Buprenorphine

Written by: Editorial Staff

Last updated on March 17, 2021

Buprenorphine is a therapeutic drug used in the treatment of heroin and other types of opioid dependence. It is approved by the FDA for use in both short-term medical detox programs, as well as longer-term maintenance and relapse prevention programs. This makes it a useful tool in the fight against opioid addiction.

According to the National Institute on Drug Abuse (NIDA), deaths due to overdose of opioid drugs such as heroin and prescription painkillers increased almost threefold from 2002 to 2015.¹ While buprenorphine alone is not enough to prevent overdose death or treat opioid addiction, it is considered a valuable piece of the addiction treatment package.

Commonly used in what is called medication-assisted treatment (MAT), buprenorphine is combined with behavioral counseling and other strategies used to treat the whole person and the individual factors that led to their addiction in the first place.²

Heroin addiction is a disease that can’t be overcome without professional help. Yet when it comes to heroin rehab, one size does not fit all. Luckily, there are different treatment options that speak to the unique needs of recovering individuals. Read More

What Is Buprenorphine?

Buprenorphine is a synthetic opioid medication that acts as a partial agonist at the opioid receptor. For managing opioid dependence, it can be taken as a sublingual tablet or administered via a longer-term, steadily-released implant (Probuphine). Buprenorphine is also combined with the opioid antagonist naloxone in the brand-name drug Suboxone. Both buprenorphine and Suboxone work to lessen withdrawal symptoms and help addiction patients avoid relapse.³

How Does Buprenorphine Work?

Buprenorphone activates the brain’s opioid receptors enough to curb the intensity of withdrawal symptoms and help prevent cravings.

Opioid agonists are substances that produce a physical response when they bind to opioid receptors in the brain. Heroin and prescription opioid painkillers such as morphine or oxycodone are full opioid agonists, meaning that they fully activate the brain’s opioid receptors, creating the pleasurable, euphoric sensation for which they’re sought after.⁴

As a partial opioid agonist, buprenorphine binds to opioid receptors in the brain, but activates them to a lesser extent than full agonists.⁴ When used as directed, buprenorphine activates the brain’s opioid receptors enough to curb the intensity of withdrawal symptoms and help prevent cravings, but not enough to elicit the euphoric highs associated with other abused opioids.⁵

This is different than opioid antagonists, such as naloxone and naltrexone. These medications completely block the activation of opioid receptors, meaning that the brain’s receptors will not produce any pleasurable effects even in the presence of opioid drugs.⁴ Naloxone has proven indispensable in treating overdose patients in emergency situations, while naltrexone is useful in deterring ongoing opioid abuse after patients have detoxed from heroin.

What Is Buprenorphine Used For?

Buprenorphine is mainly used in two ways during the recovery process. The first is during detox and the initial treatment phase, when buprenorphine is prescribed to reduce or eliminate withdrawal symptoms. When people stop using heroin or other opioids, they may experience a wide range of uncomfortable withdrawal symptoms that can include nausea, intense pain, diarrhea, and vomiting. Buprenorphine is administered to help manage these symptoms, reduce cravings, and help reduce the chances of relapse.⁶

It helps people in recovery stay clean and avoid using other drugs.

The second way buprenorphine is used is during the maintenance period after acute withdrawal has ended. Addiction patients might take buprenorphine for anywhere from a few weeks to several months or even years during long-term maintenance.⁴ This helps people in recovery stay clean and avoid using other drugs. A clinical review published in the Journal of Addictive Diseases found that maintenance treatment with buprenorphine helps patients stay in treatment, reduces their illegal opioid use, reduces cravings, and helps them function better in a social context.⁷

During the acute withdrawal phase, buprenorphine works best if people take it within 8 hours of their last use of heroin or other opioids. The length of time patients take the drug depends on how long their withdrawal symptoms last, and whether they continue to take buprenorphine during the maintenance period.⁴

When you enter rehab for opioid addiction treatment, your doctor will conduct an evaluation to determine if buprenorphine is right for you and evaluate your case to determine how long you’ll need to take the medication. Call 1-888-496-8059 Who Answers? today to learn more about the medication-assisted treatment and recovery options that might be right for your needs.

Dependence and Withdrawal in Opioid Addiction

One of the reasons opioid drugs like heroin and prescription painkillers are highly addictive is because of the cycle of tolerance, dependence, and withdrawal that accompanies prolonged use. With continued drug use over time, a person requires more of the drug to achieve the same desired results. This is a state known as tolerance.

