What is buprenorphine?

Buprenorphine is a mixed opioid receptor partial agonist/antagonist. Is it an opioid? Yes it is, but it is different from other opioids.

Buprenorphine works differently from other opioids. It binds to the opioid receptor and remains bound to the receptor. This persistant binding of buprenorphine and the opioid receptor is the blocking action of buprenorphine. By staying on the receptor, it blocks other opioids, and even the body’s natural endorphins, from activating the blocked opioid receptor.

When a person takes an opioid, such as oxycodone, fentanyl, or heroin, the drug molecules bounce on and off of the opioid receptors repeatedly. With each binding, the opioid molecule fully activates the opioid receptor.

There are other opioid receptor blockers that work similarly to buprenorphine, with respect to the blocking action of the molecule. For example, naltrexone and naloxone are both opioid receptor blockers, binding strongly to the receptor and preventing other opioid-type molecules from activating the receptor. 

What makes buprenorphine different from these other opioid receptor blockers? The difference is that buprenorphine, while it is blocking opioid receptors, it also partially activates the receptor. Buprenorphine does not fully activate the receptor, like most other opioids. It only partially activates it.

This partial activation of the opioid receptor is the reason that buprenorphine is classified as an opioid. This classification is somewhat unfair. Buprenorphine does not have many of the negative effects of other opioids.

Most opioids cause the user to become tolerant, where more opioid is needed to get the same effect over time. Buprenorphine typically does not cause opioid tolerance. 

Additionally, buprenorphine has fewer side effects compared to other opioids. It also has less of a risk of leading to overdose.

So, while buprenorphine is categorized as a mild opioid, it is very different from other opioids. It is really in a class of its own.

Is buprenorphine addicting?

Some people worry about buprenorphine treatment for opioid addiction. They think that it is simply trading one addiction for another. Can a buprenorphine patient get addicted to the drug?

First, it is very important to point out the difference between addiction and physical dependence. Addiction is self-harming behavior that is characterized by cravings for a drug and the compulsion to keep using the drug. Physical dependence, on the other hand is a condition where the body or brain has developed a physiological dendence, such that the person will feel sick if they quit taking the drug suddenly.

A person can be addicted and physically dependent on a drug. It is also possible to be addicted to a drug and not physically dependent. And, importantly, it is possible to have a physical dependence without being addicted.

When a patient takes buprenorphine as treatment for opioid addiction, the patient does develop a physical dependence on buprenorphine. However, they typically do not exhibit addictive behavior during treatment. They do not crave buprenoprhine, and they do not feel a compulsion to keep taking more of it.

Is buprenorphine a controlled substance?

Yes, it is a controlled substance. Because buprenorphine is defined as an opioid, and the government considers it to have some abuse potential, it is controlled.

While most opioids are classified as Schedule II, meaning that they have a very high abuse potential, buprenorphine is a Schedule III. It has a lower risk of abuse, and it is uncommon for a drug abuser to attempt to abuse buprenorphine.

Is buprenoprhine the same as methadone?

Both buprenorphine and methadone are used to treat opioid addiction. Methadone is a full opioid agonist, while buprenorphine is a partial agonist and antagonist. 

Methadone is a much more dangerous drug compared to buprenorphine. Patients can get up to a one month prescription of buprenorphine from their doctor, where methadone patients must go to a methadone maintenance clinic each day to get their daily dose dispensed.

Is buprenorphine a pain reliever?

Before 2000, when Congress passed the law to allow doctors to prescribe buprenorphine to treat opioid dependence, buprenorphine was used as a pain reliever. For example, there was the injectable Buprenex, which contained buprenorphine and it was used to treat pain.

Currently, there is a patch, known by the brand name, Butrans, which is left on the skin for a week at a time, and it releases small, continuous levels of buprenorphine. Butrans is approved by the FDA for the treatment of chronic pain.

Patients who are treated for opioid use disorder, who also have chronic pain syndromes, often note that their pain is improved with buprenorphine treatment. Buprenorphine is very effective at treating opioid addiction, and it is also an effective pain reliever.

