Unique pharmacology of tapentadol for treating acute and chronic pain

Introduction: Even though pain is a complex process involving many different mediators, enzymes, receptors and ion channels, pain medications usually address only individual targets. Nucynta, which addresses multiple pain targets, was the first new centrally acting analgesic to be approved by the FDA in 2008. Areas covered: Pharmacology: Tapentadol is a centrally acting opioid with two mechanisms of action, including agonism at the mu-opioid receptor (MOR) and inhibition of norepinephrine reuptake (NRI), producing analgesia individually and via a combination of both acts synergistically at the spinal and supraspinal levels. The pharmacokinetics of both forms of tapentadol (immediate release-IR and extended release-ER) is relatively predictable and stable in healthy individuals. Clinical efficacy: Tapentadol IR was studied in clinical trials involving patients mainly with postoperative pain, but also in patients suffering from acute low back pain and osteoarthritis-related pain. Tapentadol ER was approved for management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate. Expert opinion: Although future improved, well-designed prospective, randomized double-blind controlled studies are needed to determine both the relative efficacy of tapentadol and its safety, we believe that tapentadol has the potential to become a uniquely suited opioid medication in the multi-modal management of moderate-to-severe acute and chronic pain conditions.