Is 16-4 mg once daily of buprenorphine/naloxone more effective than 8-2 mg once daily for opioid use disorder?

Comment by InpharmD Researcher

Currently, there is limited data available directly comparing the efficacy of buprenorphine/naloxone (Suboxone) 16-4 mg daily and lower doses in patients with OUD. Prescribing information for Suboxone recommends a maintenance dose of 16-4 mg, noting that higher doses (>24-6 mg daily) have not been demonstrated to provide additional clinical benefit. A retrospective review found that multiple daily doses of Suboxone (total daily doses of 16-4 mg to 32-8 mg) were linked to a greater incidence of relapse and an increased likelihood of positive urine drug screens compared to once daily dosing (8-2 mg), while prospective studies have determined the lack of major differences in efficacy between 16 mg daily dosing and lower doses. Several studies evaluating individual buprenorphine doses of 16 mg or higher have reported improved efficacy for OUD in comparison to lower doses, although treatment durations and drug formulations widely vary.

Background

A 2004 randomized controlled trial (N= 179) examined the use of buprenorphine treatment in patients with concomitant cocaine and opiate dependence. Double-blinded groups received daily sublingual buprenorphine doses of 2, 8, or 16 mg; 16 mg on alternate days; or placebo. After 13 weeks, patients were tested for opiate and cocaine metabolite presence and concentration in urine. During the study, patients who received daily buprenorphine doses of 8 mg or 16 mg showed statistically significant decreases in urine morphine levels (8 mg, p= 0.0135; 16 mg, p<0.001) and metabolite concentrations (8 mg, p= 0.0277; 16 mg, p= 0.006). During the withdrawal phase, all treatment groups except patients receiving 16 mg reported increased urine morphine concentration (16 mg, p= 0.15). For this reason, the authors suggest a loss of beneficial effects on opiate use with buprenorphine doses lower than 16 mg/day. No significant between-group differences were reported for adverse events or treatment retention. Based on the results, the use of buprenorphine 16 mg daily appears to be well-tolerated and effective in patients with concomitant cocaine and opiate dependence, although it should be of note that buprenorphine was administered as a sublingual alcoholic solution, which has greater bioavailability in comparison to its tablet counterpart and thus may not be entirely comparable. Results may not be applicable to use of buprenorphine/naloxone as buprenorphine was studied individually in this trial. [1]

A 2014 Cochrane review evaluated buprenorphine maintenance treatment versus placebo or methadone maintenance. A total of 31 randomized controlled trials and 5,430 patients were included with varying buprenorphine dose conditions: low (2 mg to 6 mg daily), medium (7 mg to 15 mg daily), and high (≥ 16 mg daily). Included trials also utilized differing formulations: sublingual solution, sublingual tablet, combined buprenorphine/naloxone sublingual tablet, and implant. At all doses examined, buprenorphine was superior to placebo in treatment retention (high quality of evidence), although only high-dose buprenorphine was more effective versus placebo in suppressing illicit opioid use (standardized mean difference [SMD] -1.17; 95% confidence interval [CI] -1.85 to -0.49; 3 studies, medium quality of evidence). However, there was no difference between buprenorphine prescribed at fixed doses (> 7 mg daily) or methadone prescribed at fixed doses (≥ 40 mg daily) in treatment retention or suppression of illicit opioid use. The authors noted that buprenorphine may have advantages in settings where it may be clinically preferred, due to its alternate dosing schedule and safety profile, over methadone, and that buprenorphine overall is highly effective for heroin dependence versus placebo, especially at higher doses. [2], [3]

