Buprenorphine

Buprenorphine is an opioid drug indicated for the management of pain and opioid dependence.

Common Brand Names: Cizdol, Brixadi, Suboxone (with naloxone), Subutex, Buvidal, Bunavail

Buprenorphine belongs to a class of drugs called opioid partial agonist-antagonist. At low to moderate doses, it can produce effects such as euphoria and respiratory depression alongside its pain relief effect.

As a Schedule III medication, buprenorphine carries a low to moderate risk for physical dependence and high risk for psychological dependence. Chronic use of the drug can lead to substance use disorder in the long run.

How Is Buprenorphine Used in Medical Settings?

Buprenorphine is approved by the U.S. Food and Drug Administration for the management of acute and chronic pain. It is also used as a substitute for another opioid such as fentanyl or heroin in the treatment of opioid addiction.

The principle of substitution therapy is to replace a more potent opioid with another opioid that has a much lower abuse potential (in this case, buprenorphine) to help reverse the patient’s drug dependence. The patient will then be gradually weaned off buprenorphine to finally treat their addiction.

Buprenorphine can also be used to manage opioid-dependent patients with a contraindication or intolerance to methadone and those whose treatment with methadone has failed. Similarly, buprenorphine can be used when there is no available or nearby methadone facility.

Off-label, buprenorphine can be used for the management of withdrawal symptoms of hospitalized, heroin-dependent patients.

In What Ways Is Buprenorphine Abused?

Buprenorphine is abused much like other opioids: the tablet is often crushed, then snorted, smoked, or dissolved in water and then injected. Many of those who abuse buprenorphine take double or even triple doses in an attempt to produce more potent effects.

However, it has to be noted that more studies have reported that buprenorphine is more often misused rather than abused. Often, the individuals who misuse the drug are those trying to overcome opioid use disorder or OUD.

Buprenorphine Interactions

Buprenorphine can interact with a variety of drugs and cause unwanted side effects. These include the following:

• CNS depressants. Using buprenorphine with central nervous system (CNS) depressants like benzodiazepines and even alcohol can result in an increased risk of profound sedation and respiratory depression. It can also lead to coma and death.
• CYP3A4 inhibitors. Cytochrome P450 3A4 or CYP3A4 is a protein mainly found in the intestines and liver. People who are taking medications that inhibit CYP3A4 may experience increased or prolonged opioid effects when they use buprenorphine at the same time.
• CYP3A4 inducers. On the other hand, taking CYP3A4 inducers can result in the decreased efficacy of buprenorphine. CYP3A4 inducers may even trigger withdrawal symptoms in patients who have become physically dependent on buprenorphine.
• Serotonergic drugs. Serotonin syndrome, in which the body has too much serotonin, has been observed in patients who take buprenorphine with serotonergic drugs. These include selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), monoamine oxidase (MAO) inhibitors, and even methylene blue.

Meanwhile, patients who are taking diuretics, muscle relaxants, anticholinergic drugs, and antiretrovirals should be monitored for side effects. Should there be any, the dosage of buprenorphine should be increased or decreased accordingly.

Why Is Buprenorphine Prone to Abuse Even If It Is Considered Safer Than Methadone?

Opioid addiction is one of the biggest health problems in the US. It is also one of the most difficult class of substance use disorders to treat because patients often start on the drug as a legitimate way to manage chronic pain. Sudden deprivation of opioids after chronic use can cause severe withdrawal symptoms, so replacement drugs are often prescribed as part of the addiction treatment.

There are two kinds of drugs commonly used for opioid addiction treatment. Methadone is an opioid agonist that has a long-acting effect on the body. It is also a type of opioid drug but its effects are milder, so it is usually used as a replacement drug to control drug cravings and withdrawal symptoms.

The other drug is buprenorphine, which is also an opioid. Because it is part agonist and part antagonist, the effect is milder compared to methadone, and it is considered to be safer. With less risk for overdose, buprenorphine is more often prescribed than methadone. It also comes in “abuse-deterrent” formats like skin-implants and combinations with naloxone, but this doesn’t mean that it can’t be abused.

Buprenorphine has a “ceiling,” which means that taking more of the opioid does not increase its effect. This is supposed to prevent patients from taking more of the drug, but some patients may try to get around this safeguard by using it with other drugs.

Additionally, some studies suggest that buprenorphine abuse may be a result of attempts to self-medicate opioid use disorders.

Buprenorphine Side Effects

Buprenorphine can cause a wide range of side effects. The most common ones include:

• Dry mouth
• Impaired vision
• Headache
• Pain in the back
• Difficulty falling asleep or staying asleep (insomnia)
• Constipation and stomach pain
• Numbness or redness of the mouth
• Tongue pain
• Sleepiness

More serious side effects of buprenorphine may also manifest. These include the following:

• Hives, rashes, and general itching
• Difficulty in breathing or swallowing
• Swelling of the face, eyes, throat, tongue, or lips
• Swelling of the hands, feet, ankles, or lower legs
• Hallucinations
• Confusion
• Fever and sweating
• Fast heartbeat
• Severe muscle twitching or muscle stiffness
• Nausea and vomiting
• Diarrhea
• Loss of appetite
• Unusual bleeding or bruising
• Yellowing of the skin or eyes
• Dark-colored urine
• Light-colored stools
• Rashes or hives

Long-Term Effects of Buprenorphine:

Other adverse effects of buprenorphine can be attributed to chronic or long-term use. These include the following:

• Dependence and withdrawal
• Addiction
• Adrenal insufficiency
• Neonatal abstinence syndrome (in newborns)
• Inability to get or keep an erection
• Irregular menstrual cycles
• Decreased libido or sexual desire

Symptoms of Buprenorphine Overdose

Buprenorphine overdose can also lead to symptoms like:

• Pinpoint pupils
• Impaired vision
• Extreme drowsiness
• Sleepiness
• Dizziness
• Slow or shallow breathing
• Difficulty breathing
• Coma or loss of consciousness

Naloxone is often added to buprenorphine in order to decrease the risk of misuse and diversion. In addition, naloxone is also a viable drug to help reverse the symptoms of opioid overdose, particularly breathing difficulties and sedation.

