Sublocade

Sublocade (buprenorphine) is an extended-release injection used to treat adults with moderate to severe addiction to opioid drugs, to help reduce opioid cravings and withdrawal symptoms.

Sublocade is administered as a once-monthly injection under the skin (subcutaneously) after the initial doses. Sublocade is a partial opioid agonist.

Sublocade is FDA-approved to be used for moderate to severe addiction (dependence) to opioid drugs (prescription or illegal) in adults who have:

• started treatment with a single dose of a buprenorphine medicine in the form of a sublingual tablet or buccal film (transmucosal) followed by a one-hour observation period to confirm tolerability, or
• are already being treated with buprenorphine.

Sublocade is only available under the restricted SUBLOCADE REMS Program. You must be registered in the program and understand the risks and benefits of this medicine. It should be used as part of a complete treatment program that includes counseling and psychosocial support.

Sublocade is not for use as a pain medication.

This medication guide provides information about the Sublocade brand of buprenorphine injection. Buprenex is another brand of buprenorphine injection that is used to treat moderate to severe pain.

Sublocade is injected under the skin of your abdomen, thigh, buttock, or back of the upper arm. A healthcare provider will give you this injection.

After each injection, you may see or feel a small lump under your skin where the medicine was injected. This could last for several weeks but the lump should eventually get smaller. Avoid rubbing or massaging the skin where an injection was given and wearing tight clothing over the area.

Your doctor will determine how often you will receive Sublocade.

You will need frequent blood tests to check your liver function.

Sublocade is only part of a complete treatment program that may also include counseling and other types of addiction support. Tell your doctor if you feel that this medicine is not helping to improve your symptoms of addiction.

In an emergency, your family or caregivers should tell medical personnel that you are using this medicine. Make sure any follow-up doctor knows you use this medicine.

Do not stop using Sublocade suddenly, or you could have unpleasant symptoms (such as agitation, confusion, tingling or electric shock feelings).

Sublocade has a boxed warning for the risk of serious harm or death with intravenous administration and has a Sublocade risk evaluation and mitigation strategy (REMS).

• Sublocade must not be administered intravenously, as serious harm or death may occur.
• This medicine is available only through the restricted Sublocade REMS Program.
• Only healthcare providers and pharmacies certified in the program may order, dispense, or administer Sublocade, and they must comply with all applicable REMS requirements.

Other warnings

• Risk of addiction, misuse, and overdose: Buprenorphine can lead to addiction and abuse, misuse, overdose, or death. Your doctor should check your risk before starting treatment and continue to monitor you during treatment.
• Serious breathing problems: This medicine can cause severe or life-threatening breathing problems.
• Serious injection site reactions: Likelihood may be increased with inadvertent intramuscular or intradermal administration. Evaluate and treat as appropriate.
• Dangerous interactions with other substances: Using Sublocade with certain medicines, such as benzodiazepines, opioids, gabapentinoids (gabapentin or pregabalin) and other drugs that make you sleepy (including street drugs), or alcohol, can cause extreme drowsiness, severe breathing problems, coma, or death.
• Risk during pregnancy: Using opioids for a long time during pregnancy can cause withdrawal symptoms in a newborn after birth (neonatal opioid withdrawal syndrome). This can be serious and may be life-threatening if not treated quickly. Ensure that management by neonatology experts will be available at delivery.
• Increased pain sensitivity: In some people, opioid pain medicines can unexpectedly make pain worse or make the body more sensitive to pain. This is called opioid-induced hyperalgesia (OIH). If this happens, your doctor may lower your dose or switch you to a different pain medicine.
• Adrenal gland problems (adrenal insufficiency): This medicine can rarely affect your adrenal glands, which help your body make important hormones. If this happens, your doctor may treat you with steroid medicine.
• Risk of hepatitis or hepatic events: Monitor liver function tests prior to and during treatment
• Risk of opioid withdrawal with abrupt discontinuation: If treatment with Sublocade is discontinued, monitor patients for several months for withdrawal and treat appropriately.
• Risk of withdrawal in patients dependent on full agonist opioids: Before injecting Sublocade, verify that patients have tolerated transmucosal buprenorphine.

You should not be treated with this medicine if you are allergic to buprenorphine, or if you have severe asthma or breathing problems, or a stomach or bowel blockage (including paralytic ileus).

Tell your doctor if you also use stimulant medicine, opioid medicine, herbal products, or medicine for depression, mental illness, Parkinson's disease, migraine headaches, serious infections, or prevention of nausea and vomiting. An interaction with Sublocade could cause a serious condition called serotonin syndrome.

To make sure Sublocade is safe for you, tell your doctor if you have ever had:

• breathing problems, sleep apnea;
• a head injury or brain problem;
• alcoholism, mental illness;
• an allergy to latex;
• an enlarged prostate;
• urination problems;
• heart problems;
• an electrolyte imbalance (such as low blood levels of potassium or magnesium);
• curvature of the spine that affects breathing;
• Addison's disease (or any other adrenal gland problem);
• problems with your gallbladder or thyroid; or
• liver or kidney disease.
• tooth problems, including a history of cavities.

Buprenorphine may affect fertility in men or women. Pregnancy could be harder to achieve while either parent is using this medicine.

If you use buprenorphine during pregnancy, your baby could be born with life-threatening withdrawal symptoms and may need medical treatment for several weeks. Tell your doctor if you are pregnant or plan to become pregnant.