A recently published retrospective cohort study (N= 6,499) evaluated whether higher doses of buprenorphine treatment for opioid use disorder (OUD) are associated with improved treatment retention due to the increased spread of fentanyl addiction. Data were extracted from the Rhode Island Prescription Drug Monitoring program for patients initiating buprenorphine treatment for OUD between October 1, 2016, and September 30, 2020. Patients were categorized based on their daily dose of buprenorphine: 2 mg (0 to <3 mg), 4 mg (3 to <6 mg), 8 mg (6 to <10 mg), 12 mg (10 to <14 mg), 16 mg (14 to <18 mg), 20 mg (18 to <22 mg), 24 mg (22 to <26 mg), 28 mg (26 to <30 mg), and 32 mg (≥30 mg). The analysis primarily focused on comparing 16 mg and 24 mg daily dosing, which are the recommended and upper limit daily doses, respectively, per the FDA-approved prescribing information. An exploratory analysis also compared 8 mg daily dosing with the 16 and 24 mg daily dosing. [4]

Among 6,499 patients included for analysis, Kaplan-Meier analyses found a significantly higher proportion of patients receiving 16 mg daily dosing discontinued treatment within 180 days compared to patients receiving 24 mg daily dosing (59% vs. 24%; p= 0.005). Cox regression analyses determined patients receiving 16 mg had a higher risk for treatment discontinuation compared to those prescribed 24 mg (adjusted hazard ratio 1.20; 95% CI 1.06 to 1.37). Exploratory analyses found similar time to treatment discontinuation among patients prescribed 8 mg and 16 mg. The authors posit that buprenorphine doses higher than current recommendations may hold merit with regard to treatment retention improvement. Of note, similar results for 16 and 8 mg daily dosing may not be observed with use of buprenorphine/naloxone, as this study solely evaluated use of buprenorphine alone. [4]

A 2020 systematic review examined the effect of buprenorphine dose in treatment of OUD to determine an optimal dose or dose-range. A total of 15 studies were included, utilizing both oral liquid and tablet formulations. Studies that included a dose of 16 mg or higher reported mixed results of the efficacy of lower doses in producing blockade effects; studies that reported doses found a dose ≥16 mg to be more effective generally included higher challenge doses of a μ-opioid-receptor agonist versus studies that reported doses under 16 mg to be effective. There was no clear correlation between buprenorphine dose and reported treatment retention, nor illicit opioid use during the study periods. There was no evidence that a daily dose higher than 16 mg confers additional benefit, and data were inconclusive regarding the comparative effectiveness of 8 mg versus 16 mg. The authors concluded that buprenorphine treatment should be individualized and subject to risk-benefit assessments, as data appears inconclusive with regards to relative effectiveness between dosages. [5]

References:

[1] Montoya ID, Gorelick DA, Preston KL, et al. Randomized trial of buprenorphine for treatment of concurrent opiate and cocaine dependence. Clin Pharmacol Ther. 2004;75(1):34-48. doi:10.1016/j.clpt.2003.09.004
[2] Shulman M, Wai JM, Nunes EV. Buprenorphine Treatment for Opioid Use Disorder: An Overview. CNS Drugs. 2019;33(6):567-580. doi:10.1007/s40263-019-00637-z
[3] Mattick RP, Breen C, Kimber J, Davoli M. Buprenorphine maintenance versus placebo or methadone maintenance for opioid dependence. Cochrane Database Syst Rev. 2014;2014(2):CD002207. Published 2014 Feb 6. doi:10.1002/14651858.CD002207.pub4
[4] Chambers LC, Hallowell BD, Zullo AR, et al. Buprenorphine Dose and Time to Discontinuation Among Patients With Opioid Use Disorder in the Era of Fentanyl. JAMA Netw Open. 2023;6(9):e2334540. Published 2023 Sep 5. doi:10.1001/jamanetworkopen.2023.34540
[5] Hjelmström P, Banke Nordbeck E, Tiberg F. Optimal dose of buprenorphine in opioid use disorder treatment: a review of pharmacodynamic and efficacy data. Drug Dev Ind Pharm. 2020;46(1):1-7. doi:10.1080/03639045.2019.1706552

Literature Review

A search of the published medical literature revealed 3 studies investigating the researchable question:

Is 16-4 mg once daily of buprenorphine/naloxone more effective than 8-2 mg once daily for opioid use disorder?