If you or a loved one is being treated with buprenorphine or is using the drug, talk to your doctor about naloxone as a possible emergency overdose treatment. They will give you instructions on how to use the drug, as well as what to do while waiting for medical help.

Signs of Buprenorphine Addiction

In the Fifth Edition of the Diagnostic and Statistical Manual for Mental Disorders (DSM-5), 11 symptoms are presented as criteria for diagnosing substance use disorders. These criteria also apply to opioid use disorders like buprenorphine addiction:

• Using buprenorphine in larger amounts or for longer than prescribed
• Attempting to reduce or stop using buprenorphine but being unsuccessful
• Spending a lot of time getting, using, or recovering from use of buprenorphine
• Feeling strong cravings for buprenorphine
• Inability to manage work, school or family obligations because of buprenorphine use
• Continuing to use buprenorphine even if it causes interpersonal or relationship issues
• Prioritizing buprenorphine use over important activities
• Repeated use of buprenorphine even if it places you in danger
• Continuing to use buprenorphine despite it worsening your physical or psychological problems
• Needing higher and higher doses of buprenorphine than usual to achieve the desired effects (tolerance)
• Developing unpleasant symptoms after abruptly stopping buprenorphine use (withdrawal)

Symptoms of Buprenorphine Withdrawal

Abrupt cessation of buprenorphine use can lead to withdrawal symptoms. These may include the following:

• Anxiety
• Excessive yawning
• Bone and muscle aches
• Restlessness
• Rhinorrhoea (continuous discharge of thin nasal mucus)
• Teary eyes
• Dilation of the pupils

It’s possible to develop buprenorphine dependence even if you use the drug as prescribed. However, it is important to note that dependence simply means that your body has become used to the drug; it is not synonymous with addiction, which is a brain disorder characterized by compulsive substance use despite the negative consequences. It’s also important to keep in mind that buprenorphine itself is also used as a drug detoxification agent, particularly for many types of opioid addiction or opioid use disorders.

To safely stop the use of buprenorphine, talk to your doctor or seek help from a medical detox facility. They can create a unique tapering schedule for you so you can get off the drug without developing severe withdrawal symptoms.

Buprenorphine Detoxification

The best way to safely stop using buprenorphine is to undergo a detoxification program. This way, even if you experience withdrawal symptoms, there will be medical professionals who can assist you and provide appropriate care. Undergoing buprenorphine detox also ensures that you can safely and completely remove the presence of the drug from your body.

Here are some things you can expect during buprenorphine detoxification:

• You will be given a customized tapering schedule, which will gradually lower the doses of buprenorphine you take daily.
• You may be prescribed additional medications to help manage any withdrawal symptoms.
• Your doctors may recommend nutritional supplements to restore your body’s health.
• There will be medical professionals who will monitor your condition closely, ensuring that you feel comfortable and safe as you undergo the stages of withdrawal and detox.

Rehabilitation and Treatment for Buprenorphine Addiction

Addiction to buprenorphine is treatable. The key is to be open to the fact that you need help. It’s difficult to beat drug addiction alone, so it’s in your best interests to seek professional addiction treatment. There are usually two options available—inpatient or outpatient treatment—one of which will be more suitable than the other depending on your unique situation.

• Inpatient buprenorphine addiction treatment. Inpatient treatment is ideal if you have a severe case of addiction or a history of non-compliance with previous treatment programs—or both. In this type of buprenorphine addiction treatment setup, you will be required to stay in the rehabilitation facility throughout the duration of the treatment. You will be prescribed an intensive regimen, which may include the provision of medications and psychological therapy. Your care providers will also provide close and constant supervision to ensure the success of your treatment.
• Outpatient buprenorphine addiction treatment. For milder cases of addiction with less dangerous symptoms, outpatient addiction treatment is recommended. This is also ideal if you or your loved one has a strong support system at home and can guarantee treatment compliance. With outpatient addiction treatment, you can continue living in your own home and conducting your usual activities. You can go to work or school, and even attend to various social obligations. The difference is that you have to visit the assigned rehabilitation center to receive therapy, counseling, and other prescribed treatment programs.

Find a Treatment Center That Suits Your Unique Needs

With professional help and support from your loved ones, it’s possible to achieve a drug-free life. Having insurance makes things easier as well, since many policies provide coverage for outpatient and inpatient addiction treatment services.

Contact Better Addiction Care at (800) 429-7690 today to receive top-tier referral services from our recovery support advisors. With their help, you can get in touch with treatment centers across the country and discover the best one for your situation. They will also verify your insurance coverage or, if you don’t have insurance, assist you in finding alternative options to finance your treatment.

History of Buprenorphine

Buprenorphine, originally named RX6029, was synthesized in 1969 by researchers at Reckitt and Colman (now Reckitt Benckiser). After 10 years of attempting to develop an opioid analgesic that was comparable to morphine in terms of efficacy but without the undesirable effects, they discovered RX6029, and they found that it was successful in reducing opioid dependence in test animals.

RX6029 trials on humans began soon after, and by 1978, it was launched in the United Kingdom as buprenorphine, an injection formulation indicated for the treatment of severe pain. Sublingual formulations of buprenorphine were introduced to the market in 1982.