We are going to talk about Buprenorphine in this blog post, but I have to start by clarifying a common misconception about dopamine because the erroneous model people hold of addictions leads them to misunderstand and malign opiate replacement therapies.
Neurobiology of addiction and opiate dependency
Since dopamine is closely linked to the reward center of the brain, many people believe that it also lies at the core of addiction. This is wrong. The brain releases the neurotransmitter dopamine into the nucleus accumbens (the ‘reward center’) every time it perceives anything in the world that might have a survival value, whether it’s good or bad. Every time we are approaching anything with potential value, our dopamine increases. This includes drugs, of course, but also sex, cookies, perhaps a shiny new sports car.
Punishment also stimulates dopamine. It signals salience.However, it doesn’t necessarily mean that something is addicting simply because it stimulates the body’s reward system. The dopamine is much more responsible for the wanting of a drug, and when repeatedly stimulated, the dopamine systems entrains the organism to veer towards attaining that reward. Of course, anything that relieves pain is reinforcing and experienced as pleasurable.
When does Opiate use crossover to becoming an Addiction?
Initially, drugs and alcohol may nestle amongst many things in our lives that we find interesting: spending quality time with family and friends, embarking on an exciting career, engaging in creative pursuits and other similarly enjoyable activities are all part of the mix. Over the course of time, however, learned associations and habit circuits make drug use more and more important and compelling. Over time, learning mechanisms make the behavior more of an automatic habit, requiring less thought. But the organism still selects the most advantageous survival behavior, weighing up the complex reinforcers in its midst, which in social mammals such as humans get very complex indeed.
What pushes the organism to addiction is the engagement of liking and stress systems. Liking is much more mediated by endorphin responses – or rather the body’s endgenous (internal) opiate system. This system reduces pain from all sources, physical, emotional, social and that is definitely liked. So, emotional triggers that are uncomfortable or painful (hunger, anger, loneliness) trigger a desire for relief, as much as learned drug associations (people, places, things).
As drug use becomes habitual, other interests can fall by the wayside, and many emotions and cues in the world become associated with drug use as triggers. People turn to the drug to modulate both positive and negative emotions. There’s no great distinction between dependence and addiction. Perhaps addiction conveys a greater intensity of dependence, with a physical withdrawal if the drug is ceased. I was taught the 3 C’s of addiction: craving/compulsion, loss of control and continued use despite consequences.
When people use opiates for the first time, they get high or feel marked relief from stress, and then come down and feel straight or normal. The second time they use it, they don’t get quite the same level of euphoria because the body has developed a certain amount of tolerance, even from first use. Worse, when the drug effect wears off, they find themselves feeling slightly more depressed or despondent than when they started using. Over time, this shift makes it harder and harder to get high and the resting state is one of misery, corrected by drug use. This cycle of drug use can go on for months, even years, depending on a person’s genetic make-up and how many other things are going on in their lives. Some people, probably most, never slip into the dependent state, and many others pull themselves out. Factors like genetics and early life experience like neglect influence this capacity for correction.
The link between opiates and stress relief are interwoven at the deepest level. In fact, think of opiates as a stress hormone. One molecule of our endogenous endorphin is released for every one molecule of the hormone that stimulates the stress system. One for one the stress, which focuses and readies the body for a response, is counterbalanced by a system that says ‘it’s OK, endure the pain and get this job done’. So, if any extra boost of opiates is taken, as heroin or Vicodin or Oxycodone, the pain and suffering are forgotten completely for the duration of the drug but then, as it wears off, the stress system is back online, with a vengeance. It’s been told to ramp up to meet the opiate load, but that opiate load is now gone. The whole system’s out of whack, and the person will feel super stressed, craving for a balance of the opiate system. Because opiates alter the well-being set-point of the body, via a shift in the hypothalamic-pituitary-adrenal axis, people who are using regularly will need to take stronger and stronger doses of a drug to get to a ‘normal’ state.
The effect of drugs on the body’s stress system can last for a long time. For example, studies have been conducted on people who come out of jail and have been in prison for six or twelve months away from opiates. Even after that length of time, their bodies still show a massive dysregulation of the stress system. Their stress system is still on fire, yearning for compensation with opiates.
Drug-dependent individuals are using not to get high anymore, but just to feel normal; to be able to get up in the morning and function like ordinary people. With continued drug use, opiate-dependent individuals become fed-up, depressed and disinterested in things connected with addiction. Drug use is the only way they can feel normal. Or, they shift methods from eating to sniffing, from smoking to shooting – some even start using fentanyl. This is the point where people may overdose. Opiate-addicted individuals engage in this potentially dangerous behavior not in pursuit of a high. Instead, these behaviors simply allow them to reach a level of functioning considered normal for the general population. When drug use ceases, the now abnormal and reactive stress hormone system yearns for correction by the opioid system, driving craving for drugs.
How Buprenorphine/Suboxone Works in the Human Body
Once the body has adapted to this new state of affairs, is dependent, cessation of opiates is nearly intolerable. When a stressor or cue comes along everything – reward centers signaling value, pain centers crying for relief, stress systems yearning for soothing – bends towards obtaining more opiates. Relapse rates are 80% and up.
What opiate-addicted individuals need are treatment options that can calm the stress system down and shift it back towards normal. This is precisely what longer-term medication-assisted treatment (MAT) is designed to achieve. MAT enables addicted individuals to avoid anxious states of depression or cravings. It frees them from the massive pull and push of an agitated stress system long enough for them to reach their goals and learn self-soothing techniques and build relationships that can provide the needed comfort and protection.
