What is Sublocade?
Sublocade is an extended-release subcutaneous buprenorphine injection administered monthly for the treatment of moderate to severe opioid use disorder (OUD) in patients who have already initiated treatment with transmucosal buprenorphine or are currently being treated with buprenorphine. 1
Formulation and Administration
Sublocade contains buprenorphine in a depot formulation that is injected subcutaneously (under the skin) into the abdomen, thigh, buttock, or back of the upper arm by a certified healthcare provider 1. After injection, the liquid medication transforms into a solid depot that may be visible or palpable as a small bump under the skin for several weeks, gradually dissolving over time 1.
Dosing Schedule
- Initial dosing: Two monthly injections of 300 mg (with at least 26 days between doses)
- Maintenance dosing: Monthly injections of either 300 mg or 100 mg, depending on clinical response 2
- Patients not currently on buprenorphine must receive a test dose of transmucosal buprenorphine first to confirm tolerability before switching to Sublocade 1
Clinical Use and Requirements
Sublocade must be used as part of a complete treatment program that includes counseling and psychosocial support 1. The medication is only available through the SUBLOCADE REMS Program due to serious risks of harm or death from intravenous self-injection, and can only be administered by certified healthcare providers—it is not available in retail pharmacies 1.
Regulatory Changes
As of early 2023, special training and DEA "X-waiver" are no longer required to prescribe buprenorphine formulations for OUD—only standard DEA registration is needed 3. There are no longer DEA limits or patient caps on the number of patients a prescriber may treat 3.
Efficacy and Safety Profile
Clinical trials demonstrate sustained efficacy over 12 months of treatment 2:
- After 12 months, 61.5% of rollover participants and 75.8% of de novo participants achieved abstinence
- Retention rates at 12 months were approximately 50% for both groups
- Treatment-emergent adverse events (TEAEs) were lower in the second 6 months compared to the first 6 months of treatment
- Injection site reactions occurred in 13.2% of participants and were mostly mild to moderate 2
Special Populations
Pregnancy
Recent evidence supports the use of Sublocade during pregnancy 4. Case studies and postmarketing surveillance data (>300 pregnancies reported) show:
- Full-term deliveries with normal birthweight
- No fetal anomalies
- No medication required for neonatal opioid withdrawal syndrome in reported cases
- Safety profile consistent with established buprenorphine data 4
For pregnant patients with OUD, continue Sublocade unless clinically contraindicated 3. The medication should be considered as part of evidence-based practice prioritizing treatment access, patient stability, and patient choice during the perinatal period 4.
Cancer Pain and Chronic Pain
While Sublocade is specifically indicated for OUD, buprenorphine formulations are increasingly recognized for pain management 3. For patients with OUD admitted on buprenorphine, continue the medication unless clinically contraindicated, as stopping therapy leads to 50% relapse into OUD 3.
Critical Safety Warnings
Life-threatening respiratory depression can occur when Sublocade is combined with:
- Other opioid medications
- Benzodiazepines
- Gabapentinoids (gabapentin or pregabalin)
- Alcohol
- Other central nervous system depressants 1
Important Patient Considerations
- Detectable buprenorphine levels may persist for several months after stopping treatment 1
- Patients should not attempt to remove the depot or rub/massage the injection site 1
- Emergency personnel must be informed that the patient is physically dependent on opioids and being treated with Sublocade 1
- Naloxone should be available for overdose reversal 1
Advantages Over Sublingual Formulations
Sublocade addresses several limitations of daily sublingual buprenorphine 5, 6:
- Eliminates daily dosing requirements and associated adherence challenges
- Reduces risks of diversion and misuse
- Provides consistent medication levels without daily fluctuations
- Particularly beneficial for stabilized patients bothered by daily intake requirements
- Useful in high-risk situations such as hospital discharge or prison release 5
The medication represents a significant advancement in OUD treatment by providing a long-acting option that maintains the established safety and efficacy profile of buprenorphine while improving convenience and reducing treatment barriers 2, 6.