In seeking the pleasurable effects of opioid drugs, users who have built up a tolerance will take the drug in larger quantities and increasing frequency, which inevitably quickens the onset of physiological dependence. This means that the body and brain adapt to the presence of the drug and need it in order to function normally.⁸

When people who are dependent on heroin or prescription opioids stop using drugs suddenly, they can experience severe withdrawal symptoms. Although opioid withdrawal is not usually lethal, it can cause extreme discomfort and distress and is a difficult period to get through. Without the help of a medically managed detox and rehab program, many people will return to drug use just as a way of avoiding withdrawal symptoms. This is the cycle that leads people into addiction, which is marked by continued drug use despite negative social, physical, legal, financial, and psychological consequences.⁸

Managing Withdrawal with Buprenorphine

When patients enter addiction treatment, doctors frequently prescribe drugs like buprenorphine to manage withdrawal symptoms, alleviate pain, and help make the detox and withdrawal process as comfortable as possible.⁹ As discussed above, buprenorphine is a partial opioid agonist, so it stimulates the brain’s opioid receptors enough to lessen the severity of withdrawal symptoms, without the euphoric high and addictive properties of a full agonist.

Patients can slowly wean themselves off opioids by taking increasingly smaller doses of the maintenance drug.

By providing patients a tapering dose of buprenorphine over a customized timeline, treatment specialists give patients a better chance at success in their recovery programs. Rather than quitting opioids “cold turkey” and experiencing the full force of withdrawal symptoms, buprenorphine patients can slowly wean themselves off opioids by taking increasingly smaller doses of the maintenance drug over a predetermined time period. When withdrawal symptoms are tolerable, patients are better able to cope with them and stick to their addiction treatment program.

There isn’t just one detox protocol for all buprenorphine patients—the stabilizing dose and tapering timeline will differ depending on each patient’s individual needs and their doctor’s recommendations.

Buprenorphine vs. Methadone

Buprenorphine and methadone are both medications that are used to treat heroin and opioid addiction. Methadone was the first medication used on a large scale, and it provides a number of benefits, such as reducing cravings, decreasing heroin use, and increasing the likelihood that people will remain in treatment.¹⁰

Among addiction professionals, buprenorphine is increasingly becoming the preferred treatment medication over methadone because of the superior benefits provided by buprenorphine during the withdrawal period. These advantages include:^3,11

• Buprenorphine is less likely to produce a physical high than methadone.
• Methadone has a greater risk of addiction than buprenorphine and a greater likelihood of patient abuse.
• Methadone also carries a higher chance of overdose. One study found buprenorphine to be 6 times safer than methadone in terms of overdose risk.¹²
• For some patients, it’s easier to taper off buprenorphine than methadone. For this reason, doctors might initially prescribe methadone early on in a patient’s treatment and then switch them to buprenorphine when they are ready to detox from methadone or from opioids completely.
• Buprenorphine can be administered by any qualified physician, as opposed to methadone which must be dispensed from a designated methadone clinic—a factor that is often a barrier to patients’ recovery if a methadone clinic is not conveniently located.

How Does Buprenorphine Affect the Body vs. Methadone?

Methadone is a full opioid agonist, as opposed to buprenorphine which is only a partial agonist.³ Methadone blocks the effects of heroin and other opioids while reducing pain and other withdrawal symptoms, but because it is a full agonist, methadone can more easily lead to addiction than buprenorphine.

Methadone can cause several side effects, such as:¹¹

• Difficulty breathing.
• Shallow breathing.
• Feelings of lightheadedness.
• Feeling faint.
• Hives or rashes.
• Chest pain or racing heart.
• Hallucinations or confusion.

Buprenorphine can also result in certain side effects, including:³

• Nausea, vomiting, and constipation.
• Muscle aches or cramps.
• Cravings.
• Insomnia.
• Distress or irritability.
• Fever.

Because buprenorphine is a long-acting medication, some patients don’t need to take it on a daily basis.³ It is, however, critical to take buprenorphine on the schedule recommended by your doctor. It is also advisable to avoid using other drugs, such as benzodiazepines or alcohol, while taking buprenorphine.⁴

Who Can Administer Buprenorphine?

