Inconvenient Truth

Next month I will be presenting a paper at the annual meeting of ASAM, the American Society of Addiction Medicine. The paper discusses a new method for treating chronic pain, using a combination of buprenorphine and opioid agonists. In my experience, the combination works very well, providing excellent analgesia and at the same time reducing—even eliminating– the euphoria from opioids.
Ten years ago, I would have really been onto something. Back then there were calls from all corners to improve the pain control for patients. The popular belief regarding pain control was that some unfortunate patients were being denied adequate doses of opioid medications. I remember our hospital administrators, in advance of the next JCAHO visit, worried about pain relief in patients who for one or another reason couldn’t describe or report their pain. Posters were put up in each patient room, showing simple drawings of facial expressions ranging from smiles to frowns, so that patients in pain could simply point at the face that exhibited their own level of misery.
What a difference a decade makes! Purdue Pharma, the manufacturer of Oxycontin, was fined over $600 million for claims that their medication was less addictive than other, immediate-release pain-killers. Thousands of young Americans have died from overdoses of pain medications, many that came from their parents’ medicine cabinets. Physician members of PROP, Physicians for Responsible Opioid Prescribing, have called out physicians at the University of Wisconsin School of Medicine and Public Health for having ties to Purdue while arguing against added regulations for potent narcotics.
I have tried to present both sides of the pain pill debate, without disclosing my OWN opinions on the issue—at least until today. And I must be at least somewhat ‘fair and balanced,’ because I’ve received angry messages from both sides—from people telling me I’m evil for not understanding their need for pain medications, and from people telling me I’m evil for not respecting the danger of the medications.
By the way… I have a policy of not printing messages that simply call me names, or that tell me how bad a doctor I must be for writing what I do. I love a good argument, so please feel free to comment on ANY points that I’m trying to make. But I don’t think that making efforts to lead a discussion warrants personal attacks—so please, stick to the issues!
Today, though, I would like to share a couple thoughts on the issue. The thoughts came after a discussion with one of my patients with chronic pain. I have been presenting one side, then the other side, and back again, trying to remain neutral… but from all that I’ve seen as a psychiatrist and as an anesthesiologist, some things cannot be denied.
1. Some people do have chronic pain that responds to opioids. Many doctors—including the doctors who are afraid of the DEA, or the doctors who don’t want to deal with the hard work of prescribing opioids, or the doctors who want a simple world where ‘pain pills are always bad’—don’t want to admit the truth of this statement. This is, with apologies to Al Gore, a very inconvenient truth.
I find it interesting that doctors who don’t want to prescribe pain pills act as if chronic pain does not exist– as if the suffering of people with painful disorders is less important in some way, if it lasts too long. Every prescriber is aware of the need to treat acute pain, but when it comes to chronic pain, the difficulties that arise with treatment (e.g. abuse, diversion, tolerance) lead some doctors to act as if something magical happens on the road from acute to chronic. The phenomenon is the exact opposite of the old saying, ‘to a man with a hammer, everything looks like a nail.’ In this case, ‘to doctors who don’t want to use hammers, there ARE NO NAILS.’ But in truth, there ARE nails; some patients have lots of them. And we doctors have a duty to hammer away at them… (OK, enough with the analogy already!).
2. Just because some people divert opioids does not mean that other people shouldn’t have necessary pain relief. Treating pain is about as fundamental as medicine can be. I do not understand the doctors who say ‘I do not treat pain—you’ll have to see someone else’—especially when there are no doctors available to fill that role. More and more ‘health systems’ are adopting this position, at least in my area. What gives?!
3. At the same time, there is no such thing as ‘complete pain control.’ Tolerance removes the power of narcotics, and chasing tolerance always ends badly. Patients with chronic pain must use ALL tools available, including non-narcotic techniques.
4. Being prescribed pain medications comes with certain responsibilities; the responsibility to use the medications appropriately, to communicate openly and truthfully with the prescriber, to avoid ‘doctor-shopping,’ etc. At some point, patients who refuse to honor these responsibilities will lose access to pain medications—at least to some extent. Is this humane or fair? I think so, as access to pain relief for these patients is balanced against the lives of those killed by illicit use of these medications.
I’m sure I could go on… but for now, this is enough food for thought. Besides, it’s almost time for dinner! Feel free to comment—but please, be nice!
 

