Sublocade

Opioid Use Disorder Treatment

Sublocade is indicated for the treatment of moderate-to-severe opioid use disorder (OUD). It is used in adults who have addiction or physical dependence on opioid drugs, such as heroin or prescription pain medications.

Comprehensive Treatment Plan

This medication is not intended to be used alone. It should be part of a complete treatment program that includes:

• Counseling
• Behavioral therapy
• Psychosocial support

Treatment Initiation

Sublocade is specifically for patients who have already begun treatment with a buprenorphine-containing medication that is taken by mouth, such as a film or tablet that dissolves under the tongue or against the cheek. Before receiving the injection, patients must be on a stable dose of the oral medication for at least seven days to ensure the medicine is tolerated and effective.

Mechanism of Action

Sublocade is a long-acting injection of buprenorphine, a medication classified as a partial opioid agonist. It works by binding to the same receptors in the brain that are affected by other opioids, such as heroin or prescription pain relievers.

By occupying these receptors, buprenorphine helps to:

• Reduce cravings: It satisfies the brain's need for opioids without producing the same intense high as full opioids.
• Prevent withdrawal: It provides enough stimulation to the receptors to stop the physical symptoms of withdrawal.
• Block other opioids: Because it binds strongly to the receptors, it can block the effects of other opioids if they are taken while Sublocade is in the system.

Extended-Release Delivery

The medication uses a delivery system that turns into a solid mass, known as a depot, once it is injected under the skin. This depot slowly dissolves over time, releasing a consistent amount of buprenorphine into the bloodstream throughout the month. This steady level helps maintain stability and avoids the daily highs and lows sometimes associated with oral medications.

The Ceiling Effect

As a partial agonist, buprenorphine has a ceiling effect. This means that after a certain dose, its effects do not increase further. This characteristic makes it less likely to cause dangerous slowed breathing (respiratory depression) compared to full opioid agonists.

Common Side Effects

• Constipation
• Nausea or vomiting
• Headache
• Dizziness
• Tiredness or sleepiness
• Pain, itching, or redness at the injection site

Serious Side Effects

Contact a healthcare provider immediately if you experience serious side effects, including:

• Respiratory depression: Slowed or shallow breathing, or feeling very faint.
• Liver problems: Yellowing of the skin or eyes, dark urine, or pain in the upper right stomach area.
• Severe allergic reactions: Hives, swelling of the face or throat, or difficulty breathing.
• Adrenal insufficiency: Nausea, vomiting, loss of appetite, or extreme weakness.
• Severe sedation: Feeling extremely sleepy or having trouble staying awake.

It is common to have a small, hard lump at the site of the injection. This lump should not be rubbed, massaged, or squeezed, and it typically gets smaller over several weeks.

Boxed Warning: Risk of Serious Harm or Death

Sublocade must only be administered by a healthcare provider as an injection under the skin (subcutaneously). If this medication is injected into a vein (intravenously), the liquid turns into a solid mass that can travel through the blood and cause life-threatening blood clots, tissue damage, or lung problems (pulmonary emboli).

Because of these risks, Sublocade is only available through a restricted program called the SUBLOCADE REMS (Risk Evaluation and Mitigation Strategy). It is not available at retail pharmacies for patient use.

Respiratory and Central Nervous System Depression

Buprenorphine can cause life-threatening breathing problems (respiratory depression). This risk is significantly higher if the medication is used with other substances, including:

• Benzodiazepines or other sedatives
• Alcohol
• Other opioid medications
• Central nervous system depressants

Liver Health and Monitoring

Cases of moderate to severe liver injury have been reported in people using buprenorphine. Healthcare providers typically monitor liver function through blood tests before starting treatment and periodically during therapy. Individuals with pre-existing liver conditions may require closer monitoring.

Pregnancy and Neonatal Opioid Withdrawal Syndrome

Long-term use of buprenorphine during pregnancy can lead to neonatal opioid withdrawal syndrome (NOWS) in the newborn. This condition is expected and treatable but requires management by medical professionals at birth.

