Naltrexone is a μ-opioid receptor antagonist that blocks the euphoric effects of heroin and prescription opioids. In order to improve treatment adherence, a once-monthly, intramuscular, extended-release formulation of naltrexone (XR-NTX) [VIVITROL®] has been developed, and approved in the USA and Russia for the prevention of relapse to opioid dependence, after opioid detoxification. The clinical efficacy of this formulation in patients with opioid dependence was demonstrated in a 24-week, randomized, double-blind, placebo-controlled, multicentre, phase III trial (ALK21-013; n = 250). In this trial, opioid-detoxified patients receiving XR-NTX 380 mg once every 4 weeks, in combination with psychosocial support, had a significantly higher median proportion of weeks of confirmed opioid abstinence during weeks 5–24, compared with those receiving placebo (primary endpoint). A significantly higher proportion of patients receiving XR-NTX achieved total confirmed abstinence during this period than those receiving placebo. XR-NTX was also associated with a significantly greater reduction in opioid craving and a significantly longer treatment retention period than placebo. XR-NTX was generally well tolerated in the phase III trial. The most common (incidence ≥5 %) treatment-emergent adverse events that also occurred more frequently with XR-NTX than with placebo were hepatic enzyme abnormalities, nasopharyngitis, insomnia, hypertension, influenza and injection-site pain. Thus, XR-NTX is a useful treatment option for the prevention of relapse to opioid dependence, following opioid detoxification.
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The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made by the authors on the basis of scientific and editorial merit.
Conflict of interest
This document has been written by in-house editorial staff of Adis Publications, who have no conflict of interest.
The manuscript was reviewed by: G.E. Bigelow, Behavioral Pharmacology Research Unit, Johns Hopkins University School of Medicine, Baltimore, MD, USA; M. Fishman, Psychiatry and Behavioural Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, USA; E. Krupitsky, Department of Addictions, St Petersburg Bekhterev Psychoneurological Research Institute, St Petersburg, Russian Federation; G.E. Woody, Department of Psychiatry, University of Pennsylvania, Philadelphia, PA, USA.
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Syed, Y.Y., Keating, G.M. Extended-Release Intramuscular Naltrexone (VIVITROL®): A Review of Its Use in the Prevention of Relapse to Opioid Dependence in Detoxified Patients. CNS Drugs 27, 851–861 (2013). https://doi.org/10.1007/s40263-013-0110-x
- Mental Component Summary Score
- Opioid Dependence
- Oral Naltrexone
- Opioid Withdrawal Symptom