Is there data to support greater efficacy of long-acting naltrexone injectable compared to oral naltrexone in patients with opioid use and/or alcohol use disorder?

Comment by InpharmD Researcher

Direct comparative data on the efficacy of long-acting injectable (LAI) versus oral naltrexone are limited. In alcohol use disorder, evidence suggests comparable efficacy between the two formulations, with some findings indicating superior three-month treatment retention and increased time to relapse with the LAI formulation. However, one study reported lower healthcare utilization with oral naltrexone, implying that LAI may not offer clear advantages to justify its higher cost (see Table 1). In opioid use disorder, limited data suggest significantly improved treatment retention with LAI compared to oral naltrexone, though further comparative studies are needed to confirm these observations.

Background

A 2022 meta-analysis sought to gauge the impact of extended-release injectable naltrexone, in comparison to a placebo, on alcohol consumption among patients dealing with alcohol use disorder (AUD). The analysis incorporated seven trials involving 1,500 adults with AUD who received monthly injections of either placebo or extended-release naltrexone at doses ranging from 150 to 400 mg for 2 to 6 months. These trials were conducted in outpatient clinic settings in the United States or Europe, including specialized alcohol/substance use clinics and HIV clinics. Generally, participants were treatment-seeking adult males or non-pregnant, non-lactating females with moderate to severe alcohol use, assessed through validated tools, and a minimum of one weekly episode of heavy drinking. The analysis measured the pooled weighted mean difference (WMD) in drinking days per month and heavy drinking days per month. [1]

The WMD favored extended-release naltrexone, showing -2.0 (95% confidence interval [CI] -3.4 to -0.6; p= 0.03) for drinking days per month and -1.2 (95% CI -0.2 to -2.1; p= 0.02) for heavy drinking days per month, reflecting that treatment resulted in two fewer drinking days per month and 1.2 fewer heavy drinking days per month compared to the placebo. Trials not mandating lead-in abstinence and those lasting over 3 months reported larger reductions in heavy drinking days per month, with WMDs of -2.0 (95% CI -3.52 to -0.48; p= 0.01) and -1.9 (95% CI -3.2 to -0.5; p= 0.01), respectively. [1]

Importantly, two trials (see Tables 1-2) comparing the clinical and cost-effectiveness of oral and injectable naltrexone were identified. Due to limited available data, a meta-analysis could not be performed. Nevertheless, these studies reported 3 to 6 monthly heavy drinking days with no significant differences between groups, suggesting equal efficacy between the two formulations. [1]

A recent randomized clinical trial (RCT) compared the effectiveness of oral naltrexone versus extended-release injectable naltrexone for hospitalized patients with AUD. A total of 248 participants were enrolled, with 125 receiving oral naltrexone and 123 receiving extended-release injectable naltrexone. The primary outcome, the change in percentage of heavy drinking days (HDDs) over the past 30 days, was assessed at a 3-month follow-up. At baseline, the oral naltrexone group had a median of 66.7% HDDs, and the extended-release injectable naltrexone group had a median of 70.7% HDDs. After 3 months, the oral naltrexone group reduced their HDDs to 27.4% (-38.4 percentage points), while the extended-release injectable naltrexone group reduced theirs to 23.8% (-46.4 percentage points). The difference between the groups was not statistically significant (p= 0.14). Regarding acute health care utilization, 59 out of 109 participants (54.1%) in the oral naltrexone group and 66 out of 108 participants (61.1%) in the extended-release injectable naltrexone group reported acute health care utilization in the previous 3 months. The odds ratio for health care utilization was 1.34 (95% CI 0.77 to 2.33), indicating no significant difference between groups. Overall, both treatments led to substantial reductions in heavy drinking, with no significant difference between the two, suggesting that the choice of treatment should depend on factors such as patient preference and insurance coverage. [2]

