What is the recommended dose of Sublocade (buprenorphine) for adults with moderate to severe opioid use disorder?

Sublocade Dosing for Opioid Use Disorder

For adults with moderate to severe opioid use disorder, Sublocade is administered as a subcutaneous injection starting with 300 mg monthly for the first two months, followed by a maintenance dose of either 100 mg or 300 mg monthly, after patients have been stabilized on 8-24 mg daily of transmucosal buprenorphine for at least 7 consecutive days. 1, 2

Pre-Treatment Requirements

Critical stabilization period: Patients must complete a minimum of 7 consecutive days on transmucosal (sublingual) buprenorphine at doses of 8-24 mg daily before initiating Sublocade. 1

Withdrawal status verification: Patients must demonstrate objective signs of mild to moderate opioid withdrawal before the first transmucosal buprenorphine dose to prevent precipitated withdrawal—never initiate in patients not actively withdrawing. 1

Standard Dosing Protocol

Initial Phase (Months 1-2)

• 300 mg subcutaneous injection monthly for the first two doses 2, 3
• Administered into the abdomen, though upper arm, thigh, or buttocks are acceptable alternative sites 4
• Target therapeutic buprenorphine plasma concentrations (≥2 ng/mL) are achieved from the first injection 3

Maintenance Phase (Month 3 onwards)

• 100 mg or 300 mg monthly based on clinical response and patient preference 2, 3
• The 300 mg maintenance dose is appropriate for patients requiring higher opioid blockade 2
• The 100 mg maintenance dose may be sufficient for stabilized patients with good treatment response 2

Injection Site Options

All four sites provide comparable therapeutic exposure: 4

• Abdomen (FDA-approved primary site)
• Upper arm (39% higher peak concentration but clinically insignificant)
• Thigh (52% higher peak concentration but clinically insignificant)
• Buttocks (comparable to abdomen)

The higher peak concentrations with arm and thigh injections were not associated with increased adverse events. 4

Pharmacokinetic Advantages

• Sustained therapeutic levels: Buprenorphine concentrations remain at or above 2 ng/mL throughout the monthly dosing interval 3
• Dosing flexibility: A 2-week delay in scheduled dosing does not significantly impact efficacy due to slow decline in plasma levels 3
• Gradual offset: After discontinuation, buprenorphine concentrations decrease slowly, minimizing withdrawal risk 3

Clinical Efficacy Data

In the 12-month open-label extension study: 2

• 61.5% of rollover participants maintained abstinence after 12 months
• 75.8% of de novo participants achieved abstinence after 12 months
• Retention rates were approximately 50% at 12 months for both groups
• Incidence of adverse events decreased in the second 6 months compared to the first 6 months

A superiority trial demonstrated that monthly Sublocade resulted in 123.43 days of opioid abstinence versus 104.37 days with daily standard-of-care treatment over 24 weeks (adjusted IRR 1.18,95% CI 1.05-1.33; p=0.004). 5

Safety Profile

Common adverse events: 2

• Injection-site reactions occur in 13.2% of patients, mostly mild to moderate
• 66.8% of patients report at least one treatment-emergent adverse event
• Serious adverse events occur in 7.0% of patients, none related to study treatment

Critical contraindications: 1

• Avoid QT-prolonging agents due to risk of cardiac conduction abnormalities
• Monitor for serotonin syndrome when combining with serotonergic medications
• Maximum transdermal buprenorphine dose should not exceed 20 μg/hour due to QT concerns 6

Special Population Considerations

Elderly or medically frail patients: Slower titration of transmucosal buprenorphine during the stabilization phase is recommended before initiating Sublocade. 6

Renal impairment: Buprenorphine undergoes primarily hepatic metabolism and fecal excretion, making it particularly appropriate for patients with renal dysfunction. 7

Patients with chronic pain: Consider dividing daily transmucosal buprenorphine doses into 8-hour intervals (e.g., 16 mg daily as 6 mg/6 mg/4 mg) during stabilization before transitioning to Sublocade. 1

Common Pitfalls to Avoid

• Never skip the stabilization period: Attempting to initiate Sublocade without 7 days of transmucosal buprenorphine stabilization increases treatment failure risk 1
• Never initiate in non-withdrawing patients: Buprenorphine's high receptor affinity will displace full agonist opioids, causing severe precipitated withdrawal 1
• Do not discontinue abruptly: If stopping Sublocade, recognize that buprenorphine levels decline gradually over weeks, providing a built-in taper 3