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Sublocade: 7 things you should know

Medically reviewed by Carmen Fookes, BPharm. Last updated on Feb 9, 2021.

1. How it works

  • Sublocade is a brand (trade) name for a buprenorphine subcutaneous (SC) injection that may be used for the maintenance treatment of opioid misuse disorder in adults.
  • Sublocade (buprenorphine SC injection) is a partial opioid agonist which means it binds to and activates opioid receptors (particularly mu receptors) but less strongly than full agonists do. This means it can reduce cravings and withdrawal symptoms in a person with an opioid use disorder without producing euphoria. Sublocade helps to reduce withdrawal symptoms and curb cravings for opioids by tricking the brain into thinking that a full agonist like oxycodone or heroin has been taken. Some forms of buprenorphine can be used to provide pain relief because activating mu opioid receptors also relieves pain.
  • Sublocade belongs to the class of medicines known as narcotic analgesics. It may also be called an opioid analgesic. Sublocade is only used for the treatment of opioid (narcotic) addiction.

2. Upsides

  • May be used for the treatment of moderate-to-severe opioid use disorder in people who have already initiated treatment with either a sublingual or buccal form of buprenorphine (such as Subutex or Suboxone) and the dosage stabilized, over a minimum of 7 days. The equivalent transmucosal dose of buprenorphine is 8mg to 24mg daily.
  • Sublocade is used as part of a complete treatment program that includes counseling and psychosocial support.
  • Has advantages over other medication-assisted treatments (such as methadone and naltrexone) in that it suppresses withdrawal symptoms and cravings for opioids, does not cause euphoria (the feeling or state of intense excitement and happiness), and also blocks the effects of other opioids for at least 28 days.
  • Helps people to change their thinking, behavior, and environment. Complements education, counseling, and other support measures that focus on the behavioral aspects of opioid addiction.
  • Long-acting, only needs to be taken once a month, with a minimum of 26 days between doses. Occasional delays of up to two weeks are not expected to have a significant impact on the treatment effect. If extended travel is deemed necessary, a single 300mg injection may be given to cover 2 months.
  • Available as two strengths: 100mg/0.5mL and 300mg/1.5mL (equates to 200mg/mL). In people who tolerate teh 100mg dose, the maintenance dose may be increased to 300mg monthly.
  • When Sublocade is discontinued, take into account its extended-release characteristics and monitor the signs and symptoms for withdrawal treatment.
  • Injected subcutaneously (under the skin). The abdomen is the only site Sublocade can be administered.
  • Sublocade forms a depot of buprenorphine under the skin. If this depot needs to be removed, it can be done under local anesthesia within 14 days of injection. The removed depot should be properly disposed of as Schedule III biohazardous waste and according to federal, state, and local regulations.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

  • A headache, drowsiness/sedation, gastrointestinal disorders (eg, constipation, nausea, or vomiting), fatigue, pain, liver enzyme elevation (eg, alanine aminotransferase, aspartate aminotransferase, gamma-glutamyl transferase), and blood creatine phosphokinase, are the most common side effects reported.
  • Allergic reactions (including breathing difficulties, rash, and anaphylactic shock) and liver damage (hepatitis) have been reported.
  • Sublocade should NEVER be administered intravenously. Serious harm or death could result if this occurs because Sublocade forms a solid mass upon contact with body fluids and may cause venous occlusion, local tissue damage, and blood clots. Sublocade is not for intramuscular (IM) administration either.
  • Can only be prescribed under the Sublocade REMS Program by physicians who meet certain qualifying requirements, and who have been assigned a unique identification number that must be included on every prescription.
  • Abuse potential exists, although it is substantially lower than methadone, and because Sublocade is only administered by a healthcare professional, this limits the abuse potential of Sublocade.
  • Sublocade has been associated with breathing difficulties and death, most often the IV form and when used at the same time as benzodiazepines, alcohol, or other CNS depressant drugs. Avoid self-administration of other medications while taking Sublocade except on a doctor's advice.
  • Can also cause dependence and a withdrawal syndrome on abrupt discontinuation although this is typically milder than that seen with full agonists.
  • May cause drowsiness and affect a person's ability to drive or operate machinery.
  • May only be prescribed by healthcare providers that meet certain qualifying requirements and who have notified the Secretary of Health and Human Services (HHS) of their intent to prescribe or dispense this product for the treatment of opioid dependence. These healthcare providers have been assigned a unique identification number that must be written on every prescription.
  • Sublocade may be addictive and cause psychological dependence and withdrawal symptoms, particularly when used for long periods.
  • May interact with several other drugs including other opioids, benzodiazepines, and other central nervous system depressants resulting in profound sedation, respiratory depression, and sometimes death. May also interact with drugs metabolized through several CYP hepatic enzyme systems (such as CYP3A4 or CYP2D6) or drugs that also release serotonin (such as antidepressants, antipsychotics, and tramadol). There is a risk of heart rhythm disorders (such as QT prolongation) associated with Sublocade particularly when used with other drugs that prolong the QT interval.
  • The need for continuing medication-assisted treatment should be re-evaluated periodically.
  • Treat patients receiving Sublocade with a non-opioid analgesic whenever possible. If a person required opioid therapy then they may be treated with a high-affinity full-opioid analgesic under the supervision of an experienced physician with full monitoring of respiratory function.
  • May not be suitable for some people such as those with liver disease, cardiac arrhythmias, the elderly or frail, with a history of drug or alcohol abuse, with psychiatric disorders, previous head injury or raised intracranial pressure, a history of seizure disorders, with certain gastrointestinal conditions, respiratory disease, liver disease, physically dependent on full agonists, or certain other concomitant conditions. Use during pregnancy may cause withdrawal symptoms in the newborn baby.
  • Needs to be administered by a healthcare provider once a month. Sublocade SC injection should be kept refrigerated at 2 - 8°C (35.6 - 46.4°F), but may be taken out of the refrigerator up to 7 days prior to administration as long as it is kept at room temperature (15 – 30°C [59 – 86°F]), and discarded if not used within 7 days.
  • Not for opioid-naive individuals. May cause potentially fatal respiratory depression in children accidentally exposed to it.
  • No generic Sublocade SC injection is available.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