A 2019 protocol describes a phase 4, open-label RCT (NCT01893827) evaluating extended-release naltrexone (XR-NTX) versus oral naltrexone (O-NTX) for alcohol dependence treatment in a primary care setting. Notably, the trial was sponsored by NYU Langone Health and conducted at Bellevue Hospital Center in New York City. A total of 237 adults with alcohol dependence were recruited from the community and randomized to receive either XR-NTX 380 mg intramuscularly (IM) once monthly or oral naltrexone 50 mg daily for 24 weeks, with both groups receiving primary care–based Medical Management. The primary outcome was the percentage of participants achieving abstinence or moderate drinking, defined as ≤2 drinks per day for men, ≤1 drink per day for women, and ≤2 heavy drinking occasions per month, during the final 20 of 24 treatment weeks. According to data posted on ClinicalTrials.gov, 29% of XR-NTX participants (n= 117) and 23% of O-NTX participants (n= 120) met this outcome. Despite the availability of the protocol and trial results via ClinicalTrials.gov, no full peer-reviewed publication of the study’s findings has been identified to date. [3], [4]

A 2017 randomized pilot proof-of-concept study investigated the impact of pre-discharge administration of injectable versus oral naltrexone on post-hospitalization treatment engagement among veterans with AUD. This single-center trial randomized 54 hospitalized veterans diagnosed with DSM-IV alcohol dependence to receive either a one-time 380 mg IM naltrexone injection or a 50 mg oral dose along with a 30-day prescription prior to discharge. Participants were recruited from general medical, psychiatric, surgical, and residential treatment units and followed for 45 days post-discharge. Inclusion criteria required absence of opioid use or dependence, clinically stable hepatic function, and capacity for informed consent. Baseline assessments included alcohol consumption via Timeline Follow-back, depression and anxiety screening (PHQ-9 and GAD-7), and psychiatric comorbidities assessment using the MINI. Medication adherence was defined as receiving the second injection in the injectable group or taking ≥80% of oral doses in the other group. Among the 45 participants who received study medication, follow-up rates reached 77.8% for both 14- and 45-day assessments. Median alcohol consumption dropped significantly from 128 drinks in the 14 days prior to hospitalization to zero drinks at both follow-up points (p<0.001). Medication adherence was comparable between groups (62% oral vs. 61% injection). Although not powered to detect statistical significance, post-discharge specialty addiction treatment engagement was high, with 86.4% of injectable and 78.3% of oral naltrexone recipients attending at least one visit within 14 days. Retention in treatment over three months was numerically greater in the injectable group (40.9% vs. 21.7%). No significant differences were observed between groups in alcohol consumption, treatment engagement metrics, or hospital readmission rates. The data affirm feasibility of initiating either formulation of naltrexone in the inpatient setting, and suggest potential for enhanced care continuity post-discharge when pharmacologic treatment is integrated into the hospitalization process. [5]

Regarding opioid use disorder (OUD), a 2019 randomized, open-label, single-center trial compared the clinical outcomes of extended-release naltrexone (XR-naltrexone) and daily oral naltrexone, both administered in conjunction with a comprehensive behavioral therapy regimen, in a cohort of 60 adults diagnosed with DSM-IV-defined opioid dependence. Following inpatient detoxification and successful naltrexone induction, participants were stratified by baseline opioid use severity and then randomized in a 1:1 fashion to receive either monthly IM injections of XR-naltrexone (380 mg) or daily oral naltrexone (50 mg), with all patients concurrently enrolled in behavioral naltrexone therapy. Participants were scheduled for outpatient clinic visits two to three times per week over the 24-week treatment period, with urine toxicology monitoring at each encounter. Kaplan-Meier analysis demonstrated significantly improved 24-week treatment retention among participants receiving XR-naltrexone compared with those on oral naltrexone (57.1% vs. 28.1%, respectively; p= 0.03. Multivariable Cox regression adjusting for demographic and clinical covariates revealed a hazard ratio (HR) for dropout of 2.18 (95% CI 1.07 to 4.43) favoring XR-naltrexone. Rates of opioid use, assessed via onsite urine drug screening, did not significantly differ between groups (median proportion of opioid-positive specimens: 2.4% in XR-naltrexone vs. 8.8% in oral naltrexone; p= 0.57). The XR-naltrexone group attended more behavioral sessions on average (mean 17.0 vs. 12.3) and earned a higher mean value in voucher incentives ($371.37 vs. $197.68). Although both groups experienced common adverse effects consistent with protracted opioid withdrawal, XR-naltrexone was generally well tolerated, with only one serious adverse event (pruritic hives) directly attributed to the study drug. These findings underscore the superiority of XR-naltrexone in sustaining treatment adherence over oral formulations despite the use of intensive psychosocial support in both arms. [6]