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 ——–
Jeff

The Truth About Suboxone

More than ever, patients have easy access to information once read only by scientists and medical professionals.  And at the same time, doctors have reduced the time spent with patients during appointments.  The result has been an increase in internet-educated patients, who come to appointments armed with data from package inserts, information from internet health forums, and stacks of questions from net-savvy relatives.
There is a good side to this process, of course.  Patients are wise to take greater interest in their personal health, and to be knowledgeable of medications that they are taking.  And whether good or bad, the situation is necessary, given the abdication by many physicians of their roles as educators.
But there are downsides to the situation as well.  Package inserts provide studies and odds ratios for the risks from medications, but interpreting the studies and odds ratios requires education and experience. Some data is reported in a way that a person without considerable education in statistics would have a hard time deciphering what is or isn’t relevant.  Some patients struggle under the burden of calculating and weighing risks, and prefer to have a careful, caring doctor provide his/her opinion whether a medications is safe or not.  Speaking from my role as physician, I am frustrated when patients choose to follow advice from an online forum over a recommendation based on medical knowledge or a careful literature search..
Doctors sometimes add to the problem.  I am frustrated when doctors make claims that are not supported by best medical practice or by medical science.  Distinctions between sources of information are blurred, so that some ‘facts’ are based on nothing but rumor.  The process is like the old ‘telephone line’ game; a doctor reads a question about a medication or illness, and responds with his/her opinion.  Another doctor then hears or reads that answer, adopts it as fact, and shares it with other doctors—who then reinforce the ‘factual’ nature of the information.
People tend to take information from physician educators/writers verbatim, as if the act of putting information online, in writing, guarantees that it to be true.  People are confused when they read conflicting ‘facts’ or recommendations from people with comparable credentials.
I try, when writing here, to differentiate between facts, best medical practice, and personal opinion.  If someone asks ‘how long should I stay on Suboxone?’, I’ll reply that several studies show high relapse rates in people who stay on Suboxone for less than 6 months (fact), that more and more physicians are keeping patients on the medication long-term (medical practice), and that in my opinion, many people are best off staying on the medication for an extended period of time.  You get the idea.
I think it is because of my PhD training that I tend to take a closer look at things that everyone ‘knows’ and ask, ‘says who?’  History has given us many examples of things that everyone knew that turned out to be wrong—from the connection between autoimmune disease and breast implants that wasn’t, to global cooling, the impending disaster when I was a kid (read here)—and we all know how THAT turned out!
The treatment of opioid dependence with buprenorphine/Suboxone appears to be particularly vulnerable to misinformation.  Some examples:
The naloxone in Suboxone prevents the person from getting ‘high’: Naloxone is not active orally or sublingually, and is added to Suboxone to prevent intravenous injection of the medication.  Confusion comes in part from mistaking naloxone, an IV medication, with naltrexone, an orally-active medication that is NOT part of Suboxone.
People will abuse Subutex because it doesn’t have the opioid blocker in it: Subutex or the generic equivalent—buprenorphine—works just like Suboxone when taken correctly.  Doctors and pharmacists are mistaken when they believe that buprenorphine is more addictive if naloxone is not included.  In reality, the subjective effects of Suboxone and Subutex are identical.  There IS a relatively low incidence of intravenous abuse of buprenorphine;  Suboxone in theory causes withdrawal if injected because of the presence of naloxone.  Realize, though, that the effects of buprenorphine or Suboxone are similar, whether injected or taken correctly.  Injected buprenorphine has the same ‘ceiling effect’ as does sublingual buprenorphine, and so people on buprenorphine maintenance would NOT experience an opioid ‘high’ after injecting their medication—any more than they do when taking it sublingually.
The tablet should not be crushed or chewed: The package insert recommends that Suboxone tablets should be taken sublingually, without crushing the tablet.   I am guessing that the recommendation comes out of an attempt to standardize the bio-availability of buprenorphine.  Studies show that as little as 15% of a dose of buprenorphine is absorbed, and in my opinion, the high cost of the medication warrants efforts to reduce the amount that gets wasted.  The bio-availability is affected by the concentration of buprenorphine in saliva, the surface area available for absorption, and the time that the medication is in contact with absorptive surfaces.  Passage of buprenorphine through mucous membranes is the rate-limiting step for absorption–NOT dissolution of the tablet.  In other words, crushing or chewing the tablet does NOT cause a ‘high’, and is NOT a sign of drug-seeking behavior.  Neither does crushing or chewing hasten the onset time of a dose of Suboxone.
Discussions about chewing or crushing buprenorphine provide examples of the doublespeak that only confuses people.  My own recent discussion with another Suboxone prescriber went like this: “I don’t want patients to crush or chew the tablet because that will make it get absorbed too quickly.  In fact,  I usually recommend the film, because it dissolves much more quickly than the tablet.”  Say what?  Do we want it to dissolve more quickly or not?  The truth is that it really does not matter.  The dissolving of buprenorphine— or the film– is the LONG part of the process.
The veins under the tongue absorb the drug in Suboxone. Actually, buprenorphine passes through all of the surfaces in the mouth, eventually entering capillaries under the surface.  The veins under the tongue absorb little or no buprenorphine.
You must stop smoking cigarettes if you are on Suboxone: I have searched the literature and I have talked to folks at Reckitt Benckiser, and I can find no evidence to back up this claim.  Scientifically, I cannot think of a reason that cigarette smoking would affect the absorption of buprenorphine, except perhaps to increase production of saliva, diluting the buprenorphine in solution and reducing diffusion into tissues.  I doubt this would have any significant effect on the bio-availability of buprenorphine, and my clinical experiences backs that up.  Patients in my practice who smoke have had normal responses to buprenorphine or Suboxone.
You can’t take pain pills if you are on Suboxone: Actually you can, but they will only reduce pain if the dose is sufficient.   I often use this approach to treat people on buprenorphine who undergo surgery.  But problems ARE caused if a person does things in the opposite order.  In that case—if someone taking opioid agonists then takes buprenorphine– there is risk that the person will develope precipitated withdrawal, depending on the amount of opioid agonist that was being used.
The longer you are on Suboxone, the harder it is to stop: I have read no studies supporting this oft-read comment, and I can think of NO reason that it would be true.  The tolerance to buprenorphine is set by the ceiling effect of the drug, and once tolerance develops, typically by several weeks on the medication, longer periods of time do not push tolerance higher.
The film formulation is safer than the tablet. Says who? If we are worrying about kids getting their hands on Suboxone, yes—the little orange tablets look like candy to a toddler.  But little red strips of flavored material appear appetizing as well. ALL medications should be kept away from children.  If the safety concerns are directed toward patients—for example one doctor told me he prescribes the film because it cannot be crushed—remember that crushing Suboxone is not a problem.  I SUSPECT (only my opinion) that the change in formulation was a marketing ploy aimed toward preventing acceptance of generic buprenorphine tablets.  Reckitt Benckiser apparently convinced the state of Wisconsin to cover the film exclusively, rather than allow addicts the choice of taking generic buprenorphine—a medication that works exactly the same as Suboxone, at about half the cost.
I think you get the idea.  Whether thinking about Suboxone or another medication, I urge readers to always ask the question, ‘says who?’  There are MANY experts out there on the internet—and some exhibit more restraint in their comments than others.  Ask yourself, what is the mechanism for what is being described?  And if it doesn’t seem to make sense, consider that just perhaps, you’re the right one.
 
 

The Problem with Benzodiazepines

Last night I came across a medical student web site that included a link to a post of mine from a couple years ago, that described my feelings about Xanax, Valium, Klonopin, and other benzodiazepines.   The people commenting at that site appreciated my comments, and my comments were ‘seconded’ by other physicians.  Here’s the post again, for those who missed it the first time:
Twelve Things I Hate About Benzodiazepines
Author: J Junig MD PhD


