Sublocade: Uses, Side Effects and Dosage

Serious Warnings and Precautions

• SUBLOCADE cannot be handed to you directly.

• SUBLOCADE is ONLY to be injected:

  • by a healthcare professional
  • just under the skin (subcutaneously) in your stomach (abdomen), thigh, buttock, or back of the upper arm. It is NOT to be injected in any other way.

SUBLOCADE is injected as a liquid. After the injection it forms a solid mass (called a depot). It must not be given to you through a vein (intravenously) or into a muscle (intramuscularly) or a layer of the skin called the dermis (intradermally). Serious harm or death could result if it is given to you through a vein.

• Even if you are given SUBLOCADE as prescribed you are at risk for opioid addiction, abuse, and misuse. This can lead to overdose and death.
• Life-threatening breathing problems can happen while you are on SUBLOCADE, especially if not taken as directed. Babies are at risk of life-threatening breathing problems if their mothers take opioids while pregnant or nursing.

• If you are pregnant, planning on becoming pregnant, or are in labour or giving birth, your healthcare professional will decide if SUBLOCADE is right for you. Opioids can be transferred to your baby while still in the womb and may harm them. Your healthcare professional may consider other treatments if you are pregnant.

  If you are a woman who could become pregnant, your healthcare professional will ask you to use a highly effective birth control method during your treatment with SUBLOCADE. If you become pregnant during your treatment with SUBLOCADE, it is important that you tell your healthcare professional right away. If you suddenly stop your treatment with SUBLOCADE, it can cause a miscarriage or a still-birth. Your healthcare professional will monitor and guide you on how to stop your treatment with SUBLOCADE, if appropriate. This may help avoid serious harm to your unborn baby.

• If you were treated with SUBLOCADE at any time while you were pregnant, your baby can suffer life threatening withdrawal symptoms after birth. This can occur in the days after birth and for up to 4 weeks after delivery. Seek immediate help for your baby if it has any of the following symptoms:

  • has changes in their breathing (such as weak, difficult or fast breathing)
  • is not feeding well
  • is unusually difficult to comfort

Serious Warnings and Precautions

• has tremors (shakiness) or stiffness
• has increased sneezing, yawning, vomiting, fever, stools or diarrhea

• While you are on SUBLOCADE, alcohol should be avoided. Drinking alcohol while you are on SUBLOCADE may result in you feeling stronger effects from the drug than usual such as increased drowsiness, reduced breathing and loss of consciousness. This can possibly lead to an accidental overdose that can be fatal.

• Taking other opioids, benzodiazepines, alcohol, or other nervous system depressants (including street drugs) during your treatment with SUBLOCADE can cause severe drowsiness, decreased awareness, breathing problems, coma, and death.
• SUBLOCADE can cause problems with your heart rhythm called QTc prolongation. You may have no symptoms, or you may have dizziness, feeling like your heart has skipped or added a beat, fainting or seizures. If these symptoms continue, they can lead to sudden death. You may be more at risk if you have or have had:
• a heart attack;
• congestive heart failure;
• an irregular heartbeat or heart rhythm;
• a blockage in one or more of your arteries that affects blood flow to your heart;
• an abnormally rapid heart rate;
• heart palpitations (feeling like your heart has skipped a beat or added an extra beat);
• a family history of sudden cardiac death at less than 50 years of age;
• problems of electrocardiogram (ECG) abnormality called “Long QT syndrome”;
• diabetes;
• imbalances in the electrolytes in your body (potassium, magnesium and calcium).

What is SUBLOCADE used for?

SUBLOCADE is:

• used to treat patients (18 years of age and older) who have moderate to severe opioid use disorder.
• a drug treatment plan that should be used along with counselling and psychosocial support.

How does SUBLOCADE work?

SUBLOCADE contains buprenorphine. It works in a similar way as other opioid drugs that are used in the treatment of pain. When you stop taking opioid drugs, you can experience withdrawal. SUBLOCADE helps control the symptoms you feel when you are in withdrawal.

What are the ingredients in SUBLOCADE?

Medicinal ingredients: Buprenorphine

Non-medicinal ingredients: N-methyl-2-pyrrolidone (NMP) and 50:50 Poly(DL-lactide-co-glycolide) (PLGH).

SUBLOCADE comes in the following dosage forms:

Extended-release solution for injection available in pre-filled syringes: 100 mg/0.5 mL and 300 mg/1.5 mL.

