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Tapentadol Immediate Release

A Review of its Use in the Treatment of Moderate to Severe Acute Pain

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Abstract

Tapentadol (Nucynta™) is an orally active, centrally acting synthetic analgesic that is thought to exert its analgesic effects via two mechanisms of action (μ-opioid receptor agonism and norepinephrine reuptake inhibition). In the US, the immediate-release (IR) formulation of the drug is approved for the relief of moderate to severe acute pain in patients aged ≥18 years. In the EU, the drug is currently in the marketing authorization process.

In clinical trials in patients with moderate to severe acute (postorthopaedic surgical or musculoskeletal) pain, recommended regimens of tapentadol IR (50–100 mg every 4–6 hours) provided an analgesic effect that was superior to that of placebo, and noninferior or similar to that of oxycodone IR (10 or 15 mg every 4–6 hours). Tapentadol IR therapy was generally well tolerated; it was associated with significant reductions in the incidences of nausea, vomiting and constipation compared with oxycodone IR therapy.

Thus, tapentadol IR is an effective treatment option for the management of moderate to severe acute pain. However, further studies evaluating its clinical utility in relation to that of tramadol and opioids other than oxycodone are warranted. Because tapentadol IR offers the prospect of reduced opioid-related gastrointestinal adverse events while maintaining adequate analgesia, it is a potentially valuable addition to the analgesic armamentarium.

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  1. Adis, a Wolters Kluwer Business, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore, Auckland, 0754, New Zealand

    James E. Frampton

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Correspondence to James E. Frampton.

Additional information

Various sections of the manuscript reviewed by: A. Buvanendran, Department of Anesthesiology, Rush Medical College at Rush-Presbyterian-St Luke’s Medical Center, Chicago, Illinois, USA; D. Guay, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota, USA; C.T. Hartrick, Department of Anesthesiology, William Beaumont Hospital, Royal Oak, Michigan, USA; P.A. Sloan, Department of Anesthesiology, University of Kentucky Medical Center, Lexington, Kentucky, USA; H. Smith, Department of Anesthesiology, Albany Medical College, Albany, New York, USA.

Data Selection

Sources: Medical literature published in any language since 1980 on ‘tapentadol’, identified using MEDLINE and EMBASE, supplemented by AdisBase (a proprietary database). Additional references were identified from the reference lists of published articles. Bibliographical information, including contributory unpublished data, was also requested from the company developing the drug.

Search strategy: MEDLINE, EMBASE and AdisBase search term was ‘tapentadol’. Searches were last updated 8 July 2010.

Selection: Studies in patients with moderate to severe pain who received tapentadol immediate-release formulation. Inclusion of studies was based mainly on the methods section of the trials. When available, large, well controlled trials with appropriate statistical methodology were preferred. Relevant pharmacodynamic and pharmacokinetic data are also included.

Index terms: Tapentadol, acute pain, pharmacodynamics, pharmacokinetics, therapeutic use, tolerability.

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Frampton, J.E. Tapentadol Immediate Release. Drugs 70, 1719–1743 (2010). https://doi.org/10.2165/11204470-000000000-00000

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