Level of evidence

C - Multiple studies with limitations or conflicting results  Read more→



Please see Tables 1-3 for your response.


 

A dose–effect study of repeated administration of buprenorphine/naloxone on performance in opioid-dependent volunteers

Design

Prospective, randomized, double-blind, volunteer-based study

N= 8

Objective

To evaluate dose-related effects of repeated administration of the buprenorphine/naloxone combination product (8/2, 16/4, 32/8 mg, sublingual tablets) in eight opioid-dependent volunteers

Study Groups

Study patients (N= 8)

Inclusion Criteria

Healthy adult community volunteers, diagnosis of current opioid-dependence, eligibility for opioid agonist treatment

Exclusion Criteria

N/A

Methods

Patients resided in a closed 14-bed residential unit. Patients were assigned either 8/2, 16/4, or 32/8 mg of buprenorphine/naloxone using a random number table. Treated was administered by nurses daily at 8:00 am. Performance test was initiated after the patient had received 7-10 days of buprenorphine/naloxone administration at the randomized dose. The test was conducted at three separate timepoints: 12 hours before the daily dose, and 1 and 6 hours after the daily dose. A total of nine performance testing sessions were completed during the study.

Duration

7-10 days

Outcome Measures

Performance task which includes:

Digit symbol substitution test (DSST) a measure of psychomotor/cognitive speed

Trail-making test Part A and Part B which measures psychomotor speed and cognitive flex

Time estimation task which assessed the participant’s ability to accurately estimate the duration of 5, 20, and 80 second time intervals

Digit recall task which assessed the participant’s ability to recall 8-digit strings following short delays

‘n-back’ task which assessed the participant’s ability

Recognition memory and recall words, following an 80 minute delay

Baseline Characteristics

 

Study patients (N= 8)

   

Age, years

36 (24 to 41)    

Years of education

12 (10 to 14)    

Duration of lifetime illicit opioid use

8 (4 to 12)    

Results

Endpoint

8/2 mg

16/4 mg

32/8 mg

DSST

Number correct

Number attempted

 

33.46

39.75

 

34.77

37.73

 

38.08

41.04

Trail-making, total time in seconds

A

B

 

41.80

55.43

 

44.31

59.97

 

49.18

55.60

Time estimation

Estimate - 5 seconds

Estimate - 20 seconds

Estimate - 80 seconds

 

5.68

18.56

69.63

 

5.49

19.12

71.84

 

6.19

19.79

76.47

Digit recall, number correct

5.08

4.92

6.34

n-back

d (sensitivity)-0-back

d (sensitivity)-1-back

d (sensitivity)-2-back

RT (ms)-0-back

RT (ms)-1-back

RT (ms)-2-back

 

4.05

3.38

2.79

703

722

860

 

3.92

3.18

2.56

724

764

975

 

3.93

3.68

2.99

715

750

837

Recognition memory

d (sensitivity)*

C (response bias)

Gamma (metamemory)

 

1.92

0.32

0.54

 

2.25

0.50

0.44

 

1.61

0.46

0.13

Free recall, number correct response

14.25 13.88 12.50

*Significant effect of dose condition

Study Author Conclusions

The only significant effect of dose was an impairment in episodic/long-term memory (recognition memory) performance at the highest dose (32/8 mg) relative to the two lower doses. Future studies incorporating larger sample sizes and non-drug controls, as well as directly comparing buprenorphine to methadone and LAAM are needed to further test the hypothesis of limited impairment with buprenorphine.

