How is buprenorphine used effectively? INTERVIEW with Dr. David Simon, M.D.
Is buprenorphine the right medication for you?
When combined with a holistic program of recovery that inclues psycho-social support, buprenorphine can help people get clean (and stay clean) in long term addiction recovery. But do you know how buprenorphine works in the brain? Does buprenorphine cause physical dependence or uncomfortable side effects? What safety considerations do you need to make before starting to take buprenorphine?
Find out the answers to these questions in our exclusive interview with prescribing doctor and addiction expert, Dr. David Simon, M.D. was among the first physicians in the United States to qualify as a buprenorphine provider and prescribed Suboxone as far back as 2003! Specializing in addiction treatment, Dr. Simon maintains a private practice in Mansfield, Connecticut. Based in the NE, he provides individual medication management and counseling to clients, specializing in:
- Addiction & Recovery
- Opioid Addiction
- Other Addictions
- Smoking/Tobacco Cessation
- Suboxone Treatment
Today, he’ll help us answer questions like:
- How buprenorphine can help addicts?
- How can we access it?
- What is the safe dosage of use?
- Is buprenorphine addictive?
More here about the effective use of buprenorphine in recovery. If you still have questions about buprenorphine medication, we invite you to send us/him a question in the comments section at the end. In fact, we try to respond to all questions personally and promptly.
ADDICTION BLOG: Thank you for joining us, Dr. Simon! First, can you describe how buprenorphine works in the brain to help addicts? What’s really going on to reduce cravings for drugs like heroin, oxycodone, or codeine?
DR. DAVID SIMON, M.D.: We all have naturally occurring mu (“mew”) opioid receptors in our brains. These are the receptors that natural (endogenous) opioids like beta-endorphines attach to that give us a normal sense of well being.
Opioid drugs like heroin, morphine or oxycodone attach to these same receptors. When one of these drugs attach to the receptor it causes a conformational change that sets off a cascade of chemical reactions, which results in dopamine being released in the pleasure-reward center of the brain. These drugs are full opioid agonists, which mean the opioid receptor is fully activated and a substantial amount of dopamine is released to cause euphoria or pleasure.
However, when someone uses a full opioid agonist over a period of time the chemical reactions adapt to having excess opioid around, and the person then requires more opioid to get the same pleasurable effect. This is called tolerance. Then, when an opioid like heroin isn’t around, the pleasure-reward center of the brain is in a state of relative dopamine insufficiency – not enough dopamine effects to feel well, and the person feels sick.
Buprenorphine is a partial opioid agonist. It activates the mu (“mew”) opioid receptors in the brain about 60% compared to full opioid agonists. This results in a partial dopamine effect in the pleasure-reward center: there isn’t enough dopamine to make someone feel high, but there is enough to take away the dysphoria (bad feeling) of not having an amount of opioid that the body got used to. Compared to having no heroin, there is less craving and the symptoms of opioid withdrawal are prevented.
There is another very important property of buprenorphine that makes it an excellent medication to treat opioid addiction. Buprenorphine has a much higher affinity for mu opioid receptors than do commonly abused opioids. So, if the person is administered buprenorphine regularly, the mu opioid receptor will be occupied with buprenorphine. This will prevent other opioids with a lower affinity for the receptor, such as heroin or oxycodone, from binding the receptor. In this way, buprenorphine blocks other drugs like heroin from attaching to the receptor.
In summary, buprenorphine reduces craving for opioid, relieves opioid withdrawal symptoms, and blocks drugs like heroin from activating the opioid receptor. And, it does all this without causing the opioid tolerant person to become high. Also, buprenorphine is a relatively long acting drug, so it only needs to be administered once a day, as opposed to shorter-acting opioids like heroin or oxycodone that must be administered multiple times throughout the day.
ADDICTION BLOG: Of the brand name medicines that are prescribed which contain buprenorphine (Suboxone, Subutex, etc.) is one more effective that others? Also, why is naloxone combined with buprenorphine?
