Treatment? Or Murder?

I subscribe to Google news alerts for the phrase ‘overdose deaths.’  Google Alerts are a great way to follow any topic; subscribers receive headlines from newspapers and web sites for certain keywords from around the world. One thing that has become clear from my subscription is that there is no shortage of stories about deaths from opioids! Every day I see one article after the next, as news reporters notice the loss of more and more of their communities’ young people.

Along with the reports of overdoses are stories about doctors who are increasingly being prosecuted for the deaths of their patients. In an earlier post I described the case of Dr. Schneider and his wife, a nurse, who were tied to a number of overdose deaths in Kansas. That case stood out by the sheer number of deaths; the State charged the couple with the deaths of 56 patients. Cases involving fewer patients have become relatively common. The latest case that I’ve read about is a doctor in Iowa, who is accused of causing or contributing to the deaths of 8 people.

I try to present both sides of the argument when I write about this topic. I have been faced with the difficult decision over whether or not to prescribe narcotics many times, and I understand a doctor’s dilemma. The doctor sees a person who is in pain, and knows that there is a pill that will reduce that pain. But the doctor also knows, or SHOULD know, that initiating a prescription for narcotic pain medication always has unintended consequences, no matter how good the intentions of both doctor and patient.

In the Iowa case, the dilemma over narcotic-prescribing is very clear. The prosecution states that the doctor prescribed pain medication to drug addicts.  On the surface, that sounds bad, right? One gets the mental picture of dirty, lazy people, dissolving tablets in a spoon, over a candle, and then injecting the mixture. But reality is much more complicated. Patients with histories of opioid dependence do not always have track marks. And even if we tattooed the letter A across their chests, there are addicts who are in need of pain treatment. Are we to decide that every person who has become addicted to pain medication gives up the right to pain treatment?  And we know that many of the patients addicted to opioids became addicted through the course of pain treatment from their physician— so I would expect that on average, patients addicted to opioids would have a higher incidence of chronic pain, and vice versa.

I do not find it reasonable to make patients with addiction histories endure pain that would be treated in other patients.  Father than singling out some patients for ‘special non-treatment,’ we should prepare for the risks from opioids in ALL patients—a set of ‘universal precautions for opioid treatment,’ similar to the way we use a different set of universal precautions to avoid transmission of blood-borne infections.

There are times when doctors have to tolerate being the bad guys.  Some patients have been taught, through careless prescribing, that all pain should be treated with narcotics. Those patients are not happy when told, after paying several hundred dollars, that they do not ‘need’ narcotic pain medication– and so many of their doctors have a hard time saying ‘no.’ After all, doctors studied hard to do well in school, and usually receive praise for what they do. It is much easier to write a prescription and hear ‘thank you’ than to be called an unsympathetic jerk! But doctors are paid the big bucks to tolerate such things, and to keep the long-term health of patients in mind. And for many people with chronic pain, opioids will provide a good month or two, but for the price of many years of misery.

I’ve been told by patients “I don’t care about the risks, doc– I’d rather have three good months and then die, then have twenty years in pain.” I reply, “that’s why these medications require a doctor to consider things very carefully, and a good doctor would not allow someone to make that decision.” I’m sure that some people will be angered by that attitude. But the approach is similar to how we handle many other illnesses, where we encourage patients to tolerate short-term misery for long-term benefits. Many patients would refuse chemotherapy and give up on life if not pushed to move forward. And to depressed patients, suicide can appear a reasonable option. I’m a fan of free will, but I recognize that we don’t always choose our paths through life with full insight.

Even with full knowledge of the reasons to avoid narcotics, some doctors really struggle over withholding opioids.  I find it somewhat ironic that the doctors who are too ‘kind-hearted’—i.e. who want to please patients so much that they cannot deny even that which is bad for them—are the ones who end up getting into trouble.  The Iowa doctor is being sued over several of the deaths, likely by relatives of the patients who pled the hardest for pain pills!  Talk about good deeds not going unpunished!