Because of several highly publicized deaths from combining Suboxone with benzodiazepines or “benzos”—a class of sedative medications that includes Xanax and Valium—I am frequently asked about the safety of combining Suboxone with those medications. The risk of life-threatening respiratory depression can be mitigated fairly easily, but that does not mean that benzos are safe or appropriate medications for people with or without addictions. They are commonly prescribed medications, and there are a number of misconceptions among laypeople about their proper use, so they deserve a thorough discussion. Most doctors with a bit of experience have learned to cringe every time a patient says the word “anxiety,” knowing that in all likelihood they are about to be placed in a difficult position. They will either do the right thing and disappoint their patient, or do the wrong thing and struggle with the consequences of their actions for months or years.
The problem is that the non-medical community sees SSRI’s as “antidepressants,” and believes that the proper treatments for anxiety disorders are sedatives like Valium or Xanax. Whereas the sedatives are appropriate for acute or short-term anxiety, chronic anxiety disorders are more appropriately treated using SSRI’s or SNRI’s.
Today, I saw a new patient who asked for treatment of her addiction to pain medications. When I asked about other psychiatric symptoms, she said that she takes alprazolam and clonazepam for anxiety and panic attacks. I explained that those medications are very dangerous for addicts and are intended for short-term use, and the primary treatments for anxiety disorders are SSRIs or SNRIs. I asked her dose and wasn’t surprised to hear that her tolerance was quite high. A milligram of alprazolam doesn’t do anything, she said—intending to mean that the meds are not potent enough to worry about. I of course took it the opposite way—she has taken benzos to the point that a very large dose has no effect due to her high tolerance. She then said she also has ADD and takes Adderall (ie, amphetamine). I explained that it makes no sense to take both amphetamines and benzos, particularly a long-acting benzo like clonazepam, which has a half-life of around 30 hours. Benzos CAUSE deficient attention; that is how they work! Worry consists of too much attention to a problem or a fear, and benzos prevent the brain from attending, attaching and remembering. In fact, anesthesiologists and dentists use the short-acting benzodiazepine midazolam during uncomfortable procedures to block the patient’s memory. Most adults have had the experience of watching the medication injected into the IV tubing, and next waking up to people saying “you’re OK—it’s all done.” Don’t take a benzodiazepine if you are nervous about an exam the next day! Beyond the amnesia, it is simply a bad idea to take two polar-opposite medications as this patient is doing. Stimulants cause wakefulness, attention, tight muscles, and anxiety. Benzos cause drowsiness, amnesia, relaxation, and the inability to remember what you were supposed to worry about. Instead of taking both, take neither.
A related question came to me by e-mail yesterday:
Hello, I found your website and see that you do phone consultations. I have been having anxiety problems and attacks for over a year. It has gotten worse and worse. I’ve been to the doctors in my area but no one wants to treat me for it…they just want to keep giving me Paxil, Zoloft, Prozac, Cymbalta and all these things I’ve tried and nothing seems to be helping me. I have anxiety attacks all the time where my heart beats out of my chest and I can’t breathe and go almost into this blackout stage. I have a lot of things that trigger it; one is my anxiousness all the time. I can’t focus, and any little dilemma sets me off. Everything is a crisis to me. And on top of that, I have the responsibility to take care of a 3 year old all by myself. I’m so scattered and anxious and upset all the time it is affecting me being a good mother. I cannot take it anymore and I am at the end of my rope. I don’t know what to do; no one will treat me with anything to calm me down along with the Paxil because of all the other people in this county that have abused it.. I DO NOT know what else to do. I have no one to talk to or turn to. It’s affecting my job, my personal life and my life in general. If you can’t help me maybe you know someone who will.
The person doesn’t come right out and say it, but her comments about needing to be calmed down and about abuse of the meds by others suggest that she is asking for a benzodiazepine.
Benzodiazepines include long-acting medications like clonazepam (Klonopin) and diazepam (Valium), intermediate-acting medications like lorazepam (Ativan) and alprazolam (Xanax), and the short-acting sleeping pills from my training years like triazolam (Halcion) and temazepam (Restoril). As an anesthesiologist, I gave patients midazolam (Versed) more than any other medication. All of these medications are appropriate in certain settings. Most have a street value. Some have active metabolites that accumulate in the body over time. All are sedating, all cause tolerance, and all have the potential to cause significant withdrawal symptoms. The longer-acting medications will self-taper to some extent, but the intermediate-acting agents in particular have the potential to cause withdrawal syndromes that are severe, and even fatal. The first patient I mentioned has been taking an anticonvulsant since presenting to the ER with a grand mal seizure while stopping Xanax “cold turkey.”
All of these medications have appropriate uses, almost always for short-term conditions. When given long-term, they cause problems. In fact, from the top of my head, I can think of 12 reasons to avoid prescribing benzos for “anxiety.”
1. Many anxious patients aren’t truly anxious. When a patient complains of anxiety, he or she is often complaining of something else. If I ask a patient to describe the symptoms without using the word anxiety, I often find that the patient is bored, restless, angry, depressed, overwhelmed, or appropriately frightened. Take a look at the second patient—the one who is “scattered,” “at the end of her rope,” and “caring for a 3-year-old boy all by herself.” Do you really think she will be a better mom if she is taking alprazolam or clonazepam? She is feeling overwhelmed, angry, tired, afraid, hopeless, depressed—feelings that when added together become anxiety. Do we really want to give a person in this condition a medication that will make her sleepier, more forgetful, more scattered, and more disinhibited?
2. Even if we get it right, her relief will be short-lived due to tolerance. Patients often escalate their dose at some point—no matter how many times they promise that they won’t. Dose escalation is not the patient’s fault—it is simply what these meds do. Once a pattern of dose escalation begins, it is difficult to control; patients will call after two weeks, reporting that they are out of alprazolam, and the doctor feels pressured to issue a refill to prevent withdrawal.
3. Benzos turn manageable anxiety into an anxiety disorder. Patients get a calming effect from the medication, but as the medication wears off, the anxiety returns, including extra anxiety from a rebound effect—a miniature form of withdrawal. Patients do not usually attribute that anxiety to rebound, but instead believe they have a horrible anxiety condition that appears as soon as the medication wears off. When I worked in a maximum security prison for women in Wisconsin, many inmates were taking benzos upon arrival; several months after the benzos were discontinued, the most amazing thing happened: the anxiety disorders went away!
4. A problem specific to addicts is that they don’t take sedative medications to achieve the absence of anxiety, but rather until they feel relaxed. They are not seeking normalcy; they are seeking relaxation. There is a difference between the two states: one is feeling normal without feeling excessive worry or panic; the other is feeling relaxed, something other than feeling normal. This doesn’t make addicts bad people; it is simply a consequence of the conditioning process during addiction. Addicts are not aware that they are seeking a fuzziness that non-addicts often find to be uncomfortable.
5. Again specific to addicts, benzos (like other medications that have an immediate psychotropic effect) direct the person’s attention inward. An addict becomes obsessed with how they feel; a goal in treatment is to get the addict out of his or her own head to experience life on life’s terms. Benzodiazepines encourage the opposite effect, encouraging the addict to focus on internal feelings and sensations.
6. Addicts with one favored class of drugs, for example opiates, will often move to a different substance when the first drug of choice is removed, for example using Suboxone. This phenomenon is called “cross addiction.”
7. A final concern for addicts is that benzos help preserve the mistaken thought that the person cannot function without taking something.
8. Benzos impair driving and have the potential to impair a person working with dangerous machinery. After all, patients get anxious at work too. They also make a person appear intoxicated by causing slurred speech, forgetfulness, and sometimes loopy behavior, risking the person’s job and having other unforeseen consequences. Some people have completely different personalities when disinhibited by benzos.
9. Benzos have been linked to fetal anomalies and early miscarriage.
10. They destroy sleep in the long run through tolerance and through rebound effects. If the patient takes the benzo during the day, he or she will be trying to sleep just as the sedation is wearing off. The alternative is to take the medication at bedtime, defeating the goal of finding relief for daytime anxiety. If the person takes benzos both day and night, tolerance increases even more quickly.
11. I have already mentioned the need to taper off benzodiazepines and the risk of seizures and worse during withdrawal.
12. Benzodiazepines may calm a truly anxious patient, but they do not generally increase the patient’s function. A person who can’t get out of bed becomes less likely to get out of bed. Bills that are unpaid become even less likely to be paid. Relationships do not generally improve when one partner is nodding off as the other talks about feelings.
I do prescribe benzodiazepines, usually for the short-term or while recommending they be taken no more than every other day. Some patients do fine with them, but for others, benzos are a Pandora’s Box that should never be opened. As a psychiatrist, I often resent the treatment that led to the mess that I try my best to clean up—such as the case with the first patient I mentioned. I think most doctors who read this will understand what I am saying, and many will have similar thoughts about benzodiazepines. Perhaps others will find the use of benzodiazepine much more beneficial than harmful. Comments anyone?

