Blame Suboxone!

First Posted 3/24/2014
I recently came across the blog of a person who has dedicated his life to trashing buprenorphine treatment.  I won’t provide the name or link, as I don’t want to waste my own ‘page rank’ on supporting his misplaced anger.  But I suspect many readers of my blog have stumbled across that one as well, given the similarity of our keywords.    His blog doesn’t contain personal comments, I suppose because there are only so many ways to say ‘darn that Suboxone’.  Instead he auto-posts stories from across the country from newsfeeds, with keyword combinations of ‘Suboxone’ or ‘buprenorphine’ plus ‘robbery’, or ‘death’, or ‘overdose’, or ‘real bad person.’  I made the last one up, but you get the idea.
The person lost his son several years ago, a tragedy that would usually keep me from adding my own commentary.  But in the several years since his son’s death, he has written a number of diatribes on other anti-buprenorphine web sites.  In other words, he has contributed to the deaths of enough young people that by now, counterpoints are long overdue.
In his ‘about me’ section, he writes that his son took Suboxone for about 18 months, and died over two years after stopping buprenorphine/Suboxone.  He explains, in twisted logic, how the death is not the fault of his son’s drug addiction, or the drug dealers, or easy prescribing of prescription opioids or diversion of opioid agonists, or poppy policy in Afghanistan… but because of Suboxone.
He argues that his son’s Suboxone treatment was a ‘waste of time.’  I don’t understand that argument.  Suboxone added 18 months to his son’s life—and if his son had continued taking it, would likely continue to keep his son alive.  Hardly a waste of time.
I’m always impressed by how two people can see the same information and come to opposite conclusions.  He writes that during his son’s time on Suboxone, his son was prescribed over 13,000 pills, including opioid agonists and benzodiazepines.  He doesn’t say who it was who prescribed those 13,000 pills, and doesn’t apparently hold any ill will toward the people who did.  Instead, he blames Suboxone for not keeping his son from doctor shopping, for not keeping doctors from being duped by his son, and for his home state not having the type of database that tells doctors about problem patients.  If a ‘good medication for addiction’ is going to have to do all of those things, I wouldn’t hold out much hope for a new drug approval anytime soon!
The logic he uses on the web site brings to mind a recent encounter with a patient who has successfully stopped opioids, but who is struggling with other addictive substances.  Suboxone (or buprenorphine) is one piece of a person’s recovery, and does that one thing remarkably well.  Suboxone reduces cravings for opioids, making it much more likely that a person willing to do his part of the work will be successful in stopping opioids.   But it doesn’t do everything!  It doesn’t create an interesting life. It doesn’t keep a person from lying.  It doesn’t CURE addiction.  Buprenorphine is a tool that helps people who are ready to help themselves.  Our job as doctors is to try to match the limited treatment slots with the people who are serious about sobriety.  If the doctor treating his son was wrong about anything, it was in that regard—for taking in a patient who was not serious about staying clean.
The other thing that Suboxone or buprenorphine does, remarkably well, screams out from the tragic story.  His son stayed alive while taking buprenorphine, despite taking over 13,000 doses of other dangerous, controlled substances.  Despite the reckless drug use, buprenorphine kept his son alive.  As I’ve written many times, it is very difficult for someone taking buprenorphine or Suboxone to die from overdose.  But when the medication is stopped, that protection goes away.  Should we blame nitroglycerin for NOT stopping heart attacks because a patient chose not to take it?  When a person refuses chemotherapy and then dies from cancer, do we blame the chemotherapy?
The person with the blog writes that he is ‘all about detox and abstinence’.  Who isn’t?!  I’m ‘all about having shorter winters in Wisconsin.’  Should I blame the heating oil companies for the weather we’ve had?   He is angry that doctors who prescribe buprenorphine are not more interested in STOPPING the medication.   He is angry at RB for their lack of interest in detox, and their goal to maintain compliance with their medication.  He wants more people to be in his son’s position—fighting opioid addiction without the benefit of a medication that reduces interest in opioids and prevents overdose!
Those of us who prescribe buprenorphine know the value of the medication for keeping people alive.  I have known a number of family members who bullied patients over their use of buprenorphine.  In at least six cases, those family members won out, and the patients stopped buprenorphine.  In at least six cases, they stayed off buprenorphine, all the way up until their overdose death was announced in the obituary section.  I’m not pointing any fingers…. but I certainly wouldn’t blame the outcome on Suboxone.