But there are aspects of the case in Iowa that do not argue well for the doctor. Several of the patients who died were only seen once, but treated with narcotics for years. The DEA requires that patients are prescribed no more than 90 days of narcotic medication at one time (divided on three monthly prescriptions). I presume that patients were picking up scripts every three months, without having appointments each time. Such a practice is not strictly illegal (not that I am aware of, anyway), but the standard of care would be to evaluate patients on potent opioids every three months, or even more frequently. And one news article stated that the doctor had tens of thousands of pain patients. As a full-time practitioner with less than 1000 patients, I wonder how so many patients could be managed by one physician.

When I write about this topic I receive angry comments from some readers. Some attack me personally with comments like “I’m glad I’m not YOUR patient!” or “I hope YOU have to suffer with horrible pain some day!” I realize that this is a very hot topic, and my only intent is to educate and inform, to help people understand what is happening in the minds of physicians. Of course, the care of patients should not be determined by the need for doctors to protect their own interests. But at the same time, it is understandable that doctors are affected by headlines announcing the imprisonment of other doctors facing the same treatment decisions.

Bottom line– there are very good reasons to avoid using opioids for nonmalignant chronic pain. Just giving patients what they want, and ignoring the danger of opioids, will likely result in criminal and civil prosecution. But that reason is secondary to the most important thing– the promise all doctors make to first, do no harm. And patients should realize that their doctors may be withholding narcotics for that reason alone.

Hydrocodone (Vicodin) Addiction and Buprenorphine

I recently accepted a young man as a patient who was addicted to hydrocodone (the opioid in Vicodin), prompting a discussion about treatment options for someone who hasn’t been using very long, and who hasn’t pushed his tolerance all that high. Perhaps it will be informative to share my thought process when recommending or planning treatment in such cases. In part one I’ll provide some background, and in a couple days I’ll follow up with a few more thoughts on the topic.

Most people who have struggled with opioids learn to pay attention to their tolerance level—i.e. the amount of opioid that must be taken each day to avoid withdrawal or to cause euphoria (the latter about 30% more than the former). For someone addicted to opioids, the goal is to have a tolerance of ‘zero’—meaning that there is no withdrawal, even if the person takes nothing. That zero tolerance level serves as a goal, making having a high tolerance a bad thing, and pushing tolerance lower a good thing.

Tolerance is sometimes used as part of the equation when determining the severity of one’s addiction. But looking at tolerance alone can be misleading. Tolerance is a consequence of heavy use of opioids, and also a cause of heavy use of opioids. Tolerance usually goes up over time, so having a high tolerance probably correlates with length of addiction in some—- but not all— cases. Tolerance is also strongly related to drug availability. A person with a severe addiction, who only has access to codeine, will likely have a lower tolerance than a person with a more mild addiction, who has free access to fentanyl, oxycodone, and heroin.

I think it is more appropriate to measure the ‘severity of addiction’ by the degree of mental obsession that the patient has for opioids. Tolerance is one piece of information in determining that obsession, but tolerance alone can be misleading.

To get a sense of the obsession for opioids, I look at many factors. Has the person committed crimes to obtain the substance? Violent crimes? What has the person given up for his addiction? Has he been through treatment? How many times? How long did he stay clean after treatment? Have his parents or spouse thrown him out of the house, and if so, does he still use? Did he choose opioids over his career? Over his kids?

Answers to these questions provide a broad understanding about the addicted person’s relationship with the substance—an understanding that is necessary when considering the likely success or failure of one treatment or another. It is also important to consider the person’s place in the addictive cycle—i.e. early, likely in denial, cocky, with limited insight– or late, after many losses, more desperate—and perhaps more accepting of treatment.

I am a fan of buprenorphine as a long-term treatment for opioid dependence, as readers of this column know. I consider opioid dependence to be a chronic, potentially-fatal illness that deserves chronic, life-sustaining treatment— and buprenorphine, in my experience, is a very effective treatment in motivated patients. But tolerance becomes a factor, when considering buprenorphine for THIS patient.

