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Buprenorphine

Buprenorphine is used in medication-assisted treatment to treat dependence on opioids including heroin and prescription painkillers like hydrocodone, oxycodone, morphine, and fentanyl.

This article will discuss:

What is Buprenorphine
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What is Buprenorphine and What Does it Treat?

Buprenorphine is known as a partial opioid agonist, meaning it partially works like an opioid, but its effects are weaker than a full agonist opioid like heroin or methadone. Buprenorphine also has a “ceiling effect,” so the opioid effects level off even with further dosage increases. As a result, the risk of misuse, dependency, and side effects are reduced.

Buprenorphine lowers the effects of opioid dependency such as withdrawal symptoms and cravings to use opioids without having full opioid potency or effects.

Buprenorphine has also been used to relieve some forms of chronic pain. However, studies on how effective it is for this purpose are mixed. Many experts believe buprenorphine is not an effective pain treatment in people who aren’t addicted to opioids.

The History of Buprenorphine

Buprenorphine was developed by Reckitt & Colman Products and released in the United Kingdom in 1978. That same year, a clinical study determined that buprenorphine could be helpful in reducing cravings of pure opioids in patients with an opioid abuse disorder. A separate study published in 1982 demonstrated that buprenorphine offered excellent analgesia with blunted abuse potential.

Several medications on the market contain buprenorphine, including:

  • Bunavail (buprenorphine and naloxone buccal film)
  • Probuphine (buprenorphine implant)
  • Subutex (buprenorphine tablet)
  • Suboxone (buprenorphine and naloxone tablet and film)
  • Zubsolv (buprenorphine and naloxone tablet)
  • Buprenex (buprenorphine injection)
  • Butrans (transdermal buprenorphine)

Few buprenorphine medications were developed until Congress passed a law in 2000 that increased the availability of opioid-based medications.

Approved for clinical use in October 2002 by the Food and Drug Administration (FDA), buprenorphine represents the latest advance in medication-assisted treatment. In 2016, the federal government expanded access to buprenorphine treatment again, making it more available today than ever before.

Buprenorphine, when used in combination with counseling and behavioral therapies, provides a whole-patient approach to the treatment of opioid dependency.

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What is Buprenorphine?

Buprenorphine is used in medication-assisted treatment to treat dependence on opioids including heroin and prescription painkillers like hydrocodone, oxycodone, morphine, and fentanyl.

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Buprenorphine for Opioid Dependence

Opioids attach to receptors in the brain that affect pleasure, respiration, and pain. When a person is physically dependent on opioids, their brain is used to receiving a certain dosage of opioids each day. Without opioids, an addicted person goes into withdrawal.

Buprenorphine works by binding to opioid receptors, but it doesn’t bind in the same way other opioids do. It prevents the brain from experiencing withdrawal, but as a partial opioid agonist, its effects on pleasure, respiration, and pain are milder than those of other opioids.

Buprenorphine also blocks other opioids from binding to receptors in the brain. If a person uses heroin after taking buprenorphine, the illicit drug can’t attach to opioid receptors. As a result, the person is unlikely to feel the effects of heroin.

Buprenorphine is a long-acting opioid, and its effects can last from one to three days.

  • Under the Drug Addiction Treatment Act of 2000 (DATA 2000), qualified U.S. physicians can offer buprenorphine for opioid dependency in various settings, including in an office, community hospital, health department, or correctional facility.
  • SAMHSA-certified opioid treatment programs (OTPs)also are allowed to offer buprenorphine, but only are permitted to dispense treatment. Learn more about certification of OTPs.
  • As with all medications used in medication-assisted treatment, buprenorphine is one part of a comprehensive treatment plan that includes counseling and participation in support programs.

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Comparing Buprenorphine Products

The main differences between medications containing buprenorphine are method of administration, timing of administration, and whether naloxone is present.


Suboxone

Suboxone contains a combination of buprenorphine and naloxone. It comes in both tablet and film forms. The tablets dissolve under the tongue, and the film can be placed under the tongue or inside the cheek. Suboxone can be used during all stages of medication-assisted treatment for opioid addiction.

Subutex

Subutex is the brand name for a medication containing buprenorphine. Intended for use during the initial stages of opioid addiction treatment, it came in the form of sublingual tablets that dissolved under the tongue. Subutex does not contain naloxone, an ingredient that acts as a deterrent to continued use of opiate drugs. Subutex in sublingual form was discontinued in 2011 in the U.S., though it is still available in generic form.

Zubsolv

Zubsolv is similar to Suboxone. It comes in tablet form, and it contains both buprenorphine and naloxone. However, Zubsolv has a higher bioavailability of buprenorphine than Suboxone, meaning a lower dose of Zubsolv delivers the same amount of buprenorphine as a higher dose of Suboxone. An average Suboxone film contains 8 mg of buprenorphine along with 2 mg of naloxone, while Zubsolv provides 5.7 mg of buprenorphine against 1.4 mg of naloxone.

Bunavail

Bunavail contains buprenorphine and naloxone, and it comes in a buccal film that is placed inside the cheek. The Bunavail film has a higher bioavailability of buprenorphine than the Suboxone film. A Bunavail buccal film containing 4.2 mg of buprenorphine and 0.7 mg of naloxone is equivalent to a Suboxone film containing 8 mg of buprenorphine and 2 mg of naloxone.

Probuphine

Probuphine is an implant that is placed under the skin in the upper arm. It slowly releases buprenorphine over the span of six months. This option can often be beneficial for patients who forget to take medications on schedule. The implant is only effective in people who have already been stabilized on low-to-moderate doses (doses no more than 8 mg per day) of a buprenorphine-containing product.

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Does Buprenorphine Effectively Treat Opioid Addiction?

Opioid addiction is associated with high rates of relapse, but medication-assisted treatments have higher recovery outcomes than therapy without medication. Numerous studies have found that buprenorphine is more effective than placebo for recovery from opioid addiction.

Additional studies have shown that combination medications containing buprenorphine and naloxone are effective in treating opioid addiction. The presence of naloxone deters abuse and diversion, but it does not reduce the effectiveness of buprenorphine or increase the effectiveness of substance abuse treatment.

Side Effects of Buprenorphine

The side effects of buprenorphine are similar to those of opioids and can include:

  • Nausea, vomiting, and constipation
  • Muscle aches and cramps
  • Inability to sleep
  • Cravings
  • Fever
  • Distress and irritability

Use of Buprenorphine During Pregnancy

Available case reports have not shown significant problems resulting from the use of buprenorphine during pregnancy. The FDA classifies buprenorphine products as Pregnancy Category C medications, indicating that the risk of adverse effects has not been ruled out.

According to The American College of Obstetricians and Gynecologists, recent evidence supports the use of buprenorphine for opioid use disorder treatment during pregnancy. Buprenorphine acts on the same receptors as heroin and morphine, but functions as a partial agonist and makes overdose less likely. Advantages of buprenorphine over methadone include fewer drug interactions, the ability to be treated on an outpatient basis, and evidence of less need for dosage adjustments throughout pregnancy. In addition, several trials demonstrate evidence of less-severe neonatal abstinence syndrome.