title: Tapentadol for pain: a treatment evaluation.
abstract: Tapentadol is a newly approved novel analgesic drug with a dual mode of action: a mu-opioid agonist and an inhibitor of norepinephrine reuptake (MOR-NRI). Preclinical evidence supports a synergistic interaction between these two effects. It is the first opioid agonist to exhibit predominant norepinephrine reuptake inhibition with minimal serotonin effects. It is FDA approved for use in the US for moderate to severe pain in adults, available in the immediate release form for acute pain and as an extended-release formulation for chronic pain when continuous analgesia is required. Tapentadol has demonstrated reduced treatment-emergent opioid-related gastrointestinal adverse effects compared with pure opioid agonists. The synergistic mu-opioid and alpha(2)-adrenergic effects suggest the potential for particular utility in neuropathic pain states or other pain states associated with hyperalgesia.
authors.affiliation: Oakland University, William Beaumont School of Medicine, 525 O'Dowd Hall, Rochester, MI 48309, USA. chartrick@beaumont.edu
authors.forename: Craig T
authors.initials: CT
authors.lastname: Hartrick
authors.forename: Jose Rafael
authors.initials: JR
authors.lastname: Rodríguez Hernandez
mesh_terms: D059787:Acute Pain / Q000188:drug therapy*; D018759:Adrenergic Uptake Inhibitors / Q000627:therapeutic use*; D000701:Analgesics, Opioid / Q000627:therapeutic use*; D059350:Chronic Pain / Q000188:drug therapy*; D006801:Humans; D010636:Phenols / Q000627:therapeutic use*; D017450:Receptors, Opioid, mu / Q000819:agonists; D000077432:Tapentadol
chemical_list: D018759:Adrenergic Uptake Inhibitors; D000701:Analgesics, Opioid; D010636:Phenols; D017450:Receptors, Opioid, mu; D000077432:Tapentadol