Tapering off Buprenorphine
A comprehensive guide to tapering off buprenorphine
Summary:The purpose of a taper (instead of just stopping) is to gradually reduce tolerance, thus
distributing withdrawal symptoms over a longer period of timeminimizing the discomfort experienced on any single day.
Ending the taper at the manufacturer's lowest available dose (2mgs for Suboxone Film® and generics or 1.4mgs for Zubsolv®) can still result in significant withdrawal.1,6 Here we lay out the
rationale for tapering to much lower doses. As the data will show
2mgs/day is closer to the midpoint of a typical taper than it is to the end.
Pace the taper with the body's ability to adaptto each decrease. Dose
decreases of 25% separated by at least 10 dayshas been reported to be tolerable by many.1
Are you ready to taper?
A taper should only be considered once a successful treatment period is completed.
The whole point of buprenorphine treatment is to suppress cravings and withdrawal so that you can make big changes in behavior, routine, living situation and thinking. It's these changes which, in effect, rewire the brain and reverse some of the craving-causing brain adaptations. If this is not done first the taper will likely be shortly followed by relapse.
Have you made significant changes in behavior and had a period of time to gain experience with those behaviors? Have you been able to deal with stress, anxiety and depression without craving drugs? This takes time and doesn't happen on its own, it is a deliberate effort. If you have been in stable treatment less than six months, tapering is NOT advised.
Buprenorphine is NOT a detox medication, it is a treatment medication. If you are not clear on this distinction go to the treatment page and understand it before tapering. But assuming you are ready to taper there are some things to consider.
Tapering to very low doses minimizes withdrawal
Before we continue, it should be noted that the following is a detailed explanation for those interested in the nuances of tapering and not necessary to conduct a taper. It does however help make sense of why certain protocols are likely to be more effective than others.
To understand the tapering process there are a few concepts you should understand:
The Ceiling Effect of Buprenorphine:
In short, at a certain dose of buprenorphine nearly all available opioid receptors become occupied with buprenorphine.3 Each helps induce a small opioid effect.4 The cumulative effect created from all receptors is the maximum effect or the ceiling effect.4 The minimum dose to reach this point is the ceiling dose. Taking more than the ceiling dose involves so few additional opioid receptors that patients are unable to detect any additional opioid effect.4 Whether the patient's dose is at, near or above the ceiling dose, they experience virtually the same opioid effect. For this reason, tapering can be more aggressive (per mg.) at higher doses than at lower doses when more receptors are affected by dose decreases.2
Fig 2 is a PET scan showing the amount of available opioid receptors at various doses.3 From this evidence it is clear that, for this particular patient, at some dose above 2 mgs. and below 16 mgs. the ceiling dose is reached, as the amount of available receptors have diminished to insignificant levels.3 If we extrapolate this admittedly very limited dataset and apply a curve shape common in biology, we can estimate approximate receptor involvement at various doses. Fig 2a illustrates this concept. It should be noted that there is great variability in reality and liberties have been taken with this particular graph, but it is meant to illustrate the point that the amount of receptors involved is not a linear relationship with dose. Therefore cutting the dose in half from 32mgs to 16mgs doesn't mean that half as many receptors are affected, in fact due to the ceiling effect there would be no discernible difference.
If a taper should follow a steady and gradual decrease of involved opioid receptors, then 2mgs would be about the midpoint of the taper. In one of the few taper studies, both long and short tapers ending at 2mgs resulted in very low success rates.6 The researchers concluded: "For individuals terminating buprenorphine pharmacotherapy for opioid dependence, there appears to be no advantage in prolonging the duration of taper". They apparently gave no consideration to the possibility that maybe 2mgs is too high of dose to stop at. We will show it is and suggest their conclusion is wrong in that extending the taper well below 2mgs for a much longer period of time is beneficial.