Buprenorphine has a ‘cap’ or ‘ceiling effect’ that allows the medication to trick the brain out of craving opioids. In short, as the blood or brain concentration of buprenorphine drops between doses, the opioid effect remains constant, as long as the concentration is above the ceiling level. In order to achieve the anti-craving effects of buprenorphine, the dose must be high enough to create ‘ceiling level’ effects. If buprenorphine is prescribed in lower amounts—say microgram doses— the effect is identical to the effects of an agonist, since the dose/response curve is linear at lower levels.

Buprenorphine is a very potent opioid, and the effects of the medication are quite strong at the ceiling level. Comparisons to other opioids will vary in different individuals, but in general, a person on an appropriate dosage of buprenorphine develops a tolerance equivalent to that of a person taking 40 mg of methadone per day, or approximately 60-100 mg of oxycodone per day.

A person taking even a dozen Vicodin per day has a much lower tolerance to opioids. Such a person who starts buprenorphine treatment will obtain a very significant opioid effect from the drug— unless the dose of buprenorphine is raised very slowly over a number of days. And in that case, the person’s tolerance level would be pushed much higher.

So if our current patient starts buprenorphine, he will have a much higher opioid tolerance if/when the buprenorphine is eventually discontinued. I receive emails now and then from patients who are angry at their doctor for starting buprenorphine, feeling trapped by the considerable threat of withdrawal from stopping the drug. But at the same time, taking hydrocodone and acetaminophen in high amounts creates the risk of liver damage from the acetaminophen, as well as the considerable risks from opioid dependence.

And so the dilemma. Should buprenorphine be considered in such a case?

Jerk Counselor

Every now and then I hear about a therapist or addiction doc who is doing such a disservice to the practice of addiction medicine as to deserve special mention.  This week’s award goes to a certain counselor at a treatment program in Oshkosh, WI, who I’ll refer to as ‘This Jerk.’

I’ve made no secret, over the years, about my hope for addiction to eventually be treated with the same respect for patients and attention to medical principles as for any other illness.  I certainly try my best to work according to those ideas, and find that doing so really helps when it comes to making treatment-based decisions.  In other words, I’ll ask myself—if this person had diabetes, what would an endocrinologist do?  Or better yet—if I had diabetes, what would I want MY endocrinologist to do?

Some Jerks advocate punishing patients who struggle.

This Jerk Counselor

We all know that certain professions attract certain types of people.  Some of us have been pulled over by the cop who was the kid subject to playground taunts, now all grown up, determined to make life a living Hell for anyone with a loose seat-belt.  When I worked in the state prison system, I worked with guards who belonged in the same category; men and women who loved to carry keys to cages that held real people.  It’s the power trip, I suppose.

This Jerk apparently loves the power trip of ‘treating’ people who are sent back to jail for ‘failing’ his treatment.  He doesn’t have to worry about being a lousy therapist; he has a captive audience, and likes it that way.  One difficult aspect of being a therapist is treating patients who don’t like us for one reason or another, or who don’t kneel every time we enter the room.  But when This Jerk feels disrespected, he picks up the telephone and calls the patient’s PO to report ‘noncompliance with treatment’– then gloats about sending the patient to jail.

Treatment professionals who are in a position of unusual power over a patient must be particularly careful to empathize with their patient’s position.  In medical school, we were placed on gurneys and wheeled around by fellow students, to emphasize the vantage of patients coming to the emergency room.  We were taught to sit at the same or lower eye-level of our patients, as speaking down to people creates an unsettling power differential.

The power to prescribe or withhold buprenorphine (let alone the power to send to prison!) comes with an obligation not to abuse that power.  Withholding buprenorphine causes patients to go into withdrawal—something dreadful to people addicted to opioids.  Worse, withholding buprenorphine places patients at very high risk of relapse—which in turn places them directly in harm’s way from overdose and legal repercussions.