Lastly, a 2010 quasi-experimental analysis compared early treatment outcomes between long-acting injectable naltrexone and oral naltrexone maintenance therapy, each combined with psychosocial intervention, for individuals with heroin dependence. The study included patients enrolled in two concurrently conducted randomized trials, 69 received oral naltrexone between 1999 and 2002, and 42 received long-acting injectable naltrexone between 2000 and 2003. During the first 8 weeks following detoxification, patients treated with injectable naltrexone had significantly greater retention in treatment (p= 0.012) and improved opiate use outcomes on one of several measures (p= 0.024), favoring the injectable group. Subgroup analysis revealed that individuals with less severe baseline heroin use responded better to injectable naltrexone, whereas those with more severe use had better retention when treated with oral naltrexone combined with intensive psychotherapy. These findings suggest that while injectable naltrexone may offer advantages overall, the severity of heroin use and intensity of accompanying psychosocial support play critical roles in treatment outcomes. The authors note that results are exploratory due to the study’s quasi-experimental design. [7]

References:

[1] Murphy CE 4th, Wang RC, Montoy JC, Whittaker E, Raven M. Effect of extended-release naltrexone on alcohol consumption: a systematic review and meta-analysis. Addiction. 2022;117(2):271-281. doi:10.1111/add.15572
[2] Magane KM, Dukes KA, Fielman S, et al. Oral vs Extended-Release Injectable Naltrexone for Hospitalized Patients With Alcohol Use Disorder: A Randomized Clinical Trial. JAMA Intern Med. Published online April 21, 2025. doi:10.1001/jamainternmed.2025.0522
[3] Malone M, McDonald R, Vittitow A, et al. Extended-release vs. oral naltrexone for alcohol dependence treatment in primary care (XON). Contemp Clin Trials. 2019;81:102-109. doi:10.1016/j.cct.2019.04.006
[4] ClinicalTrials.gov. Extended-Release vs. Oral Naltrexone Alcohol Treatment in Primary Care (X-ON). Updated June 16, 2020. Accessed May 7, 2025. https://clinicaltrials.gov/study/NCT01893827
[5] Busch AC, Denduluri M, Glass J, et al. Predischarge Injectable Versus Oral Naltrexone to Improve Postdischarge Treatment Engagement Among Hospitalized Veterans with Alcohol Use Disorder: A Randomized Pilot Proof-of-Concept Study. Alcohol Clin Exp Res. 2017;41(7):1352-1360. doi:10.1111/acer.13410
[6] Sullivan MA, Bisaga A, Pavlicova M, et al. A Randomized Trial Comparing Extended-Release Injectable Suspension and Oral Naltrexone, Both Combined With Behavioral Therapy, for the Treatment of Opioid Use Disorder. Am J Psychiatry. 2019;176(2):129-137. doi:10.1176/appi.ajp.2018.17070732
[7] Brooks AC, Comer SD, Sullivan MA, et al. Long-acting injectable versus oral naltrexone maintenance therapy with psychosocial intervention for heroin dependence: a quasi-experiment. J Clin Psychiatry. 2010;71(10):1371-1378. doi:10.4088/JCP.09m05080ecr

Literature Review

A search of the published medical literature revealed 2 studies investigating the researchable question:

Is there data to support greater efficacy of long-acting naltrexone injectable compared to oral naltrexone in patients with opioid use and/or alcohol use disorder?

Level of evidence

B - One high-quality study or multiple studies with limitations  Read more→



Please see Tables 1-2 for your response.