DR. DAVID SIMON, M.D.: Buprenorphine is the active ingredient that causes all the effects described above. It is well absorbed under the tongue, and in some formulations it is well absorbed through the mucosa of the inside of the mouth.
Naloxone is an opioid antgonist – it blocks the mu opioid receptor but doesn’t activate it. The inclusion of naloxone is meant to dissuade people from abusing the medication by injecting or snorting it. Also, naloxone is not well absorbed under the tongue.
Brand medications such as Suboxone, Zubsolv and Bunavail contain both buprenorphine and naloxone as encouraged by the U.S. Drug Enforcement Administration. When these medications are administered as directed, then only the buprenorphine is effective, not the naloxone. However, if the medication is abused, such as by being injected intravenously, then the naloxone will have a relatively greater effect versus buprenorphine compared to when it is administered under the tongue. The inclusion of naloxone is meant to dissuade people from abusing the medication by injecting or snorting it.
The following medications are all effective for treating Opioid Use Disorder, or opioid addiction:
- Suboxone is an orange flavored film strip containing both buprenorphine and naloxone that is best administered under the tongue.
- Zubsolv is a menthol tasting disintegrating tablet Doesthat contains buprenorphine and naloxone that is also placed under the tongue.
- Bunavail is a citrus tasting dissolving patch that is placed inside the mouth against the inner cheek.
- Subutex is a brand name for a medication that contains only buprenorphine without naloxone. It also comes in generic versions. Buprenorphine without naloxone is recommended for treating women who are pregnant.
ADDICTION BLOG: What about one type of mode of administration (sublingual tablets vs. film vs. muccal film vs.patch)? Is one better than another?
DR. DAVID SIMON, M.D.: Films and orally dissolving tablets dissolve relatively quickly, which makes it easier for an observer to confirm the medication is being properly administered. Dissolving faster is also preferable if someone doesn’t like the taste of the medication. Rarely, someone may develop an inflammatory reaction under the tongue. The buccal patches that dissolve against the inner cheek are a good alternative for this situation.
Buprenorphine is most efficiently absorbed from the buccal patches; next most efficiently absorbed from the orally disintegrating tablets, and less efficiently absorbed from the film. Because of these different rates of absorption, 8 milligrams (“mg”) of buprenorphine in the film is equivalent to 5.7 milligrams in the orally disintegrating tablet, which is equivalent to 4.2 mg in the buccal patch.
All formulations are effective. Patient preference may influence which medicine is prescribed. Often the price of a medication as negotiated with a health insurance company is the determining factor. Some physicians prefer to prescribe the most efficient formulation, which has the least amount of buprenorphine in it, to decrease the incentive for drug diversion.
ADDICTION BLOG: Is buprenorphine “better than” methadone? Why or why not?
DR. DAVID SIMON, M.D.: Methadone is an old fashioned drug that was developed in the 1930’s. It is akin to the first antibiotic penicillin. While penicillin is still effective, there are newer, better antibiotics. Likewise, buprenorphine is a newer, and in my opinion better, drug than methadone.
Buprenorphine is a partial opioid agonist that blocks other opioids from attaching to mu opiod receptors by virtue of its high affinity for the receptor. Methadone is:
1. a full agonist that does not have the high affinity for receptors to block other opioids like buprenorphine does.
2. more likely than buprenorphine to have drug interactions with other medications.
3. more likely to cause QT-interval prolongation, an electrocardiographic sign that it adversely effects conduction of electrical impulses in the heart.
4. more likely to provoke the chance of life-threatening respiratory arrest due to opioid overdose or interaction with other respiratory depressants like sedatives and alcohol.
Also, many patients who were previously treated with methadone and are now using buprenorphine tell me they are more alert and “normal’ on buprenorphine, and they do not “nod out’ like they did when they were on methadone. In addition, methadone for treatment of addiction must be dispensed daily at highly regulated treatment programs.