Treatments for Opioid Withdrawal

I have written about this topic multiple times, but perhaps a summary is appropriate.  More and more evidence and clinical experience suggest that buprenorphine is best considered a long-term ‘remission agent’ for opioid dependence.  Such a conclusion would have been obvious years ago if not for the hesitancy to do what has been suggested by addictionologists for decades, and treat opioid dependence as a DISEASE.  While many people pay lip service to addiction being a chronic illness, the reluctance, particularly by AODA counselors, to fully accept a medication for the condition is clear evidence of the stigma that continues to force addiction into the realm of ‘character.’   AODA counselors would do well to do some serious soul-searching on this issue– at least in my opinion.
While remission therapy with buprenorphine will likely become the standard treatment for opioid dependence, there will be some cases where tapering off buprenorphine is appropriate.  The problem in such cases is that the taper process causes withdrawal, which stirs up all of the self-disgust, fear, and shame that predispose an addict toward relapse.  As I have discussed, a long-term injectable formulation (such as Probuphine, currently in the FDA approval process) would be useful for tapering off buprenorphine.  The final piece of the equation would be effective treatments for opioid withdrawal. 
A number of medications are rumored to help reduce the symptoms of opioid withdrawal.  I’ll mention a few of the medications that I have used to treat withdrawal, or that I have read about in scientific studies or case reports.
– Clonidine is the ‘standby’ agent for treating opioid withdrawal.  The medication reduces CNS excitation by effects at alpha-2 adrenergic receptors, causing less release of epinephrine and norepinephrine by central and peripheral nerve terminals.  Symptoms of withdrawal are reduced by about a third, and the primary side effect is sedation.
– Some medications target specific components of withdrawal;  Imodium (generic name loperamide) reduces bowel cramping and diarrhea; benzodiazepines reduce anxiety (but are themselves addictive); ibuprofen and acetaminophen reduce muscle aches and headache; stimulants or wellbutrin reduce fatigue (perhaps for severe symptoms, but use of stimulants would be considered controversial at best).
– Proglumide is an antagonist of two classes of receptors for a gastro-intestinal hormone called ‘cholecystokinin’, or CCK.  Proglumide used to be used in the US and elsewhere to treat gastric ulcers, before more effective medications like histamine blockers were developed (e.g. cimetadine).  There are a number of chemicals structurally related to proglumide that have similar actions, that include enhancing analgesia caused by opioids, treating Parkinsons disease, and enhancing the release of growth hormone.  Proglumide appears to ‘reset’ tolerance to opioids in people who are physically dependent, and also to reduce symptoms of withdrawal.  Proglumide appears to have dropped of the face of the planet;  if you search for the medication you will find it available in chemical supply houses in China, but not available through pharmaceutical companies.  I recently received contact from a person claiming that  proglumide is available through a company based in Pakistan, but I have not yet verified the information.  Stay tuned.
– I recently came across an article with some fairly convincing evidence that symptoms of withdrawal are reduced by the anti-anxiety medication buspirone.  A study found that self-reported withdrawal symptoms of opioid addicts were greatly reduced by treatment with buspirone, which is a pretty safe, inexpensive medication that is not itself addictive.
– Ondantreson is an anti-nausea medication used during chemotherapy and surgery.  I have seen several studies demonstrating a reduction in opioid withdrawal from the medication, which like buspirone is fairly safe and is not addictive.  Ondantreson is, however, more costly.
I have treated patients in withdrawal using gabapentin, specifically to reduce sweating and hot flashes.  I do not know if it works, or if the people who liked it were getting a placebo response.  I have not seen reports in the literature showing this benefit.
– I have mentioned the recent approval of transdermal buprenorphine, called ‘BuTrans.’  This formulation provides a lower range of doses of buprenorphine, in the tens to hundreds of micrograms (one tablet of Suboxone contains 8000 micrograms of buprenorphine).  This lower dosed formulation may find usage for tapering.
Do you have other suggestions for treating opioid withdrawal?  If so, please share them in the comments below or over at SuboxForum.  Of course, these medications must NOT be taken ‘on the street,’ but rather should be discussed with your physician if and when the time comes to taper off buprenorphine.
Thanks all,
JJ

Buprenorphine for low-dose opioid use

A reader wrote with a question that I don’t think I’ve addressed on the blog.

Do you have a threshold for how much narcotic a patient must be using before you will put them on buprenorphine? I am concerned about narcotic addicts that are using 6-10 Vicodin (hydrocodone) a day for example.  Many have very mild withdrawal symptoms, but are never-the-less unable to stop on their own.
This is an insightful question that provokes enough discussion to fill at least one blog post.  I don’t have a simple answer, other than to go on a case-by-case basis and try to determine who, if anyone, might be able to walk away from opioids completely (i.e. a person who I would be less likely to put on buprenorphine, as doing so would drive tolerance higher) vs. those who will need maintenance treatment eventually, even if their doses are not yet very high.

Patients have a right to know if they are having their tolerance increased in my opinion, given the misery involved in bringing tolerance down.  It is also important to tell people with lower tolerances that they are going to get a buzz from buprenorphine for a few days because of the potency of buprenorphine.  This opiate stimulation is likely to occur even with a very small piece of a Suboxone tablet; a quarter tab or 2 mg of buprenorphine has almost the same potency as 16 mg because of the ‘ceiling effect.’  The potent opioid effect may make the doctor liable for a car accident, or could even lead to overdose if the patient combines buprenorphine with other respiratory depressants.

In general,  the ‘break even’ point on the tolerance scale is 80-100 mg of hydrocodone or about 60 mg of oxycodone per day.  In other words, if the person is taking 8-10 of the larger-strength Vicodin per day, I would consider Suboxone to be of about equal potency.

In considering whether a person’s use and tolerance are high enough to call for buprenorphine, some people focus too much on the initial potency relationships, and forget that opioid dependence is almost always a long-term condition.  I’m not sure by your last sentence whether you realize or not that the presence or absence of bad withdrawal is a red herring for acheiving sobriety from opioids.  Many addicts mistakenly think that withdrawal is the primary force that keeps them actively addicted.  In late addiction they find that desperation helps them get through withdrawal over and over, but they continue to relapse– as soon as they feel well!

From a scientific perspective, I have not seen evidence of a correlation between the severity of addiction and the addict’s tolerance level (if anyone has seen such a study, please forward me the reference).  At the same time, I don’t think I would feel comfortable starting buprenorphine in a person taking a couple Tylenol 3’s per day.  Luckily (?), this type of situation has been rare in my experience.   I should do chart reviews and publish the exact numbers, but out of the 500 or so people presenting with opioid dependence over the past 5 years, I would guess that the average tolerance level is approx. 120-150 mg of daily methadone (range of 30-400 mg per day), or approx. 160 mg of oxycodone per day (range of 40-700 mg of oxycodone per day).  Yes, I had two people—interestingly, both women– come in at those upper daily doses of methadone and oxycodone.   The methadone patient had been labeled a ‘fast metabolizer’ of methadone as reason for the ridiculously high dosage.  The reason seemed good enough, until I found, when converting her to other agonists for pain, that her tolerance was ultra-high to ALL opioid agonists—telling me that she was not metabolizing the methadone fast enough to prevent her body’s response to the high dosage, and calling the entire ‘fast metabolizer’ issue into question.  The woman taking the large amount of oxycodone had inherited a tidy sum of money; hundreds of thousands of dollars, all gone after one year of using.

Ouch.

