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.

39 thoughts on “Optimizing Absorption of Buprenorphine”

  1. re subox film has better absorption apparently.the film has been just released in oz.
    i take my subx sublingually.
    in oz alot of idiots divert it/i.v causing big probs if pple want to travel o/s with subx.
    i went to Bali& last year could only go for 10 days.
    ( that was max dose by law my chemist could give me due to pple abusing it.)
    i love been on the film- i have been trying to get off tabs for years,but got stuck at 2mg due to finding chopping,cutting the pills messy,darn impossible to work with They just crumbles.so hard for correct dosage.
    Also made me paranoid at work having bits of powder in foil.( i work in d&a field)
    Reckitt shldve been sued for making suboxone tablets so crumbly-is not necessary.
    Im reducing off after 5+years on 6mg & have been looking at what im gunna be dealing with chemically.
    2mg subx(taking only approx 20% absorption into account) is equivalent
    (in my lay opinion)roughly to about 20mg morphine tablet.thats a serious amount of opiate.
    The 2mg sounds small and makes pple think its nothimg-mistake Beckitt.
    In Beckitts defense i LOVE THE FILMS re can cut up easy.
    -I WILL BE FREE SOON.YEEHAH.
    Due to raeding about the increased absorption film,i smartly reduced my dosage by 50% -from 5mg-3mg in the first week swapping.
    Re the ingredients ,the inactive ingredients could cause a few people allergies perhaps.white ink dosent sound the best!Mind u they would be similar inactives to the listerine film strips i suppose.
    Me On Storing the Film:
    People must remember if cutting up FILM dose. film is very light/air sensitive.
    also n.b pple to store below25c.
    Best storage method ive found–any tips much appreciated.
    Put the other piece film not using back in original foil slip & seal with sticky tape or any adhesive label.(One guy folds over tightly &uses a paper clip to secure foil slip!Another puts dose in a small baggie-can buy frm bead-jewelery shops)
    I store my unopened filmstrips at home in a small slim cigarette case.
    i dont smoke but perfect size for the films.(we dont get given the whole external cardboard box in oz.have to pick up twice a week frm chemist)
    good luck all.

  2. Doc,
    I find it difficult to crush and paint my mouth w/ the new Hi-Tech 8mg. generic subutex. They are so small, that I seem to get better results by just warming my mouth, keeping the pill under my tongue, and moving it around that way. It is hard for me to keep my mouth dry and I end up losing,(down my throat)…
    I had no problem w/ the larger pills, but I would just as soon take the smaller Hi-Techs, knowing that there is most likely less filler and excepients, which I have no use for…..
    just my opine,
    Scott…..

    1. Thanks! I notice that the study is from 1982– and the doses used are 10% of typical clinical doses used for addiction treatment. I wonder if the results for higher doses of buprenorphine would be similar– i.e. also show absorptiont to take 2-3 hours to peak? I always find it interesting when people say that their dose ‘seems to wear off after an hour or two’, given that the dose hasn’t even peaked yet by that time. Obviously there is a VERY stron psychological component to self-assessed buprenorphine levels!

      1. I hope you read this. As to your response of wearing off in a couple hours I get the same thing. I take my dose and start to feel it kick in and in 3 hours I’m hurting again almost worse than before I took it. I have a feeling it’s a absorption issue such as being rushed while taking it and or not correctly measuring out the same amount everyday. Weird part is I can dose again and nothing changes I feel good for a while about 3 hours later I feel bad. I have just learned to deal with it. Some days 3 mgs takes me all day long and some days 8 mgs does nothing.

        1. The challenge is fitting the symptoms you described with the time-course of buprenorphine absorption. The pattern of absorption after sublingual or buccal dosing is firmly established, because that data was required by all buprenorphine medications, back when they seeking approval by the FDA. Buprenorphine is absorbed over a number of hours, with peak blood levels at about 4 hours after dosing.
          I usually say ‘everyone is unique’, but with absorption, people are almost identical. We all have the same layers of tissue in the oropharynx. There are small differences in absorption related to the amount of dilution by saliva, and because of differences in blood flow. But the differences are not significant enough to cause significant symptoms like what you described.
          The time course of your symptoms suggests they occur when the blood level peaks, at the moment the level starts to drop. The other thing you wrote that gives me pause is that most people do not ‘feel it kick in’ every day. You wrote that you are ‘hurting’ when it wears off– are you talking physical pain, or withdrawal symptoms? I ask because yes, I would expect any pain-relieving properties to go down significantly as peak blood level goes down. But it is very odd for a person to have withdrawal symptoms while taking over 8 mg per day. That is a very large dose for most people.

