Buprenorphine: Uses, Side Effects & Addiction Treatment

What is Buprenorphine?

Buprenorphine is an FDA-approved medication for managing chronic and acute pain and treating opioid use disorder (OUD). According to SAMHSA, 5.7 million Americans battle opioid addiction each year.

Studies show that a person with an opioid dependency has a 20-fold increased chance of early death. However, researchers have found that when individuals are prescribed medication like buprenorphine to manage their addiction, they have a 50% lower death rate from all causes.

What is Buprenorphine Used For?

Buprenorphine is a primary medication for opioid addiction treatment due to its quick effectiveness in relieving cravings and withdrawal symptoms. It can be prescribed in an outpatient facility setting which makes it much more attractive for those who work, have families, or otherwise do not want to be admitted for inpatient care.

The opioid crisis is devastating. Over 700,000 Americans have died of opioid overdose in the last 25 years. That’s more than all the U.S. servicemen and women who have died in every war since World War I. Effective therapeutics are urgently needed and buprenorphine is on the front lines of this battle.

Studies show that individuals on buprenorphine have fewer positive drug tests for other opioids, fewer cravings, and a lower risk of emergency department visits. The research also shows that 75% remain in treatment after one year of using the meds when combined with counseling.

OUD treatment with buprenorphine works by substituting a more potent one, like fentanyl, with this longer acting alternative that activates opioid receptors to a lesser degree. This strategy works because treatment with buprenorphine mitigates the effects of withdrawal.

For someone who is physiologically dependent on opioids, complete abstinence is often untenable, at least in the first weeks and months following detox. Some clients in OUD recovery may remain on maintenance doses of buprenorphine for several months or even years.

Buprenorphine helps reduce the distressing physical and psychological symptoms of opioid withdrawal. This increases the chance of recovery by helping individuals reduce the cravings and withdrawal symptoms that may trigger a relapse.

The pharmaceutical treatments are frequently combined with psychotherapy, recovery education and emotional support to address the underlying causes of the addiction.

Buprenorphine Mechanism of Action & Effects

In order to determine if the treatment is right for you or someone you love, it’s helpful to understand buprenorphine’s mechanism of action and its effects.

How Does Buprenorphine Work?

Buprenorphine is a partial opioid agonist that works on the same receptors that opioids like fentanyl activate. Buprenorphine’s effects on the brain’s opioid receptors mitigates withdrawal symptoms when a person stops taking opioids. Its high-binding properties also block the effects of other opioids if relapse occurs, which minimizes overdose risk.

Buprenorphine’s differences from full opioid agonists like fentanyl translates into tangible clinical benefits. Buprenorphine exerts its effects for a longer period of time. This prevents the “highs” and “lows” commonly experienced when short-acting opioids are abused.

The effects of buprenorphine are also limited and reach a plateau, known as the ceiling effect. This makes potential side effects like respiratory problems, sedation, and euphoria less likely. Overdose is extremely rare, even at high doses.

Thus, it’s often a safer choice than other pharmacotherapies, such as methadone, for patients seeking OUD treatment.

Buprenorphine offers several advantages for OUD treatment. Therapeutic doses can be achieved within a short time frame. Patients benefit from flexible daily or alternate-day dosing and the convenience of office-based prescribing.

Is Buprenorphine an Opioid?

Yes. Buprenorphine is an opioid. Buprenorphine belongs to a class of medicines called synthetic opioids, which are manufactured from compounds found in the poppy flower.

Buprenorphine comes in multiple formulations, including sublingual films and tablets. In some formulations, it is combined with naloxone to decrease the risk of diversion and abuse. Brand names of this combination include Zubsolv and Suboxone. Daily sublingual buprenorphine is often the first line of treatment for opioid addiction.

Extended-release subcutaneous injections (Brixadi and Sublocade) are prescribed as a longer acting treatment for OUD. They’re generally used in patients who are already on buprenorphine, though can be used in those who are just starting treatment, as well.

These injections offer a steady release of medication into the body ranging from a week to over a month, helping you to remain stable and largely symptom-free throughout your day.

Intravenous and intramuscular injections and transdermal applications are primarily used for managing severe pain that does not respond to other medications.

Is Buprenorphine a Controlled Substance?

Buprenorphine is a DEA Schedule III controlled substance, meaning that it has a valid medical use and some potential for psychological and physical dependence.

Its legal prescribing status changed in 2022, making it the first medication for OUD that can be prescribed by any clinician with Schedule III authority. Authorized physicians, physician assistants, and nurse practitioners may prescribe buprenorphine without needing a waiver.

The purpose of relaxing prescribing requirements was to expand access to this life saving medication. Prescribers can initiate buprenorphine treatment in any ambulatory or outpatient setting, emergency department, or inpatient facility.

Buprenorphine vs. Suboxone: What’s the Difference?