Feeling 'drugged' on Suboxone (buprenorphine) and the liquefied taper method

A question and answer session with someone who is considering stopping buprenorphine.  His message first, with identifying information removed:
Hi, I just sent a donation through PayPal.
I used Norco 10/325 since 1999, about 20-40 per day for the past five years.  A month ago I went on 2 mg Subutex but don’t like the feeling of being drugged.  The next day I went down to 1 mg/day, and have been at that dose since.   I liked the Norco because I could still function, and could “feel”, including joy.  Now I have no feelings of joy at all, just feel drugged all the time.  I meditate and exercise 30 min/day, have done that for years, so maybe that kept me grounded.
Q:  What is the quickest and most comfortable way for me to taper?  Should I use Ativan to help with restless legs and sleeping?  I don’t mind a little discomfort, but if it’s too much I am afraid I will relapse to the Norco.
Thank you
My response:
Thank you very much for the donation.
(note to readers:  most days I receive from 3-6 e-mailed questions– sometimes very lengthy questions.  I answer when I can, and of course the laws of capitalism apply– i.e. a donation tends to make me feel guilty if I don’t respond!  I provide formal telephone consultations for those who need or want such a discussion, at a rate of $100 per 30 minutes.  The sessions can be set up by contacting me at the phone number provided at my home page, at fdlpsychiatry.com)
Most people who take high dose buprenorphine (HDB) have no feeling of being ‘drugged’.  It sounds like your mind is made up about stopping buprenorphine, but as an FYI, the reason that you are likely feeling drugged is because your dose of buprenorphine is too LOW.  I’ll try to explain…
If you look at the dose/response curve for buprenorphine, at low doses the ‘curve’ is essentially identical to the plot of an opiate agonist.  It is only at very high doses that the ‘curve’ flattens out in the shape of the well-known ‘ceiling effect.’  With HDB the goal is to keep the brain levels of buprenorphine high enough so that even at the end of the dosing interval, the opiate stimulation remains above the ceiling level.  If brain levels of buprenorphine stay that high, the opiate effect remains constant over time, allowing brain opiate receptors (and the brain in general) to become completely tolerant to the effects of buprenorphine.  Once completely tolerant, the person on HDB feels no opiate activity at all from taking buprenorphine;  the only thing that is potentially felt is withdrawal from a lack of opiate stimulation if the brain level of buprenorphine drops below the critical level where the ceiling effect occurs.
If a person takes an amount of buprenorphine that does NOT push brain levels above the ceiling level, the person will feel the same response to buprenorphine as he would feel from an opiate agonist.  The degree of opiate stimulation would change as the buprenorphine level goes up and down, never reaching the ceiling level where constancy is achieved.  Because the receptors are not fully stimulated, they would not become fully tolerant to buprenorphine.  The person would not, then,  feel ‘normal’ because he will never gets to the point of full tolerance.    Making things even worse, the effective half-life of buprenorphine becomes much shorter at the low doses you describe, requiring multiple dosing to avoid episodes of minor withdrawal between doses.
But back to your question, and taking the last one first, the biggest risk for relapse from what I have seen isn’t so much during the taper as it is a couple months later, when the person finally starts to feel better.  Being sick during withdrawal helps the addict remember just how horrible opiate dependence has been, serving as a motivator for sobriety.  But when the person feels better, those thoughts start coming back… that just a tiny bit would be OK.  Always remember your weakness for opiates, as your weakness for opiates will surely remember you for the rest of your life.
I have no problem with a short course of benzos during the taper of buprenorphine.  Some people argue, simplistically I think, that since benzos are addictive they must be completely avoided by addicts, no matter the reason.  In general I hate benzos, and think that they do more harm  than good in most cases.  But opiate withdrawal is so horrible that a small amount of lorazepam or clonazepam would not have to be the end of the world.  Besides, one could argue that making the withdrawal a bit milder might lessen the pull back into the world of active using.     Clonidine is of course the classic medication for easing opiate withdrawal, and I have also had some success with gabapentin in some individuals.  I would like to set up a trial someday with the old medication ‘proglumide,’ which has been rumored to reduce opiate withdrawal for a number of years.  But I do not know where the medication can be found—in or outside of the US.
The main thing about tapering is to go slow—on the order of 10% every 1-2 weeks at the fastest.  During a taper off buprenorphine you will want to think in micrograms, not milligrams—i.e. 2 mg equals 2000 micrograms.  Remember that buprenorphine is a potent narcotic in doses as low as 10 micrograms, and European trans-dermal buprenorphine delivery systems release as little as 5 micrograms per hour!  You will want to taper down to 500 micrograms per day or less  before ‘jumping’ from the medication.  I have written about the ‘liquid taper’ method both on the blog and on the forum, and you will find the experiences of many people with that method described at the forum.  The basic idea is to dissolve 8000 micrograms of buprenorphine in a milliliter or two of water, then dose with a graduated eyedropper or a tb syringe (without using the needle!).
Finally, remember that the half-life of buprenorphine markedly decreases as the dose is decreased, so as you taper down, you will need to divide the daily dose into multiple fractions.
Thanks again for your generous donation. I hope to see you around the forum!

Proglumide

Every chronic pain patient and opiate addict looks forward to the day someone finds the Holy Grail for opiates:  an agent that blocks or reduces tolerance and that eliminates withdrawal.  The two phenomena are linked and so the same agent may help with both problems,  or perhaps instead there will be a better understanding of the myriad interactions involved in opiate tolerance and not a single cure, but rather a number of medications beside the current, insufficient gold standard, clonidine.  A few weeks ago I decided to do some reading on opiate tolerance to see what we have learned lately,  and I started out with Google, searching the phrase “opiate dependence mechanism of tolerance”.  To my surprise, the first ‘hit’ was a NIDA monograph— try it for yourself, and see– then click on the link and scroll to the article in the contents a couple up from the bottom– see anyone there that you know?  That was the first research that I ever did, back in the mid-1980’s with nicotine.  You will see, though, the other articles about opiates;  that is what it was all about even back then, and we assumed that if we figured out tolerance to one drug we would understand tolerance to all drugs.  We now know that things are much more complicated.
The people at NIDA are going to wonder why one of their old monographs got 1000 hits tonight!
As I moved to more recent sources  I found that opiate tolerance is clearly much more complicated than we had hoped years ago.  A few years ago we almost got a drug called ‘morphidex’ that seemed to reduce tolerance in animals, but it didn’t work in humans–  for a minute or two it looked as if simply blocking the NMDA receptor with dextromethorphan would result in  significant tolerance reduction.   The fact that it doesn’t work has not stopped a number of compounding pharmacies from making and selling the combination at a tidy profit!  In reality there are probably multiple mechanisms for tolerance, perhaps different types of tolerance for different types of analgesia.  For example the tolerance that takes away oxycodone analgesia from shingles pain may be different than the tolerance that takes away oxycodone analgesa from broken bone pain.  Multiple transmitters and receptors and subtypes of receptors are involved– so much for brushing up quickly over the weekend.
I am generally skeptical of things– pretty much everything, to be honest.  I’m skeptical about cures for withdrawal because I have seen many of them come and go.  I’m skeptical of cures for baldness because I’ve seen many come and go!  I’m skeptical about global climate change because I remember worrying about the shortened growing seasons written about in the New York Times and Time Magazine in the 1970’s on account of ‘global cooling’.  I still have a clipping that describes the ‘growing concern among scientists that has reached a consensus’ that the earth was already being affected in the form of reduced crop production that surely was only a prelude to global famine…  the Time magazine article even mentioned some of the things that might be needed to ‘save’ the planet, including covering the polar ice caps with soot to absorb more of the sun’s heat! Yep– THAT was a good idea!  Here is a good prediction:  in a couple more years the movies about impending disaster will become cult classics.  Just as we now read the book ‘1984’ and think ‘that was silly’, we will watch movies predicting rises in sea level as we sit in chairs that were SUPPOSED to be under water years earlier.  Did I digress?
Back to opioids, with apologies to those of you who are convinced this is that beginning of the end of the planet.  But first, in case you are interested about my own beliefs, I once read a fabulous book called ‘the Song of the Dodo:  Island biogeography in an age of extinction.  What a fabulous book– it explains how things got to where they are today, and helps understand where things are going tomorrow– with occasional stories about the great explorers from hundreds of years ago, about what it was like for a white man to travel to South America to collect birds…  I can’t do it justice.  But after reading it you will understand very clearly that the Earth is fine.
Yes, we will go through a tough spell where the entire planet wildlife collection will consist of humans, squirrels, rats, grackles, bacteria, and a few plants…  but after humans die off, all of the forces that lead to speciation are still in place, and all of the diversity will return– bet on it!  So while we humans are clearly f#%@#ed, the planet will be fine.  The things that lead to extinction would surprise you until you read the book, then you will see how they are completely inevitable– and completely irrelevant.  This from a person who was a total ‘greenie’ in my younger days!   Read the book– you will stop worrying so much.


