Tapentadol (Nucynta) Prolonged Release: A Review

Tapentadol Prolonged Release: A Review in Pain Management – free full-text /PMC6422986/ – 2018 Nov

Tapentadol prolonged release (tapentadol PR) [Palexia® SR in EU] is a long-acting tablet formulation of the strong central analgesic tapentadol, which acts as both a μ-opioid receptor (MOR) agonist and a noradrenaline reuptake inhibitor.

Tapentadol PR is approved for chronic pain in various countries, with its EU indication (severe chronic pain manageable only with opioid analgesics) being the focus here.

Well-designed trials and clinical practice data support tapentadol PR use in this setting.   

Short term, tapentadol PR was an effective and generally well tolerated analgesic for moderate to severe pain of varying aetiologies, including neuropathic pain.

It provided analgesia at least as good as that of conventional strong opioids and appeared more favourable in terms of gastrointestinal tolerability, likely due to less potent MOR binding.

Severe back pain with a neuropathic component responded well to moderate-dose tapentadol PR in some patients, while for others, an increase to the maximum recommended tapentadol PR dosage provided analgesia at least as good as that of moderate-dose tapentadol PR plus pregabalin and appeared to have some CNS tolerability benefits.

Data also support the use of tapentadol PR in opioid rotation, including when conventional opioids are intolerable. Longer-term data in musculoskeletal pain conditions indicate continued benefit over up to 2 years’ treatment with tapentadol PR with no evidence of tolerance.

Thus, tapentadol PR is a useful option for the management of severe chronic pain.

The “continued benefit over up to 2 years” seems to be clear evidence of the long-term effectiveness of opioids. This study was from 2018, so they can’t simply say that opioids don’t work long-term.

Tapentadol prolonged release: clinical considerations in chronic pain

  • Acts via μ-opioid receptor agonism and noradrenaline reuptake inhibition
  • Reduces moderate to severe chronic pain of varying aetiologies, including neuropathic pain
  • At least as effective as conventional strong opioids, but more favourable GI tolerability
  • Effective and generally well tolerated over up to 2 years’ therapy, without evidence of tolerance


Chronic pain can be debilitating and is often related to a prior injury, disease or surgery with transformation into a chronic state through changes in nervous system/sensory processing.

The pain is usually nociceptive, neuropathic or a mixture of the two although its complexity, varying underlying neurobiology and non-linear trajectory make it challenging to manage.

Conventional opioids are also limited by gastrointestinal (GI) adverse events (AEs), abuse/misuse, addiction and tolerance, which can make achieving and maintaining the balance between analgesia and safety difficult.

One way to improve this balance is for opioids to be used with analgesics that act via different mechanisms, with those that provide synergistic analgesia (without additional tolerability issues) being particularly beneficial.

Such synergism is evident between opioidergic and noradrenergic drugs, the latter of which are particularly effective in alleviating chronic neuropathic pain.

A drug combining these two modes of action may therefore provide broad analgesic effects, with tapentadol being one such agent. Immediate-release (IR) and prolonged-release (PR) formulations of tapentadol are available in various countries for pain management.

This article reviews data relevant to the use of tapentadol PR tablets (Palexia® SR in EU) in the EU-approved indication of severe chronic pain in adults which can be adequately managed only with opioids.

The free full-text article contains all the details: Tapentadol Prolonged Release: A Review in Pain Management

And here’s an article that finds it to be an “effective option” for pain that’s often a combination of nociceptive and neuropathic:

Tapentadol (Nucynta): an effective option for the treatment of back pain – free full-text /PMC6526923/ – 2019 May

Back pain, including low back pain and neck pain, is the leading cause of disability worldwide. This type of pain is challenging to treat, since it presents both a nociceptive and a neuropathic component.

The latter also contributes to the evolution of pain toward chronification. Treatment selection should therefore consider the ability to prevent this event.

Tapentadol is characterized by a unique and innovative peculiar mechanism of action that makes it the first representative of a new class of central strong analgesics referred to as MOR-NRI.

This molecule acts both on the nociceptive and neuropathic components of pain, and it can therefore be effective in the treatment of a mixed pain condition such as back pain

This narrative review discusses the rationale for the use of tapentadol in both low back pain and neck pain and presents available clinical data.

Overall, data show that tapentadol prolonged release is a well-grounded treatment for chronic back pain, sustained by a strong mechanistic rationale and robust evidence.

Given also the availability of long-term efficacy and safety data, we believe that this molecule should be considered as an elective therapy for chronic back pain.

You can read the full text at Tapentadol: an effective option for the treatment of back pain.

3 thoughts on “Tapentadol (Nucynta) Prolonged Release: A Review

  1. canarensis

    When I hit “Data also support the use of tapentadol PR in opioid rotation” I couldn’t decide whether to laugh or cry. Opioid rotation! That assumes a CPP can get any opioids at all!

    I’m glad you told me about your Nucynta posts…I’m feeling more optimistic about ditching the regime that’d been sorta-kinda managing my pain, at least some of the time. I think I’ve got both nociceptive pain (the post-surgical knife-in-the-ribs feeling from 2001), & neuropathic (other issues). Plus mechanical pain…is that a thing? What category does “decades of beating your body to death by doing too much” fall into….I know you know about that one. Anyway, I’m more hopeful about Nucynta, tho I asked for the IR formula, never yet having found an ER formulation of anything that provided any detectable pain relief.

    Maybe I can crank up my optimism (if I can find it) to add a hefty hunk of placebo effect to when I finally get my scrip in the mail & wade thru the prior-auth process & the pharmacy fills it…probably be a week or two before I finally get to actually try the stuff.

    Liked by 1 person


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