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

  • Afilalo M
  • Stegmann J
  • Upmalis D
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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. © 2010 Afilalo et al, publisher and licensee Dove Medical Press Ltd.

Author-supplied keywords

  • acetylsalicylic acid
  • analgesic activity
  • binding affinity
  • celecoxib
  • clinical trial
  • constipation
  • disease severity
  • dizziness
  • dose response
  • drug blood level
  • drug distribution
  • drug dose comparison
  • drug efficacy
  • drug induced headache
  • drug metabolism
  • drug potentiation
  • drug receptor binding
  • drug release
  • drug safety
  • drug structure
  • drug tolerability
  • drug withdrawal
  • gastrointestinal disease
  • hip pain
  • human
  • knee pain
  • low back pain
  • morphine
  • mu opiate receptor
  • naloxone
  • nausea
  • neuropathic pain
  • nonhuman
  • oxycodone
  • pain
  • pain assessment
  • paracetamol
  • placebo
  • postoperative nausea and vomiting
  • postoperative pain
  • pruritus
  • review
  • somnolence
  • tapentadol
  • vomiting
  • yohimbine

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Authors

  • M Afilalo

  • J.-U. Stegmann

  • D Upmalis

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