This Jerk, I’ve been told, takes issue with psychiatrists who continue to treat patients on buprenorphine who struggle with sobriety.  He considers it ‘good care’ to withhold buprenorphine from an addict who uses, supposedly to punish the patient into sobriety.

In case This Jerk (or a similar ethically-challenged counselor) is reading, I’ll point out the obvious:  when a doctor pulls the rug from under a patient by withholding medication, that patient might easily join the ranks of other dead addicts.  On the other hand, when I work with a patient who is struggling with sobriety, keeping the person on buprenorphine and working to identify triggers for using, that person almost always ‘gets it,’ eventually.

I’ve been working with people addicted to opioids, using this approach, for so long that the other approach—the punitive, ‘cut ‘em loose for struggling’ approach—seems barbaric.  I don’t understand how people identified as healthcare workers (nothing professional in his behavior!) rationalize the dismissive approach.  I suppose, if This Jerk views addicts as the scum of the Earth, or as people with weak characters, or people who lack ‘will power,’ punishing relapse by withholding treatment feels about right.  But most of us leave that world behind when we commit to helping people suffering from illness.

What’s This Jerk’s excuse?  Is it that he just doesn’t get it?  Or are there other motives at play?  With the current cap on patients on buprenorphine, the most lucrative way to practice is to keep turnover high, rewarding practices that hire therapist-idiots like This Jerk.

Or is it the power trip– that people with difficult addictions are an affront to therapists?  I’ve met therapists with this attitude before, who seem to have a form of codependency with their patients. They take credit for any success by their patients, but think the patients who fail are not worth their time, and should be dumped, expunged, or kicked-out to relapse and die.  I suppose This Jerk would say ‘not my problem!  I did MY job!’

Readers may suspect that this topic irritates me—and they’re right.  Maybe I’ve seen more death, up close, than the typical counselor.  I’ve attended autopsies; I’ve reviewed post-mortem photos from overdose scenes; I’ve pushed IV fluids into people with fatal injuries who presented for emergency surgery.  I have spent hours with the parents of young patients who died from overdose.  I’ve seen the parents’ faces as they struggled with the thought that they could, or should, have done something else—just one more thing to save their child.  Death, to me, is not ‘theoretical.’ It is not something to toy with, and certainly not something to invite into the life of a person who made me angry, for not recovering at MY pace.

I suspect that the Jerks of the world will continue to justify their sadistic approach to ‘treatment.’ But patients—at least SOME patients—don’t have to put up with that behavior.  People like This Jerk hold power over an individual with an addiction history, but there is power in numbers.  It is not appropriate to use one’s power vindictively, or to gloat over a patient’s struggle.  It is not appropriate to humiliate a patient in front of others.  If you see that behavior, collect witnesses, and bring it to someone’s attention.  Maybe that ‘someone’ will write a blog post about it!

Doctors in particular should treat patients with ALL diseases—including addiction—with respect.  It is not respectful, or ethical, to deprive a patient of life-sustaining medication—especially out of spite.  I look forward to the day when the thought of ‘kicking someone off Suboxone’ is viewed as similar to kicking a poorly-compliant teenage diabetic off insulin.

Would THAT make sense— even to This Jerk?

The Other Opioid Dependence Medication

Today I met with representatives from Alkermes who were promoting Vivitrol, a long-acting mu opioid antagonist that is indicated for treatment of alcoholism and opioid dependence.



I admit to some pre-existing bias against the medication.  I’m not certain, to be honest, whether that bias was based upon sound clinical reasoning, or whether it was based on personal, negative reactions to naltrexone in my past.  Or maybe, as a recovering opioid addict, I have negative feelings about anything that blocks mu receptors!

Vivitrol consists of naltrexone in a long-acting matrix that is injected into the gluteal muscle each month. The medication is expensive, costing about $1000 per dose (!)  That cost is usually covered by insurance, and like with Suboxone, Wisconsin Medicaid picks up the tab save for a $3 copay.  Alkermes, the company that makes Vivitrol, also has a number of discounts available to reduce or even eliminate any copays required by insurance companies.