 

Efficacy of long-acting, injectable versus oral naltrexone for preventing admissions for alcohol use disorder

Design

Retrospective cohort study

N= 79

Objective

To compare clinical outcomes in veterans treated with long-acting, injectable naltrexone (LAI NTX) or oral naltrexone

Study Groups

Oral naltrexone (n= 65)

LAI naltrexone (n= 14)

Inclusion Criteria

First-time receipt (either an outpatient prescription or inpatient medication order) of oral NTX or LAI NTX; use of NTX for alcohol use disorder (AUD)

Exclusion Criteria

Concurrent use of acamprosate or disulfiram and use of NTX for any diagnoses other than AUD

Methods

Electronic medical record system within the VA was retrospectively reviewed to identify eligible veterans and categorized into oral and LAI NTX groups. Prior to LAI therapy, patients could receive up to 30 days of oral NTX. History and physical note was generally utilized to identify clinical encounters of interest, such as alcohol-related hospital admissions and outpatient clinic visits. Dispensing information outside of the VA pharmacy would not be used. 

Duration

First-time receipt: between January 1, 2015 and December 31, 2015

Outcome Measures

Primary: 90-day alcohol-related hospital admissions per patient (ARA90)

Secondary: 90-day outpatient clinic and emergency department (ED) visits, 30-day alcohol-related admissions (ARA30), and medication adherence

Baseline Characteristics

  Oral naltrexone (n= 65)

LAI naltrexone (n= 14)

 

Age, years

46.9 47.9  

Male

93.8% 85.7%  

Additional mental health diagnoses 

Depressive disorder

Psychotic disorder 

Anxiety disorder 

Mood disorder 

Other substance disorder 

Posttraumatic stress disorder 

 

58.5%

3.1%

26.2%

10.8%

72.3%

53.8%

 

42.9%

0

42.9%

7.1%

78.6%

42.9%

 

Baseline health care utilization in the 12 months prior to naltrexone initiation

Alcohol-related admissions, per patient 

Alcohol-related ED visits, per patient

Mental health clinic visits, per patient 

 

1.18

1.11

2.8

 

1.57

1.36

1.64

 

Include relevant baseline characteristics that will provide a general (big picture) view of the patients in the study.

Results

Endpoint (healthcare utilization after naltrexone initiation, per patient)

Oral naltrexone (n= 65)

LAI naltrexone (n= 14)

p-value

ARA90

0.17 0.64 0.06

ED visit, 90 d

0.23  0.71  0.03 

Clinic visit, 90 d

0.91 1.86 < 0.01

ARA 30

0.05 0.36 < 0.01

6-month data 

ARA 

ED visits 

Mental health clinic visits 

 

0.32

0.32

1.92

 

1.14

1.14

3.64

 

< 0.01

< 0.01

< 0.01

Medication adherence as measured by average medication possession ratio (MPR) based on medication refill dates, as well as medication administration chart notes, was 65.14% for oral naltrexone and 67% for LAI naltrexone. 

Adverse Events

N/A

Study Author Conclusions

Oral NTX was associated with lower healthcare utilization compared to LAI NTX in this veteran population. This indicates that LAI NTX may not provide additional benefits justifying the cost. This study had several limitations. Randomized trials comparing efficacy between oral NTX and LAI NTX are needed.

InpharmD Researcher Critique

The study is limited to its retrospective nature, as clinical outcomes documented in chart notes may be subject to errors. Additionally, the patient population is limited to the veteran, further limiting the generalizability to a broader patient population. Other factors,  such as medical comorbidities and homelessness, were not accounted for in outcome measurements. 