The Controlled Substances Act of 1970 classifies drugs under schedules based on the degree of their potential for addiction and abuse, which determines the level of restriction and regulation governing the substances approved for medicinal use. Methadone is classified as a Schedule II drug, which means it needs to be administered in a specialized methadone clinic. Buprenorphine, however, is listed as a Schedule III drug and therefore can be dispensed by any qualified physician who has completed the necessary requirements.¹³

Physicians qualified to administer buprenorphine can work in a variety of opioid dependency treatment settings, including hospitals, addiction centers, or even certain primary care offices. Call 1-888-496-8059 Who Answers? to speak with a treatment adviser who can help you locate a treatment center that is authorized to administer buprenorphine.

Is Buprenorphine Addictive?

Buprenorphine has some potential for abuse, but it is much lower than the potential associated with heroin or other opioids.³

Buprenorphine in Suboxone

Suboxone is another drug that is becoming widely used in addiction treatment. Suboxone is a combination of buprenorphine and naloxone, an opioid antagonist most commonly used in emergency situations to reverse the effects of heroin overdose.

Naloxone works by blocking opioid agonists from binding to the opioid receptors in the brain, and kicking off any opioid molecules that have already latched on to a receptor. Overdose victims who are given naloxone are typically revived within minutes and have no lingering high from the drug they overdosed on. In fact, many patients go into withdrawal shortly following a naloxone dose because their opioid receptors are no longer being stimulated, even if they still have opioids in their system.

The addition of naloxone to buprenorphine reduces the potential for Suboxone to be abused or diverted for sale. When taken as directed, the buprenorphine in Suboxone goes to work to manage withdrawal and reduce cravings. But if a user attempts to snort or inject Suboxone to get high, the naloxone in the drug kicks in and blocks the brain’s opioid receptors—not only preventing the patient from getting high, but actually inducing their withdrawal to worsen.⁶

Treating Addiction to Heroin or Other Opioids

Buprenorphine is only one component of a comprehensive opioid addiction treatment plan. The most effective method of treating opioid dependency combines therapeutic medications with counseling and behavioral therapies.⁶

Counseling is beneficial for helping you identify dysfunctional thoughts and behaviors, stop negative patterns, and achieve abstinence.

The counseling provided as part of an addiction treatment plan can help you identify and work through issues that contributed to either your heroin addiction or other form of opioid addiction. Behavioral therapies used by rehab programs include cognitive-behavioral therapy and contingency management. These methods are beneficial for helping you identify dysfunctional thoughts and behaviors, stop negative patterns, and achieve abstinence.¹⁴ In addition, many people participate in 12-step groups such as Narcotics Anonymous or other types of support groups as a way of maintaining abstinence throughout their recovery.

If you or someone you love is struggling with an addiction to heroin or other opioids, don’t wait until it’s too late to get help. You don’t need to suffer any longer. Call 1-888-496-8059 Who Answers? to speak to a support specialist about opioid treatment programs that will fit your needs. We are available 24/7 to assist you.

Sources

1. National Institute on Drug Abuse. (2017). Overdose Death Rates.
2. National Institute on Drug Abuse. (2016). Effective Treatments for Opioid Addiction.
3. Substance Abuse and Mental Health Services Administration. (2016). Buprenorphine.
4. Substance Abuse and Mental Health Services Administration. (2005). Quick Guide for Physicians Based on TIP 40—Clinical Guidelines for the Use of Buprenorphine in the Treatment of Opioid Addiction.
5. National Institute on Drug Abuse. (2012). Principles of Drug Addiction Treatment: A Research-Based Guide (Third Edition)—Opioid Addiction: Methadone.
6. National Institute on Drug Abuse. (2014). Heroin: What are the Treatments for Heroin Addiction?
7. Bart, G. (2012). Maintenance Medication for Opiate Addiction: The Foundation of Recovery. Journal of Addictive Diseases, 31(3),207–225.
8. National Institute on Drug Abuse. (2007). The Neurobiology of Drug Addiction: 8: Definition of Dependence.
9. National Institute on Drug Abuse. (2014). Heroin: Letter from the Director.
10. Mattick R.P., Breen C., Kimber J., Davoli M. (2009). Methadone Maintenance Therapy Versus No Opioid Replacement Therapy for Opioid Dependence. Cochrane Database of Systematic Reviews 2009, (3):CD002209.
11. Substance Abuse and Mental Health Services Administration. (2015). Methadone.
12. Marteau D, McDonald R, Patel K. (2015). The relative risk of fatal poisoning by methadone or buprenorphine within the wider population of England and Wales. BMJ Open 2015;5:e007629.
13. Substance Abuse and Mental Health Services Administration. (2017). Buprenorphine Waiver Management.
14. Substance Abuse and Mental Health Services Administration. (2016). Treatments for Substance Use Disorders.