InpharmD Researcher Critique

The study primarily reflects patients with opioid dependency but not categorized as clinical opioid use disorder. 
References:

Mintzer MZ, Correia CJ, Strain EC. A dose-effect study of repeated administration of buprenorphine/naloxone on performance in opioid-dependent volunteers. Drug Alcohol Depend. 2004;74(2):205-209. doi:10.1016/j.drugalcdep.2003.12.008

 

Outcomes associated with once-daily versus multiple-daily dosing of buprenorphine/naloxone for opioid use disorder

Design

Retrospective chart review

N= 100

Objective

To evaluate whether once‐daily versus multiple‐daily dosing differentially impacts clinical outcomes to better guide clinicians in buprenorphine management for opioid use disorder (OUD)

Study Groups

Once-daily buprenorphine/naloxone (n= 50)

Multiple-daily buprenorphine/naloxone (n= 50)

Inclusion Criteria

Age ≥ 18 years, dispensed at least 28 consecutive days of buprenorphine/naloxone, had an ICD-10 code associated with diagnosis of OUD

Exclusion Criteria

Prescribed the buprenorphine monoproduct, had known naloxone or buprenorphine hypersensitivity, were pregnant, or who had documented hepatic impairment; prescribed buprenorphine for comorbid pain

Methods

Patients were categorized into two treatment cohorts, once‐daily buprenorphine/naloxone and multiple‐daily buprenorphine/naloxone. Multiple‐daily dosing was defined as twice, thrice, or four times daily dosing. If patients were prescribed both once‐daily and multiple-daily dosing regimens during the study time frame, they were assigned to the cohort of the first dosing regimen they were prescribed. Patients were reviewed from their first maintenance fill until treatment termination or end of the study period, with termination defined as change in treatment regimen from single to multiple dose (or vice versa), self-discharge from the program, incarceration, or death.

Duration

Treated between January 1, 2016, and December 31, 2018

Outcome Measures

Primary: proportion of negative opioid urine drug screens (UDS)

Secondary:  total number of opioid relapses per cohort, average number of relapses per patient, average time to first opioid relapse in weeks, treatment retention, use of other illicit or non‐prescribed substances, opioid overdose events, naloxone prescribing, concurrent substance use disorder (SUD) treatment engagement, and medication adherence

Baseline Characteristics

 

Once-daily (n= 50)

Multiple-daily (n= 50)

 

Age, years

46 43  

Female

12% 12%  

Race

Caucasian

African American

Asian

Native American

 

86%

6%

0

0

 

78%

12%

2%

4% 

 

Prior buprenorphine/naloxone treatment

60% 30%  

Buprenorphine/naloxone dose, mg

Mode starting dose

Mode final dose

Mean number of prescription fills

 

8/2

8/2

10.58

 

16/4

32/8

12.35

 

Results

Endpoint

Once-daily (n= 50)

Multiple-daily (n= 50)

p-Value

Mean negative UDS

84% 74% 0.034 

Total relapses

Mean/patient

43/488

0.68 ± 1.3 

141/540

2.16 ± 2.16 

< 0.001 

< 0.001

Time to first relapse, weeks

14.5 ± 15.5 11.3 ± 44.36 0.75

Medication adherence

0.75 0.75 1

Treatment retention

33 (66%) 26 (52%) 0.155

Other illicit substances

Methamphetamine

Benzodiazepines

Barbiturates

Cocaine

Cannabis

 

7 (14%)

5 (10%)

1 (2%)

2 (4%)

34 (68%)

 

19 (38%)

10 (20%)

1 (2%)

4 (8%)

35 (70%)

 

0.005

0.374

1

0.4

0.829

Opioid overdose events

1 (2%) 2 (4%) 0.503

Naloxone prescribing

14 (28%) 4 (8%) 0.023

SUD treatment engagement

11 (22%) 14 (28%) 0.648

aTotal number of positive UDSs + self‐reported relapses/total UDSs in cohort.

bDays supply/number of days enrolled in treatment.

Adverse Events

N/A

Study Author Conclusions

This study found patients prescribed once‐daily buprenorphine/naloxone dosing had a significantly greater number of negative UDSs than those prescribed multiple‐daily dosing buprenorphine/naloxone. Additionally, once‐daily dosing was associated with fewer opioid relapses compared with multiple‐daily dosing. Larger, prospective studies are recommended to replicate these results and to better clarify the impact of total daily dosing on OUD treatment outcomes.