Suboxone Side Effects

I’ve received questions over the years from people claiming a range of symptoms from Suboxone or buprenorphine, from back or muscle pain to fatigue, depression, or irritability. I didn’t invent Suboxone, so I don’t take it personally when people blame commonly-occurring symptoms on the drug. But I get bored by the non-scientific thinking behind such claims— that since they started buprenorphine at some point in the past ten years, every symptom or illness that comes along must somehow be related to buprenorphine. No matter, apparently, that people who DIDN’T start buprenorphine often develop the same symptoms. And no matter that they themselves have done a number of things over the past few years BESIDES start buprenorphine. But over and over, people insist that they know, without a doubt, that buprenorphine has to be the problem.
I also get frustrated answering questions about these symptoms when people who complain about them are closed off to other explanations. When I point out that many non-buprenorphine patients have the same complaints, my comments provoke anger. Sometimes I’m accused of having a vested interest to keep people on buprenorphine (I don’t-beyond wanting to provide good medical care).
I have a long waiting list of patients and buprenorphine is only a small part of my practice, so I have no reason to compel use of buprenorphine. But I don’t like the risk that my own patients, or others, might be swayed by faulty logic and fret over problems that have no logical basis.
To the people who have written to ask about feeling depressed, anxious, irritable, numb, sleepy, wakeful, or dulled by buprenorphine, my answer is that in almost all cases, people on buprenorphine feel the same way they would feel if they were not on buprenorphine. People develop full tolerance to the effects of buprenorphine at the mu opioid receptor, so from a scientific standpoint, people on stable doses of buprenorphine should feel ‘normal’. Beyond the science, I can say that after treating over 800 patients with buprenorphine over the past ten years, I have seen no evidence that buprenorphine causes depression, irritability, chronic pain, emotional numbness, lack of interest in things, or personality changes. Honest.
Whenever I answer an email or forum post about buprenorphine I try to think of an explanation for the person’s perception. I try to give the person’s history the benefit of the doubt. I might have a couple of explanations for why someone might feel different on buprenorphine.
One case would be a person who is taking too little buprenorphine to stay above the ceiling threshold. Many doctors, and some patients, apply constant downward pressure to the dose of buprenorphine, I assume because of thinking that less buprenorphine is closer to total abstinence than a full dose of buprenorphine. But the benefits of buprenorphine are lost in doses insufficient to reach the ceiling effect of the medication. People taking too little buprenorphine will experience irritability, fatigue, sweating, and depression when the drug concentration drops below that level. The solution is to increase the dose enough for blood levels to stay above the ceiling threshold.
Another possible cause of irritability requires some speculation on my part. Actively-using addicts have very straightforward problems, which boil down to having enough narcotic to avoid getting sick every few hours. I’ve noticed that my own patients sometimes feel stressed or anxious in early buprenorphine treatment, as they become aware of all of the problems that were less-visible during active addiction. Most of that anxiety is only temporary, resolving as patients catch up with bills, settle legal issues, and feel less shame about behavior during active addiction.
Along the same line, active addiction sometimes allows people to postpone changes that really should be made, but were not possible during active addiction. Bad marriages seem less bad when surrounded by misery and chaos. But when a person finds happiness and moves forward in life, a miserable or abusive partner becomes more noticeable. Or maybe a marriage seemed ‘healthier’ when the partner was making the money necessary to support a drug habit. Effective treatment of opioid dependence empowers patients to make positive changes. But even positive changes come at the cost of emotional pain.
The people who remain convinced that buprenorphine is causing side effects would be best served by an open mind. Most of the complaints that I read about are identical to the complaints of my non-buprenorphine patients, and the most successful interventions include healthy living, stress reduction, and moderate exercise. Stopping buprenorphine is not going to be helpful in the absence of these interventions.
There is also the risk that the symptoms are caused by something other than buprenorphine—something more serious. An extreme example would be blaming buprenorphine for fatigue that in reality is caused by anemia, thyroid dysfunction, or heart disease. That situation is made even worse by the common behavior of doctors, who tend to blame any unexplainable symptom on the medication the patient is taking that the doctor knows the least about. Too often I’ve told patients to go to their GP because of unexplained muscle weakness, numbness, headaches, fatigue, or weight loss, only to have the doctor send them out without any tests or treatments, other than telling them to ‘stop Suboxone!’
Anyone reading this post, who truly suffers from adverse effects from buprenorphine, should report the side effects to the FDA web site so that clusters of symptoms, if present, can be identified.

