What Is Buprenorphine?

Buprenorphine is a medication that doctors prescribe as part of a medication-assisted treatment (MAT) program. A person may take buprenorphine if they have a history of addiction to opioids, such as heroin, oxycodone, hydrocodone, morphine, or others. This medication can be an alternative to methadone therapy or may be used as a transitional treatment from methadone to buprenorphine. 4 The medication can treat the withdrawal effects that stopping opioids “cold turkey” can cause.

When using buprenorphine as a MAT, the medication has been shown to reduce the potential for abuse and offers an increased safety profile by reducing the risks for overdose. Doctors have prescribed this medication to treat substance abuse addiction since the year 2000, when the Drug Addiction Treatment Act of 2000 was passed and allowed doctors in the United States to prescribe the medicine.

How Does Buprenorphine Work?

Buprenorphine is a medication type known as a partial opioid agonist. In the body, there are specific receptors that active different parts of the brain. Painkilling medications, such as morphine, oxycodone, and hydrocodone, and heroin, all activate opioid receptors in the brain. 1 This can cause pain relief, euphoria, and physical dependence. Activating opioid receptors can also cause unpleasant symptoms, including nausea and constipation.

When there is a physical dependence upon an opioid drug, such as oxycodone, suddenly stopping taking it can cause adverse symptoms. This includes strong cravings, nausea, muscle aches, and body pains. These symptoms can be so strong that it can lead to relapse.

Buprenorphine Effects

Buprenorphine has the effect on the body of activating opioid receptors, which can relieve some pain. Buprenorphine is more “competitive” than other opioids, such as hydrocodone. This means that if both hydrocodone and buprenorphine are in the body, buprenorphine will “beat” or even remove the other opiates to occupy the opioid receptor. This blocks the effects of other opioid medications and does not produce a euphoria or rush when taken.

Buprenorphine also has a “ceiling effect” when a person takes it. Taking more doesn’t make a person feel more pain relief. As a result, this is a deterrent for overdose. While a person can have what is known as an “abstinence syndrome” or withdrawals from stopping taking buprenorphine, this withdrawal syndrome is usually much less severe than if a person abused other opioid forms.

The medication is available as a tablet or film that can be placed under the tongue where it dissolves, and the body absorbs it. The medication is most commonly mixed as four parts buprenorphine and one part naloxone.

Side Effects

As with many medications, there are side effects from taking buprenorphine. Known side effects include:
  • anxiety
  • constipation
  • depression
  • drowsiness
  • headache
  • nausea
  • sleep problems
Additional rare but possible side effects include sweating, skin rash, itching, weight gain, stomach pains, and decreased sex drive.

What Is the History of Buprenorphine Use in the United States and Beyond?

Historically, doctors have prescribed buprenorphine as a pain reliever for several decades. 1 Not until the 1970s, however, did doctors start to consider the medication as an option for addiction treatment. Studies related to its use in addiction medicine as well as its effectiveness when compared to other available treatments, such as methadone, were conducted. Researchers in the 1990s and 2000s found using buprenorphine could produce similar results as when a person used methadone to combat addiction.

In 2002, the FDA approved buprenorphine for use in the United States. At this time, supporters such as those from the National Institute on Drug Abuse (NIDA), supported the medication’s approval and conducted extensive research regarding the drug’s effectiveness. Examples of these research studies included comparing taking buprenorphine with clonidine as well as studies comparing the appropriate amount of days (7 versus 28 days) to determine the best likely results for tapering the drug.

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What Does Buprenorphine Treatment Look Like?

Before beginning a buprenorphine treatment, a person will meet with a doctor who will be administering and prescribing their medications. A doctor will assess the person’s history of opioid use. 2 They will discuss what kinds of opioids the patient uses (heroin, hydrocodone, oxycodone, or others) to determine the best timing to start treatment. Doctors typically call this first phase the induction phase. 4 According to the Substance Abuse and Mental Health Services Administration (SAMHSA), a person eligible for treatment with buprenorphine therapy meets the following criteria:
  • has a history of opioid dependency
  • is willing to follow safety rules and regulations for buprenorphine treatment
  • does not have any health problems that could keep a person from safely taking buprenorphine
  • has considered other treatment options and evaluated the risks and benefits before beginning treatment

Timing Treatment

Because of how buprenorphine works, timing is important to when a person begins the medication. 2 If a person takes buprenorphine while too much opioids are in the system, the buprenorphine will “kick off” the opioids. This causes a condition called precipitated withdrawal where a person will experience a rapid loss of opioids on the receptor, and have strong withdrawal symptoms. Typically, some of the waiting time frames to begin buprenorphine include:

  • short-acting opioids (heroin and crushed medications, such as hydrocodone, oxycodone, or Percocet):a patient must have stopped taking short-acting opioids at least 12 to 24 hours before taking buprenorphine.
  • long-acting opioids (OxyContin taking orally): A person should usually discontinue this medication at least 24 hours before starting taking buprenorphine. A person should also have started to experience some symptoms of withdrawal, which can indicate that enough of the opioid is out of their systems.2
  • methadone: Because methadone is a long-acting opioid, patients will usually taper their methadone over the course of one week. The last dose is usually at least 36 hours before a person takes buprenorphine for the first time. Sometimes, people may have to wait at least 96 hours before starting buprenorphine because the medication can take so long before withdrawing.2

A person will then begin their buprenorphine treatments when they have withdrawn enough from the other medications. Doctors may prescribe the medication as a one-time dose throughout the day, or they may recommend splitting the dose and taking it twice a day.