Where the heck was I?  I got this message the other day about the medication ‘Afloxan’ and the chemical ‘proglumide’.  Actually, the message is a good fit with the other topics in the book, now that I think about it!  Here is the message:
I’m writing to get your opinion about an anti-inflammatory drug called ‘proglumide’.  This drug was used primarily for GI issues but has the unique characteristics of reducing opiate tolerance.  It works as a cholecystokinin antagonist, the wikipedia link is here.  I’d like to let you know, that whatever the opinion is out there about this drug, I can say that it really works.  I had to take a trip to canada for work, and while I was there I did a ‘cycle’ of Afloxan, which is not proglumide, but metabolizes into proglumide.  I thought this would be better than nothing and in going to canada, I took with me exactly 21 pills of afloxan, 12 10mg hydrocodone, 3 20mg oxycodone, and some number of kratom ‘pills’ i had made for myself (junkies can be real creative when they want to avoid dopesickness).

So the result was a very abrupt and rapid taper off of 160mg of oxycodone per day, and I was very very comfortable the entire time.  I might have lost about 2 or 3 hours of sleep a night but that was about it.  I realize this isnt exactly a ‘clinical’ setting and my observations are about as scientific as a subluxation, but the effects were definitely not placebo.
Have you heard of this drug?  And if so have you ever considered using it to withdraw people from opiates?
I do not know anything about the medication, and was not able to find out a whole lot about it either.  A guy named Brent has a web page about the drug, and I found some references to the drug on this interesting site.  I got nothing at clinical trials.gov.  I would like to look into doing a study of the medication but I don’t even know where I would find it;  the references I followed to track it down were expired.  So… if anyone knows if anyone is manufacturing this medication or related medications (it has been sold under the trade name ‘Wilid’ in the past, and a medication referred to in the message is converted to the drug– but I cannot find any of them!) please post a comment or send an e-mail to drj@suboxonetalkzone.com.  I figure SOMEBODY out there has the time to track this down!  Try Australia– I found a couple references to pharmacists in Australia that sold the medication back around 2004.  Thanks in advance for the help!
JJ

Hard Knocks, Talwin, Tapering: Q and A from SuboxForum.com

A new feature on SuboxForum.com is the ‘Q and A,’ where I select a question to answer in detail.  I will post my answer here as well.  I won’t post the original question, but it is embedded in my response so I think everyone will figure it out!

There are really a number of questions in your post, so I will do my usual thing and answer them as we go through the message. As always, these are my opinions; consult your own doctor before changing anything about your dosing or medication.

The message/my responses:

Thanks. I feel obligated to pay, and will–but I’d rather pay when the time is right for me to go thru w/d off subs. My problems are more than just getting off this suboxone. I now know I need to be in better stable frame of mind to go through this—everything I read on the blogs says be prepared to go thru this weaning.

Donations are appreciated and helpful, but don’t feel obligated, please. If someone is comfortable helping to support my time here and the site in general, please consider a donation. If you are going through hard times, take care and don’t sweat it! Two comments though: First, as you know my ‘big thing’ is recommending people STAY on Suboxone. Yes, it is expensive—but not NEAR as expensive as using, even if things go well. Throw in unexpected consequences like an arrest and the costs really go up! But my second comment is to agree with you. If you want to taper off Suboxone, you need to start at a time when things are great—because the process takes a lot out of you.

Talwin made my chest tight and my legs felt weird. And I went into full W/D by the 3rd day off suboxone. It was last Sat so I called the after-hrs nurse and told her what happened. She contacted the Dr who had my RX avail within the hour. I was fine within minutes of taking 4mg. But I had a really hard time getting back on any dosing schedule all this last week. Is this psychosomatic or something? I mean relief was immediate.

It usually takes a few days for withdrawal from buprenorphine to become severe, due to the long half-life of the drug. Relief from resuming buprenorphine usually isn’t immediate, so some of the relief may have been psychologically based. The uptake starts at about 20 minutes and is pretty much complete at 90 minutes. I remember your other letter—you were recommended Talwin, of all things, to taper off Suboxone. That was poor advice. Talwin doesn’t even bind to mu receptors, which are the receptors that buprenorphine works through. Talwin contains naloxone and pentazocine, the latter is a kappa and sigma agonist, and we all know what naloxone does! The naloxone in Talwin would if anything make you more sick during your withdrawal; pentazocine is a nasty drug that has been abused in years gone by (combined with Ritalin, for example) and that can cause seizures, hallucinations, and other dysphoric states. I do not recommend using Talwin to taper off Suboxone.

I read so many horror stories online about others who quit at 2mg who suffered for months. When I first went on suboxone I was miserable and unable to function for at least 3full weeks–out of work a whole month. My Dr says that shouldn’t be. Well be or not it was. My back was killing me–all I could do was lay around on the couch and try to get up and move as much as possible–the terrible loss of clear vision/runny eyes and dilated pupils, goose bumps, achy all over–the only help the suboxone was fast on was the desire to take more Vicodin and the diarrhea stopped.

You don’t mention the dose of opioids that you were taking at the time that you started Suboxone. What you describe sounds like ‘precipitated withdrawal’—if your total daily dose of opiates was greater than 30 mg of methadone, or 50 mg of oxycodone, or 70-80 mg of hydrocodone, then I would expect you to feel sick when starting Suboxone—unless you went a few days without any opioids and got your tolerance down a bit.

If you say it shouldn’t take too long to wean off, then why are so many people having such a hard time and taking so long with so much misery to get off either the opioids or the suboxone? I got a taste of suboxone w/d last week and it was not pretty.

Opioid withdrawal stinks! No doubt about it. I am well aware of the complaints about Suboxone withdrawal, but I have witnessed withdrawal from buprenorphine and from agonists many times (and experienced it as well!) and I know the truth of the matter—that there is no comparison. Methadone withdrawal always lasts for months—always! Fentanyl, oxycodone, and heroin withdrawal are violent—legs kicking, diarrhea and nausea, extreme weakness… I often say that the reason you read about how bad Suboxone withdrawal is, is because those people 1. Can go off Suboxone, and 2. Can still function enough to write on the internet. Neither is the case with agonists– people cannot taper off, and if they are forced off they are not able to type messages about how they are feeling! I have argued this point with the people who post ‘Suboxone w/d is the worst ever’, and they insist they are correct. All I can say is that I have seen both many times. I do notice one thing to explain the discrepancy: people ALWAYS think that their current is their worst misery. Pain experienced is worse than pain remembered.

Is it really true that .5mg suboxone is as potent as 30mg hydrocodone or 10-20mg methadone?

The kinetics are not ‘linear’. So if taken in an optimal manner, 2 mg of buprenorphine is as potent as 4, 8, 12, 16, or 32 mg of buprenorphine. They all are at the ‘ceiling’ potency, and all are equal to about 30 mg of methadone, 50 mg of oxycodone, or 70 mg of hydrocodone. Your numbers are about right.

Have I been taking huge amts of narcotics (albeit diff than full receptor opioids) for 2years now? I read up on suboxone when I started, but then haven’t paid any attention since then—too much else going on. Now I’m freaked about going off of em if they really are equivalent to pretty high doses of opioids.