Do not use SUBLOCADE if:

• your healthcare professional did not prescribe it for you.
• you are allergic to buprenorphine or any of the ingredients in SUBLOCADE, including Indivior’s proprietary delivery system.
• you have severe asthma, trouble breathing, or other lung problems.
• you have serious problems with your liver.
• you suffer from alcoholism or alcohol withdrawal.
• you have any heart problems.
• you have bowel blockage or narrowing of the stomach or intestines.
• you have a condition where the bowel does not work properly (ileus), or you have severe pain in your abdomen.
• you have increased pressure in your skull or a head injury.
• you suffer from convulsive or seizure disorder.
• you are taking or have taken within the past 2 weeks a Monoamine Oxidase inhibitor (MAOI) (such as phenelzine sulphate, tranylcypromine sulphate, moclobemide or selegiline).
• you recently had, or you are going to have planned surgery.
• you have been told that you have low levels of potassium, magnesium, or calcium in the blood.

To help avoid side effects and ensure proper use, talk to your healthcare professional before you receive SUBLOCADE. Talk about any health conditions or problems you may have, including if you:

• have a history of illicit or prescription drug or alcohol abuse.
• have problems with your thyroid, adrenal or prostate gland.
• have asthma, other breathing problems, or lung problems.
• have problems with your liver.
• have problems with your kidneys.
• have a history or a family history of heart problems.
• have circulatory problems (e.g., body does not get enough oxygen and nutrients to function properly due to lack of blood flow).
• have low or decrease in blood pressure.
• have past or current depression.
• suffer from chronic or severe constipation.
• have problems with your gallbladder or pancreas.
• have difficulty urinating.
• have a curve in your spine that affects your breathing.
• have severe mental problems or hallucinations (seeing or hearing things that are not there).
• suffer from migraines.
• have a condition that causes weakness or frailty.
• are pregnant or planning to become pregnant or are in labour or giving birth.

Other warnings you should know about:

SUBLOCADE can cause the following serious side effects:

• Allergic reaction: Serious allergic reactions (e.g. swelling of lips and throat, difficulty breathing or swallowing, skin rashes, hives, itchy skin) have been reported in patients receiving therapy with buprenorphine. Seek medical attention immediately.

• Disorder of the adrenal gland: You may develop a disorder of the adrenal gland called adrenal insufficiency. This means that your adrenal gland is not making enough of certain hormones. You may experience symptoms such as:

  • nausea, vomiting
  • feeling tired, weak or dizzy
  • decreased appetite

You may be more likely to have problems with your adrenal gland if you have been taking opioids for longer than one month. Your healthcare professional may do tests, give you another medication, and take you off SUBLOCADE, if this happens

• Serotonin toxicity (also known as serotonin syndrome): SUBLOCADE can cause serotonin toxicity, a rare but potentially life-threatening condition. It can cause serious changes in how your brain, muscles and digestive system work. You may develop serotonin toxicity if you take certain antidepressants or migraine medications during your treatment with SUBLOCADE. Serotonin toxicity symptoms include:

  • fever, sweating, shivering, diarrhea, nausea, vomiting;
  • muscle shakes, jerks, twitches or stiffness, overactive reflexes, loss of coordination;
  • fast heartbeat, changes in blood pressure;
  • confusion, agitation, restlessness, hallucinations, mood changes, unconsciousness and coma.

See the Serious side effects and what to do about them table for more information on these and other serious side effects.

Opioid dependence and addiction: There are important differences between physical dependence and addiction. It is important that you talk to your healthcare professional if you have questions or concerns about abuse, addiction or physical dependence.

Breast-feeding: SUBLOCADE is not recommended while breast-feeding. Opioids can be transferred to your baby through breast milk. SUBLOCADE can then cause life-threatening breathing problems in your nursing infant. Your healthcare professional will determine if the benefits of SUBLOCADE outweigh the risks to your nursing infant.

Treatment of short-term pain: When you are on SUBLOCADE treatment, there may be times when you need to take other medicines, including other opioids, to treat short term pain. Since SUBLOCADE may make it difficult to get full pain relief from other opioids, you should tell your healthcare professional that you are on SUBLOCADE if they are treating you for pain.

Sexual function and reproduction: Long-term use of opioids may lead to a decrease in sex hormone levels. It may also lead to low libido (desire to have sex), erectile dysfunction or being infertile.

