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What is Buprenorphine

What is Buprenorphine

According to statistics published by the National Survey on Drug Use and Health, approximately 948,000 people in the United States said they’d used heroin in the previous year. The number of users has increased steadily since the year 2007. The trend is driven predominantly by people between the ages of 18 and 25, in which group there has been the greatest increase in the number of heroin users.

The same NSDUH data indicated that approximately 170,000 people used heroin for the first time during 2016, which is almost twice as many as had tried it for the first time 10 years prior in 2006. Because heroin is such an addictive substance and heroin addiction is so difficult to overcome, a number of pharmaceutical and therapeutic options have been developed to help. Among them is buprenorphine.

Buprenorphine is a drug that is used to treat opioid addiction or pain. It is marketed in the United States and elsewhere under the Subutex brand name. It has been proven effective in treating people who are addicted to heroin or other opioids like morphine, codeine, hydrocodone, oxycodone and fentanyl.

History of Buprenorphine

The drug was developed over the course of more than a decade at a company called Reckitt & Coleman. The goal of development was to come up with a drug whose structure was substantially more complex than morphine such that it might convey the positive effects of morphine without the negative side effects. At industry conferences, the drug attracted the attention of many pharmacologists because it was presented as a good painkiller that lacked a high potential for abuse.

It took nearly 30 years following the discovery of the drug in 1966 for it to be utilized for therapeutic purposes. An under-the-tongue version of the drug was developed and marketed under the brand name Subutex. It was first released in France in 1995 and was approved for addiction treatment in 2002 in the United States. At the same time, the FDA also approved use of buprenorphine in combination with naloxone, marketed as Suboxone.

Subutex was discontinued in 2011, following the approval of generic buprenorphine by the FDA in 2009. Suboxone tablets were likewise discontinued in 2012, and the FDA approved generic Suboxone drugs in 2013.

Effects on the Brain

Opioids produce effects in users by attaching to brain receptors, causing three primary consequences: euphoria, decreased pain and slowed respiratory function. The greater the quantity of opioids consumed, the greater the effect. The way that opioids bind to brain receptors might be thought of as mechanical with better “fits” resulting in better effects.

Buprenorphine does not fit to the receptors as well as other opioids, so it occupies the receptor without providing the high and the other effects as well. The brain is fooled into believing that its opioid receptors have been satisfied, but the person does not experience the feelings of euphoria or the respiratory slowing. Because the receptor is occupied, it will not bond with full opioids simultaneously, so the patient will not experience the high of heroin or morphine even if he or she has them in the bloodstream.

The drug is effective as part of replacement therapy because it is “stickier” than other opioids, continuing to block receptors in the brain much longer than they do. It is because of this stickiness that this drug lasts up to three days before its effects dissipate.

Side Effects

Possible side effects of buprenorphine treatment include:

  • Back pain
  • Constipation
  • Hoarseness in the throat or cough
  • Fever
  • Headache
  • Chills
  • Nausea or stomach discomfort
  • Sneezing, stuffy nose or runny nose
  • Difficulty falling or staying asleep
  • Diarrhea
  • Dizziness or feeling lightheaded
  • Weakness or loss of strength
  • Redness or flushing of the neck and face
  • Feelings of warmth or sweating
  • Vomiting

Legal Status

Buprenorphine has been listed among the classes of controlled substances in several different countries. Its legal status in various countries is as follows:

  • Australia: S8 controlled substance
  • Canada: Schedule I
  • Denmark: Anlage III
  • United Kingdom: Class C
  • United States: Schedule III

The drug is available in most places only via prescription or as part of a substance use disorder recovery program.

Use in Addiction Treatment

The most common use for buprenorphine is the treatment of opioid addiction. It can be administered once withdrawal symptoms from opioids have begun and used thereafter as a means of opioid replacement therapy.

The drug on its own is a partial opioid agonist, meaning that it produces the typical opioid high and other effects, but not to the extent that they are produced by full opioid agonists like heroin and methadone. At low doses, it produces strong enough agonist effects that people who are addicted to opioids can take it to come off other drugs without going through withdrawals.

Because it is a partial agonist, use of the drug results in:

  • Reduced potential for addiction or abuse
  • Milder symptoms of withdrawal
  • A ceiling on the high caused by opioids
  • Lessened physical dependence and euphoria

The effects of the drug that cause a high in the user will increase in a linear fashion as the dosage level increases until they plateau and do not further increase, a phenomenon referred to as the ceiling effect. Because of the ceiling effect, this drug has lower risks of addiction or abuse than full agonists. The drug can be used to block the effects of full agonists if administered while there are other opioids in the bloodstream of the patient, bringing on withdrawal symptoms and beginning the recovery process.

