Buprenorphine Extended-Release Injection (Sublocade)

Buprenorphine Extended-Release Injection (Tradename: Sublocade) is a long acting monthly subcutaneous injectable opioid for use in patients with moderate to severe opioid use disorder. It is the long-acting form of sublingual Suboxone.

• Adults who have agreed to be treated for opioid use disorder and have already undergone induction and stabilization on a buprenorphine-containing medication to manage opioid withdrawal, delivering the equivalent of 8-24 mg/day of buprenorphine for a minimum of 7 days.

• Sublocade should not be given to patients with pre-existing severe hepatic impairment. Patients who develop severe hepatic impairment should be discontinued from the medication and additional doses should not be administered.

• Sublocade has a long half-life and should only be administered monthly. A minimum of 26 days is required between consecutive doses.

• Patients must be initiated on suboxone (sublingual buprenorphine/naloxone) and stabilized on a dose of 8-24 mg per day for a minimum of 7 consecutive days prior to initiating Sublocade therapy.
• Efficacy of transitioning patients who are on sublingual Suboxone doses higher than 24 mg has not been established

• Initiation: inject 300mg subcutaneous every 4 weeks for the first 8 weeks (total of 2 doses)
  • There is NO need for overlap with sublingual suboxone therapy once the injection is started
• Maintenance: inject 100mg subcutaneously every 4 weeks
  • A minimum of 26 days is required between consecutive doses
  • Up to 42 days (6 weeks) may elapse from last injection date without the need to supplement with sublingual Suboxone (i.e. - there are an additional 2 weeks leeway where patients may be in mild withdrawal and there is no need to add sublingual Suboxone)
  • The maintenance dose may be increased to 300 mg/month only if the patient does not demonstrate satisfactory clinical response to and can tolerate the 100 mg dose (clinical trials have shown that 300 mg/month is associated with a higher incidence of adverse events and also discontinuations)

If discontinued, patients should be monitored for several months for signs and symptoms of opioids withdrawal and treated appropriately. After steady-state has been achieved (4-6 months), patients discontinuing Sublocade may have detectable plasma levels of buprenorphine for 12 months or longer. The correlation between plasma concentrations of buprenorphine and those detectable in urine is not known.

• Risk of tissue damage from intramuscular injection
• Adrenal insufficiency
• Cardiovascular: Orthostatic hypotension in ambulatory patients
• Elevation of cerebrospinal fluid pressure: Caution in patients with head injury, intracranial lesions, and other circumstances when cerebrospinal pressure may be increased
• Elevation of intracholedochal pressure: Administer with caution to patients with dysfunction of the biliary tract
• Serotonin syndrome: Use with caution in combination with other serotonergic drugs.

• Patients who are hypersensitive to Sublocade or any component of the Atrigel Delivery System
• Patients with severe respiratory insufficiency (e.g. - acute or severe bronchial asthma, chronic obstructive airway, status asthmaticus, acute respiratory depression and/or cor pulmonale)
• Severe hepatic impairment.
• Acute alcoholism or delirium tremens.
• Known or suspected mechanical gastrointestinal obstruction (e.g. - bowel obstruction or strictures) or any diseases/conditions that affect bowel transit (e.g. - ileus of any type)
• Suspected surgical abdomen (e.g. - acute appendicitis or pancreatitis)
• Severe central nervous system (CNS) depression, increased cerebrospinal or intracranial pressure, and head injury
• Concurrent monoamine oxidase (MOA) inhibitors use (or within 14 days of such therapy)
• Seizure disorders
• Congenital Long QT Syndrome or QT prolongation at baseline
  • Or those taking Class IA antiarrhythmic medications, Class IC antiarrhythmic medications, or Class III antiarrhythmic medications.
  • Particular care should be exercised when administering Sublocade to patients who are suspected to be at an increased risk of experiencing torsade de pointes during treatment with a QTc-prolonging drug
• Uncorrected hypokalemia, hypomagnesemia, or hypocalcemia

• Sublocade use should be avoided in women of childbearing age who are not on contraception or are judged not able to comply with contraceptive methods
• Nursing women, labour and delivery: SUBLOCADE is not recommended to be used in nursing women and during labour and delivery unless, in the judgement of the physician, the potential benefits outweigh the risks.

• Sublocade is stable at room temperature for 7 days from the time of dispensing, and it should be kept securely under supervision until time of administration.
• Allow the product to stay at room temperature for at least 15 minutes prior to administration to reduce discomfort for the patient.
• A small lump may form at the area of injection, this is Atrijel formation of the medication, and it will slowly reduce in size over the next 14-28 days as the medication is slowly released into the body
• Not all pharmacies carry the product and may need up to one week to complete the registration process
• Patients cannot pick up the medication themselves from the pharmacy. It must be picked up by a health care provider OR delivered from the pharmacy to the prescriber’s office/clinic for administration

• Patients should be provided with education prior to initiating therapy to ensure Sublocade aligns with their current recovery and wellness goals. Sublocade is intended for use in conjunction with psychosocial interventions
• In general, drug use for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, respiratory and/or cardiac function, concomitant disease or other drug therapies. If the decision is made to prescribe to individuals 65 years of age or older, patients should be monitored for signs and symptoms of toxicity or overdose
• Prolonged maternal use during pregnancy can result in a neonatal opioid withdrawal syndrome, which may be life threatening. Prolonged maternal use of opioids during pregnancy can also result in neonatal respiratory depression.