          1. What i mean by kicking in is the withdraw goes away and then 2 hours or 3 hours later my legs start hurting again depending on the dose.

          2. Also I’m not saying I’m different I’m just wondering what I am doing that’s screwing up the absorbtion.

          3. I don’t mean to ignore you- I’m just not sure what is happening. I don’t remember how long you’ve been on buprenorphine, but sometimes people with high tolerance take a while to get used to the medication. There are also effects of buprenorphine metabolites outside of the nervous system… I’m wondering if norbuprenorphine, a breakdown product, could be doing something to the muscles to ease the pain…. but I have no idea what that effect would be, because I don’t believe there are opioid receptors on muscle tissue. Maybe the aching legs is related to histamine release… that can occur when white blood cells are bound by some opioids…
            I’m guessing though at this point.

      2. Hello Dr.
        Ive been on suboxone for 3 years 16mg daily with no problems I loved it. About 5 months ago something changed. Since then (Aug 2018), I have been experiencing what I call withdrawl symptoms almost daily. Tremors.. Extreme hot and cold. Excessive sneezing, Vomiting anf full pupil dilation. I have not changed my dose nor changed any meds. I only takr subs and birth control pills and like I said I have been fine for 3 years. My docs put me on Busprione (5mg/ 3times per day) in adddition to the 16mg of subs. My doc had me try taking my subs throughout the day to ensure absorption. It did not help so we went back to administering it once a day in the morning. Nothing has changed in terms if feeling better. I just keep thinking there is not enough saturation of my receptors. What happened? I dont know what rlse to do except maybe switching to methadone but I’m so scared. If I still have thrsr w/d symptoms then maybr its sonething else. According to my doc “this” does not happen to patients who have been on bupenorphine for an extended period of time. It usually makes you sick when yo first start taking it according to him. He thinks it’s a gastro issue that is mimicking w/d symptoms. What? Even if it is a gastro issue, is there something additional I can take to stop the sickness? I think its the medication not being absorbed adequately. Any similar situatuion, advise, comments, questions???? I feel so hopeless.

  3. I have been taking my sub you text incorrectly for a few years, I’ve decided to pull it together and start to taper off. My doctor is concerned that my levels are 10 times what he would expect a person on 12 mg to be. Could this be because I take it frequently throughout the day instead of at one time, and builds up in my body? I get no pleasure from anything anymore, I don’t listen to music, laugh, hang out with friends etc. I feel that my reward system is completely broken. I also have not had a menstrual period for the entirety of my treatment.
    I never take more than 12 mg, I’m wondering if there’s any other reason my UAs are coming back being that high?
    If there’s anyway I could have a phone consultation with you even for five minutes it would be so appreciated

    1. I’ll try to answer questions, but I can’t do the phone consultation for a number of reasons. I would not be able to have a 5 minute discussion; we would never be able to communicate on all of this in less than 30 minutes! But more important, a consultation means I’m a part of your medical decision-making, providing ‘care’- which can (and does) lead to Board problems. I CAN provide answers that are general in nature, that don’t recommend a specific course of action, with the reminder that anything you do needs to be discussed with your doctor.
      Taking buprenorphine frequently would not cause the drug to build up in your system, but it could interfere with testing of levels. Your doctor might be checking ‘trough levels’ of buprenorphine, i.e. he may be expecting you to dose at 8 AM on Monday and no other time through the day, and then check levels on Tuesday at 7 AM, before you dose. That’s how methadone programs measure blood levels. If that is the case, taking a dose, even a low dose, a few hours before the urine test could have big effects on the blood level of the drug.
      There are also things that interfere with the breakdown of buprenorphine. If you go on Wikipedia and look up ‘CYP 3A4’ you will see a list of medications that suppress that enzyme, potentially raising blood levels of buprenorphine. But genetic difference in enzyme activity result in even much greater effects– so that it is not uncommon to see differences in buprenorphine blood levels. A good doctor uses drug tests as a TOOL– not as lie detector, and not as an easy way to make decisions about discharge.
      I get emails several times each month describing problems with drug tests– levels of buprenorphine or norbuprenorphine that are too high or too low. The people who write get no benefit from writing me, so I tend to believe most of them. It is clear to me that many, many treatment decisions made in error by doctors who place more trust in drug tests than in their patients. Yes– there is a great deal of dishonest to deal with when patients are actively abusing substances. But there is also a great deal of variability with drug testing, especially when related to the metabolic activity of patients from varying ethnic backgrounds, ages, and genders.
      In general in a case like yours, I recommend identifying what your doctor is worried about– e.g. is he worried you are taking tens time too much buprenorphine? If so, patients could ask, given that my metabolism appears to be different, what ELSE might we do to clarify the issue?
      Shame on any doctor who doesn’t try to figure out a way to sort things out.