The Stabilization Phase

The second phase after the induction phase is known as the stabilization phase.4 This phase is when a person no longer has cravings or side effects as a result of not using opioids any more. At this time, a doctor may adjust the buprenorphine dosage. Sometimes, a doctor may even recommend taking the medication every other day instead of every day as they are stabilized on the medication.

The Maintenance Phase

The third phase is the maintenance phase. This is when a patient is taking a steady dose of buprenorphine and has successfully abstained from taking other opioids for some time. The length of this phase can vary. Some patients may take the medication on an indefinite basis while others may wish to start a medically supervised withdrawal program. This program is when a person may start to taper their buprenorphine dosage. However, they will usually continue in a rehabilitation program, such as a 12-step program or therapy, to prevent a potential relapse.

How Effective Is Buprenorphine In Addiction Treatment?

Researchers have studied buprenorphine as an addiction treatment compared to other medication-assisted treatment options, such as methadone. They’ve also studied buprenorphine as a treatment on its own to determine how effectively program participants are in reducing their opioid use.

According to an article published in the journal “Pain Management,” buprenorphine has shown to be effective in treating the following patients (1):

  • People taking HIV/AIDS medications: According to the journal, taking buprenorphine has been shown to increase compliance in taking antiretroviral medications in a person with HIV or AIDS that is addicted to opioids (1). Patients with substance abuse histories taking antiretrovirals and buprenorphine have also been shown to have increases in their CD4 count and reductions in their viral load. These are signs of improved management of AIDS/HIV.
  • Women: Some studies have shown that taking buprenorphine is associated with less neonatal withdrawal than methadone in pregnant women.1 One study found that babies born to moms who took buprenorphine typically have shorter hospital stays and require fewer withdrawal treatments than newborns born to mothers taking methadone. However, doctors do caution that taking any medication – whether methadone or buprenorphine – is far safer than not taking medications at all when a person has an opiate addiction.
  • Adolescents: Although the FDA has only approved buprenorphine for treatment in those ages 16 and older, the medication is reportedly effective in treating addiction in adolescents. However, there are some concerns regarding misuse or diversion of buprenorphine in this patient population.

Another research project from the National Institute on Drug Abuse studied administering buprenorphine to patients who were on waiting lists for methadone or buprenorphine treatment programs.3 Participants were given a tamper-proof device that would dispense one buprenorphine pill per day to participants. Using this method reduces some of the clinical oversight and monitoring that traditionally is involved within buprenorphine prescriptions. The NIDA conducted two rounds of clinical trials. In the first trial, there were 10 participants that had used opiates for an average of 8.4 years. After taking buprenorphine:

  • 90 percent of participants were negative for illegal opioids at 2 and 4 weeks
  • 60 percent of participants were negative for illegal opioids for 8, 10, and 12 weeks

The researchers also performed a second trial, this time enrolling 25 participants.3 The results of this study included:

  • 90 percent of participants who took buprenorphine provided negative urine samples at weeks 4 and 8
  • almost 70 percent of participants who took buprenorphine provided negative urine samples at 12 weeks

This study also featured a control group, who did not take buprenorphine. At the same time frames, no participants provided opioid-negative urine samples at the end of the trial. While currently, patients must be in a buprenorphine monitoring program to take the medication, the results of this study show promise into new methods to distribute the medication and help others overcome their addiction.

How Long Does Buprenorphine Therapy Last?

There is no definitive timeline for buprenorphine therapy. Doctors do know based on research that patients with co-existing disorders such as untreated medical conditions or mental health disorders, may require long-term therapy.1 They also know that using buprenorphine for too short of a time (such as during a medical detox stay only) carries an increased risk for relapse.

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Buprenorphine Treatment Results

An estimated 2.4 million people in the United States struggle with opioid dependence.5 Because withdrawal symptoms can be so extreme related to opioid withdrawals, many opioid abusers relapse because it is difficult to tolerate the withdrawal symptoms. Treatments like methadone and buprenorphine have aimed to reduce a person’s dependence on opioids, thus saving lives and helping other build new, healthier futures. According to SAMHSA, an estimated 21,236 clients at substance abuse treatment facilities took buprenorphine as a therapy in 2015. As treatment programs expand and more is known about how effective buprenorphine can be in treating opioid addiction, this number will likely rise with time.

If a person is ready to stop abusing opioids, they should talk to their doctor about buprenorphine and if it may be the right treatment for them.