What is Buprenorphine?
Buprenorphine, often sold under the brand name Subutex, is a medication that is used to treat people who are addicted to opioids. Taking the drug can help alleviate the symptoms of opioid withdrawal that occur when people stop taking drugs like heroin, oxycodone, or fentanyl.
Buprenorphine is available via a wide variety of routes of administration. These include sublingual methods wherein the drug is dissolved under the tongue or against the cheek, as a skin patch, by injection, or via a surgically implanted device.
The drug has been available in the United States since 1981, and since then it has become an essential drug in the treatment of opioid addiction. As of 2017, 14.6 million prescriptions were written for buprenorphine in the United States alone.
The drug is designed to be used as part of a medication-assisted treatment program (MAT) run by physicians and addiction treatment professionals. Medication-assisted treatment is a type of addiction treatment program that utilizes a combination of medication, psychotherapy, and behavioral health services.
While it can help alleviate the cravings and painful symptoms of opioid withdrawal, it is not a cure. Rather, addiction experts emphasize that buprenorphine treatment is useful early on during a treatment program because, by mitigating the most excruciating symptoms, it can help people be more responsive to other treatment modalities.
It is difficult to get much out of a cognitive-behavioral therapy session, for instance, when one is vomiting or in a cold sweat. Thus, it is essential to take the drug only under medical supervision when one is enrolled in an addiction treatment program like an outpatient treatment center.
Taking the drug without the support of a treatment center or physician is not only ineffective, it can be dangerous. Buprenorphine is an opioid. Unlike other opioid medications, however, buprenorphine is designed to have limited intoxicating or euphoric effects. In fact, taking it at high doses has a “ceiling” that makes it impossible for a person to experience stronger effects.
The usefulness of buprenorphine in opioid addiction treatment lies in the drug’s ability to activate opioid receptors, thereby alleviating cravings and withdrawal symptoms, without, however, providing the same high that recreational opioids offer.
Nonetheless, as an opioid, the drug does come with an assortment of risks. Taking it at higher doses than prescribed or misusing the drug by injecting it can result in an overdose. Buprenorphine abuse, while less common than other forms of opioid abuse, does occur, and the risks ought to be understood.
Buprenorphine History & What’s it Used For
The story of buprenorphine begins with the birth of opioid replacement therapy. During World War II, methadone was used by the United States military to treat the severe pain associated with injuries on the battlefield.
In the years following, physicians discovered that methadone could be used to provide relief to individuals suffering from opioid withdrawal. They recommended a course of action that involved quitting recreational opioids and taking methadone instead. While methadone was itself an opioid, it did not offer the same high and was reported to be easier to quit.
The idea was that over time and under medical supervision, an addicted individual could wean off of methadone, gradually reducing their dosage or dosage frequency, until they were completely sober. This approach was found to be in many cases more effective than simply quitting opioids “cold turkey.” Methadone revolutionized opioid addiction treatment and for many years dominated the market.
Decades passed before the emergence of a new drug that could compete with methadone. That drug turned out to be buprenorphine, which has a similar level of efficacy as well as its own unique advantages.
Buprenorphine was not originally developed to be used for treating opioid addiction. It was developed by researchers at British company Reckitt and Colman who aimed to synthesize a new opioid that would effectively treat pain without offering the negative effects or high risk of addiction that other opioids possessed.
This development process lasted ten years, but eventually animal testing revealed that they had indeed synthesized their dream drug. Studies on animals showed that taking the drug did not result in high levels of intoxication or opioid dependence.
In 1978, the United Kingdom approved the drug for the treatment of pain. Originally making it available only via injection, Reckitt and Colman made available a sublingual formulation in 1982. It was shortly thereafter discovered that when opioid addicts take buprenorphine, their withdrawal symptoms could be managed.
Across the ocean, in the United States the release of buprenorphine was delayed until 2002. A number of controversies surrounded the approval of the medication. At the time, the United States did not allow for narcotics like buprenorphine to be prescribed by physicians who did not work at inpatient addiction treatment centers.