    2. Katie, I would go get a hormone panel done. I felt the same way and my testosterone levels were basically non-existent when I started treatment for that I felt like myself again finally. Obviously it will be different for females, but there’s a strong correlation with opiates (even suboxone) lowering testosterone levels. I haven’t read up on what it can do to females hormonally, but females do need some testosterone to function and if it messes up the HPTA axis in males I’m sure it can affect similar systems in females. Not having a period is definitely something you need to get checked out regardless. Most doctors won’t tell you this, but I tell everyone guy that complains about lack of motivation, etc. to get a hormone panel done and it’s almost always either extremely low or at least on the lower end of the “normal” spectrum.
      Now finding a good endocrinologist is a whole different story. It took me 3 years to find someone who would prescribe me testosterone and the proper ancillary drugs.

  4. Hi, I have been on Sub for a number of years. Recently I had a surgery on my back. I was prescribed a extra 8 mg a day, for two weeks after the surgery for pain. I was taking 4 mg before my surgery. After getting that extra dose I became dependent on a higher dose. I am prescribed 16 mg a day. I usually would take 3/4 of a pill when I woke up, and toke 4 mg later in the day. I have a similar situation to the person above. I felt fine when I took 4 mg a day, once a day. Since I’ve increased my dose I feel like I can’t get myself to feel normal no matter what. That was till yesterday. I was switched last week from Actavis to Amneal. My brother offered me a small line of the Amneal. I don’t enjoy snorting anything. I haven’t snorted anything in 3 years, but when I snorted only a 2 mg piece I felt instantly perfect. No more cold chills that I would normally have all day. I learned to live with it after a while. My question is, why does snorting not even half the amount I has taking under my tongue work so much better? I don’t want to screw up my nose, but I also don’t want to go back to accepting being partially dope sick everyday. Before I would wake up and feel a little cold chill. After I would place 3/4 of a tablet under my tongue things would get worse. The cold chills and hot flashes would increase in intensity. After a couple hours it would get better, but I would never feel 100%. I would just keep trying to take more. Some days I would feel ok with more, some days it would only make it worse. Am I getting a more in my blood stream by letting the bupe sit my nose?

    1. On average, people absorb about 30% of a dose of buprenorphine sublingually. I don’t know of any studies looking at the percent absorbed through the nasal route, but perhaps it is more than 30%. BUT– Don’t do that. Most of us who got addicted to opioids made a series of small, bad choices. This is one of those bad choices. I don’t know of any safety data looking at the effect of the powders and packing products on nasal membranes– but I doubt they are good for those membranes. And the behavior may be hard to stop, especially if you keep doing it for very long. I think a better choice would be to find a different way to deal with the issue– maybe by temporarily getting on a higher dose.
      BTW– I do NOT agree with giving more buprenorphine to treat surgical pain. The extra analgesia is not that significant, and in most cases people need an opioid agonist after surgery.

