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Oxycodone/naloxone is a fixed-dose combination (FDC) prolonged-release analgesic developed by Mundipharma Research for the management of moderate to severe chronic pain. The formulation combines oxycodone, a semi-synthetic mu-opioid receptor agonist, with naloxone, a potent opioid receptor antagonist. This combination is specifically designed to provide systemic analgesia while preventing opioid-induced constipation (OIC). Naloxone has very low systemic bioavailability (<3%) due to extensive first-pass hepatic metabolism, allowing it to act locally as a competitive antagonist on opioid receptors in the gastrointestinal tract without compromising the central analgesic efficacy of oxycodone. Marketed under brand names such as Targinact, Targin, and Targiniq, it is also approved in certain regions for the treatment of severe restless legs syndrome.
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