Why is it so hard to stop using Suboxone?

None of our patients want to take Suboxone for the rest of their lives, and understandably so. No one wants to take any medication for the rest of their lives.   But in the case of Suboxone, most patients find it very difficult to stop.  The opioid dependence that they have built up is very difficult to beat.  Why is it so difficult?

Stopping Suboxone is difficult but not impossible. Here's why:

Long term opiate addiction causes "upregulation" of the receptors, or an increase in the number of receptors. The more opiates one uses, the more receptors one develops and the higher the dose of opioids is needed to occupy those receptors. This is called tolerance. It is a vicious cycle of use and tolerance building. Long term use creates an overabundance of these receptors (upregulation) that without opiate replacement therapy makes abstinence very difficult. The receptors are numerous and screaming for both the endogenous (natural) and chemical opioids. 

Opioid Tolerance Cycle

Opioid Tolerance Cycle

When people stop using opioids, they begin to "down regulate", or reduce the number of opioid receptors in their brains.  How long does it take for down regulation to occur? Meaning how long does it take for those receptors to return to a more normal number? We don’t know exactly and varies across patients. It usually takes weeks to months. 

For Suboxone patients, its a slightly different process because they have moved from prescription or street opioids to a replacement therapy.  Suboxone only fills the receptors partially, which is why Suboxone does not get patients "high". By satisfying the demand of the receptors, Suboxone allows people to avoid withdrawal. 

When patients start on their Suboxone regimen, they are generally dosed by their doctor at the lowest dose that allows them to avoid withdrawal. When they are ready to taper off, they will start to reduce their dose, according to their doctor's instructions.   

Suboxone has a very long half life of 24 to 36 hours. The half-life describes how long it takes the body to eliminate half the dose. Suboxone patients have higher than normal tolerance for opioids and are taking a medication that takes a long time to leave the body. The combination of those factors can make Suboxone withdrawal difficult and long for some patients.

Patients frequently report they get down to a low dose of Suboxone and can’t stop without experiencing withdrawal. Why is this? Greenwald et al in 2003 found that PET scans showed that at 16 milligrams, 92% of receptors are occupied and at 2mg 48% of receptors are still occupied. This means that even if a patient is only taking 2 milligrams a day of Suboxone, half of their brain's opioid receptors are still being occupied by Suboxone.

Many practitioners say that staying on a low dose of Suboxone is a crutch but PET scans show that the two milligrams dose is actually continuing to occupy receptors. There is a physical reason why it is so difficult to go from two milligrams of Suboxone down to zero. Practitioners need to recognize this and taper patients off Suboxone slowly and over a long period of time. Patients can slowly taper and start to spread out their doses to make that transition from low to zero more tolerable.

Patients can also start more pleasurable activities like hiking, yoga, mediation, reading and other hobbies as well as increase their counseling during this time so that this time of transition to zero opiate replacement therapy is more tolerable.