I’ll leave the indication of Vivitrol for alcoholism for another post.  The indication for opioid dependence came more recently, and appears more obvious, given the actions of naltrexone at the mu opioid receptor.

In short, naltrexone blocks the site where opioids—drugs like oxycodone, heroin, and methadone—have the majority of their actions.  Blockade of that site prevents opioids from having any clinical effect.  There is some dose, of course, where an agonist would regain actions— an important feature in the case of surgery or injury.  But even in those high doses, the euphoric effects of addictive opioids would be muted.  People on Vivitrol, essentially, are prevented from getting high from opioids.

Back in my using days, I took naltrexone, thinking that doing so would help me get ‘clean.’  I didn’t wait long enough, however, and so I became very sick with precipitated w/d.  The makers of Vivitrol recommend waiting at least a week, after stopping opioids, before getting an injection of Vivitrol.  I suspect that a week is not long enough to prevent w/d, but I realize that it would be very difficult to expect patients to last longer, without using anything.  I would expect that any precipitated w/d could be reduced through use of comfort medications, at least for a day or two until the symptoms are mostly gone. This requirement, though, to be clean for a week or more is one of my problems with the medication.

As an aside, I was also prescribed naltrexone (oral tabs) at the end of my three months in residential treatment, and I took the medication for another three months.  I had no withdrawal or other side effects to naltrexone at that time.

Another issue was the concern that naltrexone has been connected to hepatic toxicity.  We discussed that issue today, including the studies that led to that connection—which are not compelling.  The discussion allayed most of my concerns about liver problems from Vivitrol.

Finally, I have always recommended buprenorphine over naltrexone because of the anti-craving effects of buprenorphine that result from the ‘ceiling effect’ of the medication.  I worried that naltrexone, by blocking the actions of endorphins, would actually increase cravings.  But that is not what the data shows.  In the studies with Vivitrol, cravings for opioids were dramatically reduced by the medication.  The mechanism of that effect is not entirely clear;  some of the anti-craving effect may be psychological, as addicts stop wanting something when they know there is no way to get it.  But there may be other complicated neurochemical effects at presynaptic opioid receptors that are not fully understood.

The bottom line is the result of treatment;  the very sick opioid addicts treated in the studies used by Vivitrol to gain FDA approval showed a profound reduction in opioid-positive urines, over a span of 6 months.

I suspect that I will continue to favor buprenorphine.  I do not buy into the ‘need’ some people describe to ‘get of buprenorphine as fast as possible.’  Buprenorphine is a very effective, safe, long-term treatment for inducing remission of opioid dependence.  But because of the cap, I am glad that another option is available to treat this potentially-fatal condition.  And I admit to perhaps being too quick to judge Vivitrol, which appears to be a safe alternative—particularly for people who have a lower opioid tolerance that do not want to push it higher, or for people who have been free of opioids for a week or two.

I would invite local people who are on my buprenorphine waiting list to consider Vivitrol as an option.


Buprenorphine for Treatment of Cocaine Dependence

This is not all that new, but it was just pointed out to me recently and I figure many of you will find it interesting.  As most readers know, the receptors that mediate the actions of cocaine are completely different than the receptors that are activated during use of opioids.  I will be posting related information in the next few days.

From DataMonitor:

Alkermes, Inc., an integrated biotechnology company, has announced positive topline results from a Phase I clinical study of an investigational combination of ALKS 33 and buprenorphine, an existing medication for the treatment of opioid addiction, for the treatment of cocaine addiction.

Data from the study showed that the combination therapy was generally well tolerated and sublingual administration of ALKS 33 effectively blocked the agonist effects of buprenorphine. Based on these positive results, Alkermes expects to initiate a phase IIa study of the combination therapy in the first half of calendar year 2011, the company said.

The phase I study was a randomized, double-blind, multi-dose,placebo-controlled clinical trial that assessed the safety, tolerability and pharmacodynamic effects of the combination of ALKS 33 and buprenorphine when administered alone and in combination to 12 opioid-experienced users.