Suboxone Makes Me Fat and Boring and Stupid

Originally posted 3/6/2013
A late post tonight, since my new exercise program has pushed my blogging back by an hour or so each night.  My suspicions about exercise were correct, by the way; it is much easier to suggest exercise to other people than it is to actually exercise.  I’ve been at it since the beginning of the year, and I at least feel a bit less hypocritical.
While I’m on the topic…  I’ve received many comments over the years from people complaining that they’ve been taking Suboxone or buprenorphine for X many years, and they have no energy, they feel stressed, they have gained weight, they don’t sleep well or they sleep TOO well… and concluding that all of the problems are from Suboxone.
Suboxone causes… everything!
They aren’t (from Suboxone).   Not at all.  But I wonder, at this point, if regular readers of my blog know EXACTLY what I’m going to say.  I’m tempted to stop typing and ask people answer so I get a sense of how predictable I’ve become.    But then I’d have to wait and then come back, read, and assess the situation….  I really can’t imagine much positive to come out of THAT experience, so I’ll just finish my thoughts, about the problems that people often blame on Suboxone.
The problems are the result of other things, including things that tend to occur naturally as our lives become less chaotic and more outwardly-secure.  The problems I mentioned above, for example, come from inactivity.  They come from thinking that we’ve ‘paid our dues’ at the age of 30, and it’s time to coast in life.  They come from failing to seek out challenges, and from failing to do our best to tackle those challenges.  They come from letting out minds be idle, smoking pot or watching American Idol  instead of responding to the naggings sense of boredom that ideally pushes people to join basketball, tennis, or bowling leagues.
Our minds and bodies are capable of SO much.  I (honestly) am not a network TV viewer, but I love the contrast of ‘before and after’ scenes on ‘Biggest Loser.’  People magazine (it sits in my waiting room) had a section a while back about people who lost half their body size, by exercise and dieting.  The part I found most interesting was the deeply personal answer that each person had to the question, ‘what was your turning point?’  Each cited an episode of humiliation or shame that lifted the veil of denial, and helped them do what they knew, all along, needed to be done.
We are not all capable of ‘Biggest Loser’ comebacks. But it is important for people to understand that feeling good, physically or mentally, takes work.   That incredible feeling of a ‘sense of accomplishment’ only comes when we accomplish something.  We don’t need to eliminate global hunger or cure cancer; sometimes we just need to shovel the driveway, mow the lawn, or do a crossword puzzle.  I’ve learned, as a psychiatrist, that the people who walk around with smiles on their faces usually did something that made the smile happen.  I’ve learned that ‘feeling happy’ does not just happen for most people.  And I don’t think I’ve ever met a person who answered, when asked about stress, ‘no—I don’t have anxiety.’
Once someone blames Suboxone for their problems, it becomes less likely that the real causes of those problems will become apparent. For example, If I think that my glasses are giving me headaches, I’m less likely to make changes in my diet that might make the headaches better.  Once we have something to blame, our problems become more and more engrained, and the real solutions become less and less evident.
I’m truly sorry if I am coming across as ‘preachy’; understand that I’m just trying to make my way through life like everyone else.  But I now take note of all those people power-walking at 6 AM, and I understand why they do it.  Some of them might be on Suboxone.  Some of them might not be.  But I respect all of them for opening their minds, and for their willingness to do the hard work that brings happiness—or at least points in that general direction.