  5. I am 1.3 years clean from all recreational, street, or un-prescribed drugs. I have only taken my Subutex in that time. I have been on the same dose for this entire time, 12mgs. There was a time when I would take much less of my medication and be fine. Then it started to be that I was taking 16 mgs a day and sometimes 20 mgs. Of course with no results. In addition to that, I do not ever even feel like I want to get high. I never feel as though I need to use drugs. I just get to a point of feeling as though I don’t feel “normal” and when I start thinking of wanting to feel differently than I do, I typically attribute that to needing more subutex. Could this have anything to do with absorption at all? Or could this simply be an addicts behavior, but i am justifying it by it being my medication? I have been on the small, hi tech brand 8mg pills and when I use your method, it makes it hard for me to not build up saliva quickly. I end up swishing an ENTIRE mouth full of spit for over 30 minutes while working. I don’t feel as though my dose is doing what it should but how do you know the difference between addictive behaviors and actually just needing a higher dosage or more absorption? Your blog has been a godsend. Thank you. I really hope you have a chance to reply!

    1. I see the same thing happen to other people. My impression is just an educated guess, but I suspect that early on buprenorphine people remember all of the misery associated with using agonists, and that memory, combined with buprenorphine, keeps them on track. Over time, people tend to revert back to who they were before treatment. We see that with all treatments, btw– which is why relapse rates are high with residential and non-medication treatments. But as they revert, they go back to that state of mind where they ‘need’ something to deal with the depression, or boredom, or lack of spirituality, or loneliness, or whatever… that pushes people toward using opioids. I don’t think they GET anything from taking extra buprenorphine beyond a placebo effect, but that placebo effect can be very powerful, especially for a person who is not taking any other controlled substances.
      That’s just my guess… I would try to ‘treat’ it by spending a lot of time thinking about the worst parts of the using world, when you would wake up sick each day, when you felt ashamed, etc. Every time you think of an extra dose, try to think about those days– and reinforce those memories.
      It could be something else too; nobody seems to like the hi-tech pills, and I wonder if their small size contributes to the thought that they aren’t doing enough.

      1. Thank you Dr. Junig, that helps me a ton! I think your educated guess was spot on. I forgot about the wording and meaning of “needing” something to feel differently. Lately I’ve been hovering in between depression and what I can only describe as literally feeling nothing. The nothingness feeling is what made me keep thinking I needed my subutex when in all reality it’s likely that I’m feeling this way because my spirituality isn’t good right now at all. Upon reading your response it made me realize that how I’m feeling ‘nothing’ all the time and that my communication with My higher power isn’t good, is probably a result of each other, not my subutex! Wow. Incredible. I can’t thank you enough for this response. I always try to explain how I feel to my psychiatrist, but can never get the wording right until I’m having those feelings in that exact moment. Because I was having all those feelings, I came back to this blog and decided to ask you your thoughts and you gave me and idea of what could be going on and now I have somewhere to start to help me get back to where I need to be! I am so glad I decided to comment. Thank you Dr Junig!

      2. Hello I could use a opinion Please from you. I am on Suboxone tablet and I take at least 8 mg everyday for the past few years. I had a awful stomach flu and couldn’t take my Suboxone for two days and went to my Suboxone Dr and told him of my sickness I take my urine test and it was negative for Suboxone!!! he sent it to a lab and it came back negative for Suboxone!!how did it go out of my system so fast ? I took my regular doses the past week. I keep my tablet under my tounge for thirty minutes every time.but yesterday I went back and he claimed that test was negative also !!!! what in the world is going on? How can I fix this? If I fail again I will be kicked out of the program and I can’t do without my Suboxone it would make me incredibly sick. Any advice please? Thanks

        1. Boy, I don’t know. I realize that some doctors look to lab tests as if they are the Holy Grail of medicine. We all learn in med school to ‘treat the patient, not the lab test’, but some people seem to forget it!
          Understand that every test has a ‘cut-off’ – i.e. a minimal level where it comes back as ‘zero’. The lab may be saying that the test that was used is not sensitive enough to measure that level accurately.
          Or it maybe that you metabolize the medication more quickly, and that those two days were long enough to metabolize it. That’s not a problem unless you start focusing on how you feel, and telling yourself that you’re having withdrawal when you’re actually doing fine.
          For your doc, I would suggest doing a witnessed dosing at the doc’s office and then do labwork the next day. That would give an idea of how fast you metabolize the medication.