  • Sublocade is a once-monthly injection that is used to treat adults with opioid misuse disorder and is administered subcutaneously (under the skin) into the abdomen. It forms a depot under the skin which releases buprenorphine slowly. A headache, drowsiness/sedation, gastrointestinal disorders (eg, constipation, nausea, or vomiting), fatigue, pain, and liver enzyme elevations are the main side effects reported. It should be used in conjunction with a complete treatment program that includes counseling and behavioral therapy.

5. Tips

  • Sublocade should always be used as part of a complete treatment plan that includes counseling and psycho-social support. A sublingual or buccal form of buprenorphine (such as Subutex or Suboxone) must be used and the dosage stabilized for at least 7 days before Sublocade is first injected.
  • Continued treatment with Sublocade usually depends on compliance with all elements of the treatment plan and abstinence from illicit drug use. When used to treat drug addiction, it is important that you take advantage of any social support and counseling services offered to you as withdrawal from opioids is a long and often difficult process and a successful outcome is dependent upon a multi-targeted approach.
  • Seek immediate medical help if you develop blurred vision, are excessively sleepy or uncoordinated, have slurred speech, have slowed reflexes or breathing, or have significant problems thinking.
  • Sublocade must be injected by a qualified and certified healthcare provider every 28 days (minimum 26 days).
  • Tell your doctor if you experience any difficulty with breathing or shortness of breath after Sublocade has been injected, especially within the first 24 to 72 hours of initiating therapy. Also tell them if you have any bleeding, pain, numbness, yellowing of the skin or eyes, unexplained abdominal pain, or unusual tiredness.
  • Rise carefully from a sitting to a standing position to minimize blood pressure lowering effects from Sublocade which may result in dizziness increasing your risk of falls.
  • Sublocade may cause constipation. Talk to your doctor about taking laxatives as a preventive against constipation if you are prescribed Sublocade.
  • Sublocade has been associated with androgen deficiency which may cause symptoms such as low libido, impotence, erectile dysfunction, amenorrhea, or infertility. Talk to your doctor if this happens to you.
  • Always talk to your doctor or pharmacist before buying anything over-the-counter to check if it is compatible with Sublocade. If Sublocade is administered with other drugs that also release serotonin, such as tramadol, lithium, antidepressants, a condition called serotonin syndrome may develop. Symptoms include agitation or restlessness, sweating, diarrhea, headache, confusion, rapid heart rate, and high blood pressure, dilated pupils, loss of muscle coordination, twitching muscles, or muscle rigidity. See your doctor immediately.
  • If you are a woman of child-bearing age you should use adequate contraception to ensure you do not become pregnant while being administered Sublocade. If you inadvertently become pregnant, tell your doctor straight away as there is a risk your baby may be born with neonatal withdrawal syndrome which will need to be treated. Do not breastfeed while being administered Sublocade.
  • Do not drive or operate machinery if you are prescribed Sublocade because it may impair your ability to perform these tasks unless you are tolerant to its effects.
  • You should not drink alcohol while you are prescribed Sublocade because it may impair your ability to concentrate and also increase the risk of side effects such as respiratory depression.
  • Sublocade is a schedule III product.

6. Response and Effectiveness

  • Two key studies that demonstrate the effectiveness of Sublocade in moderate to severe opioid use disorder are an opioid blockade study and a Phase 3 efficacy and safety study.
  • In the opioid blockade study, 300mg SC Sublocade was shown to be not inferior (not substantially more likable) to IM hydromorphone (6mg or 18mg) over 20 weeks; however, there were wide variations in isolated measurements from individual subjects. As a comparison, sublingual buprenorphine failed to provide full blockade to 18mg of hydromorphone.
  • In the Phase 3 efficacy and safety study, the proportion of patients achieving treatment success (>/= 80% opioid-free weeks) was significantly more in both the Sublocade arms of the trial compared to placebo.

7. Interactions

Medicines that interact with Sublocade may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with Sublocade. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Common medications that may interact with Sublocade include:

  • antidepressants, such as tricyclic antidepressants (eg, amitriptyline), monoamine oxidase inhibitors (eg, isocarboxazid, phenelzine, and tranylcypromine), or SSRIs (eg, fluoxetine, sertraline)
  • antipsychotics (such as butyrophenones, phenothiazines, or thioxanthenes) and atypical antipsychotics (eg, olanzapine, quetiapine, ziprasidone)
  • any medication that inhibits or induces CYP3A4
  • any medication that may cause drowsiness, such as amphetamines, benzodiazepines (eg, diazepam, lorazepam), first-generation antihistamines (such as doxylamine or promethazine), metoclopramide, or opioids (such as codeine, methadone, or morphine)
  • HIV medications such as ritonavir
  • naloxone and naltrexone
  • QT-prolonging medications such as amiodarone and flecainide
  • rifampin
  • St. John's Wort.

Avoid drinking alcohol or taking illegal or recreational drugs while taking Sublocade.

Note that this list is not all-inclusive and includes only common medications that may interact with Sublocade. You should refer to the prescribing information for Sublocade for a complete list of interactions.

References

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Sublocade only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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