InpharmD Researcher Critique

Significant dose disparities were reported between the two cohorts, with a starting Suboxone dose of 8/2 mg in the once-daily dose cohort and starting dose of 16/4 mg in the multiple-daily dose cohort, but with doses ultimately ranging up to 32/8 mg in the multiple-dose cohort. This study was conducted within a Veterans Affairs Health Care System with a small sample size primarily consisting of Caucasian males, limiting external validity. The retrospective design means results are reliant on the accuracy of documented data. 



References:

Allen SM, Nichols TA, Fawcett J, Lin S. Outcomes associated with once-daily versus multiple-daily dosing of buprenorphine/naloxone for opioid use disorder. Am J Addict. 2022;31(3):173-179. doi:10.1111/ajad.13267

 

Effects of buprenorphine/naloxone in opioid-dependent humans

Design

Randomized, double-blind study

N= 8

Objective

To assess and compare the effects of intramuscular (IM) versus sublingual (SL) buprenorphine/naloxone in opioid-dependent volunteers

Study Groups

Study patients (N= 8)

Inclusion Criteria

Age 18 to 55 years, diagnosis of current opioid dependence, eligible for opioid agonist treatment

Exclusion Criteria

Pregnancy, significant medical or non-substance use psychiatric illness

Methods

Patients were recruited primarily via newspaper advertisements to enroll into the study. Two patients were initially treated as a pilot safety subject, tested in a non-randomized escalating dose order. As the two patients tolerated all doses, the remaining 8 were officially enrolled. Volunteers were maintained on 40 mg of choral hydromorphone per day while housed in a residential research ward. Patients were tested with both intramuscular and sublingual buprenorphine/naloxone 1/0.25, 2/0.5, 4/1, 8/2, 16/4 mg. Test sessions were twice per week.

While the primary objective was to compare intramuscular and sublingual formulations, the purpose of this table will primarily present the outcomes in 8/2 and 16/4 sublingual tablets

Duration

10 weeks

Outcome Measures

Subjective and observer-rated measures of different indices

Visual analog scale (100-point scale of high, drug effects, good effects, bad effects, liking, and sick)

Adjective rating questionnaire (0-4, with 4 being extremely)

Baseline Characteristics

 

Study patients (N= 8)

 

Age, years

36 (27 to 45)  

Female

2  
African-american

8

 
Duration of illicit opioid use, years

8.5 (4 to 14)

 

Results

Endpoint

8/2 mg

16/4 mg

Visual analog scale, subjective measure

High

Drug effects

Good effects

Bad effects

Liking

Sick

 

13.3

14.4

14.0

0.3

14.4

0.3

 

14.5

13.0

13.6

0

14.5

0.9

Adjective rating scales, subjective measure

Agonist

Withdrawal

 

14.0

1.5

 

14.5

1.6

Adjective rating scale, observer-rated measures

Agonist

Withdrawal

Withdrawl signs score

 

13.4

1.0

2.8

 

13.8

1.3

2.5

Study Author Conclusions

Intramuscular injection of buprenorphine/naloxone precipitates withdrawal in opioid dependent persons; therefore, the combination has a low abuse potential by the injection route in this population. Sublingual buprenorphine/naloxone by tablet is well tolerated in opioid dependent subjects, and shows neither adverse effects (i.e., precipitated withdrawal) nor a high abuse potential (i.e., opioid agonist effects).

InpharmD Researcher Critique

The primary purpose of the study was to compare intramuscular injection with sublingual. However, comparisons between the 8/2 and 16/4 mg doses are the focus of this table. Due to small sample size and volunteer nature of the study, the extrapolation of results are limited.



References:

Stoller KB, Bigelow GE, Walsh SL, Strain EC. Effects of buprenorphine/naloxone in opioid-dependent humans. Psychopharmacology (Berl). 2001;154(3):230-242. doi:10.1007/s002130000637