Again, you do not say what you were on before the buprenorphine. But yes, to some extent you are correct in your statement. I wouldn’t say ‘huge’ doses, but I would agree with ‘high’ doses. To put things into perspective, methadone clinics officially shoot to have addicts on at least 60 mg, but usually have them at 100 mg or more. Most oxy addicts I see take two 80’s per day or more— 160 mg of oxycodone at a minimum. The largest dose I have seen taken by an addict was 700 mg of oxycodone per day—she had inherited $300,000 and it was all gone after one year. So in comparison, 30 methadone-equivalents of a partial agonist is not ‘huge’, but it does represent significant opiate activity.

I now know I have to wean to less than 2mg a day to go off this stuff, and I am planning to set aside 3weeks from work to go through this. You say the worse thing to do is lay on the couch–keep moving. I’ll do whatever I can to make it better, but I cant go through last week again until I have time off from my frantic life! And my frantic life —no real sleep for 15months..isnt going to end until I get out from under my financial mess. So I will plan a good 3weeks minimum to get over this stuff.
And now I read about others that are weaning way way back to tiny slivers of subox to quit and still going through hell when they finally do.

Three weeks is not enough. But that is not the fault of Suboxone; three weeks isn’t enough to get off any opiate! I mean, REALLY! Look what you, and other people, are asking for! You haven’t mentioned what you took but some people will use for ten years… then go on a year or two of Suboxone, and if everything isn’t perfect in three weeks—THREE WEEKS!!!—they complain about Suboxone?! Talk about expecting miracles! Talk about expecting an easy way out!! My active using lasted several months—that was it!! I was in detox, sick as sh…, then in residential treatment… for 14 weeks!! I then was in aftercare for 6 years, going to AA several times per week, PLUS group therapy twice per week. And while I treated my addiction aggressively, there were and are many, many people who treat it as aggressively or more! In the place where I am medical director, we send many people to a year of living in a sober community—a halfway house, essentially—and that is AFTER six weeks in residential treatment and three months in a halfway house. And that amount of treatment, in my opinion, is a bit light!

I have to repeat this because people don’t seem to get it. I used for several months– Adding 1993 and the 2001 relapse together, my total opiate use was less than one year! And my treatment was 14 weeks in residential AFTER detox, then six more years of meetings and group therapy—THAT is how you get clean before the world of Suboxone!!

As for the ‘tiny slivers’… read about ‘micrograms’ on my blog so I don’t have to repeat it. Two mg is way to high to ‘jump’ from. The withdrawal from quitting two mg is about the same as the withdrawal from 16 mg, for reasons I mentioned above. One person on the forum is in the process of tapering down to the low micrograms and writing about it—he uses a technique I have written about (but that I didn’t invent—it was sent to me by a reader) where the buprenorphine is dissolved and taken with an eyedropper.

Do you not see that these people that are going through pure misery to get off of this stuff?

Yes—and I’m sorry, but I consider those people fools. Their lives were saved once—they might not be so lucky the next time. And for the vast majority, there WILL be a next time. That is just the fact of the matter. They all have the same fantasy—a fantasy I once shared—of being ‘normal’ again. It ain’t happenin’, folks. I’m sorry to break it to you. All the misery you are going through tapering off Suboxone… some day in a few years you will be saying to yourselves, ‘why the heck did I stop that med, when everything was going so well?!’

I found one plan that says to cut back 25pct for 4days and if no problems keep cutting back till it’s over. If I dont make it, take a sliver to stop the w/d then start that 4days over. I saw you have 2 tapes explaining your “tried and true” method to detox from subs…
I will order your tapes when I’m ready to go off the subs. ( I have 6weeks off starting Sept 1 this year)
.

My tapes aren’t magic, and the method isn’t ‘tried and true’. I don’t say that. I wouldn’t say that. It is very hard to taper off any opiate, INCLUDING SUBOXONE. My tapes describe what I have seen to work the best. I provide all of the same info as on the tapes in the blog itself—so if you have read through the blog, don’t worry about buying the tapes. I do try to give some extra motivational stuff, but the techniques, the meds, the ‘how to tell when you are ready’… I’m sure I have covered it in the blog itself by now. But if you want to save some time and provide me some support at the same time, by all means purchase a tape, with my thanks.

Right now I am facing extreme pressure having to sell my home and everything I own and quit my job of 31yrs and move back home to Iowa to live with my mom. I’m 54yrs old and have lost everything–even my credit. All cuz of a steady stream of bad luck (dont blame the drugs–I wasn’t on them till I was recovering from my last accident) It’s very humiliating and disheartening to work so hard and so long and then nothing worked out and I have to start over at my age.

I’m sorry for what you have been through. All the more reason, in my opinion, to keep the Suboxone going if you can get it paid for. Look into Medicaid. Ask the doc if his patent assistance plan is full (every doc gets a couple spots). You don’t need any more problems right now, so KEEP YOUR ADDICTION TREATED.
You got your pictures in the paper for being a hero (cool eh)…

Thanks for noticing—the high point in my life for sure. Posted on my site at wisconsinopiates.com.

I got mine in for bad luck (I just moved into a home I built myself and the next month it flooded–the local County bought it and tore it down-top story on local TV showing them bulldoze all my hard work down in about 8min. –then a frikkin tornado hit down and only damaged two homes–my two rental houses that are next to each other–the paper reported it as a freak tornado–we don’t have tornadoes in WA.) Then the injury accidents –fell off a rental house roof–then fell down a spiral staircase, then got rear-ended by a huge Ford Econoline that lost his breaks..Then fell fixing an awning on my new home up on a hill away from flooding rivers. But I got over it…I was doing great–my shoulder and neck surgeries were healing very well ….went on my first vacation in a long time and my brand new car hit a soft spot on a dirt road (the Idaho Sheriff called it a freak accident) and my car plummeted down a steep cliff and crashed into a tree that saved me from drowning in the river below—still got over that –but 9mo out of work forced me to refinance my home to a subprime because I was financially strapped being on a medical leave without pay—but I was determined to get back to work–I paid extra loan origination points to buy down this awful loan to 1year-no prepay penalties–and I worked very hard to have good credit so I’d refinance into a nice 30yr fixed in a year. But a year later I had no house to refinance.

A freak windstorm knocked a tree down and totaled my home on the hill.–I’ve have to live in hotels, rentals, my RV and now back in the home that insurance finally fixed–I couldn’t refinance after my 1yr because the contractors were jerks and went on vacation and left my house with nothing but a few walls left (it was a total rebuild)…no bank will refinance if an appraiser can’t find a house to appraise. By the time I finally had a house again, and was signing the last page on my refinance loan 4months later— it was too late–the bottom had fallen out on the real estate market—even my good credit didn’t matter—no refinance—no one was loaning. That was 15months ago. I haven’t had a good night’s sleep since then. I work full time and still have to drum up double what I make every month to pay that subprime mortgage loan each month. It is killing me. And of course just when I really need my roommate (male companion) to come through for me and pay more than his pathetic tiny amount each month…he has no work and no money at all) The only way out is to sell. And the contractors screwed up and left a zillion things that weren’t done so I have had to do that too. Plus sell everything of value I owned. I’ve been to every counseling service looking for help and there is no one out there who can help me save the home…..all the same advice–dump the deadbeat guy and sell the house. So I am.
I tell you this cuz I’m angry everyone thinks all those people who took out subprime loans were greedy and bought more than they can pay for and now we’ve ruined it for everyone else. I’m angry there is no help out there for someone like me who has worked my whole life and now my credit is ruined (can’t pay hardly anything except that huge mortgage–I pay more than a house that’s for rent right now near Bill Gates mansion on Lake Washington–it rents for 2950.00mo….my mortgage is 3400.00 mo! for a tiny 2b 1ba 1150sq ft house) So tell everyone there are some that took those crappy loans for a short term catastrophic event and worked VERY hard to have great credit to get out of the loan–but couldn’t because of bad misfortune, not greed.