In the years leading up to the approval of the drug, Reckitt and Colman spent money and lobbied Congress to pass the Drug Addiction Treatment Act (DATA), an act that allowed physicians to prescribe narcotics to help their patients detox.
As a result, it has a unique advantage over methadone: whereas methadone can only be taken in specifically licensed inpatient drug addiction clinics, buprenorphine can be prescribed by just about any doctor and can be taken on an outpatient basis.
Nonetheless, to increase protections, the Drug Enforcement Agency reclassified buprenorphine from a Schedule V drug to a Schedule III drug immediately after DATA was passed. This did not stop the Food and Drug Administration from approving it in 2002, after which it emerged as an essential drug in addiction treatment.
In the years following its approval, a number of pilot programs have demonstrated the effectiveness of the medication. New Jersey, for instance, is the first state that allows paramedics to treat overdose victims with buprenorphine. This allows them to treat overdoses as well as help these individuals begin a path of opioid replacement therapy. By treating addiction and connecting victims to long-term treatment approaches, the state’s pilot program is saving lives.
Nonetheless, not all the developments following the approval of the drug have been positive. It has been found that despite the limited nature of buprenorphine’s high, the drug can nonetheless be abused. Illegal buprenorphine is regularly confiscated by law enforcement agencies.
In response to the high abuse potential, pharmaceutical companies developed another drug, Suboxone, that combined buprenorphine with another drug, naloxone. This combination drug makes it far more difficult for it to be abused and is today more frequently prescribed than buprenorphine alone.
How is Buprenorphine Made & Who manufactures it?
Buprenorphine is developed by scientists working in laboratories owned by pharmaceutical companies. As a semi-synthetic opioid, it is actually derived from another substance, thebaine. Thebaine is an alkaloid of the poppy Papaver somniferum. When scientists. When thebaine is modified and transformed into its analogue, buprenorphine, the result is an opioid partial agonist.
Unlike the common recreational opioids, such as heroin and morphine, which are full agonists, partial agonists like buprenorphine do not provide the same degree of side effects or euphoria. It is produced in many different forms, from the buprenorphine patch, which is applied to the skin, to the buprenorphine pill. While buprenorphine is most commonly produced to treat opioid addiction, buprenorphine for pain is manufactured in the same labs.
Buprenorphine Street Names
When it is taken as prescribed, is most commonly known by its brand name or generic medical name. A wide variety of companies produce buprenorphine for a variety of purposes, but some of the most common brand names for buprenorphine are Cizdol, Subutex, Zubsolv, Bunavail, Sublocade, Probuphine, Temgesic, Buprenex, Norspan and Butrans. Each one offers different potency levels and is taken via a unique route of administration — though all of them contain buprenorphine.
However, when the drug is abused or distributed illegally on the black market it is often known by other names. This is because drug dealers prefer to use alternative terms for their products to avoid being detected by law enforcement agencies.
Recreational drug users also often use alternative names for it because drug culture has its own set of terms for drug-seeking, drug-taking, and drug effects. While these vocabularies are ever-changing with the trends, it can be helpful to understand some of the more common street names for buprenorphine. These slang terms include:
- Big Whites
- Small Whites
- Orange Guys
Some of these words apply to buprenorphine alone. However, the slang terms are often used loosely or interchangeably. Therefore, many of these street terms are applicable to the buprenorphine-naloxone combination drug known as Suboxone.
In 2015 alone, researchers at the Substance Abuse and Mental Health Services Administration estimated that 2.4 million individuals in the United States suffered from an opioid use disorder. Most of these individuals never receive treatment.
The opioid epidemic, which has largely been driven by the rise of high-potency synthetic opioids like fentanyl, is inflicting enormous damage on the population. Between 1999 and 2018, the number of people who died from opioid overdoses exceeded 450,000. Looking at the death toll on a more immediate basis, more than 130 people die every day due to opioid overdoses.
The opioid epidemic has only gotten worse since the 1990s, when pharmaceutical companies marketed opioid analgesics as risk-free and non-addictive medications for treating pain. In 2010, widely available and affordable black tar heroin exacerbated the opioid epidemic. In 2013, fentanyl and other illicitly produced synthetic opioid analogues drove the death rate even higher.
