Tapentadol immediate release: a new treatment option for acute pain management

Marc Afilalo¹, Jens-Ulrich Stegmann², David Upmalis³

¹Sir Mortimer B. Davis Jewish General Hospital, Montréal, Canada; ²Global Drug Safety, Grünenthal GmbH, Aachen, Germany; ³Johnson & Johnson Pharmaceutical Research and Development, L.L.C., Raritan, New Jersey, USA

Abstract: The undertreatment of acute pain is common in many health care settings. Insufficient management of acute pain may lead to poor patient outcomes and potentially life-threatening complications. Opioids provide relief of moderate to severe acute pain; however, therapy with pure µ-opioid agonists is often limited by the prevalence of side effects, particularly opioid-induced nausea and vomiting. Tapentadol is a novel, centrally acting analgesic with 2 mechanisms of action, µ-opioid receptor agonism and norepinephrine reuptake inhibition. The analgesic effects of tapentadol are independent of metabolic activation and tapentadol has no active metabolites; therefore, in theory, tapentadol may be associated with a low potential for interindividual efficacy variations and drug–drug interactions. Previous phase 3 trials in patients with various types of moderate to severe acute pain have shown that tapentadol immediate release (IR; 50 to 100 mg every 4 to 6 hours) provides analgesia comparable to that provided by the pure µ-opioid agonist comparator, oxycodone HCl IR (10 or 15 mg every 4 to 6 hours), with a lower incidence of nausea, vomiting, and constipation. Findings suggest tapentadol may represent an improved treatment option for acute pain.

Keywords: tapentadol IR, acute pain, opioid, gastrointestinal tolerability