You just told them yourself. Gosh, I’m sorry. You have had a horrible series of events. But you are here, and you are a survivor, and for that I give you a great deal of credit. It sounds like time to just live each day, and to do your best to avoid looking too far forward. And remember—once things are gone, there is nothing they can take from you anymore. I know it hurts, but try to avoid feeling like a bad or evil or worthless person. You have done great things to last through all of this—that is your heroic record.

Then what…My sister got cancer, my dad died, a coyote got my cat that was the love of my recent life.
I GIVE UP. I’M GOING HOME to my mom in Iowa. She’s all alone now, and I need to quit whining about myself and help her so I feel useful in this life I have. My last day at my airline job is 31Aug09. I need to be off this suboxone no later than November. I hope to use the first part of Sept to get over it. I hope your tapes show a way that is painless—if my house does sell I have no idea where I’ll be in the interim before moving to Iowa.

Why do you have to stop the Suboxone? Pretty much all of my patients have jobs, and many get drug tested—it hasn’t shown up yet. If it does, tell them the truth—that you are taking it for chronic pain because it doesn’t ‘mess up your thinking’ like ‘REAL’ pain pills do.

There is NO painless way to withdraw in a few weeks. My tapes recommend reducing very, very slowly over a number of months, to a very low, microgram dose.

Sorry for the ramblins…if you dont read it that’s ok…it’s just another hard-knock story.

You only asked about Talwin..it SUCKS===dont recommend it. That’s probably why it’s hard to find at most pharmacies–no one uses it. I can’t go thru any w/d right now–I just finished the interior floors in my house–it’s almost ready to sell–took me 15months to do all the stuff that didnt get done by contractors–so I HAVE TO FOCUS on selling this place now.
What do I want—I will get your tape for w/d from suboxone. And I need to learn to let go of anger, regret and fear. Easier said than done. Do I use positive repetition to retrain my thoughts to quit worrying so much?

That would be ‘CBT’, and another long process. For now, you take one day at a time and do a daily inventory at the end of each day, reflecting on the good things you have done and giving yourself some credit. If you REALLY need to be off Suboxone by September, the time to start weaning is now—but you do it so slowly that the w/d is very small. Ten percent reduction every couple weeks.

I truly wish you the best. I will send you a link to download the tapes without charge; maybe that will be the start of your luck turning around.

Is My Suboxone Dose Too High to Have Surgery?

Thanks, all of you who wrote comments to my last post.  I remind everyone once again to consider taking your comments here and after writing them, also taking them to SuboxForum.com.  I am going to put up a new category to discuss topics that were initiated here;  it would be great to get a spirited, respectful ‘give and take’ on some of these topics.  As I have mentioned before, the only thing that I will block on that site would be debating whether people on Suboxone are ‘in Recovery’– just because there are plenty of other sites for that, and I want the forum to be for people who have made their decision– and don’t want to be harassed over it.  I will be upgrading that site shortly and changing the hosting account;  hopefully I will pull it off without erasing everything!
OK, tonight’s topic: I am taking my post from a different forum and posting it here also to save wear and tear on my keyboard…  I responded to a person who is taking 32 mg of Suboxone daily and who is concerned that the relatively high dose will raise her tolerance higher than she would like.  She has surgery coming up, and is concerned that the high tolerance will get in the way during or after the surgery.    My reply addresses the level of opiate tolerance in relation to dose of buprenorphine.  Incidentally though I will quickly say that buprenorphine poses little problem during an anesthetic;  it does not interfere to a large degree with general, epidural, or spinal anesthesia.  But buprenorphine DOES interfere with the treatment of post-operative pain.  I will also comment that I consider 32 mg of daily Suboxone to be a waste of money;  my experiences treating people with Suboxone have only reinforced my opinion that there is no benefit, and often considerable harm, in taking more than 16 mg of Suboxone per day,  and in dosing more than once per day.  But that discussion will have to wait.
My Response:
I will talk about buprenorphine, the active medication in Suboxone, just to simplify things a bit– although Suboxone will have the same effects. First, when talking about the dose, it is important that the method one takes it is identified– as that is what determines how much active drug ends up in the bloodstream. I will assume that the person is taking steps to get maximal absorption of Suboxone; for example keeping it exposed to mucous membranes for a long-enough time, and not rinsing the mouth with liquid for at least 15 minutes after dosing, to avoid rinsing away drug that is attached to the lining of the mouth but not yet absorbed. As an aside, there is a post somewhere on this blog entitled ‘maximizing absorption of Suboxone’ for those who want more info.

When a person takes Suboxone, he is taking a ‘supra-maximal’ dose of buprenorphine. Buprenorphine is used to treat pain in microgram doses; the BuTrans patch is used in the UK to treat pain, and it releases buprenorphine at a rate of 5-20 MICROGRAMS per hour! One tablet of Suboxone containes 8000 micrograms! So whether a person is taking one, two, three, or more tabs of Suboxone per day, he is taking a very large dose of buprenorphine— a dose large enough to ascertain that he is up on the ‘ceiling’ of the dose/response curve. It is important to be on the ceiling, as this is the flat part of the curve (I know– a silly statement) so that as the level of buprenorphine in the bloodstream drops, the opiate potency remains constant, avoiding the sensation of a decreasing effect which would cause cravings.


I have read and heard differing opinions on the dose that gets one to the ‘ceiling’ but from everything I have seen the maximal opiate effect occurs at about 2-4 mg (or 2000-4000 micrograms), assuming good absorption of buprenorphine. I base this on watching many people initiate Suboxone; if a person with a low tolerance to opiates takes 2 mg of buprenorphine, he will have a very severe opiate effect; if he takes that dose for a few days and gets used to it, and then takes a larger dose, there is no significant increase in opiate intoxication– showing that once he is used to 2 mg, he is used to 16 mg— and is ‘on the ceiling’ by definition. I see the same thing in reverse; there is very little withdrawal as a person decreases the dose from 32-24-16-12-8 mg, but once the person gets below 4 mg per day, the real withdrawal starts. This again shows that the response is ‘flat’ at those high doses, and only comes down below about 4 mg of buprenorphine.

The flip side of all of this is that tolerance reaches a maximum at about 4 mg of buprenorphine, and further increase in dose of buprenorphine does not cause substantial increase in tolerance. Tolerance and withdrawal are two sides of the same coin; the lack of withdrawal going from 32 to 8 mg of buprenorphine is consistent with no significant change in tolerance across that range.

So in my opinion, being on 32 vs 4 mg of Suboxone doesn’t raise your tolerance. But in regard to upcoming surgery, there is an additional concern. One issue with surgery on buprenorphine is the high tolerance, but the second issue is blockade of opiate agonists by buprenorphine– and this effect is directly related to the dose of buprenorphine. A person on 32 mg of Suboxone will need much, much higher doses of agonist to get pain relief than will a person on 4 mg of Suboxone– not because of tolerance but because of the blocking effect, which is competitive in nature at the receptor. When people are approaching surgery I recommend that they lower their dose of Suboxone as much as possible– to 4-8 mg if possible. Because of the very long half-life (72 hours), this should be done at least a week before the surgery. Then I have them stop the Suboxone three days before the surgery; it usually takes 2-3 days for significant withdrawal to develop. I say all of this to give a general sense of the issues involved; people should discuss the issue with their physician rather than act on what I am describing here.