Tell your healthcare providers if you are breastfeeding or plan to breastfeed. Sublocade can pass into your breast milk and harm your baby. Talk to your healthcare provider about the best way to feed your baby during treatment with this medicine. Monitor your baby for increased drowsiness and breathing problems if you breastfeed during treatment with Sublocade.

Get emergency medical help if you have signs of an allergic reaction to Sublocade: hives, difficult breathing, swelling of your face, lips, tongue, or throat.

Opioid medicine can slow or stop your breathing, and death may occur. Get emergency medical help right away if you:

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

Ask your healthcare provider about medicines like naloxone or nalmefene that can be used in an emergency to reverse opioid overdose. If naloxone or nalmefene is given, you must call 911 or get emergency medical help right away to treat overdose or accidental use of an opioid

A person caring for you should give naloxone and/or seek emergency medical attention if you have slow breathing with long pauses, blue colored lips, or if you are hard to wake up.

Sublocade may cause other serious side effects.

Call your doctor at once if you have:

• weak or shallow breathing, breathing that stops;
• severe drowsiness or dizziness, loss of coordination;
• a light-headed feeling, like you might pass out;
• opioid withdrawal symptoms - shivering, goose bumps, increased sweating, feeling hot or cold, runny nose, watery eyes, diarrhea, vomiting;
• liver problems - loss of appetite, stomach pain (upper right side), tiredness, itching, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes); or
• decreased adrenal gland hormones - nausea, vomiting, stomach pain, loss of appetite, feeling tired or light-headed, muscle or joint pain, skin discoloration, craving salty foods.

Seek medical attention right away if you have symptoms of serotonin syndrome, such as: agitation, hallucinations, fever, sweating, shivering, fast heart rate, muscle stiffness, twitching, loss of coordination, nausea, vomiting, or diarrhea.

Tell your doctor right away if you develop withdrawal symptoms or an allergic reaction even weeks or months after your last dose of Sublocade.

Common Sublocade side effects may include:

• feeling tired;
• nausea, vomiting, constipation;
• pain, redness, itching, burning, irritation, or skin changes where the injection was given;
• pain and burning when you urinate;
• trouble sleeping;
• headache; or
• abnormal liver function tests.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Usual Adult Dose for Opiate Dependence - Maintenance:

Before administration: Patients not currently taking buprenorphine should receive an initial dose (for example, 4 mg) of transmucosal buprenorphine before administering the first injection of Sublocade.

• Initial dose: 300 mg subcutaneously once a month for 2 months
• Maintenance dose: 100 mg subcutaneously once a month The maintenance dose may be increased to 300 mg monthly for those tolerating lower dose and demonstrating a less than satisfactory clinical response, e.g. self-reported illicit opioid use or positive urine drug screens.

Comments:Initiating therapy with subcutaneous injections has not been studied; subcutaneous injections should only be initiated following induction and dose-adjustment with a transmucosal buprenorphine-containing product.Monthly doses should allow for a minimum of 26 days between doses; occasional delays in dosing of up to 2 weeks are not expected to have a clinically significant impact on treatment effect.

Call your doctor for instructions if you miss an appointment for your Sublocade injection.

In a medical setting, an overdose would be treated quickly.

Your doctor may recommend you get naloxone (a medicine to reverse an opioid overdose) and keep it with you at all times. A person caring for you can give the naloxone if you stop breathing or don't wake up. Your caregiver must still get emergency medical help and may need to perform CPR (cardiopulmonary resuscitation) on you while waiting for help to arrive.

Anyone can buy naloxone from a pharmacy or local health department. Make sure any person caring for you knows where you keep naloxone and how to use it.

Avoid driving or hazardous activity until you know how this medicine will affect you. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Dizziness or drowsiness can cause falls, accidents, or severe injuries.

Do not drink alcohol. Dangerous side effects or death could occur.

Fatal side effects may occur if you also drink alcohol or use other drugs that cause drowsiness or slow breathing.

Using opioid medicine during pregnancy may cause life-threatening withdrawal symptoms in the newborn.

Sublocade is available only under a special program. You must be registered in the program and understand the risks and benefits of this medicine.

Sometimes it is not safe to use certain medicines at the same time. Some drugs can affect your blood levels of other drugs you use, which may increase side effects or make the medicines less effective. Tell your doctor if you also use an antibiotic, antifungal medication, seizure medication, or medicine to treat HIV or hepatitis C.

Many other drugs can be dangerous when used with opioid medicine. Tell your doctor if you also use:

• medicine for allergies, asthma, heart problems, motion sickness, irritable bowel, or overactive bladder;
• other opioid medicines;
• a benzodiazepine sedative like Valium, Klonopin, or Xanax;
• sleep medicine, muscle relaxers, or other medications that make you drowsy; or
• medications that affect serotonin, such as antidepressants, stimulants, or medicine for migraines or Parkinson's disease.

This list is not complete and many other drugs may interact with buprenorphine. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

Active ingredient: buprenorphine.Inactive ingredients: ATRIGEL delivery system: biodegradable 50:50 poly(DL-lactide-co-glycolide) polymer and a biocompatible solvent, N-methyl-2-pyrrolidone (NMP).

Curia Global Inc., Albany, NY 12203, USA.