Role of Tapentadol Immediate Release (Nucynta) in the Management Of Moderate-to-Severe Pain

Widespread in the U.S., pain is associated with significant adverse economic, clinical, and quality-of-life outcomes: from 15% to 20% of patients in the U.S. experience acute pain, up to 75% of patients experience pain after surgery, and 68 million people have chronic pain each year.1,2 Uncontrolled pain is the leading cause of disability; it may also delay patient recovery from surgery, increase risk of life-threatening events (such as deep-vein thrombosis or myocardial infarction), and lead to the development of chronic pain.1 For back pain alone, total health care expenditures in 2004 and 2005 were estimated at $85 billion to $100 billion.3 Current pharmacological treatment options commonly used for moderate-to-severe pain include anticonvulsants, antidepressants, nonsteroidal anti-inflammatory agents (NSAIDs), tramadol (Ul-tram, PriCara), and opioids. Anticonvulsants and antidepressants are associated with intolerable adverse effects (AEs) and numerous drug interactions, and successful analgesia is achieved in only 50% of patients with neuropathic pain.2 NSAIDs are effective for managing chronic pain, but their use is limited by their gastrointestinal (GI) and cardiovascular toxicity, adverse renal effects, and an increased risk of bleeding. Opioids are highly effective for acute and chronic pain, but their use is limited by nausea, vomiting, constipation, and sedation, as well as the possibility of addiction or dependence. Tramadol is an attractive alternative to opioids, but it is subject to genetic polymorphism because it is metabolized by cytochrome P-450 (CYP) 2D6, has a neurotoxic metabolite, and may predispose patients to serotonin syndrome.4 Despite the availability of these numerous options, pain continues to be under-treated,2 indicating a need for a potent analgesic with a low side-effect profile. Tapentadol HCl immediate release (IR) (Nucynta, PriCara), a centrally acting analgesic, was approved by the FDA on November 20, 2008, for the relief of moderate-to-severe acute pain. A long-acting formulation is being investigated.