Of the millions of individuals who are currently addicted to opioids, most will never receive treatment. One of the primary reasons people avoid opioid addiction treatment is the belief that opioid withdrawal is necessarily excruciating — or even intolerable.
A large body of research has confirmed the efficacy of the drug for treating opioid dependence. A Swedish study, for instance, compared the effects of buprenorphine with a placebo. Half of the individuals in the study were given it for a short period of time and were then switched over to placebos. The other half took a regular dose of buprenorphine consistently during the duration of the study.
The results of the study were quite striking. Among the placebo-treated individuals, the dropout rate for treatment was 100%. However, the group given buprenorphine only had a 25% dropout rate.
A meta-analysis of the study concluded that patients who receive buprenorphine are 1.82 times more likely to stay in treatment programs compared to those who do not receive the medication. They are also 14.2% less likely to test positive on opioid tests.
However, the most important conclusion the study reached was that individuals who drop out of treatment programs have a 20% mortality rate. This means that receiving buprenorphine is often a matter of life and death to people suffering from opioid addiction.
Fortunately, buprenorphine is becoming more widely available. While methadone has been the most popular and well-known opioid replacement drug for a long time, it is also quite dangerous: 1 in 3 prescription opioid overdoses is directly attributable to methadone abuse. The number of Opioid Treatment Programs offering buprenorphine has increased from 11% to 2003 to 58% in 2015.
Research suggests that buprenorphine has a similar efficacy to methadone, but it allows individuals more flexibility, since it can be prescribed on an outpatient basis. The emergence of buprenorphine has given both doctors and people suffering from addiction an increased range of options for opioid addiction treatment.
How Does Buprenorphine Work to Treat Opioid Addiction?
Buprenorphine is generally prescribed in the context of an opioid addiction treatment program, most notably a medication-assisted treatment (MAT) program. Unlike methadone, it can be prescribed on an outpatient basis, allowing for more flexibility.
Due to the buprenorphine half life and its rapid onset, it is most frequently prescribed for short-acting opioids, though buprenorphine can be used on a long-term basis under medical supervision as well.
Taking buprenorphine helps individuals get relief from some of the more deleterious effects of opioid withdrawal. Opioid withdrawal results in a wide range of symptoms. Some of the more common symptoms of opioid withdrawal that buprenorphine alleviates include:
- Cold flashes and goosebumps
- Sleep problems
- Gastrointestinal problems, such as diarrhea and vomiting
- Uncontrollable leg movements
- Muscle and bone pain
- Severe cravings
Individuals in MAT programs usually begin taking buprenorphine after stopping recreational opioid use. During the beginning, it is inevitably that a person will experience some degree of withdrawal symptoms. However, buprenorphine reduces the intensity of the physical symptoms, the mental unease, and the cravings. It does so by activating the same opioid receptors that recreational opioids activate, preventing the body from reacting to a lack of opioids.
Buprenorphine, however, unlike other opioids, does not offer the same intensity of high. This allows individuals to remain functional. By helping people in early recovery reduce cravings and remain functional, buprenorphine therapy allows them to engage in other treatment modalities that ensure their long term sobriety.
The maintenance phase of buprenorphine treatment can have variable lengths. Some people maintain their dosage of buprenorphine for several weeks or months. Others stay on buprenorphine for years. Ultimately, the length of time depends on a number of factors particular to the individual, such as their mental health, the severity of their addiction, and the stability of their life.
When medical professionals and addiction treatment experts deem it safe, however, they will generally work with patients to begin the next phase. The final phase of buprenorphine treatment is the tapering phase.
Taping, sometimes referred to as weaning off, is a process of gradually reducing buprenorphine dosage. Doing so slowly and methodically ensures that withdrawal symptoms do not return with a vengeance. It is also important to taper off of buprenorphine under proper medical supervision to ensure that there are no complications. While tapers can have varying lengths, once a person is off of buprenorphine, they are entirely opioid-free.
