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Published online: 23 January 2014
© Springer International Publishing Switzerland 2014
Abstract A combination of prolonged-release (PR) oxycodone with PR naloxone (Targin ®, Targiniq®, Targinact®) in one tablet with a fixed 2:1 ratio is available for the treatment of patients with severe pain, which can only be adequately managed with opioid analgesics. The aim of this formulation is to counteract opioid-induced constipation through the local antagonist effect of naloxone in the gut wall, while maintaining analgesia due to the low bioavailability of oral naloxone. Three large, 12-week, randomized, double-blind, phase III trials in patients with moderate to severe, chronic, non-malignant pain, plus a prospectively planned pooled analysis of two of these studies, demonstrated that oxycodone/naloxone PR improved bowel function, as measured by the bowel function index, compared with oxycodone PR. Additionally, oxycodone/naloxone PR relieved pain more effectively than placebo and no less effectively than oxycodone PR after 12 weeks. Phase II efficacy data in cancer patients are consistent with those observed in patients with non-malignant pain. Oxycodone/ naloxone PR was generally well tolerated; the most frequently reported adverse events were of gastrointestinal origin, consistent with those known to occur with opioid therapy. Of note, numerically lower rates of constipation were observed in the oxycodone/naloxone PR group compared with the oxycodone PR group. A cost-utility analysis predicted that oxycodone/naloxone PR would be a costeffective option compared with oxycodone PR in patients with non-malignant pain. Although more comparative data are needed, oxycodone/naloxone PR is an effective option for use in patients with severe chronic pain, particularly among those with opioid-induced constipation.
1 Introduction
Oxycodone, a strong opioid analgesic, is used across a broad spectrum of severe non-malignant related pain con- ditions such as somatic (e.g. osteoarthritis), neuropathic (e.g. diabetic neuropathy) and visceral (e.g. pancreatitis) pain, and in patients with moderate to severe cancer pain [1]. Although oxycodone is very effective for pain relief, its use is often restricted by adverse events, like all opioid agonists [2]. Around 80 % of patients treated with opioids will experience at least one adverse event during treatment [3].
As a result of the undesired action of oxycodone on the l-opioid receptors in the gastrointestinal (GI) tract, patients receiving long-term opioid therapy often experience opi- oid-induced bowel dysfunction, the most common...