Suboxone Side Effects Pt. 2

Originally posted 1/2/2013
We can now leave naloxone out of the discussion, and focus on the side effects of Suboxone that are caused by buprenorphine.
Side effects are symptoms caused by a given medication that are not part of the therapeutic benefit of that medication.  Whether a symptom is a side effect depends on the reason for taking the medication.  For example, decreased intestinal motility is the desired effect of opioids used to treat diarrhea, but a bothersome side effect when taking opioids for pain.  The term ‘side effect’ is not on the package insert for medication, the symptoms and actions instead referred to as ‘adverse reactions.’  Package inserts also have a section entitled ‘warnings and precautions’ where the most dangerous adverse reactions are listed.
Some medications have a ‘black box warning’ for adverse reactions that are particularly common or particularly dangerous, consisting of a frightening statement at the start of the package insert (enclosed, naturally, by a black box). Black box warnings in psychiatry include the warning for increased suicidal ideation in children and adolescents treated with antidepressants, and the increased risk of death in people with dementia treated with atypical antipsychotics.
Increased risk of cancer or mutations, and effects on fertility or fetal development, are listed in yet another section entitled ‘nonclinical toxicology.’  They are listed as ‘nonclinical’ because the events do not involve the intended physiologic system or pathway targeted by the medication.  For example, slowing of intestinal activity by opium is either treatment of diarrhea or unwanted constipation, but in either case the outcome is caused by actions of opioids at opioid receptors.  If the opium molecule happened to bind to DNA and cause cancer, the cancer would be nonclinical toxicology, not a side effect.  Carbamazepine decreases the excitability of neurons to prevent seizures, and the sedation caused by the slowing of neurons is considered an adverse reaction. Carbamazepine impairs fetal development through different actions, considered nonclinical toxicology.
All of these divisions can be picked apart so that division of symptoms to one category or another will appear arbitrary.  The system is not precise, by a long shot.  But it may be helpful to be aware that one person’s ‘adverse reactions’ are another person’s intended therapeutic effect.  Some people find the mood stabilizer quetiapine too sedating;  others find the sedation critical to a good night’s sleep.
Allergic reactions are yet another issue.  To put it simply, medication allergies are not something that the medication does to the body, but rather something that the body (the immune response) does to a medication—and the inflammatory fall-out from that reaction.  While the distinction sounds like splitting hairs, the true nature of a reaction can be important.  Nausea is a common adverse event from the action of opioids, used for pain control, at opioid receptors.  Through intellectual laziness, a patient with nausea from morphine in a hospital is often incorrectly labeled as having a morphine allergy. Because of the bureaucracy of modern medicine, the patient has had a very useful medication removed from the armamentarium of treatment options, in essence forever.  Analogous situations are ‘allergies’ to antibiotics like erythromycin.  Allergies tend to become worse with each medication exposure, whereas adverse reactions often go away over time.
Am I going to need a part 3?
Things actually get pretty simple from here. Buprenorphine, like other opioids, has a range of predictable effects that occur along the dosage spectrum— a spectrum that is relative to the person’s opioid tolerance.  Doses of buprenorphine low on the person’s tolerance spectrum fail to have the desired action of preventing withdrawal.  Doses that are close to a person’s tolerance level have the desired therapeutic effect, i.e. blocking withdrawal and a reduction in cravings for opioids.  Doses in this range commonly cause ‘ileus’, i.e. disruption of the normal movement of the intestine.  Ileus in turn causes a number of symptoms, including constipation, cramping, bloating, loss of appetite, and nausea.  Constipation can lead to increased intestinal pressure, leading to hemorrhoids or diverticular disease.
Apart from ileus, buprenorphine and all opioids have direct actions at the base of the brain, at the ‘area postrema’.  Actions at the area postrema cause nausea as an adverse reaction, or in other cases the desired therapeutic effect of induced vomiting.  Nausea is very common when doses of opioids are taken that are at the upper end of tolerance, making nausea particularly common with potent opioids like buprenorphine.  Impaired coordination, slow reflexes, sedation, slurred speech, and somnolence are also caused by strong opioid effects.  Combinations of these effects are obviously quite dangerous.
Opioids reduce the tone of the ‘gastroesophageal sphincter’, increasing the chance of acid reflux, heartburn, hoarseness, and theoretically even esophageal cancer in severe cases.
Cough suppression by opioids might be a therapeutic benefit, but can be an adverse reaction if gastric contents are aspirated into the lungs.
Opioids reduce the response of the brain’s respiratory centers to carbon dioxide, resulting in less drive to breathe.  Carbon dioxide level therefore goes up, and the rise in CO2 increases brain blood volume and in turn, intracranial pressure.  The increased brain pressure reduces the flow of fresh, oxygenated blood into the brain.  Because of this potentially-disastrous sequence of events, opioids must be used with caution in people with head injuries.
Respiratory depression is a common reason for overdose, but even that adverse event can be a desired therapeutic benefit in some cases, for example in patients who are on a ventilator and triggering the machine to cause hyperventilation.  Respiratory depression is even used therapeutically to reduce ‘air hunger’ in people at the end of their lives, to relieve suffering in patients and patients’ family members who are witnessing the death.
I realize that a simple list of side effects would have been easier to read, but like the proverb says about giving a man a fish, I’m hoping that running through the processes will help people figure out, for themselves, what their medications are doing.
What else…  pruritis or ‘itching’ is a common side effect of potent opioids, that doesn’t respond very well to the usual anti-itching treatments like diphenhydramine or steroids.  All common opioids except meperidine (Demerol) constrict pupils, which often makes daytime vision sharper, but impairs night vision by allowing less light to fall on the retina.
Opioids reduce immune function through a number of physiologic interactions, including the presence of opioid receptors on immune tissue. Opioids can have a range of effects on mood and mood disorders.  All opioids, including buprenorphine, have the potential to reduce testosterone levels in men, which in turn can affect mood, libido, and sexual performance.  Opioids alter the release of vasopressin, changing how much water is conserved by our kidneys—which in some people results in more trips to the bathroom at night.
Buprenorphine and other potent opioids interfere with the initiation of ‘micturition’, i.e peeing, particularly in men who are already struggling from an enlarged prostrate.
I know that I’m missing something, and I invite people to write and help me out.  I also realize, as I write this, that I don’t have a package-insert category for a particularly common worry about Suboxone, that it is hurting one’s teeth.  Such a reaction, were it found to be attributable to Suboxone, would probably be considered nonclinical toxicology, although a recent case report proposed that buprenorphine could increase cavities by reducing the immune response in teeth, which sounds more like an adverse reaction.  In either case, I’ve written about the lack of evidence for tooth damage from Suboxone, but the topic still appears on my forum now and then.
That’s all for now…

Sick from naloxone, maybe?

A person wrote about feeling sick after taking Suboxone, thinking that naloxone is to blame and frustrated that her physician would not prescribe Subutex:
I first read your blog last week as I was going through the despair and misery of withdrawal from Percocet, and considered suicide. I didn’t want to die, or create anymore suffering for my family; I just didn’t see any options or hope. Your well written words (I thank you deeply) about the hell of withdrawal got my attention & brought me to tears. I continued to read, found out about Suboxone, which led me to message boards from others like me. For the first time I felt hopeful. I found a doctor and made an appt, and after the initial, office administered dose I found myself feeling the best I had in years– no withdrawal and no physical pain – wow! At the 2hr follow-up I told (the doctor) that my pain was completely gone, which she disputed, saying it’s not prescribed for pain. What I know now is that she had given me Subutex in the office, and a Suboxone prescription to take home!!I filled the prescription, took the ½ pill dose, and within minutes my stomach hurt/gnawed, and I developed a very strange headache and mild to moderate chest pain. By the evening I’d vomited and the headache worsened. By next morning I had the worst headache ever and started vomiting large amounts of bile, all of which continued throughout the day. My doc insisted I show up for the follow up appt. that day, even though I was too sick to hold my head up. She insisted I was sick from withdrawal

Image result for chemical structure of naloxone 3d
Naloxone, a mu-opioid receptor antagonist

To date I’m taking 3 Excedrin for migraine within an hour of every Suboxone dose as I get a bad headache every time.  I also wake up with a moderate headache every day. The last few days I’ve noticed I don’t feel emotions, joy, or happiness. I feel depressed & don’t care about things that would typically give me happy goose bumps – my grandkids, my dogs, sunsets.