Driving and using machines: SUBLOCADE can cause you to feel:

• drowsy,
• dizzy, or
• light-headed.

This may happen more often in the first few days after your injection. Before you do tasks which may require special attention, you should wait until you know how you react to SUBLOCADE.

Testing and check-ups: Your healthcare professional may do blood tests before you start SUBLOCADE and during your treatment to check:

• that your liver is working properly. This includes checking if you have a hepatitis infection caused by a virus.

Tell your healthcare professional about all the medicines you take, including any drugs, vitamins, minerals, natural supplements or alternative medicines.

Serious Drug Interactions

Serious drug interactions with SUBLOCADE include:

• benzodiazepines used to help you sleep or that help reduce anxiety.

• central nervous system (CNS) depressants used to slow down the nervous system. These can include:

  • other opioids and opioid antagonists used to relieve pain (e.g., methadone, naltrexone, tramadol, tapentadol);
  • hypnotics used to help with sleeping;
  • antidepressants used for depression and mood disorders (e.g., fluoxetine, citalopram; tricyclic antidepressants such as amitriptyline, imipramine, maprotiline, mirtazapine, trazodone; serotonin norepinephrine re-uptake inhibitors [SNRIs]; and selective serotonin re-uptake inhibitors [SSRIs] such as St. John’s Wort);
  • anxiolytics, tranquilizers, and phenothiazines used to treat mental or emotional disorders;
  • muscle relaxants used to treat muscle spasms and back pain (e.g., baclofen);
  • pregabalin, used to treat nerve pain;
  • gabapentin, used to prevent and control seizures in the treatment of epilepsy;
  • general anaesthetics used during surgery;
  • antipsychotics and neuroleptics used to treat mental health disorders (e.g., chlorpromazine, pimozide, haloperidol, droperidol, ziprasidone, and risperidone);
  • antihistamines used to treat allergies;
  • antiemetics used to prevent nausea or vomiting (e.g., domperidone, ondansetron);
  • sedatives which may enhance the drowsiness;
  • beta blockers used to lower blood pressure;
  • alcohol. This includes prescription and non-prescription medications that contain alcohol. Do not drink alcohol while you are on SUBLOCADE. It can lead to drowsiness, usually slow or weak breathing, serious side effects, or a fatal overdose.
• monoamine oxidase inhibitors (MAOIs) used to treat depression. Do not take SUBLOCADE with MAOIs or if you have taken MAOIs in the last 14 days.

The following may also interact with SUBLOCADE:

• medicines used to treat epilepsy (such as carbamazepine, phenytoin and phenobarbital)
• anticoagulants and other medicines used to thin the blood and/or prevent or treat blood clots (such as warfarin)
• medicines used to treat certain viral infections (such as ritonavir)
• medicines used to treat fungal infections (such as ketoconazole, fluconazole, voriconazole, amphotericin B)
• medicines used to treat bacterial infections (such as erythromycin, clarithromycin, azithromycin, moxifloxacin, levofloxacin, ciprofloxacin, pentamidine, rifampin)
• medicines used to treat malaria (such as quinine, chloroquine)
• diuretics (used to treat high blood pressure - also known as “water pills”)
• some heart medication (such as quinidine, procainamide, disopyramide, amiodarone, sotalol, ibutilide, dronedarone, flecainide, propafenone, ivabradine)
• medicines used to treat cancer (such as sunitinib, nilotinib, ceritinib, vandetanib, arsenic trioxide, vorinostat)
• medicines used to treat asthma or other lung diseases (such as salmeterol, formoterol)
• grapefruit juice
• medicines used to treat migraines (such as triptans)
• medicines used to suppress the immune system (such as tacrolimus)
• medicines used to treat inflammation (such as corticosteroids)
• medicines used to reduce the amount of stomach acid (such as proton pump inhibitors)
• laxatives
• enemas

How SUBLOCADE is given:

• Before you start treatment with SUBLOCADE, your healthcare professional will start you on at least one dose of a transmucosal buprenorphine-containing medicine. They will determine your dose and how long you will take the transmucosal buprenorphine-containing medicine. You will then be transitioned to SUBLOCADE.
• You can only get SUBLOCADE from a certified healthcare professional who has received instruction and training.

• SUBLOCADE will be injected by your healthcare professional:

  • once a month. The second injection may be injected as early as one week after your first injection, if recommended by your healthcare professional.
  • just under the skin of the stomach, thigh, buttock, or back of the upper arm area. It is NOT to be injected in any other way.

