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02. Naltrexone: Potential Indications and Administration in Children and Adolescents

Published on August 1, 2022 Expired on August 1, 2025

David R. Rosenberg, M.D.

Chair of the Department of Psychiatry & Behavioral Neuroscience - Wayne State University School of Medicine

Key Points

  • There are no FDA-approved pediatric indications for naltrexone.
  • Off-label use regularly occurs in conditions associated with abnormalities of the endogenous opioid system.
  • Current evidence supporting the use of naltrexone in children and adolescents is limited and conflicting.
  • Low-dose naltrexone effectively blocks opioid receptors and is well tolerated.
  • Mild hepatic toxicity has been reported at high doses.
  • Consider liver function tests before initiation and periodically during chronic treatment.

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Slides and Transcript

Slide 1 of 24

So turning to video 2, naltrexone: Potential indications and administration in children and adolescents.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 1 of 24

Slide 2 of 24

Opiate antagonists don’t readily cross the blood-brain barrier but they are potent competitive inhibitors with an affinity for mu-receptors which are found in very high concentration in bronchial smooth muscle and the digestive tract. So endogenous opioid peptides such as endorphins and enkephalins are present naturally in the brain and are released during times of physical pain or stress. Opiate antagonists block these effects and this blockade is the mechanism through which their psychiatric effects are derived.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 2 of 24
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Slide 3 of 24

Opiate antagonists have been observed to reverse hyperphagia and obesity, decrease social aggression, and attenuate drug- or stress-induced stereotypy associated with elevated endogenous opiate levels.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 3 of 24

Slide 4 of 24

Now, in terms of mechanism of action for naltrexone, naltrexone is a potent opioid antagonist with a high affinity for mu-opioid binding sites which completely and reversibly blocks the effects of endogenous and exogenous opiate derivatives.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
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Slide 5 of 24

And there is more and more evidence regarding the efficacy and side effect profile of naltrexone for psychiatric conditions but again this is mainly derived from adult studies of substance use and there’s considerable variability in response rates. Indeed, there aren’t any currently FDA-approved pediatric indications for naltrexone.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 5 of 24

Slide 6 of 24

That being said, off-label use regularly occurs in conditions associated with the opioid reward pathway such as self-injurious behaviors, eating disorders, hyperactivity, and restlessness in autism spectrum disorders and alcohol abuse disorders.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
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Slide 7 of 24

Potential indications, self-injurious behaviors. This is an area of high attention because elevated levels of endogenous opioids and decreased pain perception are hypothesized to contribute to the etiology or cause of many self-injurious behaviors. So naltrexone may actually be helpful for reestablishing pain perception and decreasing self-injurious behaviors in individual patients.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
  • Sabus, A., Feinstein, J., Romani, P., Goldson, E., & Blackmer, A. (2019). Management of self‐injurious behaviors in children with neurodevelopmental disorders: A pharmacotherapy overview. Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, 39(6), 645-664.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 7 of 24

Slide 8 of 24

That being said again, there is little evidence of long-term efficacy or information on possible long-term side effects in children. Self-injurious behaviors also persist for many years and it’s unknown whether a tolerance to opiate antagonism can develop. Several placebo-controlled studies have reported a reduction of self-injurious behaviors with naltrexone treatment but many of these studies have been conducted in very small samples and over a very limited time period and other studies did fail to demonstrate any effect whatsoever. Thus, additional research exploring long-term clinical benefits is critical.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
  • Sabus, A., Feinstein, J., Romani, P., Goldson, E., & Blackmer, A. (2019). Management of self‐injurious behaviors in children with neurodevelopmental disorders: A pharmacotherapy overview. Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, 39(6), 645-664.
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Slide 9 of 24

The current evidence supporting the use of naltrexone for self-injurious behaviors is limited and conflicting. Therefore, naltrexone should be reserved only for extreme cases of self-injurious behavior refractory to other more usual treatment options.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
  • Sabus, A., Feinstein, J., Romani, P., Goldson, E., & Blackmer, A. (2019). Management of self‐injurious behaviors in children with neurodevelopmental disorders: A pharmacotherapy overview. Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, 39(6), 645-664.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 9 of 24

Slide 10 of 24

Now, naltrexone also has a potential indication for autism spectrum disorder. And symptoms seen in opioid intoxication such as social withdrawal, stereotypies, and sensory sensitivity led to the hypothesis that there could be abnormalities of the endogenous opioid system playing an etiologic role in autism. As such, naltrexone was considered as a potential treatment for autism.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
  • Roy, A., Roy, M., Deb, S., Unwin, G., & Roy, A. (2014). Are opioid antagonists effective in attenuating the core symptoms of autism spectrum conditions in children: A systematic review. Journal of Intellectual Disability Research, 59(4), 293-306.
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Slide 11 of 24

An initial study of naltrexone in autistic children actually found improvements in both autistic, decreased social withdrawal, increased verbal production, reduced stereotype behaviors, and nonautistic that is decreases in restlessness and tantrum symptoms. Subsequent randomized controlled trials also found that naltrexone produce significant improvement in nonautistic symptoms, impulsivity, hyperactivity, and irritability and led to decreases in self-injurious behaviors and improved global assessment scores. However, in these same studies, naltrexone failed to improve the core symptoms of autism and had no significant effect on social and stereotypic behaviors.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
  • Roy, A., Roy, M., Deb, S., Unwin, G., & Roy, A. (2014). Are opioid antagonists effective in attenuating the core symptoms of autism spectrum conditions in children: A systematic review. Journal of Intellectual Disability Research, 59(4), 293-306.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 11 of 24