Buprenorphine is used for the treatment of opioid addiction, despite its own potential for abuse. Combining ALKS 33, an opioid modulator, with buprenorphine, a partial opioid agonist, may block the agonist effects of buprenorphine thereby reducing the potential for the development of opioid dependence while still maintaining effective therapeutic action. Furthermore,
the pharmacologic properties and low dose of ALKS 33 required to effectively block mu opioid receptors may allow for a co-formulation with buprenorphine as a single sublingual tablet, the company added.

Elliot Ehrich, chief medical officer of Alkermes, said: “We look forward to continuing the recent momentum in our R&D efforts by initiating a phase IIa clinical trial to generate further data, as we advance the ALKS 33 and buprenorphine combination therapy as part of Alkermes’s growing pipeline of proprietary product candidates.”

The REAL Future of Partial Agonist Treatment— Pharma are you Listening?

I just wrote a note to a friend who works in the molecular sciences– she has been studying opioid receptors since the early 1980′s, when things were just getting started on a molecular level.  I’m keeping her name to myself, but I’ll share a few thoughts about what is needed to advance the treatement of opioid dependence– and make a few million dollars along the way (are you listening, RB?)

Hi ——,

(private chit chat that would bore everyone)

Anyway, today I realized what is needed in order to take partial agonist treatment of opioid dependence to the next level.

The problem with buprenorphine is that the ‘ceiling effect’ occurs at a relatively high tolerance level, approximately equal to 40 mg of methadone.  That causes at least two problems.  First, going off Suboxone is a lot of work, as the person still has a great deal of withdrawal to go through.  That may be a good thing early in the process, as it may help keep people on Suboxone, but after a year or so, when people want to try going off the medication, it is a major barrier that opens the floodgates to those old memories of using, etched in the emotions associated with withdrawal.

The second problem with the high ceiling/tolerance level is that surgery is a hassle.  People needing surgery need HIGH amounts of oxycodone to get any analgesia—I usually give 15-30 mg every 4 hours.  Pharmacists shudder to release those doses, and some surgeons and anesthesiologists balk.

The horizontal part of the dose/response curve is the essential part of buprenorphine;  that is what tricks the brain into ‘thinking’ that nothing is wearing off, and in that way eliminating cravings.  But that flat dose/response relationship could occur at lower tolerance levels and still work the same way.

Since I’m wishing for the moon, a series of molecules with progressively lower ceiling levels would be ideal, with the last molecule in the series being Naltrexone.  Although actually, naltrexone doesn’t work—it has NO mu agonism, so there is no tricking of the brain, and no reduction of cravings.  We would want something close to naltrexone, but with a tiny bit of opioid activity that does not vary with dose.

A shorter half-life would also be helpful.  Preparing for surgery requires weeks to get the buprenorphine out of the system.  Of course a shorter half-life means it is easier to get around buprenorphine by people who want to play with agonists, so again, these new molecules would be intended as ‘step down’ meds from early-stage buprenorphine treatment.

Do we know enough about molecular actions at the mu receptor to design molecules with these properties?  Or are we still at the point of making somewhat random changes and assaying the result?  Do you know of any labs doing this type of work?

I figured you’re the person to ask!

Thanks ——–


Optimizing Absorption of Buprenorphine

I wrote this a couple years ago, and still get questions about the topic today.  Studies show that a small fraction of the amount of buprenorphine in a tablet or film strip actually gets absorbed through mucous membranes;  the rest is swallowed.  The 15%-30% amount of absorption is referred to as the ‘bio-availability’  of the drug.

People who feel like they are not getting enough buprenorphine to remove cravings can review the principles below, to see if there are ways they can easily improve the absorption of buprenorphine.  NOTE:  improving absorption is NOT an ‘addictive’ behavior, for a couple reasons…. first, because of the ceiling effect, increasing the amount absorbed will NOT cause a ‘buzz’ or high, but will only make the medication last the full 24 hours without wearing off.  Second, crushing a tablet will NOT cause a ‘rush’ or ‘high’ for two reasons– first, because of the ceiling effect as I just described, and second, because the rate-limiting step for absorption is the passage through tissue— NOT the dissolution of the tablet.  This is why, by the way, the film does not cause a ‘rush’, even though it dissolves more quickly.

