What is the loading dose of Sublocade (buprenorphine)?

Sublocade Loading Dose for Opioid Use Disorder

The loading dose of Sublocade (extended-release buprenorphine) is 300 mg administered subcutaneously monthly for the first two months, followed by maintenance dosing of either 100 mg or 300 mg monthly based on clinical response. 1, 2

Induction Protocol

Patients must be transitioned from sublingual buprenorphine before initiating Sublocade - direct induction with the extended-release formulation is not recommended. 1

Pre-Sublocade Requirements

• Stabilize patients on sublingual buprenorphine/naloxone (typically 8-24 mg daily) for at least 7 days before the first Sublocade injection. 3, 4
• For patients dependent on short-acting opioids (heroin), initiate sublingual buprenorphine only when objective signs of moderate withdrawal appear, not less than 4 hours after last opioid use. 3
• For patients on methadone or long-acting opioids, wait at least 24 hours after last use and until clear withdrawal signs emerge before starting sublingual buprenorphine. 3

Sublingual Induction Dosing

• Day 1: 8 mg sublingual buprenorphine 3
• Day 2: 16 mg sublingual buprenorphine 3
• Days 3-7: Continue 16 mg daily (or adjust between 4-24 mg based on withdrawal suppression) 3

Sublocade Dosing Schedule

Loading Phase

• Month 1: 300 mg subcutaneous injection 1, 2, 4
• Month 2: 300 mg subcutaneous injection 1, 2, 4

Maintenance Phase (Month 3 onward)

• 100 mg or 300 mg monthly based on clinical response and patient preference 1, 2
• The 300 mg maintenance dose is selected for patients requiring higher opioid blockade or those with inadequate response to 100 mg. 2, 4

Clinical Efficacy of Loading Regimen

This two-dose 300 mg loading regimen provides potent and durable blockade of exogenous opioid effects. 4

• After two 300 mg injections, Sublocade blocks the subjective effects and reinforcing efficacy of hydromorphone (18 mg IM) for at least 12 weeks. 4
• Patients receiving this loading regimen demonstrate significantly greater opioid abstinence (mean 123 days over 24 weeks) compared to daily sublingual maintenance (mean 104 days). 2

Critical Safety Considerations

Common adverse events during loading include injection site pain (mild-moderate, rapidly resolving) occurring in approximately 81% of patients. 2

• Serious adverse events are uncommon (7% in clinical trials) and none were attributed to the medication itself. 2
• Do not administer Sublocade to patients not already receiving sublingual buprenorphine - this can precipitate severe withdrawal due to buprenorphine's high mu-receptor affinity displacing other opioids. 5, 6
• Patients on methadone >30 mg are at higher risk for precipitated withdrawal during the sublingual induction phase. 3

Pitfalls to Avoid

• Never skip the sublingual stabilization period - attempting direct induction with Sublocade risks severe precipitated withdrawal. 3, 1
• Avoid mixed agonist-antagonist opioids (pentazocine, nalbuphine, butorphanol) during treatment as they will precipitate withdrawal by displacing buprenorphine from mu-receptors. 5
• Monitor for respiratory depression if combining with benzodiazepines or other CNS depressants - this represents a pharmacodynamic rather than pharmacokinetic interaction. 6
• Patients requiring acute pain management while on Sublocade may need higher doses of full agonist opioids due to competitive receptor binding, with careful monitoring for respiratory depression. 5, 7