I asked the sub doc to put me on Subutex which she refused to do. I explained that if someone was this ill from BP or diabetes meds, and there were other options, it would be unethical to not help the patient. I spend $180 for medication that makes me ill- every day.
I’ve spent the day trying to find a doc who will prescribe Subutex, with no success. Ironically, a few years ago my own doc recommended this drug for my back/leg pain.  I don’t know what to do.  I can’t stay on Suboxone or go off. Do you have any suggestions? 
 My answer:
I hope that your weekend is going OK.  I have a few thoughts about your situation, but I don’t know how much help they will be, as ultimately you are dependent on the prescribing doc.  But maybe we will find something that will help.
It sounds like you have a pretty good understanding about buprenorphine and Suboxone, but there are a couple areas that need clarification.  For most people- more than 95% of people in my estimation—there is no difference in the subjective experience from taking Suboxone vs. Subutex.  The active drug, buprenorphine, is present in both, and the naloxone that is present in Suboxone has no significant effect.  The ceiling effect of Suboxone is due to buprenorphine;  naloxone plays no role in that effect.  Both Suboxone and Subutex can be used for pain, and both can be used for ‘induction.’  There are some misguided physicians out there who think that Subutex is a better choice for induction, thinking that naloxone will cause withdrawal during the induction process—but those doctors are wrong.  Both Suboxone and Subutex cause precipitated withdrawal, which comes from buprenorphine, not naloxone.  Naloxone does not pass through the mucous membranes lining the oral cavity, and instead ends up being swallowed, and taken up into the portal vein from the proximal small intestine.  In MOST people, naloxone is then rapidly destroyed by the liver before getting into the systemic circulation.  In a FEW people, though, naloxone causes side effects.  Side effects are of two basic types.  The first type is an allergic reaction to naloxone, causing flushing, wheezing, and perhaps nausea, vomiting, and/or rash.  Allergic reactions can occur from very small amounts of a substance, and so people can have allergic reactions to naloxone even when the drug is essentially cleared by the liver and too little remains to cause symptoms of withdrawal.
A second type of reaction is more common in my experience, and that is where the naloxone is not destroyed well be the liver and instead gets into the systemic circulation and then to the brain and spinal cord, where it blocks the opiate effects of buprenorphine.  In this case the person would have typical symptoms of withdrawal, including headache, depression, anxiety, restlessness, pain, diarrhea, and nausea.  Naloxone is not a long-lasting medication, so I would expect the withdrawal-type symptoms to last only for several hours.
As I mentioned, naloxone is usually destroyed very efficiently by the liver before reaching the systemic circulation, a process called ‘first pass metabolism.’.  There are many medications that interfere with liver enzymes, although I do not know of specific inhibitors of the enzymes that destroy naloxone.  In other cases, people have a genetic background that results in reduced metabolism of certain substances including naloxone.  Your symptoms occur shortly after each dose, which is what we would expect in a person who is not fully metabolizing naloxone.
I do not know why your physician is refusing to prescribe Subutex, but it sounds as if she is concerned about diversion.  In my opinion, concern in this instance is misguided.  Yes, there is a diversion problem with buprenorphine, but there is not a difference between Suboxone and Subutex in this regard—i.e. BOTH are diverted.  Studies suggest that buprenorphine is not generally diverted for the purpose of ‘partying’ or getting high, but rather is taken by addicts who are trying to treat themselves to get off opiates, or who need something to carry them over when heroin or oxycodone are not around.  In either case, the presence of naloxone does nothing to reduce diversion.  As you likely know, naloxone only prevents against intravenous use of Suboxone—a type of diversion that accounts for a very small percentage of cases.
You are welcome to share this with your physician.  Unfortunately there are some thin-skinned doctors out there though, so be careful that you do not get yourself kicked out of treatment!  I have a couple other suggestions that might be safer.  First, you are welcome to send me a list of medications you are taking, and I will check to see if any of them are inhibitors of the liver enzymes that metabolize naloxone.  Prozac, for example, is a potent inhibitor of one group of enzymes, and therefore can affect the half-life of a number of medications.
A second thing you can do has been described in earlier posts.  The idea is to absorb the buprenorphine without absorbing the naloxone.  Since naloxone is taken up only at the intestine, the key is to avoid swallowing the naloxone.  Start with a dry mouth.  Put the tablet in your mouth and bite it into pieces to get it dissolved in a small volume of saliva.  Then use your tongue like a paint brush, and spread the concentrated saliva over the mucous membranes in your mouth for about 10 minutes.   After ten minutes spit out the saliva, which contains the bulk of the naloxone.  Be sure to avoid eating or drinking for about 10 more minutes, as you don’t want to rinse away the buprenorphine that is attached to the surfaces in your mouth.   This method of dosing seems to be more efficient than placing a tablet under the tongue, and allows more control over the absorption of naloxone.   I’ve had a number of patients who initially felt that their dose of buprenorphine was too low, who then felt better dosing this way.  And I have had a few patients who believed they were getting headaches from naloxone, who had fewer headaches after dosing this way and spitting out the naloxone.
One final thought.  I did not address your comments about joy, happiness, passion, or depression because it is usually not a good idea for us addicts to focus on whether we are adequately ‘feeling’ those things.  Opiate addicts tend to spend too much time looking ‘inward,’ thinking about how they feel.  One goal with treatment is to get them thinking about things OUT THERE in the world, rather than about how they are feeling ‘inside’  (Don’t confuse this point, though, with ‘feelings work.’  Addicts tend to have a hard time identifying feelings and recognizing the nuances between one feeling and the next, and there is much to be gained in working on identifying and recognizing feelings during group or one on one psychotherapy.  This work is to be distinguished from the self-obsessed search for happiness that many of us addicts get wrapped up in from time to time).  Once a person decides he/she is not feeling ‘passion,’ the absence of passion becomes a self-fulfilling prophecy.  The same holds for feeling sad, lonely, or depressed.  I do not have an explanation for why Suboxone vs. Subutex would result in a lack of happiness or passion, except perhaps by causing low level withdrawal symptoms that affect mood.  I SUSPECT that those feelings are more ‘psychological’ than anything else.   I also do not know why your symptoms on Suboxone last all day long, although I suppose it is possible that for some reason your body metabolizes naloxone extremely poorly, causing it to sicken you for the entire period of time between doses.
If the ‘spitting technique’ works, that is one more bit of data that you can take to your physician.  Hopefully, if that is the case, she will have a change of heart.