You might be wondering if buprenorphine is the same as Suboxone? The short answer is no, they are not the same. Buprenorphine is the active ingredient in Suboxone. But Suboxone, a brand name, is a sublingual formulation that contains a combination of four parts buprenorphine and one part naloxone.

Suboxone is one of the primary medications used in opioid recovery treatment. While buprenorphine alone can be effective, adding naloxone reduces the risk of abuse.

Buprenorphine has excellent sublingual absorption but naloxone does not. This is important because it means that, when a buprenorphine/naloxone combination product is taken sublingually, the naloxone will not have an effect. If both had similar sublingual absorption, naloxone would counteract buprenorphine’s effects

Naloxone is a short-acting opioid antagonist, which means it functions as an opioid antagonist, reversing the effects of opioids.

So why is naloxone included in Suboxone? It all comes down to preventing misuse. When people misuse buprenorphine, they sometimes do so by dissolving tablets or films and injecting them.

If a person injects Suboxone, naloxone becomes fully active, blocking buprenorphine’s euphoric effects and potentially triggering withdrawal symptoms, discouraging abuse and reducing the likelihood of overdose.

Though Suboxone is commonly prescribed for those with opioid addiction, buprenorphine alone is still prescribed in some cases. Certain patients may experience withdrawal symptoms when they take the combination product while others respond better to a naloxone-free formula.

Buprenorphine as a standalone treatment may be prescribed in medical cases where a physician determines it is the best option.

FAQs

How Long Does Buprenorphine Stay in Your System?

Buprenorphine is poorly absorbed when taken orally because the liver and intestine metabolize it too fast. This is the reason why sublingual administration is typically preferred. Sublingual absorption is faster and peak effects are reached after 3-4 hours.

Buprenorphine stays in the body for about 38 hours but this varies. Depending on the individual, buprenorphine may remain in the body from 25 to 70 hours after consumption.

How is Buprenorphine Different from Other Opioids?

Buprenorphine has unique pharmacological properties that distinguish it from other opioids. And these differences are what make it advantageous for OUD treatment.

As a high-affinity partial agonist at the µ-opioid receptor (MOR), buprenorphine activates MOR with a limited effect compared to full agonists like methadone, resulting in a ceiling effect that reduces the risk of overdose and respiratory depression. It’s also an antagonist at κ-opioid (KOR) and δ-opioid (DOR) receptors, which may result in less euphoric effects that can dissuade abuse.

Buprenorphine also disengages from opioid receptors at a very slow pace. This property means it can exert its effects for longer, relieving withdrawal symptoms for up to 24-36 hours and facilitating treatment protocols that employ a one-day dose.

Also, animal studies suggest buprenorphine may influence opioid receptor recovery after intense opioid abuse by modulating receptor availability in the brain. More research is needed but the evidence is promising.

Compared to methadone, which is another common medication for OUD treatment, buprenorphine may be a safer choice with fewer side effects.

Buprenorphine is associated with reduced euphoric responses, fewer heart contraindications, lower risk of drug interactions, and decreased likelihood of respiratory depression and overdose.

Moreover, it is less stigmatized and does not require dispensing from specialized clinics, making it easier to access for patients in need.

What Are the Risks of Buprenorphine Use?

Individuals should take buprenorphine only under physician guidance. Like all opioids, buprenorphine has a risk of abuse, tolerance, and addiction.

Consuming buprenorphine while taking other opioids could augment the risk of withdrawal symptoms. Fatal respiratory depression is a risk for older individuals and those with breathing problems. Physicians must carefully consider such risks when commencing treatment or augmenting doses.

Manipulating buccal or transdermal formulations to inject, swallow, snort, or chew the drug can deliver large doses that may result in overdose and death.

Using buprenorphine with medications that depress the central nervous system is a significant risk. Benzodiazepines, hypnotics, sedatives, certain antidepressants, allergy medicines and alcohol can interact with buprenorphine, generating life-threatening respiratory depression, coma, and death.

Studies indicate that overdoses of buprenorphine alone are rare and that most fatal events include co-occurring consumption of benzodiazepines (94%) and illicit drugs (63%).

When a person ends treatment with buprenorphine, their tolerance to opioids can diminish. If they relapse, they may expose themselves to an overdose risk if they consume the quantities they used to take due to being more sensitive to opioids.

Stopping buprenorphine abruptly is not recommended as it can lead to withdrawal symptoms like anxiety, flu-like congestion, and other uncomfortable reactions.

Can Buprenorphine Be Used for Pain Management?

Yes. Buprenorphine is used for the management of severe pain that is not responsive to alternative treatments. Its effects can ease the physical and emotional reaction a person has to pain.

An extended-release buprenorphine patch can be used to control severe and long-term pain that requires ongoing treatment. Injections are also used in healthcare settings to manage short-term pain, such as from surgery. Buprenorphine tablets are generally not prescribed to alleviate pain.