Drug Addiction Treatment With Medication-Assisted Treatment

What is the best way to prevent relapse? When it comes to substance abuse, nothing is more difficult to quit, or more dangerous, than an opioid or opiate. Mental health experts have struggled with various forms of therapy to find a way to treat this addiction and to keep people in sobriety. After many years of trying just about everything, we must conclude that treatment for drug addiction works best when medication is used when the drug of choice is an opiate. In fact, alcohol addiction can be treated with medication as well in a similar manner.

Withdrawal symptoms are a major reason that people avoid treatment.

To an outsider, it may seem like the solution is obvious. Suffer through a few days of withdrawal symptoms and then just don’t use the drug again. Unfortunately, this sort of treatment, or lack of treatment, is ineffective. First of all, withdrawal symptoms are often severe and intolerable. For someone who has not experienced prolonged opioid withdrawal symptoms, words cannot express the suffering involved in getting through the withdrawal period after quitting an opioid. And, this time period can be much longer than just a few days. While there are medications to ease withdrawal somewhat, the benefits are minimal and we must be aware of potential side effects.

Treatment programs can help people with medical addiction treatment.

Medication-assisted treatment is considered to be the gold standard of opioid addiction treatment and relapse prevention. While short-term treatment can help, it has been shown that long-term maintenance of medical treatment works best. Drug addiction is a difficult condition to overcome. When it comes to opioid and opiate addiction, it can be much harder than other addictive drugs. First, opioid withdrawal symptoms are very difficult to face. Additionally, a relapse can be a far more life-threatening situation with an opioid compared to many other drugs. Not to mention, medical professionals prescribe opioid pain relievers regularly for acute pain, sometimes without being aware that the person has an addiction issue. Ongoing therapy with medication-assisted treatment for opioid addiction can provide the medical and therapy support that the patient needs to avoid relapse and to maintain sobriety.

Methadone is still the gold standard of medical addiction treatment.

While it would be great if we did not need methadone, it is still the gold standard. Methadone has a 75% success rate in treating opioid addiction, which is quite high. We are hopeful that addiction medicine scientists will come up with new safer and more effective treatments in the future, but, in the meantime, we have three main medications to work with: methadone, buprenorphine and naltrexone. Methadone has the highest success rate of the three. Still, naltrexone and bupe have a respectable 50% success rate, which is far higher than treatment that does not involve medication therapy.

Naltrexone helps with alcohol addiction and opiate addiction.

Naltrexone would seem to be the best medical treatment available for addiction. It has the ability to reduce cravings for an opioid or opiate. And, it can reduce cravings for alcohol for an alcoholic. There have been reports that it may reduce cravings for other drugs as well, though I am not aware of any drug abuse studies that confirm this. Unfortunately, this substance abuse treatment medication has limited use because the patient must be clean from opioid and opiate drugs for an extended period of time. However, drug treatment programs have a unique opportunity to start patients on this medication if the person has already been clean as an inpatient for at least a week. Alcohol patients can be started on naltrexone right away, as long as they have not been using an opioid as well. Disulfiram is an additional medication that can help an alcoholic to remain sober.

Mental health treatment programs are an important part of medical addiction treatment.

Cognitive behavioral therapy as well as other forms of mental health treatments for addiction patients can be essential. The best chance of long-term recovery requires psychotherapy in addition to medication-assisted treatment. In fact, psychotherapy is an integral part of MAT. So, if someone is prescribed Suboxone or another form of buprenorphine with naloxone, counseling must be recommended as a core part of the rehabilitation program. In rehab, behavioral therapies must be included not only as major part of the rehab program, but also in aftercare as an outpatient.

Medical addiction treatment is the first step to long-term sobriety.

Helping with behavioral issues and providing support with medical therapies as a part of drug rehab and private addiction treatment can greatly increase the chances of success, particularly with respect to opioid and opiate addiction. This is important because of the dangers of relapse on these highly toxic drugs, particularly the opioids that are on the streets today. It is time that rehab programs start providing full medical addiction treatment to high-risk patients. Using the best tools available will help to increase success rates in both the residential treatment center and private treatment outpatient program.

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