Buprenorphine doesn't completely metabolize between doses. It typically takes between 24-42 hours to metabolize half of it, but could range as much as 20-70 hours.9,10,11 We use 37 hours as an average in our calculations, but be aware of the range if your results don't meet expectations. Therefore, after the first 37 hours, only about ½ of the buprenorphine has been metabolized, while half remains to continue to elicit an effect. After another 37 hours half of that remains and so on. At typical maintenance doses, previous doses can contribute to the overall blood levels for 5-12 days (depending on actual metabolic elimination rate). At very low doses, by day three the amount of buprenorphine still un-metabolized is so small its effects are negligible.
Buprenorphine Blood Level Buildup, Stabilization
As patients take subsequent doses of buprenorphine before the prior dose has completely metabolized, a buildup occurs in blood levels. (Fig 3) The buildup continues for approximately 5-12 days at which time the dose taken 5-12 days prior has nearly fully metabolized. This is the stabilization period. When dose is decreased the effects of this build up should be considered before the effects of the new lower dose can be evaluated.
Putting It All Together
We now know that doses at or above the ceiling dose can be decreased more aggressively than lower doses. We know that 2mgs/day is not the end of the taper but closer to the midpoint. We know that due to the half-life, buprenorphine builds up in the blood and may still produce effects 5-12 days later, particularly at higher doses. Armed with these considerations we can construct a taper plan which will minimize discomfort.
Buprenorphine Taper Plan
By coupling what we learned above with anecdotal taper testament found online, we can estimate that dose decreases of 25% with 10 days between drops should be tolerable.1 Furthermore, if our initial dose is at, near, or above our estimated ceiling dose we can taper more aggressive initially, maybe as much as 50% drops. As we approach 2mgs and below, we should expect more noticeable differences between each dose decrease and may need to slow down the pace. Once at a very low dose (less than 0.5mgs) we can speed up the pace once again as the buprenorphine is metabolized down to insignificant levels in just a few days.
Emergency Buprenorphine Taper
If you find yourself in a situation where you must taper off immediately for some reason and don't have the time or enough buprenorphine for a planned taper, you can try an emergency taper. With the emergency taper you stop all buprenorphine until the onset of withdrawal. At that time you take small doses (<= 1mg) every hour until withdrawal is tolerable. Then, take buprenorphine only when symptoms become intolerable and only enough to stop the withdrawal. Although this method minimizes withdrawal intensity for a given amount of available buprenorphine, there could still be considerable withdrawal depending on tolerance and the amount of buprenorphine available.
Which brand of buprenorphine to use
As of late 2016 there are 3 name brand and at least 4 generic buprenorphine products to choose from. For ongoing treatment something can be said for the newer brands; with their better bioavailability side effects may be fewer and some dose and copay card combinations make it the least expensive option (including generics). (see cost page) But when tapering, particularly at doses below 2mgs, Suboxone Film (as pictured above) offers the advantage of being larger thus easier to cut into the fractional doses necessary for the taper. Pieces of film left over between doses should be stored in a childproof pharmacy bottle with a silica gel pack to absorb humidity and prevent the opened film from becoming sticky. (see storage section)
When to take your taper dose
Taking your buprenorphine first thing in the morning is best. There is good reason for this. By taking your dose in the morning, buprenorphine blood levels are lowest while you are asleep. Therefore, when the buprenorphine is providing the lowest level of craving and withdrawal suppression you are asleep and aren't dealing with it. Another reason is, you want to avoid anticipation of taking the dose, because this is the type of brain activity you want to eliminate. Anticipating the dose then receiving the reward of the dose, may be reinforcing the behavioral patterns you have worked so hard to eliminate. By taking it early in the morning, there is no need to think about it for the rest of the day. Exception: If insomnia becomes acute, you may benifit from taking your daily dose at night.
Take your full day's dose all at once
Don't split up the day's taper dose. As mentioned above, taking it early prevents you from thinking about and anticipating your dose. Also, once you finally stop, it is an easier transition from taking something once a day to zero times a day, than it is from taking something 2-4 times a day, to zero times a day. Also avoid complicated rituals like dissolving the medication in water and metering out portions for the taper. Simply cutting the film or tablet is all you need to do. Exception: Again, if insomnia becomes acute, splitting the dose up by taking some in the morning and some at night might help.
