Systematic review of tapentadol in chronic severe pain

Riemsma, Rob; Forbes, Carol; Harker, Julie; Worthy, Gill; Misso, Kate; Schäfer, Michael; Kleijnen, Jos; Stürzebecher, S

doi:10.1185/03007995.2011.611494

Cited by 71 publications

(41 citation statements)

References 40 publications

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“…The effect of repeated dosing with tapentadol matches very well many chronic pain conditions (Riemsma et al, 2011) with impaired CPM such as OA pain (Steigerwald et al, 2012b), LBP (Buynak et al, 2010;Steigerwald et al, 2012a;Baron et al, 2016), painful peripheral diabetic neuropathy (Schwartz et al, 2015;Vadivelu et al, 2015), and cancer pain (Kress et al, 2014).…”

Section: Targeting Descending Pathwaysmentioning

confidence: 72%

Assessment and manifestation of central sensitisation across different chronic pain conditions

Arendt-Nielsen

Morlion

Perrot

et al. 2017

European Journal of Pain

517

494

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Different neuroplastic processes can occur along the nociceptive pathways and may be important in the transition from acute to chronic pain and for diagnosis and development of optimal management strategies. The neuroplastic processes may result in gain (sensitisation) or loss (desensitisation) of function in relation to the incoming nociceptive signals. Such processes play important roles in chronic pain, and although the clinical manifestations differ across condition processes, they share some common mechanistic features. The fundamental understanding and quantitative assessment of particularly some of the central sensitisation mechanisms can be translated from preclinical studies into the clinic. The clinical perspectives are implementation of such novel information into diagnostics, mechanistic phenotyping, prevention, personalised treatment, and drug development. The aims of this paper are to introduce and discuss (1) some common fundamental central pain mechanisms, (2) how they may translate into the clinical signs and symptoms across different chronic pain conditions, (3) how to evaluate gain and loss of function using quantitative pain assessment tools, and (4) the implications for optimising prevention and management of pain. The chronic pain conditions selected for the paper are neuropathic pain in general, musculoskeletal pain (chronic low back pain and osteoarthritic pain in particular), and visceral pain (irritable bowel syndrome in particular). The translational mechanisms addressed are local and widespread sensitisation, central summation, and descending pain modulation. Significance Central sensitisation is an important manifestation involved in many different chronic pain conditions. Central sensitisation can be different to assess and evaluate as the manifestations vary from pain condition to pain condition. Understanding central sensitisation may promote better profiling and diagnosis of pain patients and development of new regimes for mechanism based therapy. Some of the mechanisms underlying central sensitisation can be translated from animals to humans providing new options in development of therapies and profiling drugs under development.

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Section: Targeting Descending Pathwaysmentioning

confidence: 72%

Assessment and manifestation of central sensitisation across different chronic pain conditions

Arendt-Nielsen

Morlion

Perrot

et al. 2017

European Journal of Pain

517

494

View full text Add to dashboard Cite

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“…Preclinical data reveals an independence of these complimentary modes of action yet a synergy between these two mechanisms (Schroder et al, 2011). Tapentadol is effective in patients with acute and chronic pain states, such as post-operative pain, osteoarthritis, peripheral neuropathy and lower back pain, and has similar analgesic effects to oxycodone and morphine, but with significantly fewer side effects and discontinuations (Hale et al, 2009;Wade and Spruill, 2009;Lange et al, 2010;Riemsma et al, 2011;Pergolizzi et al, 2012). In cancer patients, controlled studies of tapentadol are still lacking.…”

Section: Introductionmentioning

confidence: 99%

Spinal neuronal correlates of tapentadol analgesia in cancer pain: A back‐translational approach