High Dose Buprenorphine (HDB) and Toxicity Concerns

Several weeks ago an article with a provocative title was posted at Suboxone Forum.  I don’t remember the exact title, but it was something like ‘Toxicity from High Dose Buprenorphine (HDB).  Before everyone gets too excited, there was nothing all that new in the article, which consisted of three case reports about deaths of people taking buprenorphine.  One case consisted of a suicide from very large doses of buprenorphine, one was a death from combining buprenorphine with other respiratory depressants, and the third death was in a person with liver failure who took buprenorphine with other psychotropic medications.  There are a couple issues brought up in the article that are worth mentioning.
First, I appreciate their use of the term ‘high dose buprenorphine,’ and this was the first time I came across the distinction between the historical use of buprenorphine in microgram doses for treating pain and the more recent use of milligram doses for treating addiction.   Buprenorphine is an extremely potent opiate; the ceiling effect protects from overdose in the absence of other respiratory depressants (with some exceptions– see below) and places a ‘cap’ on tolerance to the medication, but buprenorphine reaches maximal effect at a very low dose.  The potency of buprenorphine is more similar to that of fentanyl or sufentanil than to morphine or oxycodone.  Transdermal formulations of buprenorphine used for pain release doses of buprenorphine between 5 and 75 MICROgrams per hour.  The most popular dose of buprenorphine used for opiate dependence in the US is the 8 mg Suboxone tablet, which contains 8000 micrograms of buprenorphine!  It is likely that one reason for the occasional death from buprenorphine ingestion relates to fact that a fraction of an 8 mg tablet is about as potent as an entire 8 mg tablet, and novices to buprenorphine make the mistake of thinking that a very small piece will be less likely to kill them than taking an entire tablet.  Because of the ceiling effect and high potency, there is little if any protection in taking a small piece of a tablet.
While the ceiling effect offers some protection against overdose from buprenorphine, there is no protective ceiling effect to the actions of the drug’s primary metabolite, norbuprenorphine.  There have been deaths attributed to the ingestion of very large doses of buprenorphine where the metabolite accumulated to levels that caused respiratory arrest.  It appears that norbuprenorphine does not accumulate to levels sufficient to cause respiratory arrest in people with intact liver function who are taking standard, FDA-approved doses of Suboxone.  But there are a number of medications that inhibit certain liver enzymes, and it is conceivable that the right combination of medications and a large dose of buprenorphine could result in potent respiratory depression.  A number SSRI’s interfere with liver enzymes, the most potent perhaps being fluoxetine or Prozac, but in the case of SSRI’s the enzyme affected converts buprenorphine to norbuprenorphine.  Fluoxetine may in fact then offer a protective effect by preventing conversion of buprenorphine to the more-dangerous metabolite norbuprenorphine.
The respiratory depression potentially caused by norbuprenorphine again draws attention to the fact that very high doses of buprenorphine are used when treating opiate dependence.  We know much about the metabolism and actions of microgram doses of buprenorphine, as the medication has been around for over three decades.  But a number of attributes of the medication change at very high doses.  One very significant change is in the half-life of the medication.  Microgram doses are metabolized in several hours, but at milligram doses the metabolizing enzymes become overwhelmed, increasing the half-life to one to three days.  This increase in half-life is very useful when using buprenorphine to treat opiate dependence… but can be cumbersome when trying to rid the body of buprenorphine, say before elective surgery.
The most frightening question about HDB is whether there are toxic effects from such use that have not been apparent after years of microgram dosing of the medication.  Because of this blog I receive a number of messages from people who take buprenorphine.  I have heard of several cases of neurological illness in people taking buprenorphine, but I have no idea whether the reports represent higher frequencies of illness than would be expected in the general population.  Specifically, I have heard about a person with dementia, a person with encephalopathy, and a relatively young young person who developed symptoms of Parkinson’s Disease.  In all cases, the person was taking buprenorphine for several years.
At this point I must say DON’T HAVE A COW.  To date, several hundred thousand patients have been treated with HDB;  we would expect a number of those people to come down with these conditions in the ABSENCE of any connection between buprenorphine and neurological illnesses.  I continue to prescribe buprenorphine, and I believe WITHOUT RESERVATION that the medication is the best, most appropriate treatment for MOST cases of opiate dependence.  I think it is probably clear to most readers by now that I am not in bed with Reckitt-Benckiser;  I will always write about any concerns that I come across about the medication without delay.  I regularly scan the literature for articles about buprenorphine, and I run literature searches in response to any serious concerns by people in my practice or on the forum.  I also ask that if anyone is aware of a case of neurological illness in a patient who takes buprenorphine, that they contact me so that I can report the information to the FDA.
JJ

