Tapentadol hydrochloride: a next-generation, centrally acting analgesic with two mechanisms of action in a single molecule.
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.
Tzschentke
Thomas M
TM
Grunenthal GmbH, Aachen, Germany. thomas.tzschentke@grunenthal.com
Jahnel
Ulrich
U
Kogel
Babette
B
Christoph
Thomas
T
Englberger
Werner
W
De Vry
Jean
J
Schiene
Klaus
K
Okamoto
Akiko
A
Upmalis
David
D
Weber
Horst
H
Lange
Claudia
C
Stegmann
Jens-Ulrich
JU
Kleinert
Regina
R
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
D018759:Adrenergic Uptake Inhibitors; D000700:Analgesics; D010636:Phenols; D017450:Receptors, Opioid, mu; D000077432:Tapentadol