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Yesterday someone wrote about the high potency of buprenorphine. He also wrote that it is hard to get off buprenorphine medications. I ended up writing more than I intended, which occurs often and keeps me up too late most evenings. I decided to share my anwer, as the issue comes up often on the forum and in my practice treating patients on buprenorphine medications (Suboxone, buprenorphine, Zubsolv, Bunavail, etc.)
My answer, partially edited:
Yes, buprenorphine is ‘potent’, but that potency is limited. Buprenorphine has strong opioid effects in microgram amounts, which is one aspect of potency. But the potency of buprenorphine is limited to a certain maximum effect, and in that regard buprenorphine is not potent at all. No matter how many milligrams, grams, or pounds of buprenorphine a person ingests, injects, or absorbs sublingually, the medication is NOT more potent than one 80 mg tablet of Oxycontin or five 10 mg tablets of methadone.
Likewise, an adult human cannot typically overdose on buprenorphine alone, even if that person has never used opioids. But it is very easy for adults to overdose from oxycodone or fentanyl. So from the danger standpoint, buprenorphine is not potent at all.
As for the difficulty stopping buprenorphine, the brain has NO idea which opioid drug or medication you are stopping. The brain (more accurately, the neurons in your endorphin pathways) only know that your opioid receptors have a high tolerance, and the activity in those endorphin pathways will come to a halt until tolerance returns to normal.
The degree of misery caused by stopping any opioid is a function of only two things: the degree of tolerance and the rapidness that exogenous opioids are removed. Buprenorphine cannot raise tolerance higher than the effect of 40 mg of methadone, which limits the severity of withdrawal. Almost every heroin addict I’ve met over the past 2 years– about 300 people coming in as new patients in a methadone program– have tolerances much higher than 40 mg of methadone. The average, in my best guess, is 3-4 times higher, judged by the very small effect that 40 mg of methadone has on their withdrawal symptoms.
The severity of withdrawal comes up often, and the reality is very simple. The problem is the change in mu receptors, not anything specific to buprenorphine.
Buprenorphine has features that make it easier to ‘come off’. We always use long-acting agents to taper medications. People coming off Xanax are changed to clonazepam, for example. It is not really possible to taper off something that has a blood level that goes up and down throughout the day. Tapering requires a stable blood level, and that blood level is then slowly decreased. With oxycodone, the blood level goes from very high to zero in 4 hours; with heroin in 8 hours. Medications administered by patch, such as transdermal fentanyl, can be tapered because of the constant blood level that patches provide.
As for the length of withdrawal, it takes 6-12 weeks off exogenous opioids for opioid receptors to return to normal, no matter the opioid. People always remember it differently, not surprising given how memory works. Think back about how long you had pain after your last surgery, or how long you had a bad cough after you had the flu. Unless the memory is pegged to something (like days off work), nobody remembers those types of things. We all have ‘impressions’, formed by what we’ve said or what we’ve read from others. But human memory is not good at remembering how long something happened. That’s probably why women go through pregnancy over and over. They wouldn’t more than once if they remembered the entire experience better!
Thanks for reading, as always. And again, I hope to see you at the Forum!
10 Comments
Michael Cornelius · April 26, 2017 at 8:20 pm
Guess people need to blame something g for their pain. Been through a life of unbelievable situations. Suboxone works! Try a life of Hollywood and prison, cults, snuff movies, and then tell me different? Ha, no clue!
Charles Anthony Foutch · April 27, 2017 at 7:34 pm
At one time i was injecting ten number 4 Dilaudid after i had 3 days of WDs after that I was fine until 90 days later i would start craving. I then started taking 15 to 30 mg of Methadone a day with the occasional D I tried to quit but couldn’t so i went into treatment which was 5 days in patient then 25 days out patient I suffered for 2 weeks gave up and used. In my experience the long acting opoids such as Suboxone and Methadone take a lot longer to kick. Dr. Dean Edell says the same thing and I have talked to people who say the Paws last 6 months from Suboxone.
srgmac · July 26, 2017 at 10:09 am
I don’t want to sound judgmental but I don’t believe you tapered off methadone properly. I’ve gone thru a few sub tapers in my life and every time I experienced the same thing — getting down to 2mg a day is easy as it can possibly be. Minimal discomfort if any. Getting past that requires tiny dosage reductions, a lot of patience, and a lot of time. I’m no doctor but if you’re doing a taper off of either sub or methadone it’s common sense that it should be done as slowly as possible with the dosage reductions as small as possible. I’ve found that for myself, sub tapers over a period of six months with small dosage reductions after 2mg is the best way to go. You’ve gotta keep in mind, it’s not a race! And if you’re feeling too crappy, perhaps you dropped down too fast, it’s OK to go back up if you need to for a few days or a week and try again!
The whole point of a taper is to make it as comfortable as possible on you. Otherwise you might as well just quit cold turkey.
Jeffrey Junig MD PhD · July 30, 2017 at 7:48 pm
I agree with the buprenorphine comments. The taper is all stacked at the end, because of the shape of the dose/response curve with buprenorphine. With methadone, the size of each reduction gets lower at lower doses, because the PERCENT reduction is what determines the withdrawal– not the absolute reduction. Usually people tolerate a 5% reduction without too much trouble. So at 100 mg, they can drop by 5 mg. But from 20 mg, that means a reduction of 1 mg would be about the same as a 5 mg reduction from 100 mg. I realize I’m phrasing all of this in an awkward way… hopefully you get my point!