Steady-state opiates enable a person to feel normal without suffering massive ups and downs. Agonist drugs (such as methadone and fentanyl) are strong and can cause overdoses themselves, but methadone is often required to satiate the person who has used very large quantities for a long time. Antagonist drugs (such as Naltrexone, Vivitrol), are not addictive in and of themselves, but they do not relieve drug cravings either. Buprenorphine is a partial opioid agonist drug that produces a pleasurable sensation but blocks full opioids for a full 24 hours. It has low rates of overdose, especially in those who are already used to opiates and can be taken by mouth rather than injection, reducing risks.
The effectiveness of Buprenorphine, the active ingredient in Suboxone, in treating opiate addiction is well documented. However, as with any drug addiction treatment, there are negative consequences as well. This is what we will explore below.
Buprenorphine/Suboxone Treatment: Positive Effects
Buprenorphine is very sticky on receptors and it sits on the cell effectively blocking heroin (or other drugs) from getting in. Opiate-addicted individuals taking suboxone experience no buzz. They feel normal. This gradually breaks the massive pull and push of emotions and cues associated with drug use. It curtails drug cravings and slowly balances a dysregulated stress system.
Because of the balancing effect of Buprenorphine in the body, the person who is using is able to function longer in a ‘normal’ state. This gives them the ability to hold down a job, repair relationships with family and friends, and pursue short-term as well as long-term goals. It’s like a force field – people can walk through a stressful life and respond like anyone else. During the time the drug is taken, perhaps for years, the therapy helps change relationships, peers, work, self-esteem, and underlying psychological vulnerabilities. Supportive communities including 12-step (AA) can be immensely helpful.
The effectiveness of Buprenorphine is backed by solid research conducted over decades in many countries and populations. Up to 80-90 percent of opiate-addicted individuals taking Buprenorphine stay drug-free while those who do not relapse 90% of the time. The difference between those on the drug and those off is black and white. Drug-free treatment works for the tiniest minority of people. Many die, get HIV, Hepatitis C or criminal records and destroyed social worlds as they stick to an abstinence route. It’s not the acute withdrawal part that’s tough, this takes a week. It’s the months and months afterward where the brain and body is constantly attuned to obtaining the drug and stress is intense, when the rubble of addiction makes everything harder. Taking suboxone eliminates cravings, eliminates withdrawal and blocks the ability to get high. People stop shooting drugs, engaging in criminal activity and have an opportunity to recover.
Buprenorphine/Suboxone Treatment: Possible Side Effects
Taking Buprenorphine can cause several undesirable physical symptoms such as dry mouth, constipation, and decreased libido. Perhaps long-term use can contribute to thinner bones. It is also possible for a person to overdose on Buprenorphine if they are also taking other drugs like alcohol or benzodiazepines. However, people can take Buprenorphine safely for years, perhaps forever. It can be used in pregnancy, and is way safer than cycles of opiate use and withdrawal, though sometimes the infant will need weaning.
Additionally, it can take a while for Buprenorphine to take full effect. It is not a magic bullet and cannot be resorted to as a quick fix. It needs to be used as a daily medicine, at a proper dose. Unfortunately many take it at low doses, irregularly, and to bridge between the use of heroin or oxycodone. They say they’ve tried suboxone and it didn’t work. But in fact, they were using it just like they were using oxycodone, in response to feeling craving, not as a medicine. Taking Buprenorphine probably works better if the addicted individual is also engaged in therapy. I say ‘probably’ as it’s the professions believe and makes sense, but research has not actually shown marked improvements in outcome, for various reasons.
Furthermore, it can be quite challenging to completely wean a person from Buprenorphine after they have been taking it for an extended period of time. It’s the last few milligrams that are tough. And this is the case whether someone starts at 2 or 32mg a day. It is relatively easy to come down to 1 or 2mg, but then things have to move very slowly while coaching and supporting recovery and perhaps with other meds to assist. If not done properly, tapering the use of Buprenorphine can re-ignite the body’s cravings for drugs and disrupt the stress system all over again. It’s like that force field is coming down: the person beneath had better have done their therapy work and changed their outside World or relapse is inevitable.
Opiate dependency means people are triggered to use by people places and things, value the drug above the things they cared about, and are in a state of heightened stress and pain without opiates. Prolonged and unmitigated drug use resets the body’s well-being (stress hormone) set-point. This means that over time, a person resorts to taking drugs not to experience a ‘high,’ but to simply function normally. The effects of drugs remain in the body even if the person stops abusing drugs for several months. For any drug addiction treatment to work, it must bring the person’s well-being set-point back to normal, bring the attentional and decision-making systems back to regular valued things (and people); and allow stressors to register as manageable rather than alarming and demanding of drugs. They should also be administered safely, without injection and last a long time. Medication-assisted therapy (MAT) has been found to be highly effective in the treatment of opiate abuse. In particular, the use of the partial opioid agonist drug Buprenorphine is well established and satisfies all of the above criteria.
As with any drug treatment option, there are some drawbacks to using Buprenorphine. Completely weaning from Buprenorphine can also be tricky. Perhaps the most positive benefit that can be derived from Buprenorphine treatment is the protection that it gives someone who has become drug-dependent. Time to repair relationships set new career goals and live a more purpose-filled life that is no longer defined by drug use.
In a future article, we’ll compare Naltrexone (Vivitrol) with Buprenorphine.