However, it is important to emphasize that addiction treatment does not end when a person has quit opioids or stopped taking buprenorphine. Buprenorphine is a tool that helps people in the initial days of addiction treatment, but even when it is no longer necessary, those who hope to remain sober long-term must continue to manage their substance use disorders.
There is no ultimate cure for addictions; no matter how long one has remained physically sober, it is necessary to continue to treat and manage the condition to prevent a relapse.
How is Buprenorphine Abused?
While buprenorphine is designed to provide less intense of a high than other opioids, this is only true when it is used as prescribed. Nonetheless, abusing buprenorphine is possible. Many people who are legitimately prescribed buprenorphine may be tempted to take it more frequently than prescribed or to take larger doses than recommended.
These individuals may be misusing buprenorphine because they are seeking relief from the symptoms of opioid withdrawal, or they may simply be trying to get high. A thriving black market for buprenorphine also exists. While it is rarely the first drug of choice for recreational opioid users, its wide availability and ability to help with the symptoms of opioid withdrawal has resulted in increased popularity.
Even though many of the people misusing or abusing the drug are doing so to get relief from withdrawal symptoms, that doesn’t make their illicit buprenorphine abuse any safer. In fact, taking it without proper medical supervision or guidance is likely to result in medical complications. Regular abuse without the structure of a treatment program can actually worsen opioid addiction. Inconsistent or overly high doses can lead to an opioid overdose.
Individuals who aim to get high off of the drug face numerous obstacles. The nature of the drug itself is the main one: It has a ceiling after which it is impossible to get any higher, even if greater quantities of the medication are taken. Nonetheless, by tampering with the medication it is possible to get high. Many dissolve their medications in water in order to inject it directly into their bloodstreams.
Doing so can help drug users achieve the euphoric effects that are normally difficult to obtain with buprenorphine. However, injecting it makes a life-threatening overdose likely. When recreational users combine the drug and alcohol, or with other depressants or stimulants, the risk of a life-threatening overdose further increases. Interactions make it difficult for the cardiovascular and respiratory systems to keep up with demands, which can lead to respiratory failure.
It is also important to understand that when buprenorphine is combined with naloxone, in the case of the combination drug Suboxone, injecting the drug will not result in a high. Suboxone was developed to prevent the abuse of buprenorphine. When this combination drug is taken as prescribed sublingually, the buprenorphine functions normally. However, when it is injected the presence of naloxone sends users into immediate opioid withdrawal. Unsupervised opioid withdrawal is not only excruciatingly painful, it can lead to health complications.
Who is Most Likely to Become Addicted to Buprenorphine?
While buprenorphine is open to abuse by just about anyone, ranging from legitimate prescription holders to people buying it on the black market, the most common indicator that a person is likely to abuse the medication is a history of substance abuse.
Suffering from a substance use disorder makes people more likely to abuse buprenorphine, either because they are seeking to get high or because they hope to obtain relief from the debilitating withdrawal that follows getting high.
While physicians must prescribe buprenorphine to addicts, it is ironically this very population that is most likely to misuse and abuse buprenorphine. While some people who are prescribed buprenorphine for their opioid dependence will use it as prescribed, others may only do so for a short period of time before abusing it or relapsing entirely. Doctors must operate on good faith alone.
While no one is destined for addiction, a number of factors do increase the likelihood that an individual will suffer from an opioid use disorder during their lifetime. None of these factors cause addiction in isolation, but when a number of these factors predominate together, a person should exercise caution because they are more vulnerable to addictive behavior. These factors include:
- Trauma. Suffering from trauma, especially during early childhood, is correlated with higher rates of substance use disorder. Individuals who suffer from post-traumatic stress disorder (PTSD) are particularly vulnerable.
- A history of addiction in the family. Individuals whose parents abused illicit drugs have a 45% to to 79% increased risk of developing substance use disorders themselves. Addiction has a genetic component, but early exposure through the examples of family members can further entrench a person in addiction. The behavior of addicted family members can also lead to a traumatic and unpredictable upbringing, which can drive people to illicit substances as a way of achieving temporary relief and calm.
