that the drug is glucuronidated and not involved with cytochrome is a real advantage in polymedicated patients (not only in oncology, but also in chronic administration for non cancer pain).
Dear Colleagues,
In France, this product have clinical interest for severe cancer pain (http://www.has-sante.fr/portail/jcms/c_1751167/fr/palexia-lp-tapentadol-antalgique-opioide).
Clinical interest seems to be weak for non cancer chronic pain.
In my opinion, it's easier to prescribe any drug than to stop it when chronic-pain-patients are tired with side-effects.
So, as our colleague Burga says, if there's a multimodal management of chronic pain, drugs have a place (tapentadol and all others antinociceptive drugs) but not all the place.
Best Regards
Dear Collegues
i totally agreee with Dr. Rault. In Italy the slow release formulation of this drug is avaliable since 2013 (more or less, i don't remember exactly). In my clinical experience (partucularly on chronic pain in non-oncologic patients) none of the drugs avaliable today for pain treatment is a "magic bullet" , depending on mechanism of pain , metabolism, pharmacogenetics and co-morbidities of the patient that you need to cure and tapentadol is not an exception to this rule.
Tapentadol seems to me to be a weaker analgesic than reported in the early studies, reffering to the iso-analgesic ratio to morphine and oxycodone..
it is an interesting drug, also for its dual mechanism of action , but it' s only one of our possible choiches and not a solution to all problems!
In a recent article from British Journal of Pain, 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.
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