Buprenorphine Taper Schedule Calculator
The taper calculator below accounts for the information presented above. Because everyone is different this should only serve as a suggestion and might need to be tweaked for individuals. One convenient feature is it estimates the total time and total amount of buprenorphine required to conduct the taper. The taper schedule can be edited and printed out as well.
Remember, the taper schedule is not etched in stone. Individuals will respond differently to the same taper schedule. It is meant as a rough guide which must be tailored to match an individual's body and circumstance. The main concept is to pace taper rate with the individual's ability to adjust to each decrease. However it can be helpful to have a guide to loosely follow and to estimate about how long it will take and how much buprenorphine will be required.
Buprenorphine and Pain
Buprenorphine is a painkiller. A return of minor aches and pains is to be expected when you stop taking a painkiller. This is not withdrawal, it's the pain the painkiller was killing but isn't killing anymore. Aleve® or some other OTC painkiller, might help but only when and if you need it. Hyland's® Restful legs tablets have also been reported to be effective especially, at night. For sleep, patients have suggested Valerian root and Melatonin. Maintaining good overall nutrition and keeping well hydrated is also important. But maybe the most important thing is to keep busy, preferably away from home. Sitting home waiting for symptoms to appear is a sure way to fail.
Pain is progress
The discomfort you feel while tapering can be thought of as an indication of your tolerance diminishing. The necessary discomfort stimulates the body to produce endorphins. If you can possibly motivate yourself to exercise, even brisk walking, the pain will be less noticeable and you benefit form the exercise. It might also help you sleep better.
Depression and Tapering
Along with being a painkiller, buprenorphine has been recognized as an anti-depressant.7,8 Just as when you stop taking a painkiller, pain comes back, when you stop an anti-depressant, depression may come back too. The severity of the depression could determine the success or failure of the taper. Be prepared to deal with the reemergence of depression, particularly if you suffered from it before starting buprenorphine treatment. This might entail working with a psychiatrist and having antidepressant medication on the ready, before concluding the taper.
Pausing the Taper
If you hit a dose level which produces unacceptable levels of withdrawal discomfort, it is acceptable to go back up in dose, one step, for a few more days. Alternatively, you can hold at that dose for a longer period of time than indicated on the taper schedule. Since everyone’s body and brain is unique, the generic taper schedule may need to be tweaked slightly. Once your body adjusts to the dose level the taper can be resumed.
It's okay to take a break from the taper if you need to, as long as it is minimal and infrequent. An example would be if you have been at 0.5mgs/ day for a week and still feel withdrawal discomfort, taking up to 1-2mgs one day will remove all withdrawal symptoms for that day and possibly the next, giving you time to refocus, get things done, and prepare for the final leg of the taper. One day at a higher dose will not increase your tolerance, thus reversing your progress, as long as you limit such higher doses to once or twice during the taper. If you can, try and not take any the following day. This may not be that difficult since about half will still be present the next day. Then resume the taper schedule.
- Anecdotal evidence compiled from several social media sites over a period of several years
- National Alliance of Advocates for Buprenorphine Treatment- www.NAABT.org
- PET scans- mu receptors- Effects of Buprenorphine Maintenance Dose on mu-Opioid Receptor Availability, Plasma Concentrations, and Antagonist Blockade in Heroin-Dependent Volunteers - 2003 - www.nature.com
- TIP-40, buprenorphine treatment clinical guidance - government document 2004
- Results produced by the NAABT.org taper engine (beta)
- Buprenorphine tapering schedule and illicit opioid use- Clinicaltrials.gov, Identifier: NCT00078117 -Ling - study
- Buprenorphine treatment of refractory depression, Bodkin [study]
- The Buprenorphine Effect on Depression, Richard Gracer, MD [article PDF]
- Zubsolv full prescribing information submitted to the FDA - Zubsolv PI
- Bunavail full prescribing information submitted to the FDA - Bunavail PI
- Suboxone Film full prescribing information submitted to the FDA - Suboxone Film PI