- Chronic pain. The majority of opioid addictions actually begin when a person is prescribed opioids to treat legitimate problems. Individuals who suffer from chronic or severe pain are the most likely to be prescribed opioids. Some people misuse or abuse the medications, but even those who use them as prescribed are at a high risk of developing a dependence. Over time, many turn to heroin or to higher potency synthetic opioids, such as fentanyl.
- Mental health conditions. Aside from PTSD, other mental illnesses like depression, anxiety, bipolar disorder, and schizophrenia increase the likelihood that a person will abuse drugs and develop a dependence on them. This is because substance abuse for many people begins as a form of self-medication. Illicit drugs like opioids can provide relief for many of the symptoms of mental illness, though drug abuse tends to worsen these symptoms over time.
- Poverty and lack of resources. Suffering from poverty, especially early on in life, is highly correlated with increased substance abuse patterns. Individuals who suffer from poverty are also less likely to have access to proper addiction treatment facilities and resource centers.
- Limited social support system. Individuals with smaller friend groups and social support systems are more likely to turn to drug abuse. Having a stronger social support system also improves addiction treatment outcomes. Unfortunately, drug addiction tends to drive people into further isolation, which results in a vicious cycle that exacerbates drug addiction.
It is important to understand that even though the above-listed factors increase the likelihood of a person suffering from addiction, many people with substance use disorders successfully use buprenorphine as a tool in their addiction recovery. The single greatest factor that determines whether or not a person will abuse buprenorphine is their level of involvement in a substance use disorder treatment program.
Medical detox programs, outpatient programs, and inpatient programs allow people to have access to addiction professionals, medical guidance, and to develop a firm sober social support system that facilitates long-term sobriety. Using buprenorphine in this context decreases the likelihood that the drug will be abused, but moreover it increases the likelihood that an individual will avoid relapse over the long term.
Signs of Buprenorphine Abuse and Withdrawal?
Buprenorphine abuse follows similar patterns to other forms of opioid abuse. When the drug is taken as prescribed, it can be used to release a person from the cycle of opioid dependence. When the drug is taken to get high or at improper doses, the result is an opioid high, which can impair a person’s ability to function normally.
The side effects of buprenorphine range from the physical to the psychological. The intensity and longevity of these symptoms depends on the route of administration, the dosage, and the personal history of the person taking the drug. Common side of effects of buprenorphine abuse include:
- Muscle pain
Not all of the above-listed symptoms are life-threatening. Many of them, however, can make it difficult for a person to function successfully in their own lives. When a person is taking buprenorphine as prescribed, they may struggle, but each passing day brings them closer to sobriety and full-functionality as they begin to implement new skills and make positive life changes.
However, buprenorphine abuse, as with other forms of opioid abuse, can inflict enormous damage on a person’s life, weakening or harming interpersonal relationships, causing financial and legal problems, and causing or exacerbating existing health problems.
Buprenorphine abuse can also lead to life-threatening overdoses, especially when it is used in conjunction with other recreational drugs like alcohol or benzodiazepines.
Symptoms of a buprenorphine overdose include:
- Blurred vision
- Constricted pupils
- Loss of coordination
- Gastrointestinal distress, including vomiting, nausea, and stomach pain
- Loss of consciousness
- Heavy sweating
- Slurred speech
While buprenorphine is designed to treat the symptoms of opioid withdrawal, it is important to understand that those who abuse it are likely to go into withdrawal as a direct consequence of this abuse. Furthermore, opioid withdrawal is an inevitable part of even proper medical usage of buprenorphine; when addicts in recovery begin the tapering phase of their buprenorphine treatment, some degree of withdrawal symptoms is inevitable.
Nonetheless, when proper protocol is followed and buprenorphine doses are tapered slowly, the withdrawal symptoms are weaker in intensity than other recreational opioids.
