Comparable efficacy and superior gastrointestinal tolerability (nausea, vomiting, constipation) of tapentadol compared with oxycodone hydrochloride

Etropolski, Mila; Kelly, Kathleen; Okamoto, Akiko; Rauschkolb, Christine

doi:10.1007/s12325-011-0018-0

Cited by 46 publications

(30 citation statements)

References 23 publications

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“…It has recently been launched onto the market for treatment of pain in humans and has subsequently received attention in the veterinary field (Giorgi et al, 2012Lee et al, 2013Lee et al, , 2014Lavy et al, 2014) due to its efficacy in pain control (Biondi et al, 2013;Etropolski et al, 2011;Schwartz et al, 2011;Vadivelu et al, 2011) and good safety profile (Schwartz et al, 2011;Imanaka et al, 2013;Lange et al, 2010) in humans, compared with classic opioids. Moreover, TAP appears to have analgesic effects in chronic neuropathic pain (Christoph et al, 2010) in addition to its proven effect for acute pain.…”

Section: Introductionmentioning

confidence: 99%

Synergistic interaction between tapentadol and flupirtine in the rat orafacial formalin test

Lee

Vito

Giorgi

et al. 2015

European Journal of Pharmacology

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Section: Introductionmentioning

confidence: 99%

Synergistic interaction between tapentadol and flupirtine in the rat orafacial formalin test

Lee

Vito

Giorgi

et al. 2015

European Journal of Pharmacology

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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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“…Also aligning with these findings, TAP had a weaker inhibitory effect than morphine at equianalgesic intraperitoneal doses on both (i) gastrointestinal motility assessed from charcoal transit and (ii) prostaglandin-induced diarrhoea (Tzschentke et al, 2006). Several comparative human preclinical studies involving other analogue opioids confirm these experimental findings (Afilalo et al, 2010;Etropolski et al, 2011;Wilhorn and Kraus, 2011).…”

Section: Tapentadolmentioning

confidence: 61%

Tramadol Vs Tapentadol: Anew Horizon in Pain Treatment?

Giorgi¹

2012

American Journal of Animal and Veterinary Sciences

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Problem statement: Acute and chronic pain is a common presenting sign in animal species and human beings. Approach: Classical opioids provide very effective pain relief, although they may be less effective in the treatment of chronic pain due to their limited therapeutic windows and the induced opioid receptor down regulation. Atypical opioids, such as tramadol and tapentadol, have a dual mechanism of action and have been designed to overcome these issues through an opiate-sparing effect. Results: Tramadol activates mu opioid receptors and in addition, inhibits serotonin and noradrenalin reuptake. These actions are the result of the different enantiomers and tend to be reliant on their metabolism. Indeed, the O-desmethyltramadol phase I metabolite, is 200-300 times more potent for mu opioid receptor activation than the parental compound. For these reasons, the drug's effectiveness can vary among subjects. In veterinary medicine its effectiveness, especially after oral administration, is still uncertain and controversial. Tapentadol is a novel, atypical opioid with a unique mechanism of action. It was launched on the European drug market at the end of 2011. It has been proposed as the first representative of a new pharmacological class of centrally acting analgesics, namely, the mu opioid receptor agonist, noradrenalin reuptake inhibitors. The first human studies describe this molecule as safe and effective (equianalgesic to morphine). The drug has great potential for veterinary use because it exists as a single enantiomer only, it does not require metabolic activation to be effective and adverse effects triggered by the serotonin reuptake inhibition action are negligible. Conclusion/Recommendations: For these reasons, TAP is a promising compound however at this stage, more investigation is required before it can be recommended for regular use in veterinary medicine, the possibility of undesirable effects is yet to be entirely excluded.

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Comparable efficacy and superior gastrointestinal tolerability (nausea, vomiting, constipation) of tapentadol compared with oxycodone hydrochloride

Cited by 46 publications

References 23 publications

Synergistic interaction between tapentadol and flupirtine in the rat orafacial formalin test

Synergistic interaction between tapentadol and flupirtine in the rat orafacial formalin test

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

Tramadol Vs Tapentadol: Anew Horizon in Pain Treatment?

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