  6. I’m an addict in recovery on Suboxone films… About 4mg /morning…. My cat has cancer and her tumor has burst…. I can’t afford anything, luckily insurance covers me. My question is this: can I put a piece of my film onto her open wound and work to reduce any possible pain? I’ve heard of ppl giving cat’s buprephenorphine injection for pain and I do know how to separate out the naloxone… But I don’t wanna stab my cat or put anything in the out-hole only… And if “drank/eaten” I’m sure won’t help… I hope as an addict yourself u r not too judgemental…. And I doubt addicts will put films on cuts to get high, so info isn’t dangerous. But feel free to private email me. Plz help

  7. Hello my Suboxone got stuck to my tooth! I still didn’t swallow or anything like normal will I still feel the suboxoSuor did I mess it up?! Please help me

  8. I was wondering if anybody has had problems with Suboxone tablets losing potency over the course of each month? For some reason when I first get my refill everything is good and I can stay stable on 8mg or less, but after a couple of weeks the tablets seem to dissolve really fast and I need more to ward off withdrawals. My guess is they’re absorbing moisture since sublingual tablets are designed to absorb moisture underneath your tongue and the bottle they originally come in has silica gel packets and is sealed. I bought a hygrometer which says my room is usually at around 45% humidity which shouldn’t be too bad, and the temperature never get above 75 degrees which is within the guidelines. I also store them away from sunlight. Just wondering if anybody has had any problems similar to this or has any solutions. Thanks!

    1. I think you’re right about the absorption of moisture, probably in some tabs more than others. But I don’t know about potency. Buprenorphine is a stable molecule, even in high temperatures, and medications that aren’t in solution tend to last far beyond their expiration dates. But as you’re suggesting, sunlight and moisture in combination might increase the breakdown of any substance.
      The other issue is absorption through the oral mucosa. Whenever you have low bioavailabity, the impact from small changes in absorption become magnified.
      At the same time I have not heard any of my patients bring up this concern, and it is very common especially for patients new to buprenorphine to feel like the medication isn’t lasting. I don’t know where you are in the process, but in the first year the mind often replays minor withdrawal experiences. I see the same pattern over and over- early on patients feel that a dose isn’t enough to manage their withdrawal, and later they find that they get by with much less. I think part of that is from the fading of memories of withdrawal. People using opioids also become very ‘somatic’, focusing on how they feel at every minute of the day to guage the need for opioids. I see people recover from that somatic preoccupation with time in treatment.
      Maybe somone else will share their thoughts. Also feel free to use the forum!

      1. I thought the same thing that moisture shouldn’t affect the stability of the actual buprenorphine, but whatever is going on is severely reducing the potency of my tablets. Each month I have the pharmacy give me the original bottles of Suboxone since they’re sealed. The other night I was using Suboxone tablets that had been opened for about a week and I took SIX of them but was still having bad withdrawals. Finally I took 3 teaspoons of kratom which alleviated the symptoms better than any of those tablets did. Then today I opened a new bottle and 4mg made me feel totally symptom free. I’m so lost on what to do because not only do the withdrawals come and go over the course of the month, but I can’t get any real taper going. I’ve talked to people that say Suboxone doesn’t work consistently for them, but I haven’t heard of anyone having these same exact problems.

        1. I don’t know what to tell you. I can’t imagine Kratom having any significant effect in a person taking even tiny doses of buprenorphine. It takes a few days, if not weeks, to get buprenorphine levels low enough for even potent opioids to activate opioid receptors. I don’t know if you read my comments about psychological effects, and people generally don’t accept that explanation. But that’s the sense I’m getting. Kratom is a weak opioid, and I just can’t imagine a person feeling actual relief of withdrawal symptoms while on any buprenorphine. I’m dancing around the issue but I’m saying that to me it seems that the symptoms are being generated by your mind – not by opioid receptors.
          People can tell by my dancing around the issue that this topic is uncomfortable. I don’t know why, but patients get angry when I suggest that psychological factors are to blame. I don’t understand the anger; I’m just some dude guessing about the issue from afar. But I’ve been yelled at over this issue more than any other.
          If you really need to know what’s going on, have blood tests done of your peak and trough buprenorphine levels. Urine is not adequate because of concentration effects; you need blood levels. But just do that and see if your blood levels are lower when you’re taking older pills. Remember that above a certain blood level, there is no change in opioid effect… and my guess is that the levels will be similar at both times. But who knows.