• SUBLOCADE is injected as a liquid. After the injection it forms a solid mass (called a depot). It must not be given to you through a vein, or into a muscle or a layer of the skin called the dermis. Serious harm or death could result if it is given to you through a vein.

  The depot may be seen or felt as a small bump under your skin at the injection site for several weeks. The depot will get smaller over time. Do NOT rub or massage the injection site and be aware of any restrictive clothing such as belts or waistbands, or sleeves that could cause irritation of the injection site.

• You should tell your family members that you are on SUBLOCADE to treat your opioid dependence.

Usual Dose:

You will be started on a SUBLOCADE dose of 300 mg. Depending on how you respond, your healthcare professional will give you your second dose of 300 mg as early as one week and up to one month after the first dose. You will then receive a maintenance dose of 100 mg or 300 mg per month, depending on your needs.

Stopping your treatment:

Discuss with your healthcare professional the best way to stop your treatment with SUBLOCADE to minimize withdrawal symptoms. Once you stop your SUBLOCADE treatment, your healthcare professional should monitor you for several months for the signs and symptoms of withdrawal. If you experience withdrawal, your healthcare professional may give you other medication to treat it.

Symptoms of withdrawal may include:

• body aches
• diarrhea
• goosebumps
• loss of appetite or nausea
• feeling nervous or restless
• runny nose
• sneezing
• tremors or shivering
• stomach cramps
• rapid heart rate
• having trouble sleeping
• an unusual increase in sweating
• an unexplained fever
• weakness
• yawning

By reducing or stopping your SUBLOCADE treatment, your body will become less used to opioids. If you start using opioids again, you may overdose if you use a dose you have used in the past. If you wish to restart SUBLOCADE treatment again, your doctor will determine the best dose to restart the treatment.

Overdose:

Signs of overdose with SUBLOCADE may include:

• unusually slow or weak breathing
• pinpoint pupils (pupils that are abnormally small under normal lighting conditions)
• dizziness
• confusion
• extreme drowsiness
• blue or purple lips
• slow heart rate
• nausea and vomiting
• low blood pressure
• toxic leukoencephalopathy (a brain disorder affecting the brain’s white matter)

If you think you, or a person you are caring for, have been given too much SUBLOCADE, contact a healthcare professional, hospital emergency department or regional poison control centre immediately, even if there are no symptoms.

Missed Dose:

If you miss a dose of SUBLOCADE, see your healthcare professional right away.

What are possible side effects from using SUBLOCADE?

These are not all the possible side effects you may feel during your SUBLOCADE treatment. If you experience any side effects not listed here, tell your healthcare professional.

Side effects may include:

• Pain, itching, redness, bruising or swelling where you got the shot
• Headache, drowsiness, or dizziness
• Fainting or feeling faint
• Nausea, vomiting, or a poor appetite
• Dry mouth
• Problems with vision
• Feeling weak or tired
• Itching
• Sweating
• Constipation. Talk with your healthcare professional about ways to prevent constipation when you start your SUBLOCADE treatment.
• Low sex drive, impotence (erectile dysfunction), infertility
• Trouble swallowing
• Chest pain

Serious side effects and what to do about them

If you have a troublesome symptom or side effect that is not listed here or becomes bad enough to interfere with your daily activities, tell your healthcare professional.

Reporting Side Effects

You can report any suspected side effects associated with the use of health products to Health Canada by:

• Visiting the Web page on Adverse Reaction Reporting (https://www.canada.ca/en/health-canada/services/drugs-health-products/medeffect-canada/adverse-reaction-reporting.html) for information on how to report online, by mail or by fax; or
• Calling toll-free at 1-866-234-2345.

NOTE: Contact your health professional if you need information about how to manage your side effects. The Canada Vigilance Program does not provide medical advice.

Storage:

SUBLOCADE will be stored by your healthcare professional.

If you want more information about SUBLOCADE:

• Talk to your healthcare professional.
• Find the full product monograph that is prepared for healthcare professionals and includes this Patient Medication Information by visiting the Health Canada website (https://www.canada.ca/en/health-canada/services/drugs-health-products/drug-products/drug-product-database.html); by e-mailing the manufacturer at PatientSafetyNA@indivior.com, or by calling 1-877-782-6966.

Last revised: DEC 02, 2025