Read on:

I often answer questions about Suboxone that require the qualification ‘if it is being absorbed properly’. If a person asks how long it takes for Suboxone to wear off, or at what dose does the ceiling effect occur, I need to be sure that the person is taking it in a way that maximizes absorption; otherwise all bets are off. If a person simply swallows the tablet, for example, the level of buprenorphine in the bloodstream will be much lower than if it is taken correctly.

The usual instructions for taking Suboxone are to place a tablet under the tongue and let it dissolve.  It is important that Suboxone be taken once per day, in the morning; this instruction is included in the course for physicians but is too often ignored.  I will talk another time about the philosophy for dosing once per day; the basic reason is to extinguish the behavior that has been conditioned as part of the addiction.  But the point of this post is the absorption of buprenorphine from the tablet into the bloodstream, and how to maximize that absorption.  It is important to maximize absorption, particularly if one is trying to save money by reducing the daily dose of Suboxone.

From my experiences as an anesthesiologist, as an addict**, and as a PhD chemist, I recognize that three factors will maximize absorption.  The first is the concentration of buprenorphine in the saliva, as the drug diffuses into tissue down a concentration gradient.  This gradient is maximized by having a small volume of saliva.  I recommend that a person start with a dry mouth, place the tablet in the mouth, and crush the tablet between the teeth until it is dissolved in a small volume of a concentrated solution.

The second factor that affects absorption is the amount of surface area.  Buprenorphine is absorbed through all mucous membranes (the tissue lining the inside of the mouth), passing through the surfaces and entering capillaries, the route into the bloodstream.  So the concentrated solution should be ‘painted’ repeatedly over all of the surfaces inside the oral cavity;  the inside surface of the cheeks, the tongue, the roof of the mouth, under the tongue, the back of the throat…  swished around in the mouth over and over, repeatedly bringing the concentrate into contact with new areas of mucous membranes.

The third factor is time– the longer period of time, the longer for the buprenorphine to make contact with the mucous membranes, attach to the surface, get absorbed into the tissue, and enter the capillaries.  The initial process will be the saturation of the surfaces of the mucous membranes, and the slower process will be the passage into the tissue;  that is why the amount of surface area has such an important effect on absorption.  Fifteen minutes is probablysufficient for most of the absorption to occur;  there may be drug remaining that is attached to the surface but not yet fully absorbed, and so I recommend avoiding eating or drinking within another fifteen minutes or so after swallowing the left-over saliva.

If you pay attention to these principles you will maximize absorption of the drug.  The ceiling effect will occur under these conditions at a dose of about 2-4 mg;  the long half-life of the drug will guarantee that if you take over 4 mg or so each morning, you won’t have any significant withdrawal for over 24 hours– allowing once-per-day dosing.  Yes, early in treatment patients will feel as if they need to dose more frequently– but that is not because of too little buprenorphine, but rather because of conditioned behavior.  A person early in Suboxone treatment will have feelings or minor withdrawal in the late afternoon or evening after dosing in the morning;  those minor withdrawal sensations will go away in about 15 minutes if the person takes more Suboxone, and will also go away in 15 minutes if the person doesn’t take Suboxone.  If the person takes more Suboxone, it will reinforce the sensations and the person will get stuck on dosing twice per day.  If, on the other hand, the person uses distraction and avoids dosing, those minor withdrawal sensations will completely disappear in a week or two, as the conditioned behavior is extinguished.

**I mentioned my experience ‘as an addict’;  for a period of time my preferred route of administration of lipid-soluble opioids was ‘trans-mucosal’ or ‘trans-buccal’.  Since the amount of substance available was finite (albeit a fairly large finite amount!) I did all that I could to optimize absorption, including reading about diffusion of lipid-soluble molecules through mucous membranes.

