Sublocade®

Sublocade® contains buprenorphine encased in a gel-like substance called Atrigel.

Buprenorphine for opioid use disorder works as a maintenance treatment with a long duration of action, with the added benefit of providing only partial mu-opioid receptor agonism along with high receptor affinity. In pharmacology, partial agonists like buprenorphine are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist like methadone.  These neurophysiological properties make buprenorphine attractive as a long-term maintenance treatment of opioid use disorder. Buprenorphine’s high receptor affinity protects against both overdose and reinforcing effects in the case of use with full agonist opioids. At the same time, the only partial agonism at the mu (μ)-opioid receptor prevents overdose and intoxication related to buprenorphine itself.  Sublocade® is an alternative to other forms of opioid addiction treatment. It is used to treat adult patients that have a moderate to severe opioid use disorder (OUD) and are currently taking a maintenance dose of 8-24 mg/day of a transmucosal buprenorphine-containing product (Suboxone®) for at least 7 days.  Both Sublocade® and Suboxone® contain buprenorphine.  This molecule’s benefit in opioid addiction treatment (OAT) stems from its slow reversible engagement from the mu (µ)-opioid receptors in the brain, prolonging its activity at the receptor, thus leading to reduced opioid withdrawal symptoms.

Following induction and maintenance with Suboxone® at a dose of 8-24 mg/day for at least 7 days, patients can be transitioned to Sublocade® starting with 300 mg/month for 2 months and then stepped down to the 100 mg/month formulation. 

In clinical trials, the 300 mg/month maintenance dose did not provide additional efficacy as compared to the 100 mg/month dose and was associated with a higher incidence of adverse events. Sublocade® has a long half-life and should only be administered monthly. A minimum of 26 days is required between consecutive doses.

Sublocade® contains buprenorphine. It is injected by a certified treatment provider (nurse or physician) as a liquid and, once inside the body, turns to a solid gel called a depot (dee-poh).  The injection site alternates monthly around the navel.

Transient pain and bleeding can occur immediately after injection but may be mitigated with the use of ice-packs prior to injection.  Skin infection may occur hours to days later.  An allergic reaction is possible and is manifested by a rash, hives or more seriously, swelling of the lips, tongue with associated difficulties in breathing and swallowing.  The latter can lead to a loss of consciousness. 

Emergency care should be sought immediately by calling -911 in Ontario.

Possible side-effects include constipation, nausea, vomiting, headache, fatigue, insomnia, liver enzyme increase, jaundice (yellow skin and white of the eyes, light-coloured stools and dark urine), injection site pain and itch.  

Discuss your medical history with your treatment provider.

You should talk to your prescriber and pharmacist prior to starting Sublocade® to ensure they are aware of all medications and herbal medicines you are taking. Severe reactions are possible when buprenorphine is combined with other medications that act on serotonin, such as tricyclic antidepressants and serotonin reuptake inhibitors; medications used to treat depression. These combinations must be avoided. Symptoms of a reaction may include muscle rigidity and spasms, difficulty moving, changes in mental state including delirium and agitation. Coma and death are possible. Sublocade should not be used if you are currently taking or have taken a MAO inhibitor (e.g., phenelzine, tranylcypromine) within the past 14 days.

Supplements, caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

Before starting SUBLOCADE®, tell your healthcare provider about all of your medical conditions, including if you have:

• trouble breathing or lung problems
• a curve in your spine that affects your breathing
• Addison’s disease
• an enlarged prostate gland (men)
• problems urinating
• liver, kidney, or gallbladder problems
• alcoholism
• a head injury or brain problem
• mental health problems
• adrenal gland or thyroid gland problems

This medication should not be used during pregnancy unless the benefits outweigh the risks. Using this medication during the last three months of pregnancy can harm the developing baby and cause the baby to experience withdrawal symptoms after birth. If you become pregnant while taking this medication, contact your doctor immediately.

• Opioid-dependent women on buprenorphine maintenance therapy may require additional analgesia during labor. If you receive SUBLOCADE® while pregnant, your baby may have symptoms of opioid withdrawal at birth that could be life-threatening if not recognized and treated.
• Breastfeeding or plan to breastfeed? Sublocade® can pass into your breast milk and harm your baby. Talk with your healthcare provider about the best way to feed your baby during treatment with Sublocade®. Monitor your baby for increased drowsiness and breathing problems.

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The answer is yes, particularly if instructions are not followed and other medications or drugs are used.

Sublocade® may cause serious and life‐threatening breathing problems. Get emergency help right away if you:

• feel faint
• feel dizzy
• are confused
• feel sleepy or uncoordinated
• have blurred vision
• have slurred speech
• are breathing slower than normal
• cannot think well or clearly

Do not take certain medicines during treatment with Sublocade®. Taking other opioid medicines, benzodiazepines, alcohol, or other central nervous system depressants (including street drugs) while on Sublocade® can cause severe drowsiness, decreased awareness, breathing problems, coma, and death.

• In an emergency, have family members tell emergency department staff that you are physically dependent on an opioid and are being treated with Sublocade® .
• You may have detectable levels of Sublocade® in your body for a long period after stopping treatment with Sublocade®.

Death has been reported in those who are not opioid dependent who received buprenorphine sublingually.

In Ontario, call -911 in an emergency.

Sublocade® is meant to be administered roughly every 26 days and should NOT be given earlier. Clinical simulations have shown that occasional delays in dosing up to 2 weeks would not have any clinically significant impact on treatment effect. Thus, while monthly dosing is needed for optimal exposure, the slow-release characteristics of the ATRIGEL delivery system allow coverage of the patient if he/she occasionally does not have an injection at the scheduled time.

Sublocade® is designed to deliver buprenorphine at a controlled rate over a month span. As shown in previous studies with Suboxone®, at least 70% brain mu (µ)-opioid receptor occupancy by buprenorphine is required to block the subjective effects (opioid blockade) of full agonist-induced responses.  Recent studies with Sublocade® using positron emission tomography scans (PET) of the brain have revealed binding in excess of 75-92% to opioid mu (µ)-receptors with buprenorphine from Sublocade® in currently used dose formulations.

Each dose of Sublocade® is provided as a sterile pre-filled syringe which is then injected subcutaneously in the stomach area, just under the skin.  A small bump or “depot” will form upon injection of Sublocade® and will likely dissipate after several weeks as the buprenorphine is released via diffusion from, and the biodegradation of, the mass.  If injected into a vein, Sublocade® can cause severe harm or death.  The person injecting the substance must be a certified health care professional (RPN/RN/NP or MD) with training in Sublocade® injections.

Clinic visits with the doctor are fully paid for if you have a valid OHIP card.

In general, costs of medications may be covered under government plans such as Ontario Drug Benefits (ODB) or Non-Insured Health Benefits (NHIB), a private medical plan, or Trillium Drug Plan (TDP). Your pharmacist may try to assist you if you are having difficulty with payment.

Set up an intake appointment by contacting us by telephone or on-line as shown below. You can also drop by a RTR clinic and present your OHIP card. An initial appointment will be scheduled as soon as possible.

To become a patient you must:

• Be 18 years of age or older
• Have valid photo identification,including a valid OHIP number
• Opioid use disorder evidence must be present as per DSM-V criteria
• Agree to follow program policies & procedures
• Give full consent prior to starting medication assisted treatment (to be agreed upon and signed by the patient)
• A urine sample will be obtained periodically to assess for recent drug use