William Taylor, MD · April 28, 2017 at 7:59 am
I’m pleased that one of your hats is that of a methadone clinic doctor. Both drugs are lifesaving, and the treatment programs are complementary.
Jeffrey Junig MD PhD · April 28, 2017 at 3:35 pm
Yes– I had some misconceptions about methadone treatment, but I’ve become a fan after seeing how it comes together, especially for the most-difficult patients.
srgmac · July 26, 2017 at 9:51 am
I have a question regarding detox protocols using bupe.
Given the “oxy 80mg” ceiling / limitation of bupe, why is it used with people who have much higher habits than that who are trying to detox as comfortably as possible?
I personally have had situations where I’ve had a massive tolerance, spending hundreds of dollars each day for months and injecting H all day long, tracks all over, and then when I tried to detox (sometimes going into a hospital or detox center under the care of physicians) using bupe, it was a total nightmare.
I feel that in such cases, at least from my own personal experience, that the bupe actually makes the withdrawal experience worse.
Maybe it’s for psychological reasons, because you’re in such agony and you’re taking something, expecting to get at least to a point where you are well enough to take a shower and maybe eat some toast, and not only does nothing happen, it becomes even worse and prolonged!
To clarify, I’m NOT talking about PWD.
I’m talking about when a person has such high tolerance that no amount of bupe is going to help them transition off their opioid of choice comfortably because of it’s potency (or lack thereof).
So why do many detox centers not use methadone for such cases?
Why put people thru agony like that?
It just seems almost cruel in a way, especially when methadone would almost certainly work much better, not to mention, we’re dealing with a life and death struggle here — and you would want to do everything you can to keep said individual away from the street & injecting H or whatever else it is they are doing, especially in such a sensitive time…I’ve been in detoxes before where I’ve seen people walk out, go use, and come back in a body bag!
Jeffrey Junig MD PhD · July 30, 2017 at 7:45 pm
I just got back today from an ASAM course. Every lecture repeated the same thing about detox–that there is rarely a legitimate reason to simply detox someone addicted to opioids. Yes– the death rate is high after detox, whether it is done in a clinic, a jail, or a short-term treatment program.
But I can’t explain your experiences with buprenorphine as a detox tool. I don’t treat people with it in that way, so my clinical experience using bupe as a detox tool is not great. But a number of studies have looked at the use of buprenorphine for detox, and found that symptoms were reduced by the use of buprenorphine. The way it appears to me from the binding properties of buprenorphine, bupe appears to pull tolerance lower immediately after induction– and then the person has less ways to go to get tolerance down to zero.
I hear people on the forum claim, over and over, that bupe is harder to detox from than heroin or other agonists. But 1. that is the opposite of what has been found when people are detoxed with or without it, in studies; 2. it makes no sense that buprenorphine would be harder given the limit on tolerance created by buprenorphine; and 3. whenever I really get into the stories of people claiming heroin was easier, the stories fall apart. For example someone will say their heroin detox was easier, but then they say that they got as far as 2 weeks into that detox before using again. It is very hard to find anyone who has detoxed off heroin outside of a locked environment– but I know many people who have tapered off buprenorphine.
Finally– my own detox off fentany, 17 years ago, was horrible. I was in treatment for over 3 months, and I was still sick at 2 months. By 3 months I was getting my appetite back. So I know that resetting tolerance simply takes a LONG time, no matter what drug raised that tolerance.
About methadone… yes, I always tell people starting buprenorphine that it is easier to taper methadone because of the size of doses of buprenorphine. BUT– it is no possible to use methadone in that way outside of methadone clinics, because it is not legal to treat adddiction or tolerance using methadone in any other setting. And in those settings, the maximum dose that can be given initially is 30 mg of methadone– a Federal law. Another 10 mg can be given the first day after a period of observation… but then the dose has to gradually be increased, as the person’s tolerance comes down. It is not possible to just ‘match tolerance’ using methadone because of the huge variability betwen individuals in how the drug is metabolized.
Lola · August 12, 2017 at 2:11 pm
I just found this site today !!! It is excellent!! God has blessed me. I’m rather confused as how to leave comments other than use reply but, I will
Find the time to learn… now I am just enjoying all the knowledge . Thanks to u Dr and everyone
sara · October 20, 2017 at 6:38 pm
no matter what anyone says, if you haven’t been on suboxone you don’t know what it is like, the problem is they should only use this to help with withdrawals, not long term use. Thats where these doctors go wrong.ive been on subs for 9 months now, my hair is falling out like crazy, tooth decay is forming, mood swings. fatigue and no sex drive at all. i have made my mind up that i will not continue this drug. My delima is that i want off soon as possible but unfortunately i don’t have the opportunity to go to a detox.i have kids to take care of. So what do people do in these situations? “Tapper Off”? does it really work? i can’t imagine being on something that is making bald and my teeth fall out any longer! i am only 28 years old, and in good health, well was. its taken my life just like drugs did. we all want to get better but turning to another drug just isn’t the answer. wish i had more knowledge before accepting this.