Tapentadol: an initial analysis

Journal of Opioid Management
Eric Prommer

Abstract

Tapentadol hydrochloride (17(-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol) is a newly released analgesic that works at two levels: by acting as a p-opioid agonist and as a modulator of descending inhibitory pathways through its effects on neurotransmitters involved in these pathways. The theoretical advantage is the provision of synergistic analgesic activities, which may lessen the need for opioid escalation. The advantage is its potential as a possible new agent in neuropathic pain. Preclinical models confirm analgesic properties in acute pain and neuropathic pain models, but with less potency than morphine. Tapentadol has minimal CYP 450 interactions limiting potential for drug interactions. Human clinical trial data in nonmalignant pain suggest less potency than a step-3 opioid, and the drug remains to be tested in patients with cancer pain and neuropathic pain.

Citations

Apr 3, 2012·Drugs & Aging·Eric Prommer, Brandy Ficek
Sep 3, 2011·Journal of Pain Research·Nalini VadiveluRaymond Sinatra
Feb 15, 2014·Expert Review of Clinical Pharmacology·Bansri DesaiFadia T Shaya
Mar 5, 2011·British Journal of Pharmacology·Odd-Geir Berge
May 6, 2011·CA: a Cancer Journal for Clinicians·Judith A Paice, Betty Ferrell
Jul 13, 2017·Neurological Sciences : Official Journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology·Edvina GalièAndrea Pace

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