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Cited by 175Opioid Use Disorder TreatmentSubstance Abuse Treatment and OutcomesNeuropeptides and Animal Physiology

Depot naltrexone: long-lasting antagonism of the effects of heroin in humans

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Comer, Sandra, Collins, Eric, Kleber, Herbert, Nuwayser, Elie, Kerrigan, James, Fischman, Marian·2002·Psychopharmacology
DOI 10.1007/s002130100909PMC PMC4079470
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Abstract

Rationale Naltrexone, an opioid antagonist, is currently approved as a treatment for heroin dependence. However, naltrexone is generally not well accepted by patients, and medication non-compliance is a difficult obstacle to treatment. A sustained-release form of naltrexone may improve compliance.Objective The present study was designed to evaluate the time course, safety, and effectiveness of a depot formulation of naltrexone (Depotrex).Methods Twelve heroin-dependent individuals participated in an 8-week inpatient study. After a 1-week detoxification period, six participants received 192 mg naltrexone base and six participants received 384 mg naltrexone base. For safety, the low dose of depot naltrexone was tested before the high dose. The effects of heroin (0, 6.25, 12.5, 18.75, 25 mg, i.v.) were evaluated for the next 6 weeks. One dose of heroin was tested per day on Mondays through Fridays, and the entire dose range was tested each week. Active heroin doses were administered in ascending order during the week, while placebo could be administered on any day. Subjective, performance, and physiological effects were measured both before and after heroin administration. The hypotheses were that depot naltrexone would antagonize the effects of heroin, and that the high dose of depot naltrexone would produce a more effective and longer-lasting antagonism than the low dose.Results The low and high doses of depot naltrexone antagonized heroin-induced subjective ratings for 3 and 5 weeks, respectively. Plasma levels of naltrexone remained above 1 ng/ml for approximately 3 and 4 weeks after administration of 192 mg and 384 mg naltrexone. Other than the initial discomfort associated with the injection of depot naltrexone, there were no untoward side-effects.Conclusions These results suggest that this depot formulation of naltrexone provides a safe, effective, long-lasting antagonism of the effects of heroin.

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Crossref · 10.1007/s002130100909

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  • Extended-release naltrexone is efficacious relative to placebo for preventing relapse to opioid dependence.

    “Extended-release naltrexone gradually releases sufficient naltrexone to block the euphoric effects of opioids for approximately 1 month after injection and is efficacious as compared with placebo.9–12”

    From Extended-release naltrexone to prevent opioid relapse in criminal justice offenders (2016) · cites this paper as [9]

  • Extended-release naltrexone releases enough naltrexone to block opioid euphoria for about one month after injection.

    “Extended-release naltrexone gradually releases sufficient naltrexone to block the euphoric effects of opioids for approximately 1 month after injection and is efficacious as compared with placebo.9–12”

    From Extended-release naltrexone to prevent opioid relapse in criminal justice offenders (2016) · cites this paper as [9]

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Authors
Comer, S., Collins, E., Kleber, H., Nuwayser, E., Kerrigan, J., & Fischman, M.
Affiliations
New York State Psychiatric Institute (US)
ORCID
Comer, Sandra
Venue
Psychopharmacology
Publisher
Springer Science and Business Media LLC
Published
2002-02-01
Volume
159
Issue
4
Pages
351-360
ISSN
  • 0033-3158 (ISSN-L)
  • 1432-2072
DOI
10.1007/s002130100909
PMC
PMC4079470
OpenAlex
W1985094131
Cited by
175
References
42
Citations by year
2026: 2 · 2025: 5 · 2024: 5 · 2023: 3 · 2022: 3 · 2021: 5 · 2020: 8 · 2019: 9 · 2018: 2 · 2017: 4 · 2016: 3 · 2015: 1 · 2014: 5 · 2013: 5 · 2012: 7
FWCI
12.24
Type
journal article
Language
en
Open access
Licence
www.springer.com/tdm (tdm)
Locations
  • Psychopharmacology (publishedVersion)
  • PubMed (publishedVersion)
  • PubMed Central (acceptedVersion)
Funders
National Institute on Drug Abuse (DA-09236, P50DA009236)
Topics
  • Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Opioid Use Disorder Treatment
  • Health Sciences › Medicine › Epidemiology › Substance Abuse Treatment and Outcomes
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
Keywords
heroin addiction, opioid antagonism, sustained-release formulation, medication adherence, opioid detoxification
MeSH terms
Adult, Affect, Analysis of Variance, Chemistry, Pharmaceutical, Delayed-Action Preparations, Heroin, Dose-Response Relationship, Drug, Heroin Dependence, Humans, Injections, Intravenous, Male, Naltrexone, Narcotic Antagonists, Narcotics, Pupil

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