Other Precautions

• Adrenal Insufficiency: Chronic use of opioids may lead to a condition where the adrenal glands do not produce enough cortisol.
• Allergic Reactions: Severe allergic reactions, including anaphylaxis and swelling of the face or throat, have occurred.
• Physical Impairment: This medication may impair the mental or physical abilities needed to perform potentially dangerous tasks, such as driving or operating machinery.
• Pre-existing Conditions: Caution is advised for individuals with a history of head injury, increased intracranial pressure, or certain digestive conditions.

Pregnancy Considerations

If Sublocade is used during pregnancy, the baby may experience neonatal opioid withdrawal syndrome (NOWS) after birth. This is a recognized and treatable condition that can occur with the use of opioid medications during pregnancy. Healthcare providers monitor newborns for signs of withdrawal, which may include:

• High-pitched crying and irritability
• Abnormal sleep patterns
• Tremors or jitteriness
• Vomiting or diarrhea
• Failure to gain weight

It is important not to stop treatment for opioid use disorder during pregnancy without medical guidance. Untreated addiction can lead to serious complications for both the pregnant person and the fetus. Decisions regarding the use of Sublocade should be made in consultation with a medical professional to balance the benefits of treatment against the risks of withdrawal for the newborn.

Breastfeeding

Buprenorphine, the active ingredient in Sublocade, passes into breast milk in small amounts. While breastfeeding is often possible for those on stable treatment, it is important to monitor the nursing infant closely. Parents should watch for signs of:

• Increased sleepiness or difficulty waking up
• Difficulty breathing or slow breathing
• Limpness or poor feeding

Discuss the risks and benefits of breastfeeding with a healthcare provider to determine the safest approach for the infant and the parent.

Available Forms

Sublocade is available in the following form:

• Extended-release subcutaneous injection: This medication is provided as a liquid in a prefilled, single-use syringe.

The injection is administered by a healthcare provider under the skin of the abdomen. After injection, the delivery system forms a solid mass known as a depot, which slowly releases the medication into the body over a period of time.

Due to safety requirements, this medication is not available for self-administration and must be administered in a clinical setting by a trained professional.

FDA Approval and Indication

The U.S. Food and Drug Administration (FDA) approved Sublocade in November 2017. It is indicated for the treatment of moderate to severe opioid use disorder (OUD) in adult patients who have initiated treatment with a transmucosal buprenorphine-containing product and have been on a stable dose for at least seven days.

Boxed Warning and Administration

Sublocade carries a Boxed Warning regarding the risk of serious harm or death if the medication is administered intravenously. Because the medication forms a solid mass upon contact with body fluids, an intravenous injection could cause a blood clot, damage to local tissues, or a pulmonary embolism. To mitigate this risk, Sublocade must only be administered by a healthcare provider as a subcutaneous injection in the abdominal region.

REMS Program

Due to the risks associated with improper administration, Sublocade is only available through a restricted distribution program called the Sublocade Risk Evaluation and Mitigation Strategy (REMS) Program. Healthcare settings and pharmacies that dispense the medication must be certified in the program to ensure it is only administered by healthcare providers and not dispensed directly to patients.

Regulatory Safety Communications

The FDA has issued communications regarding medications for opioid use disorder (MOUD), emphasizing that these treatments should generally not be withheld from patients taking benzodiazepines or other central nervous system depressants. While combining these substances increases the risk of serious side effects, the FDA advises that the benefits of OUD treatment often outweigh these risks, provided that healthcare providers manage the treatment plan carefully.

Withdrawal Symptoms

Stopping Sublocade can cause opioid withdrawal symptoms as the medication levels in your body decrease. These symptoms may include:

• Nausea, vomiting, or diarrhea
• Muscle aches and joint pain
• Sweating, chills, or goosebumps
• Anxiety, irritability, or restlessness
• Sleep disturbances
• Runny nose or watery eyes

Delayed Onset

Because Sublocade is an extended-release injection, the medication stays in your system for a long time. Withdrawal symptoms may not appear immediately after a missed dose; instead, they might emerge weeks or even months after your last injection. Your healthcare provider will typically monitor you for several months after your final dose to manage any late-emerging withdrawal signs or cravings.

Safety Considerations

You should not stop treatment abruptly or without medical guidance. If treatment is discontinued, your doctor will monitor you for signs of withdrawal and the potential return of opioid use disorder. It is important to keep all follow-up appointments even after you stop receiving the injections.