title: Tapentadol hydrochloride: a next-generation, centrally acting analgesic with two mechanisms of action in a single molecule.
abstract: Tapentadol exerts its analgesic effects through micro opioid receptor agonism and noradrenaline reuptake inhibition in the central nervous system. Preclinical studies demonstrated that tapentadol is effective in a broad range of pain models, including nociceptive, inflammatory, visceral, mono- and polyneuropathic models. Moreover, clinical studies showed that tapentadol effectively relieves moderate to severe pain in various pain care settings. In addition, it was reported to be associated with significantly fewer treatment discontinuations due to a significantly lower incidence of gastrointestinal-related adverse events compared with equivalent doses of oxycodone. The combination of these reduced treatment discontinuation rates and tapentadol efficacy for the relief of moderate to severe nociceptive and neuropathic pain may offer an improvement in pain therapy by increasing patient compliance with their treatment regimen.
authors.affiliation: Grunenthal GmbH, Aachen, Germany. thomas.tzschentke@grunenthal.com
authors.forename: Thomas M
authors.initials: TM
authors.lastname: Tzschentke
authors.forename: Ulrich
authors.initials: U
authors.lastname: Jahnel
authors.forename: Babette
authors.initials: B
authors.lastname: Kogel
authors.forename: Thomas
authors.initials: T
authors.lastname: Christoph
authors.forename: Werner
authors.initials: W
authors.lastname: Englberger
authors.forename: Jean
authors.initials: J
authors.lastname: De Vry
authors.forename: Klaus
authors.initials: K
authors.lastname: Schiene
authors.forename: Akiko
authors.initials: A
authors.lastname: Okamoto
authors.forename: David
authors.initials: D
authors.lastname: Upmalis
authors.forename: Horst
authors.initials: H
authors.lastname: Weber
authors.forename: Claudia
authors.initials: C
authors.lastname: Lange
authors.forename: Jens-Ulrich
authors.initials: JU
authors.lastname: Stegmann
authors.forename: Regina
authors.initials: R
authors.lastname: Kleinert
mesh_terms: D018759:Adrenergic Uptake Inhibitors / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D000700:Analgesics / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D002986:Clinical Trials as Topic; D004353:Drug Evaluation, Preclinical; D006801:Humans; D010146:Pain / Q000188:drug therapy*; D010636:Phenols / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D017450:Receptors, Opioid, mu / Q000819:agonists; D000077432:Tapentadol
chemical_list: D018759:Adrenergic Uptake Inhibitors; D000700:Analgesics; D010636:Phenols; D017450:Receptors, Opioid, mu; D000077432:Tapentadol