Tired and Sick on Suboxone: What Would Junig Do?

I recently receive e-mails or read posts at Suboxone Forum that go something like this:
I used all kinds of pain pills over the past ten years—Vicodin, then oxycodone, methadone, and even fentanyl patches. Then I got into heroin for a year and finally hit my rock bottom. I went to a Suboxone doctor and he put me on 16 mg per day. At first everything was great, but I don’t like the side effects. I get so tired every day. I’m not happy like I used to be. I wake up in the morning and don’t have any energy or excitement for life. I really don’t like what the Suboxone is doing to me and want to stop.
Sometimes it is a little different—the first part is the same, but then the person writes:
I really wanted to stop taking it so that my body is free of chemicals so I stopped. I was real sick for a month and now I don’t feel like myself—I am tired, I feel depressed and angry, and I’m wondering what the Suboxone did to my opiates—am I ruined forever?
I am a psychiatrist, and only about a third of my practice consists of addiction work. I get e-mails at times after people read the blog for my psychiatric practice at www.patienttimes.fdlpsychiatry.com. A typical message will be similar to this:
Dear Dr. Junig (they tend to be more polite to me there),
I used to be a very happy, energetic person. In high school I was outgoing and everybody liked me, and I had tons of friends. The problem? Now I am in my 30’s and I’m never happy anymore. I have worked at the same place for ten years (or maybe, I change jobs every 18 months) and every day I wake up and dread getting out of bed and going to work. I keep telling myself I should exercise, but I never get started actually doing it. I’m single and don’t have any interest in dating (or maybe, I’ve been married to the same person for ten years and sometimes I can’t stand the look of him). I’ve read about vitamin D deficiency and wonder if that is my problem—all I know is that I am getting more and more depressed and tired. My sleep is crappy too. What should I do?

I have an answer to the first two messages, and the third message is a hint. Does anyone know how I would reply to the first two messages? What would I say? If you get my point and describe it correctly in the comments section—either describe the -general point, or write the reply that I would write– by 6 PM Central time tomorrow, Sunday, September 27, I will send you a free copy of my e-book ‘user’s guide to Suboxone’. EVERY person who gets it correct will get a copy. The ONE person who explains my point the best will receive the user’s guide plus a copy of each of these three recordings—stopping Suboxone, how long will you take that stuff, and opiate dependence treatment options. That’s like almost a thousand—or a hundred dollars—something like that. You don’t have to put your real name or e-mail address, but your comment MUST be entered in the comment section after this post. I might have to approve it if you haven’t written a comment before, but that’s OK—it will still count, as long as it is written and submitted by 6 PM. C’mon folks—take a shot!
JJ

Suboxone and Urination

OK, so this isn’t the most exciting title one will see about Suboxone… but urinary complaints are some of the more frequent side effects that I hear about from Suboxone.  The complaints fall into two or three different categories.  Realize that these are NOT complaints that I have read about in the literature or heard about from the manufacturer;  these are things that I hear in the course of my practice from patients on Suboxone.
Frequent Waking to Urinate
During normal sleep the body does several things to turn off the production of urine by the kidneys.  The pituitary gland releases a drug called vasopressin or ‘antidiuretic hormone’, causing the kidneys to reabsorb more of the water in the distal tubules of the kidney, making the urine more concentrated and lower volume.  Other hormones like renin and angiotensin are released by the kidneys and adrenal glands, causing the pressure in the filtration area to decrease and sodium to be absorbed in another part of the kidneys.  All of these things are intricately connected and balanced;  they are thrown off when you go to a late movie and order a large bag of salty popcorn and wash it down with a big coke, which adds fluid to your system and also caffeine, which stimulates water to flow from the bloodstream to the urine at an increased rate.
But in the absence of the popcorn and coke at the movies, the kidneys generally shut down so that you can sleep without the interruption of a full bladder.  Opiates throw all of this off a bit by affecting the secretion of these hormones.  The major effect is on antidiuretic hormone, but opiates have effects that are more subtle on a number of hormone systems.  The result is that patients on Suboxone make urine at night while they are trying to sleep, and their bladders fill up and wake them up, sometimes several times per night.  I suggest that people limit fluid intake toward the end of the day;  that will reduce the formation of urine and perhaps improve sleep.  There are other options for extreme situations;  a drug called ‘desmopressin’ is sold as a nasal spray, and it will shut down the kidneys for the night if necessary.  It is also used in children to reduce bedwetting.
I Gotta Go… Right Now!!
I have heard several patients complain that they will not have to ‘go’, but then suddenly… they WILL.  In fact, they suddenly have to go SO BAD that they will have an ‘accident’ if they aren’t near a tree to run behind.  I assume that this is the result of bladder spasms– sudden tightening of the muscles that squeeze the bladder and force urine to come out.  I don’t know the mechanism for this one, except that urination is a function of the ‘parasympathetic nervous system’– a part of the nervous system that controls all of our organ systems, including the bowel and the heart.  As I said before, opiates have effects throughout the brain, spinal cord, and peripheral organ systems;  some subtle, others more dramatic.  I have not heard about bladder spasms and Suboxone from the literature, although given the complaints by several patients I do watch for reports along those lines.