          1. I understand someone thinking that this would be a psychological issue, but it’s not. I used to get angry when someone would tell it’s all in my head, but it’s not worth getting worked up about. I’m not surprised people get angry though because most know their body and if something’s wrong, so to be told otherwise is a little insulting. I’ve been on Suboxone for 10 years and know when something is in my head. The kratom definitely made me feel better, so that shows how little buprenorphine was in my system. I came across a post in the forum where a lady said she had the same problem of Suboxone losing its potency over the course of the month. I’m going to call my doctor’s office and look into trying the Sublocade injection. That would eliminate the need to take the tablets at all and would give me a steady level of buprenorphine in my system.

  9. I have been on 2 8mg strips and feel like crap, high anxiety, bad mood, so I tried just 1 8mg film other day and I felt alot better. With subs more is not better I know it’s hard to think like that coming from an addict but it’s true with subs. Plus subs are alot easier to come off of than methadone. I was on methadone for 2 years and finally got off of it it was hell almost as bad as herion

    1. Yes, the opioid receptor effects of buprenorphine max out, from my patients, at around 4 mg per day. But as with most medications the side effects are dose-dependent. I suspect you’re feeling effects from actions at non-mu, maybe non-opioid receptors at those higher doses. As for methadone, I understand the reasons people develop negative feelings about the medication over time. But most of the people needing help for addiction in my community NEED methadone-assisted treatment. I have buprenorphine spots, but I would have no success with people using IV or crack cocaine and methamphetamine, in addition to IV heroin. But on methadone they have the structure of seeing a nurse every morning, having a counselor to speak to, and a medication that almost always relieves most withdrawal symptoms. Some of our patients get discharged from treatment because of cocaine or methamphetamine use, which completely destroys the benefit of methadone treatment… and yes, those people get sick. But the successes – and we have many – taper off methadone by about 3% per week, and at that rate there is little withdrawal.
      I think the best approach these days is to start most patients on methadone and then convert to buprenorphine when they are ready. If a person isn’t using cocaine or methamphetamine, I’ll try buprenorphine first, but I’m less optimistic. And the rare people out there who are still only using oral or nasal pain pills tend to do very well on office-based buprenorphine.

  10. Could you explain your comment regarding the ceiling effect occurring at 2 to 4mg of Buprenorphine daily? My understanding is that the ceiling effect is approached at 8mg as at this dose and above the graph demonstrating the percentage of occupied opiate receptors per buprenorphine dose starts to level out.

    1. I struggle with this issue. As you know, only 30% of a typical dose is absorbed, and we have little information about that distribution. What’s the standard deviation of that 30% number? Do some people absorb 50% or 60%? Are typical patients dosing in ways similar to whoever was involved in the studies that showed 30% absorption? Or do typical patients dose longer, with greater care in doing it right?
      So when we talk about the ‘dose’, one person’s 4 mg may be another person’s 8 mg. That’s one problem. Another problem is the difference between receptor binding studies and subjective experiences.
      From my clinical experience, the ‘ceiling’ occurs around 4 mg or so. But there are so many variables… the ones mentioned above, plus difference in cytochrome function. I see patients on methadone vary in blood levels by 1000 percent! Then there are differences in brain penetration, differences in volume of distribution because of protein binding… so when I say 4 mg, I say that as a general, clinical guideline.
      I have had many, many patients taper off buprenorphine over the past ten years. And I see a pattern over and over – that they can taper to about 4 mg per day with very little trouble. But after that, my patients have had a harder time. They get stuck at 4 mg. Or they have to go much more slowly, and have greater need for clonidine or other comfort meds.
      I used to do receptor binding studies in my grad school days. Those ‘in vitro’ studies have receptor environments that are much different than the environment ‘in vivo’. My personal opinion is that those studies are useful to compare agonists to each other, but not to determine doses in a clinical setting.

  11. Your comment about why trying to maximize absorption isn’t an addictive behaviour is nonsense. It could be an addictive behaviour, but it also might not. There is no reason to exclude is as a possible behavioural sign of addiction.

  12. This by far, is the most informative and understandable article about how Suboxone absorbs and how to do it. I have looked and asked, and still felt like I wasn’t getting the full idea. Thank you, and I truly mean that.

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