Slide 12 of 24

And due to significant heterogeneity of available trials, small sample sizes, evidence to support the use of naltrexone for treating the core symptoms of autism is still lacking. That being said, I find this a very promising area so please stay tuned.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
  • Roy, A., Roy, M., Deb, S., Unwin, G., & Roy, A. (2014). Are opioid antagonists effective in attenuating the core symptoms of autism spectrum conditions in children: A systematic review. Journal of Intellectual Disability Research, 59(4), 293-306.
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Slide 13 of 24

Now, naltrexone, potential indications for eating disorders. This is also an increasing area of use and study. Abnormal endorphin levels may underlie the etiology of binge or disordered eating. Naltrexone has been used to treat binge eating and purging in adults. That being said, again, there are a few controlled studies that have been conducted and none have been conducted with adolescent participants.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
  • Stancil, S. L., Adelman, W., Dietz, A., & Abdel-Rahman, S. (2019). Naltrexone reduces binge eating and purging in adolescents in an eating disorder program. Journal of Child and Adolescent Psychopharmacology, 29(9), 721-724.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 13 of 24

Slide 14 of 24

In a recent retrospective chart review of adolescent patients receiving low dose, that means 50 mg per day of naltrexone, it was well tolerated and was associated with reduced purging or urge to purge.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
  • Stancil, S. L., Adelman, W., Dietz, A., & Abdel-Rahman, S. (2019). Naltrexone reduces binge eating and purging in adolescents in an eating disorder program. Journal of Child and Adolescent Psychopharmacology, 29(9), 721-724.
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Slide 15 of 24

While additional studies are clearly needed, low-dose naltrexone appears to be well tolerated and to reduce symptoms and urges of binge eating and purging with no serious side effects.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
  • Stancil, S. L., Adelman, W., Dietz, A., & Abdel-Rahman, S. (2019). Naltrexone reduces binge eating and purging in adolescents in an eating disorder program. Journal of Child and Adolescent Psychopharmacology, 29(9), 721-724.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 15 of 24

Slide 16 of 24

Potential indications for alcohol abuse disorder. The use of naltrexone for alcohol dependence is well established among adult patients. Data on safety and effectiveness with adolescents though are quite limited. There are results of a small open-label trial suggesting that naltrexone is well tolerated in adolescents seeking treatment and appears to support efficacy in adolescents. That being said, additional research is needed before naltrexone can be recommended in pediatric populations routinely.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
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Slide 17 of 24

It is being used but the recommendation at present is to try other more standard interventions prior to naltrexone and when it is used to use a smaller or lower dose.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 17 of 24

Slide 18 of 24

For autism and autism-related self-injurious behaviors, naltrexone has been studied in children in a dosage range from 0.5 to 2 mg/kg/day. And for alcohol dependence in adolescents, the studies recommend a daily dose of 50 mg per day.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
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Slide 19 of 24

Side effects. Mild sedation was the most commonly reported side effect in children as well as insomnia, fatigue, and nausea.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 19 of 24

Slide 20 of 24

Mild hepatic toxicity has also been reported at high doses but not at low doses which still appear to effectively block opioid receptors. Liver function tests should be considered though before initiating treatment and periodically during chronic treatment to monitor for this rare but obviously concerning effect. Abuse and dependence of naltrexone has not been described and there are no reported cases of overdose.
References:
  • Rosenberg, D., & Gershon, S. (2012). Pharmacotherapy of child and adolescent psychiatric disorders. John Wiley & Sons.
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Slide 21 of 24

So key take-home points here are there are currently no FDA-approved pediatric indications for naltrexone. However, off-label use regularly occurs in conditions associated with abnormalities of the endogenous opioid system such as self-injurious behaviors, eating disorders, autism spectrum disorders, and alcohol use disorders.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 21 of 24

Slide 22 of 24

Current evidence supporting the use of naltrexone in children and adolescents is limited and conflicting but low-dose naltrexone appears to effectively block opioid receptors and is well tolerated with few side effects.
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Slide 23 of 24

Mild hepatic toxicity has been reported at high doses and liver function tests should be considered before initiation of treatment and periodically during chronic treatment.
Naltrexone: Potential Indications and Administration in Children and Adolescents Slide 23 of 24

Slide 24 of 24

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Next Section

03. Memantine: Potential Indications in Children and Adolescents

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Certification expiration date: August 1, 2025

CME Information

Learning Objectives:

After completing this activity, the learner will be able to:

  1. Identify the different atypical psychopharmacologic strategies for children and adolescents.
  2. Discuss the available evidence about nonstandard psychoactive drugs in the pediatric population.
  3. Recognize pediatric patients who could benefit from atypical psychopharmacologic strategies and utilize them accordingly.

Original Release Date: August 1, 2022

Review and Re-release Date: March 1, 2024

Expiration Date: August 1, 2025

Expert: David Rosenberg, M.D.

Medical Editor: Paz Badía, M.D.

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None of the faculty, planners, and reviewers for this educational activity have relevant financial relationships to disclose during the last 24 months with ineligible companies whose primary business is producing, marketing, selling, re-selling, or distributing healthcare products used by or on patients.

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  1. View the required educational content provided on this course page.

  2. Complete the Post Activity Evaluation for providing the necessary feedback for continuing accreditation purposes and for the development of future activities. NOTE: Completing the Post Activity Evaluation after the quiz is required to receive the earned credit.

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Medical Academy designates this enduring activity for a maximum of 1.25 AMA PRA Category 1 credit(s)™. Physicians should claim only the credit commensurate with the extent of their participation in the activity.

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