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Oxycodone/Naloxone Prolonged Release: A Review in Severe Chronic Pain

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Abstract

Oral oxycodone/naloxone prolonged release (PR) [Targin®, Targinact®, Targiniq®] is a 12-hourly opioid receptor agonist and opioid receptor antagonist fixed-dose combination product that is approved in countries in the EU for the management of severe pain (adequately manageable only with opioid analgesics) in adults. Oral naloxone prevents oxycodone from binding to μ-receptors in the gastrointestinal (GI) tract, thereby counteracting opioid-induced constipation (OIC). In short-term (5- to 12-week) clinical trials of adults with moderate to severe, chronic pain and OIC (OXN3001, OXN3006, OXN3506), oxycodone/naloxone PR significantly improved OIC while providing noninferior analgesia relative to oxycodone PR; results were consistent between cancer and non-cancer patients in OXN3506. Analgesia and improvements in bowel function were sustained with an additional 24–52 weeks of oxycodone/naloxone PR treatment in long-term extension studies. Results in real-world studies were consistent with those in clinical trials. Oxycodone/naloxone PR was generally well tolerated, with nausea, hyperhidrosis, and diarrhoea (generally transient) reported as the most commonly occurring adverse events. Thus, oxycodone/naloxone PR is a useful treatment option to consider in adults with severe chronic pain that can be adequately managed only with opioid analgesics, particularly in those with OIC.

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Acknowledgements

During the peer review process, the manufacturer of oxycodone/naloxone PR was also offered an opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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  1. Springer, Private Bag 65901, Mairangi Bay, 0754, Auckland, New Zealand

    Esther S. Kim

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  1. Esther S. Kim
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Correspondence to Esther S. Kim.

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Funding

The preparation of this review was not supported by any external funding.

Conflicts of interest

Esther Kim is a salaried employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.

Additional information about this Adis Drug Review can be found at http://www.medengine.com/Redeem/61FBF0607FA89FDE.

Additional information

The manuscript was reviewed by: D. Dupoiron, Department of Anaesthesiology and Pain, Institut de Cancérologie de l’Ouest, Angers, France; S. Müller - Lissner, Berlin, Germany.

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Kim, E.S. Oxycodone/Naloxone Prolonged Release: A Review in Severe Chronic Pain. Clin Drug Investig 37, 1191–1201 (2017). https://doi.org/10.1007/s40261-017-0593-1

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