Journal ArticleDOI
Tapentadol in pain management: a μ-opioid receptor agonist and noradrenaline reuptake inhibitor.
TLDR
Clinical trial evidence in acute and chronic non-cancer pain and neuropathic pain supports an opioid-sparing effect that reduces some of the typical opioid-related adverse effects for tapentadol, which results in improved tolerability and adherence to therapy for both the immediate- and extended-release formulations of tapENTadol.Abstract:
Several mechanisms can be proposed to explain an apparent synergistic analgesic action between μ-opioid and α2-adrenergic receptor agonists. Combining both effects in a single molecule eliminates the potential for drug-drug interactions inherent in multiple drug therapy. Tapentadol is the first US FDA-approved centrally acting analgesic having both μ-opioid receptor agonist and noradrenaline (norepinephrine) reuptake inhibition activity with minimal serotonin reuptake inhibition. This dual mode of action may make tapentadol particularly useful in the treatment of neuropathic pain. Having limited protein binding, no active metabolites and no significant microsomal enzyme induction or inhibition, tapentadol has a limited potential for drug-drug interactions. Clinical trial evidence in acute and chronic non-cancer pain and neuropathic pain supports an opioid-sparing effect that reduces some of the typical opioid-related adverse effects. Specifically, the reduction in treatment-emergent gastrointestinal adverse effects for tapentadol compared with equianalgesic pure μ-opioid receptor agonists results in improved tolerability and adherence to therapy for both the immediate- and extended-release formulations of tapentadol.read more
Citations
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Journal ArticleDOI
Pharmacotherapy for Neuropathic Pain: A Review.
TL;DR: An overview of current drugs available for the treatment of neuropathic pain with an emphasis on their mechanism of action is provided, including antidepressants and anticonvulsants acting at calcium channels.
Journal Article
Pharmacologic therapy for acute pain.
TL;DR: There is little evidence that one opioid is superior for pain control, but there are some pharmacologic differences among opioids.
Journal ArticleDOI
Pharmacological Treatment of Neuropathic Cancer Pain: A Comprehensive Review of the Current Literature
TL;DR: A comprehensive review of the latest knowledge regarding NCP pharmacological management is presented, resulting in significant mechanism‐based treatment advances for the future.
Journal ArticleDOI
The perception and endogenous modulation of pain.
TL;DR: Genomic studies of individuals with congenital insensitivity to pain or paroxysmal pain syndromes considerable increased understanding of the function of peripheral nociceptors, and especially of the roles of voltage-gated sodium channels and of nerve growth factor/TrkA receptors in nocICEptive transduction and transmission.
Journal ArticleDOI
Do All Opioid Drugs Share the Same Immunomodulatory Properties? A Review From Animal and Human Studies.
TL;DR: It is concluded that it is not correct to generalize immunosuppression as a common side effect of all opioid molecules.
References
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Journal ArticleDOI
Persistent postsurgical pain: risk factors and prevention
TL;DR: Strategies for identification of patients at risk and for prevention and possible treatment of this important entity of chronic pain are outlined.
Journal ArticleDOI
Cortical Representation of the Sensory Dimension of Pain
TL;DR: A double dissociation of cortical modulation indicates a relative specialization of the sensory and the classical limbic cortical areas in the processing of the Sensory and affective dimensions of pain.
Journal ArticleDOI
An Overview of Drug Combination Analysis with Isobolograms
TL;DR: Determination of the additive isobole is a necessary procedure for assessing both synergistic and antagonistic interactions of the combination and the mathematical formulas needed to distinguish these cases are provided.
Journal ArticleDOI
(-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties.
Thomas M. Tzschentke,Thomas Christoph,Babette-Yvonne Koegel,Klaus Schiene,Hagen-Heinrich Hennies,Werner Englberger,Michael Haurand,Ulrich Jahnel,Thomas I. F. H. Cremers,Elmar Friderichs,Jean De Vry +10 more
TL;DR: Tapentadol exhibited analgesic effects in a wide range of animal models of acute and chronic pain and its relative resistance to tolerance development may be due to a dual mode of action consisting of both MOR activation and NE reuptake inhibition.
Journal ArticleDOI
The hypoalgesic effect of tramadol in relation to CYP2D6
Lars la Cour Poulsen,Lars la Cour Poulsen,Lars la Cour Poulsen,Lars Arendt-Nielsen,Lars Arendt-Nielsen,Lars Arendt-Nielsen,Kim Brøsen,Kim Brøsen,Kim Brøsen,Søren H. Sindrup,Søren H. Sindrup,Søren H. Sindrup +11 more
TL;DR: It is concluded that formation of (+)‐M1 by way of CYP2D6 is important for the effect of tramadol on experimental pain.