Buprenorphine Side Effects & Risks

Buprenorphine can produce a host of side effects like:

• Nausea
• Drowsiness
• Constipation
• Low blood pressure
• Abnormal heart rhythm (QT prolongation)
• Increased seizure risk
• Dizziness
• Headaches
• Memory loss
• Vomiting
• Sweating
• Adverse sexual effects
• Fatigue
• Dry mouth
• Tooth decay
• Insomnia
• Addiction
• Withdrawal symptoms
• Respiratory distress
• Overdose
• Coma
• Death

Suboxone side effects may include:

• Cough
• Fainting
• Chills
• Lightheadedness
• Headache
• Fever
• Feeling heat or warmth
• Sweating
• Hoarseness
• Pain
• Flushing
• Difficulties urinating
• Depression
• Anxiety
• Restlessness
• Swelling
• Rapid heartbeat

Some of the above symptoms could indicate an overdose. Seek immediate medical assistance if you experience:

• Breathing difficulties
• Confusion
• Blurred vision
• Blueish lips, skin, or fingernails
• Extreme drowsiness
• Pinpoint pupils

Is Buprenorphine Addictive?

Buprenorphine can be misused and may lead to addiction. SAMSHA data shows that 619.000 Americans misuse buprenorphine every year.

As an opioid, buprenorphine’s effects can disrupt how the brain works and may lead to physical and psychological dependence that can put a person’s health at risk.

Symptoms of buprenorphine addiction include using more than prescribed, experiencing withdrawal symptoms, needing to use larger amounts to achieve desired effects, constantly thinking about taking it, and an inability to quit despite wanting to.

What Are the Treatment Options for Opiate Addiction?

As has been seen above, opioid addiction is a treatable disease. Here are some options.

Detox is a medical approach that helps patients cope with withdrawal symptoms after they stop using opioids. Specialized facilities provide this service that includes continuous medical supervision to guarantee safety and the use of medications (if needed) to manage withdrawal symptoms.

Inpatient programs combine medical treatment that may employ medications like buprenorphine. Evidence-based behavioral interventions delivered in peaceful facilities to help you disconnect from harmful environments and work full-time on your recovery.

Outpatient programs offer opioid addiction treatment for individuals on a part-time basis. These programs provide the flexibility of accessing evidence-based behavioral interventions and may prescribe medication, if necessary, that can help you minimize withdrawal symptoms while holding a job or living at home.

Medication assisted treatment (MAT) is a valuable tool to combat opioid addiction. Clinicians in these programs will take care of you by using medication like Suboxone and other prescriptions that help your brain recover from a substance use disorder, manage cravings and access therapy to deal with trauma and other reasons behind drug abuse.

Recovery from opioid addiction is a long-term process. You will need the help of aftercare programs that equip you with a plan to develop personal and professional skills, strategies to avoid triggers that may precipitate relapse, and emotional support to rebuild your life.

What Should I Expect During Buprenorphine Treatment

Buprenorphine treatment for opioid abuse is usually divided into three stages: induction, stabilization, and maintenance.

Induction

During induction, a person stops using illicit opioids and begins a controlled regimen with buprenorphine. Typically, you will need to have a period of abstinence from illicit opioids prior to taking your first dose of buprenorphine.

The length of this will be decided by your physician, but is usually 12 hours for short-acting opioids (heroin), 24 hours for long-acting opioids (morphine), and between 48-72 hours for ultra long acting opioids like methadone and fentanyl patches. A typical first dose of buprenorphine is 2–4 mg.

Stabilization

After the initial dose, the next step depends on your symptoms and how your body responds to the medication. If tolerated, your dose will be increased (usually in increments of 2-4 mg) until finding the lowest effective dose that provides 24 hours of relief from withdrawal symptoms to prevent relapse.

This phase can last between 2-4 days. Its purpose is to find, through gradual and controlled increases, the ideal dose to address your physical and psychological needs to minimize discomfort and increase treatment outcomes.

Maintenance

Maintenance treatment is recommended for at least 90 days, but depending on your physician’s criteria, and personal preferences, it can extend for longer periods (1-2 years) or more. Some people stay on buprenorphine for years. The most common maintenance doses are between 8 and 24 mg per day and depend on your unique circumstances and medical criteria.

Other Considerations

During the first 30 days of treatment, it is frequent that your dose is adjusted to find the most effective one. Your doctor may decide to switch how you receive your buprenorphine. Sublingual doses, the most common route, can be changed to extended-release injections if desired.

At the early stages of treatment, you may need to visit your doctor’s office frequently to evaluate progress. Urine tests can be performed randomly as well as pill/film counting to monitor potential relapse or misuse.

Tapering off

If you and your medical team decide to stop treatment, it should be done in a methodical way. Your healthcare provider can help you gradually taper off the buprenorphine over several weeks to months to avoid withdrawal symptoms and prevent relapse.

A New Life is Possible

Addiction to opioids can happen to anyone. It’s not a moral failure but rather a treatable medical condition. If you are struggling with opioid abuse, help is available and recovery is possible.