Falk

Patel

Heegaard

et al. 2014

European Journal of Pain

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Background: Pain is a common and highly debilitating complication for cancer patients significantly compromising their quality of life. Cancer-induced bone pain involves a complex interplay of multiple mechanisms including both inflammatory and neuropathic processes and also some unique changes. Strong opioids are a mainstay of treatments but side effects are problematic and can compromise optimal pain control. Tapentadol is a novel dual-action drug, both stimulating inhibitory μ-opioid receptors (MOR) and mediating noradrenaline reuptake inhibition (NRI) leading to activation of the inhibitory α-2 adrenoceptor. It has been demonstrated to treat effectively both acute and chronic pain. We here demonstrate the efficacy in a model of cancer-induced bone pain. Methods: MRMT-1 mammary carcinoma cells were inoculated into the tibia of 6-week-old rats and 2 weeks after, the neuronal responses to a wide range of peripheral stimulation were evaluated. The recordings were made from wide-dynamic range neurons in lamina V of the dorsal horn before and after administration of tapentadol as well as antagonists of the two mechanisms, naloxone or atipamezole. Results: We found marked inhibitions of the neuronal activity with efficacy against mechanical, thermal and electrically evoked activity following tapentadol administration. In addition, the effects of the drug were fully reversible by naloxone and partly by atipamezole, supporting the idea of MOR-NRI dual actions. Conclusions: These findings add to the mechanistic understanding of cancer-induced bone pain and support the sparse clinical data indicating a possible use of the drug as a therapeutic alternative for cancer patients with metastatic pain complication.

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“…Both preclinical and clinical studies show that tapentadol is a novel centrally acting analgesic drug that has efficacy comparable with that of strong opiates in a broad spectrum of acute and chronic pain conditions, with an improved tolerability profile compared with classic opiates (Tzschentke et al, 2007(Tzschentke et al, , 2009Kress, 2010;Sloan, 2010;Etropolski et al, 2011;Riemsma et al, 2011;Hartrick and Rodríguez Hernandez, 2012;Pergolizzi et al, 2012). Tapentadol combines MOR agonistic activity with norepinephrine reuptake inhibition (NRI) in a single molecule (Tzschentke et al, 2007;Bee et al, 2011;Hartrick and Rozek, 2011;Schröder et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

The Noradrenergic Component in Tapentadol Action Counteractsμ-Opioid Receptor–Mediated Adverse Effects on Adult Neurogenesis

et al. 2014

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Opiates were the first drugs shown to negatively impact neurogenesis in the adult mammalian hippocampus. Literature data also suggest that norepinephrine is a positive modulator of hippocampal neurogenesis in vitro and in vivo. On the basis of these observations, we investigated whether tapentadol, a novel central analgesic combining m-opioid receptor (MOR) agonism with norepinephrine reuptake inhibition (NRI), may produce less inhibition of hippocampal neurogenesis compared with morphine. When tested in vitro, morphine inhibited neuronal differentiation, neurite outgrowth, and survival of adult mouse hippocampal neural progenitors and their progeny, via MOR interaction. By contrast, tapentadol was devoid of these adverse effects on cell survival and reduced neurite outgrowth and the number of newly generated neurons only at nanomolar concentrations where the MOR component is predominant. On the contrary, at higher (micromolar) concentrations, tapentadol elicited proneurogenic and antiapoptotic effects via activation of b2 and a2 adrenergic receptors, respectively. Altogether, these data suggest that the noradrenergic component in tapentadol has the potential to counteract the adverse MOR-mediated effects on hippocampal neurogenesis. As a proof of concept, we showed that reboxetine, an NRI antidepressant, counteracted both antineurogenic and apoptotic effects of morphine in vitro. In line with these observations, chronic tapentadol treatment did not negatively affect hippocampal neurogenesis in vivo. In light of the increasing longterm use of opiates in chronic pain, in principle, the tapentadol combined mechanism of action may result in less or no reduction in adult neurogenesis compared with classic opiates.

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Systematic review of tapentadol in chronic severe pain

Abstract: Taken together, the benefit-risk ratio of tapentadol appears to be improved compared to step 3 opioids.

Cited by 71 publications

References 40 publications

Assessment and manifestation of central sensitisation across different chronic pain conditions

Assessment and manifestation of central sensitisation across different chronic pain conditions

Spinal neuronal correlates of tapentadol analgesia in cancer pain: A back‐translational approach

The Noradrenergic Component in Tapentadol Action Counteractsμ-Opioid Receptor–Mediated Adverse Effects on Adult Neurogenesis

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