Symptoms of buprenorphine withdrawal include:
- Gastrointestinal problems, such as diarrhea, vomiting, and abdominal cramps
- Muscle and bone pain
- Cold flashes and goosebumps
- Muscle spasms and uncontrollable leg movements
- Runny nose
- Constricted pupils
- Sleep problems, ranging from insomnia to oversleeping
- Fluctuating blood pressure
- Severe cravings
The majority of these symptoms begin within hours after stopping buprenorphine use. Symptoms of opioid withdrawal reach their peak a few days after quitting, after which they gradually wane over the following weeks. Most people find that after a month, most symptoms have disappeared or have become significantly less severe. Following a medically supervised tapering schedule is the best way to reduce the symptoms of opioid withdrawal.
Individuals who quit buprenorphine without assistance “cold turkey” are at the highest risk of suffering from severe symptoms. Rapid and unsupervised withdrawal from buprenorphine can even lead to health complications, especially when an individual suffers from other health conditions. While buprenorphine withdrawal can indeed be a healthy and necessary element of addiction treatment, doing so in the context of a treatment program is requisite for long-term sobriety.
Why is Buprenorphine Addictive?
As an opioid replacement therapy drug, buprenorphine is helpful precisely because it does satisfy the needs of opioid addiction. Buprenorphine, like other opioids, works by activating the opioid receptors that are naturally located throughout the brain and body. When opioids turn on these opioid receptors, the brain responds by releasing enormous quantities of dopamine.
Dopamine is a neurotransmitter that is released when the brain wants to reward itself. It can be released when a person wins a match of tennis or has sex. This feel-good chemical plays an important role in the brain’s decision-making, since it works by reinforcing behavior. Because opioids release such high amounts of dopamine, the drug-taking behavior rapidly becomes reinforced, leading people to abuse buprenorphine even if they have no conscious desire to get high.
The chemical changes that dopamine creates in the brain are only the beginning of the story, however. Over time, the brain actually acclimates to the effects of opioids. This phenomenon, known as desensitization, comes about when the brain manufactures more opioid receptors as a response to opioid abuse. When these receptors increase, a user must take more frequent or larger doses of buprenorphine to achieve the same effects.
Doing so is likely to further entrench a person in the cycle of dependence. As tolerance to the effects of opioids increases, so too do the withdrawal symptoms that accompany the absence of the drug. Most users find these withdrawal symptoms so excruciating that they will do just about anything to obtain buprenorphine or another opioid. At this point, the combination of tolerance and withdrawal-avoidance has resulted in opioid dependence.
Most addiction experts stress that opioid dependence and opioid addiction are two separate phenomena. Some people suffer from opioid dependence and are able to quit on their own. Addiction, however, is characterized by an inability to stop using drugs despite negative consequences and a strong desire to do so.
Addiction, which stems from a variety of factors ranging from the genetic to the interpersonal, is nonetheless a natural and common consequence of opioid dependence. Ironically, buprenorphine is prescribed to treat opioid dependence. While this drug can provide relief from the symptoms of withdrawal, when it is taken outside the context of an addiction treatment program it is likely to exacerbate opioid dependence.
Buprenorphine Addiction Treatment
Rarely do people develop opioid addictions from using buprenorphine alone. The majority of opioid addictions in the United States stem from prescription pain relievers. Currently the most problematic drugs responsible for the United States’ opioid epidemic are high-potency synthetic opioid analgesics such as fentanyl, though black tar heroin also plays a destructive role as well.
Nonetheless, buprenorphine addiction is a serious condition that directly stems from the high rates of addiction associated with these other drugs. Individuals who abuse buprenorphine generally do so because they hope to obtain relief from the painful symptoms of withdrawal they experience when they do not have access to recreational opioids. While some people misuse buprenorphine in an effort to treat their addiction, doing so without outside help is likely to exacerbate the addiction in the long run.
It is important to understand that buprenorphine addiction and other opioid addictions cannot be cured through solo efforts. While our culture stigmatizes addiction and constantly relays the message that people need to be independent, strong-willed, and pick themselves up by their bootstraps, addiction is a serious medical condition that requires outside intervention.
Suffering from addiction does not make one weak or “less than.” It can happen to anyone, from the most destitute people to those who feel they have everything. Reaching out for help can be embarrassing or seem difficult, but it is in fact an act of courage.