Your doctor may prescribe buprenorphine (Sublocade) injections if you have moderate to severe opioid use disorder (OUD). Buprenorphine works best when it’s part of a larger treatment program that includes counseling and psychosocial support.
How Does Buprenorphine (Sublocade) Work?
Buprenorphine is a synthetic (manmade) opioid. It’s considered a controlled substance because it could potentially lead to addiction. But it affects your body differently than other opioids.
It helps your brain learn to work without them. That’s because it has a weaker effect when used as prescribed. And it doesn’t cause a “high.”
Buprenorphine may help ease cravings and curb the satisfying effects of other opioids. This might make you less likely to use them.
Who Can Take Buprenorphine (Sublocade)?
In most cases, you can try buprenorphine if you’ve been on another form of it for at least 7 days.
What’s the Dosage for Buprenorphine (Sublocade)?
Your doctor will give you 300 milligrams monthly for the first 2 months. Then you’ll get a “maintenance dose” of 100 milligrams once a month.
Your doctor might up the maintenance dose to 300 milligrams if your body’s not responding to 100 milligrams. This could happen if you’ve started to misuse opioids again.
If you miss a dose, you should get the next one as soon as possible. You’ll get the following dose no fewer than 26 days later.
If you have to travel for a long period of time, ask your doctor about changing the dosage. For example, instead of 100 milligrams once a month, you might be able to move to a 2-month regimen. This means you would get one 300-milligram dose every 2 months instead. You can go back to your 100-milligram treatment once you return to a stable schedule. You may notice stronger side effects going from 100 to 300 milligrams.
Does Buprenorphine (Sublocade) Interact With Other Drugs?
Before you start treatment with buprenorphine, you should be aware of drugs it may react badly with. Your risk for respiratory depression (when your lungs don’t work as well as they should) is higher if you use buprenorphine with:
- Benzodiazepines
- Other sedatives/hypnotics
- Anxiolytics
- Tranquilizers
- Muscle relaxants
- General anesthetics
- Antipsychotics
- Opioids
- Alcohol
Inhibitors of CYP3A4. Experts haven’t studied the interactions between Sublocade and these medications. But they’ve looked at how forms of buprenorphine taken through your mouth interact with inhibitors of CYP3A4, like macrolide antibiotics such as erythromycin (E.E.S. Granules, E.E.S. 400, Ery Pads), azole‐antifungal agents like ketoconazole (Extina, Nizoral, Xolegel), and protease inhibitors like ritonavir (Norvir). Since buprenorphine is processed into norbuprenorphine mostly through the enzyme CYP3A4, the two drugs taken together could cause interactions. They might lead to stronger or longer opioid effects.
CYP3A4 Inducers. Experts also haven’t studied this interaction. But your body processes buprenorphine into norbuprenorphine through CYP3A4. As with inhibitors of CYP3A4, drugs that affect CYP3A4 – like carbamazepine (Equetro, Tegretol, Tegretol XR), phenobarbital (Luminal Sodium, Solfoton, Tedral), phenytoin (Dilantin Infatabs, Dilantin Kapseal, Phenytek), and rifampin (Rifadin) – might interact with buprenorphine. This could affect how well buprenorphine works.
Antiretrovirals: Non‐nucleoside reverse transcriptase inhibitors (NNRTIs). Experts have found interactions between some NNRTIs – like delavirdine (Rescriptor), efavirenz (Sustiva), etravirine (Intelence), and nevirapine (Viramune, Viramune XR) – and buprenorphine. The drug might heighten the effects of the NNRTIs.
Protease inhibitors (PIs). Some PIs, like atazanavir (Reyataz) and atazanavir/ritonavir (Norvir), caused higher levels of buprenorphine and norbuprenorphine after a person took buprenorphine. Some people also noticed more sedation.
Serotonergic drugs. When you use buprenorphine, don’t take selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), triptans, 5‐HT3 receptor antagonists, drugs that affect the serotonin neurotransmitter system, certain muscle relaxants, monoamine oxidase (MAO) inhibitors like ones that treat psychiatric disorders, and others like linezolid (Zyvox) and intravenous methylene blue (Provayblue).
If you take one of these with buprenorphine, it could lead to serotonin syndrome. This is a condition that happens when too much serotonin causes different symptoms like mild shivering and diarrhea or severe muscle rigidity, fever, seizures, or even death.
Monoamine oxidase inhibitors (MAOIs). If you take drugs like linezolid (Zyvox), phenelzine (Nardil), or tranylcypromine (Parnate) with buprenorphine, you could develop serotonin syndrome or opioid toxicity, which will show up at respiratory depression or even coma.
Muscle relaxants. Buprenorphine can strengthen the effects of muscle relaxants. This could worsen respiratory depression.
Diuretics. Buprenorphine can cause diuretics to not work as well.
Anticholinergic drugs. If you use these drugs alongside buprenorphine, it could put you at a higher risk for urinary retention (when you can’t pee fully) or severe constipation. If you have intense constipation, it could lead to paralytic ileus (blocked intestines).
Warnings and Safety Issues with Buprenorphine (Sublocade)
This medication is a shot your doctor gives you subcutaneously (under the skin). It’s unsafe to attempt to give yourself a shot. Other potential problems include:
Risk of drug abuse. Buprenorphine can be abused just like other opioids. During treatment, your doctor will watch for any signs your OUD is getting worse.
People with breathing conditions. Misuse of buprenorphine can lead to life-threatening respiratory (breathing) issues. But this can also happen if people who use the drug have respiratory issues like chronic obstructive pulmonary disease (COPD), cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or other forms of respiratory depression. Because of this, if you have one of these conditions, your doctor will watch you closely if you need treatment with buprenorphine.
Treatment with opioids can also lead to sleep-related breathing disorders like central sleep apnea (CSA) or sleep-related hypoxemia.
Injection site reactions. In some cases, you may notice pain, redness, itchiness, abscess, ulceration, or necrosis (death or cells or tissue) after buprenorphine injections. The risk of this goes up if someone injected the medication the wrong way.
Neonatal opioid withdrawal syndrome (NOWS). NOWS can happen with all long-term use of opioids during pregnancy. This is when an infant is born with symptoms from exposure to opioids like severe crankiness, feeding issues, breathing problems, and seizures. It can be life-threatening if it’s not found and treated in the newborn child. If you’re pregnant and on treatment for an OUD, you and your doctor will weigh the pros and cons of treatment.
Adrenal insufficiency. This is when your adrenal glands don't make enough of the hormone cortisol. Some cases of this have been reported, mostly in people who have used buprenorphine for over a month. Symptoms might include nausea, vomiting, anorexia, fatigue, weakness, dizziness, or low blood pressure. See your doctor right away if you notice these symptoms.
Risk of hepatitis or hepatic (liver) events. There have been some reports of cytolytic hepatitis and hepatitis with jaundice in buprenorphine clinical trials.
People with moderate to severe liver damage should not be on treatment with injectable buprenorphine.
Naloxone and Buprenorphine (Sublocade)
When you begin treatment for OUD, it’s important that you ask your doctor about naloxone. This is an emergency treatment for opioid overdoses. A caregiver or loved one can give it to you if they think you’ve overdosed. Your doctor will go over how to get naloxone in your specific state.