The act of ‘going’, or ‘micturition’, requires the parasympathetic nervous system to open things up…  this system shuts down for some guys when they are standing at the urinal at Lambeau Field, a long line of impatient guys behind them anxious to get back to watching the game. This is also called a ‘shy bladder’, and it occasionally leads to drunk men yelling ‘c’mon, just go and be done with it’ from the back of the line, usually as they dance around to avoid peeing their pants. Opiates interfere with this system as well. In fact, patients who receive spinal or epidural narcotics sometimes need to be catheterized in order to urinate for up to 24 hours. When I was an anesthesiologist we had a rule against using spinal narcotics for day surgery, and one reason was to prevent pateints from needing to return to the ER to have their bladders emptied. High doses of oral or parenteral opiates will often prevent a person from peeing as well.
I… Can’t… Go…
Those darn prostate glands!  Older guys get a bit blocked off by the prostrate gland;  this is aggravated by any drug that has ‘anticholinergic’ side effects. This can be a problem with some opiates, but I have not seen it as a problem from buprenorphine.
There it is… all you wanted to know about urination and more. Most people are also well aware of the effects of Suboxone on the ‘other’ part of bathroom business… but that is for another story. Until then… eat prunes and drink lots of liquids… but drink them early in the day so you don’t have to get out of bed to pee! All of this is just more evidence for the obvious… that the body works best when it is in its native state, and that any medication is going to throw things out of whack a little bit. With a potentially fatal illness like opiate dependence, the effects of buprenorphine on number one and number two are just trade-offs that must be made. Remember that we are in the very early stages of a new way of treating opiate dependence; in the future we will certainly have medications that avoid many or all of these side effects. Your job for now is to make sure you live that long!
SD

Runny Nose, Back Pain, Withdrawal in New Patient

This new patient has been on suboxone for two weeks, and reports having low back pain and a runny nose. He also feels that the 16 mg dose of Suboxone that he takes in the morning wears off by the end of the day. You can read my answer, and feel free to add your own experiences or suggestions:
Hi XXXXXXX,
I received your message.A couple thoughts…As far as pain goes, the suboxone has the analgesic potency of about 30 mg of methadone or about 50-60 mg of oxycodone.Your best bet, with or without Suboxone, is to avoid treating back pain with opiates– that is a dead end street with a pile of messed up lives at the end of it.It may be that you were treating aches and pains that you didn’t know that you had– often people on opiates will hurt their backs, knees, whatever, without knowing it, and continue to do more and more damage without the usual warning that our bodies give us (as pain).If you try to treat back pain with opiates long term, the tolerance requires higher and higher doses of meds, and the patients gets more and more messed up by the obsession for opiates.
Treatment for your back should include 1) rehabilitation either through physical therapy or by your own exercise and stretching routine, 2) anti-inflammatory medication like ibuprofen or naprosyn (over the counter as aleve), 3) avoid re-injury by learning correct lifting technique and avoiding certain things that you know will aggravate it, 4)ice after over-use, heat to loosen muscles at night, 5) getting enough sleep, and avoiding things that cause muscle spasm like caffeine, opiates, and alcohol.
Runny nose… that is sometimes a symptom of withdrawal. That along with your other questions suggests that your tolerance is higher than the opiate effect of suboxone. Give it time, and it will go away– if it is still there after a couple weeks I would start to think it is something else, like a virus.As far as the meds ‘wearing off’, I have had the benefit of seeing the pharmacologic data on the drug buprenorphine when I was doing my ‘treatment advocate’ training with the company. The drug lasts forever in us humans– when a person stops taking subox the ‘real withdrawal’ doesn’t hit for 3-5 days.In your case, you are likely feeling a combination of things. First, as I said in the prior paragraph, you are having mild withdrawal from ‘mismatch’ between your tolerance and the Suboxone– this will resolve soon. Second, it is not uncommon for people to have full- blown withdrawal symptoms that come from our brains ‘replaying’ our earlier withdrawals. Usually the more we focus on them, the worse they become. They will fade away as your tolerance adjusts– by the time I see you again they should be gone. In the meantime try to keep busy and distract yourself as soon as you sense them coming, or if they come at a certain time each day try to keep busy at that time. More Suboxone will not help, because of the ceiling effect of the drug– your receptors are all bound up at 8-16 mg/day.
J