Nevertheless, methadone is an important treatment alternative where buprenophine providers are not available. I will refer a patient to a methadone clinic who continues to abuse illicit opioid while prescribed buprenorphine, not because methadone is a better drug, but rather because that person requires a higher level of observation and accountability that a methadone clinic offers. Any medication is only effective if the person actually administers it – at methadone clinics the person is witnessed administering methadone daily.
ADDICTION BLOG: What kinds of questions do GOOD buprenorphine prescribers ask of their patients. What kind of consulting work is required for best results? How much “counseling”?
DR. DAVID SIMON, M.D.: Ideally, buprenorphine stabilizes a person by getting them out of the vicious cycle of:
- feeling sick
- hunting for drugs
- spending money on drugs or
- committing crimes to support a drug habit
This then allows the person to do the real “recovery work.”
Addiction is a biopsychosocial phenomenon. There is a biological component having to do with brain chemistry, genetic predisposition, etc.; a psychological component, which often involves learning new coping skills; and, a social component where one changes the social milieu of one’s life – staying away from the wrong people, places and things. Sometimes, the drug addicted person uses opioids or other drugs to self-medicate an underlying, often undiagnosed, psychiatric problem. Stabilization on buprenorphine often allows these previously neglected underlying problems to be adequately addressed with counseling and/or medication.
Buprenorphine is prescribed for Opioid Use Disorder or addiction in a variety of settings. One setting is a dedicated outpatient treatment program for substance abuse. These have levels of intensity varying from:
- daily sessions (partial hospitalization)
- groups three days a week (intensive outpatient)
- weekly support groups (such as relapse prevention)
Other settings are private practice offices with a psychiatrist, an addiction medicine specialist, or a primary care physician. In addition, there are private practice behavioral health counselors credentialed in alcohol and other substance abuse counseling. Each provider has a method tailored for the particular setting.
ADDICTION BLOG: Is buprenorphine easy or difficult to access?
DR. DAVID SIMON, M.D.: Unfortunately, the demand for buprenorphine prescription outweighs the supply of buprenorphine providers in many communities. In addition, lack of health insurance or unaffordability is a serious impediment to treatment.
ADDICTION BLOG: What is the recommended safe dosage of buprenorphine? What would happen to a patient who takes more buprenorphine than described?
DR. DAVID SIMON, M.D.: One interesting feature of buprenorphine is that it has a “ceiling effect.” Because buprenorphine only partially activates an individual mu opioid receptor to about 60% of maximum, if all receptors are activated by buprenorphine then the maximum effect of all receptor activity due to buprenorphine is 60% of what a full opioid would cause. This makes buprenorphine a relatively safe medication.
Nevertheless, a patient should never administer more buprenorphine than prescribed by his or her physician. Recommended dosages vary based on a multitude of factors that are best determined by a properly trained physician.
ADDICTION BLOG: Does buprenorphine cause physical dependence? If so, how do doctors plan for withdrawal?
DR. DAVID SIMON, M.D.: Buprenorphine is an opioid. Think of it as a 60% opioid. Patients seeking buprenorphine treatment for addiction or Opioid Use Disorder are already physiologically dependent on opioids. They are not dependent on any particular opioid drug, rather there is a dysfunction in the opioid regulatory mechanism starting at the mu opioid receptor and continuing through various brain pathways including the parts of the brain regulating pleasure and reward.
Many patients are maintained indefinitely on buprenorphine due to the high relapse and recidivism rates for those with Opioid Use Disorder who discontinue buprenorphine. Nevertheless, many people are successful in discontinuing buprenorphine.
The best plan is a slow and gradual taper of buprenorphine that is adjusted based on how the person feels physically, whether there is a return or increase in craving or drug dreams, if there is reemergence of previous mental health issues, or there are objective signs of drug lapse (e.g. urine toxicology). Medications may be prescribed to treat specific symptoms or psychiatric problems that may manifest.