Upcoming Changes in Pain Medication Regulations

This is a repost from my blog on PsychCentral:

There are changes afoot in the use of opioid agonists for chronic pain treatment. This blog has described the epidemic of opioid dependence that has killed tens of thousands of people across the country over the past few years, and the changes are directed toward reducing the harm caused by this epidemic.

A number of interventions have been proposed. Vicodin, the number one-selling medication in the country, contains the opioid hydrocodone combined with acetaminophen, the agent in Tylenol. Hydrocodone and Vicodin are currently ‘Schedule III’ medications, and will likely move to Schedule II, where oxycodone, Oxycontin, and Percocet are currently assigned. The change will have significant impact on the use of Vicodin and hydrocodone, since medications classified as Schedule II must be ordered on written prescriptions—i.e. they cannot be called in to the pharmacy. There are a number of other limitations on Schedule II medications; the prescriptions cannot have refills for example, and a maximum of 90 days of medication can be ordered at any one time. The laws that govern diversion of Schedule II medications are more strict as well, meaning that trading or selling Vicodin or hydrocodone to a friend or relative will carry significant risk of prosecution—and incarceration.

There are proposals for additional certification and training for doctors who prescribe pain medications, beyond the current DEA licenses that typically allow registrants to prescribe all of the controlled substances, without distinguishing between classes or uses of medications. These proposals anger the ‘pain treatment lobby,’ whose members claim that additional certification requirements will lessen the availability of pain medications. And they are correct—that is, after all, the whole point of the proposed changes.

There are a couple issues that merit discussion that have no clear right or wrong answer—at least in my opinion. First, in the debate over additional certification, there is little argument that such changes would reduce the number of doctors who prescribe opioids. Many doctors will decide that it is not worth the hassle and cost to obtain the special certification. Some others will see the requirement as a golden opportunity to leave the pain med prescribing to others, as they will be able to tell their patients ‘I’m sorry—I’m not allowed to prescribe them’—an easy way to avoid confrontation with patients asking for pain pills who doctors consider to have borderline indications for them.

We don’t know, though, whether other doctors will see the changes as business opportunities—growth in a new specialty of ‘pain pill prescribing’ for example—and fill the void left by less-frequent prescribers. And if there is a reduction in pain medication prescribing, will the reduction affect the people who don’t really NEED pain medications—i.e. the patients with mild lumbar strain, who would do much better using a heating pad and ibuprofen, and perhaps learn to lift without bending at the waist? Or will people with severe pain that truly warrants opioid medication find it impossible to have their pain adequately treated?

People should be aware that there are very significant differences in opinion over the proper use of opioid pain medications between physicians. For years, doctors were taught that people with ‘real pain’ rarely become addicted to pain medications. I was stunned when I read a study a couple years ago that claimed that less than 10% of patient who are prescribed pain medications develop opioid dependence. My clinical experience, after working for ten years in pain treatment and for about 20 years as a physician, suggest a number at least five times higher.

More and more doctors are realizing that for most people, opioid pain medications do little to increase function. People become tolerant to whatever dose of pain medication they are taking, and with that tolerance, the pain relief goes away—unless the dose is increased, which only repeats the cycle at a higher tolerance level. Patients become slaves to their medications, developing severe withdrawal from missing even one dose. Their high tolerance makes it difficult to treat pain from surgery, or from other painful conditions that the patient may develop. Finally, there is more and more evidence for the phenomenon of ‘opioid-induced hyperalgesia’ where pain symptoms are ultimately increased by opioid pain medications.

But patients still want pain medications when they are in pain, no matter how many lectures they hear about ‘decreased function,’ hyperalgesia, or tolerance. Doctors are placed in the position of giving patients what they ask for, even if it is ultimately bad for them— or protecting patients and standing up to their anger. Standing up to patient anger is not what many doctors signed up for when they went to medical school, and goes against their desire to help people—and to be liked for helping people.

And I don’t know if any course or certificate will help doctors deal with THAT.