References:

Beatty A, Stock C. Efficacy of long-acting, injectable versus oral naltrexone for preventing admissions for alcohol use disorder. Ment Health Clin. 2018;7(3):106-110. Published 2018 Mar 23. doi:10.9740/mhc.2017.05.106

 

Treatment outcomes of long-acting injectable naltrexone versus oral naltrexone in alcohol use disorder in veterans

Design

Retrospective chart review

N= 32

Objective

To compare the effectiveness, defined by time to relapse, of long-acting injectable (LAI) naltrexone versus oral naltrexone

Study Groups

Oral Naltrexone (n =16)

Long-Acting Injectable Naltrexone (n = 16)

Inclusion Criteria

Subjects prescribed either oral or LAI naltrexone, greater than 21 years of age, had a diagnosis of alcohol use disorder (AUD) or alcohol dependence, received treatment in the Substance Use Disorder Recovery Program (SUDRP) at the Veterans Affairs Medical Center (VAMC) main campus, and were abstaining from alcohol use at medication initiation

Exclusion Criteria

Prescribed naltrexone for any indication other than AUD, pregnant, initiated on either dosage form during hospital admission, discontinued LAI naltrexone after 1 dose, or relapse was not documented

Methods

Those prescribed oral naltrexone were randomized to match LAI naltrexone subjects at a 1:1 ratio. 

For oral naltrexone, medication possession ratio (MPR) was defined as number of tablets dispensed during a time period divided by days in that time period. For LAI naltrexone, MPR was defined as number of injections given multiplied by 28 days divided by the number of days in the time period.

Duration

August 1, 2016 to July 31, 2018 

Outcome Measures

Primary: time to relapse defined as patient, family, or friend volunteered report; hospitalization for alcohol intoxication; positive ethyl glucuronide; or elevated blood alcohol concentration

Secondary: MPR, comorbid mental health diagnosis, substance use, past pharmacological treatment, liver and kidney function, and enrollment in addiction-focused psychosocial therapy

 

Baseline Characteristics

 

Oral Naltrexone (n =16)

Long-Acting Injectable Naltrexone (n = 16)

 

Age, years

49.25 ± 13.12 56.81 ± 12.93  

Female

12.5%  18.7%   

White

68.8% 56.3%   

Co-occurring mental health diagnosis

Depressive

Psychotic

Mood

 

62.5%

0

12.5% 

 

56.3%

6.3%

18.7% 

 

Posttraumatic stress disorder

Other

None

 

12.5%

25%

 

18.7%

18.7%

 

Results

Endpoint

Oral Naltrexone (n = 16)

Long-Acting Injectable Naltrexone (n = 16)

p-value

Time to relapse, days

50.5 ± 78.8  150.5 ± 108.9 0.009

Medication possession ratio

81.0%  76.2%  0.478

Other substance use

13 (81.3%) 14 (87.5%) 0.626
Past pharmacological treatment

4 (25.0%)

3 (18.7%) 0.669
Engagement in alcoholics anonymous

3 (18.7%)

1 (6.2%) 0.285

Adverse Events

No statistically significant differences were found in safety parameters between the 2 groups, including serum creatinine, aspartate transaminase, or alanine transaminase greater than 3 times the upper limit of normal.

Study Author Conclusions

In conclusion, based on the results of this study, LAI naltrexone is associated with increased time to relapse compared to oral naltrexone at this VAMC. This study showed no difference in patient adherence or safety outcomes. Moving forward, LAI naltrexone should be considered as a first-line agent for veterans diagnosed with alcohol use disorder.

InpharmD Researcher Critique

The study's retrospective nature, small sample size, and restriction to a single practice center pose limitations, affecting the generalizability of findings. The 7-year age difference between groups introduces a confounding variable, potentially influencing treatment outcomes. Reliance on volunteered reports for assessing relapse and the recorded date may introduce subjectivity and inaccuracies. Exclusion of patients not enrolled in the studied treatment program introduces selection bias. While patient self-reporting increases variability, its consistency between oral and LAI naltrexone groups is a positive aspect, though it warrants consideration of the potential impact on study reliability. 



References:

Leighty AE, Ansara ED. Treatment outcomes of long-acting injectable naltrexone versus oral naltrexone in alcohol use disorder in veterans. Ment Health Clin. 2019;9(6):392-396. Published 2019 Nov 27. doi:10.9740/mhc.2019.11.392