When administered in appropriate dosages, the drug:

  • Decreases opioid cravings
  • Suppresses opioid withdrawal symptoms
  • Inhibits the effects of other opioids
  • Discourages the use of illicit opioid drugs
  • Helps patients remain in treatment programs

Phases of Buprenorphine Treatment

Typically, treatment of opioid addiction with this drug occurs in three distinct phases.

  • Induction Phase: This phase is usually performed in a certified opioid treatment program or a doctor’s office using approved products. The drug is given to the patient after he or she has not used any opioids for between 12 and 24 hours, and the patient is in the first stages of withdrawal. For patients who still have heroin, morphine or other opioids in their systems and who have not yet begun withdrawal symptoms, administering the drug can bring on acute symptoms of withdrawal.
  • Stabilization Phase: The stabilization phase begins once the patient has reduced or discontinued their use of illicit opioids and no longer has drug cravings. The patient should also be experiencing only few or no side effects at this point. Dosages of the drug may require adjustment during the stabilization phase to help the patient maintain a balance. Because this drug has long-lasting effects, patients on buprenorphine may be able to switch from an everyday administration schedule to an alternate day schedule.
  • Maintenance Phase: Once the patient has settled in and is doing well on steady administration of the drug, the maintenance phase begins. The specifics of every case are unique, and the time the patient remains in the maintenance phase may be longer or shorter depending on his or her circumstances. The maintenance phase might continue indefinitely in some cases. After the patient has achieved a reliable level of stabilization, he or she may be moved out of the maintenance phase by virtue of a medically supervised withdrawal period. This smooths the transition out of physical dependency for the patient.

Buprenorphine Treatment and Counseling

Treatment of opioid dependency with this drug is most effective when used in combination with counseling. Individual or group therapy, wherein the patient discusses his or her substance use disorder and the factors that led thereto, can be of help in reaching a state of independence. Qualified professional counseling, in conjunction with drug treatments, can facilitate better results for opioid-addicted persons than either option alone.

Treatment programs commonly make use of one or more types of counseling alongside drug treatment:

  • Individual Treatment Therapy: In this type of therapy, a professional addiction counselor or another healthcare professional works with the patient to talk through the factors and triggers that lead to his or her drug use. The goal of individual therapy is to reach the heart of the substance use disorder so that the patient might fully recover.
  • Group Treatment Therapy: In group therapy sessions, a group of people at various stages of the addiction recovery process gather together to talk about their experiences, the ways they cope, their goals or dreams, positive or negative feelings, and other topics that might move them all toward recovery. These meetings generally happen under the supervision of a trained substance use disorder counselor.
  • Family Treatment Therapy: Because family matters are often tied closely to the development and continuation of addictive behavior, some who are struggling with addiction might benefit from family therapy. Here, the patient and members of his or her family meet and talk with a trained therapist to identify and remedy problems in the familial relationship that might contribute to addiction.

Buprenorphine Versus Methadone as Treatment Options

Methadone is another drug that is used to treat addiction to heroin or other opiates. It is a synthetic opioid and has effects and usages similar to morphine. It is often used in the treatment of opioid dependency, but because of its risk of abuse, methadone treatments are generally only performed in a structured environment under strict medical supervision.

Treatment with buprenorphine, on the other hand, is the first type of opioid replacement medication therapy that can be dispensed and prescribed in doctor’s offices, thus radically increasing access to treatment for people with opioid dependency. By the terms of the Drug Addiction Treatment Act of 2000, doctors in the U.S. can give patients the drug in less controlled settings than methadone. It might be administered in the doctor’s office, in a hospital, in prisons or at a health department.

Patients who are in methadone treatment can switch to treatment with buprenorphine instead. Because of the differences between the drugs, though, the patients may not be immediately satisfied. According to studies, buprenorphine is as effective as methadone in moderate doses, but it may not be as effective for patients who are highly physically dependent on opioids as optimal dose methadone. There are a number of factors that may impact whether a patient who is currently on methadone should consider switching.

Consistent Sobriety Helps to Prevent Relapse

When people come out of addiction, and as they work their way through it, they might find that they are not yet ready to return home or to their previous lives. Encountering friends and family or other triggers in the world can cause the person to relapse and revert to addictive behaviors. For these reasons, sober living communities are often effective for people who are transitioning out of substance use disorder. A sober living community is a place where all of the residents are dealing with similar struggles and trying to recover from addiction.

With consistent effort and the right treatment, it is possible for any person to achieve a permanent state of recovery. During the initial phases of recovery, sobriety is of paramount importance. It can also be important to avoid or discontinue relationships that have enabled the addiction or that are built around drug use. Early intervention and professional, science-based treatment options, which might include buprenorphine therapy or other measures, can help the patient overcome substance use disorders.

The number of people who are trying heroin in the United States for the first time is on the rise, and the number of people who are becoming addicted is still increasing at an alarming rate. Heroin addiction is difficult to overcome, but recovery is possible with therapeutic drugs like buprenorphine and other treatment options.

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