BUPRENORPHINE 

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Buprenorphine is an opiate medication that is widely used as an aid in stabilizing patients with opiate dependency.  It can be used for detoxification, and in pain management.  It is also being used as a maintenance agent, an alternative to methadone maintenance.

The drug is a schedule three opiate agonist.  It used to be a schedule five medication which indicates its low abuse potential.  However, when it received the indication for use in addiction, it was rescheduled for closer regulatory observation.

It has a unique profile of actions in the brain.  Most importantly, it is a drug that stimulates the mu opiate receptors; but it stimulates the receptor weakly.  This means that molecule for molecule; it is weaker than heroin, Vicodin etc.   We refer to this property of less than maximal stimulation as a partial agonism.  Since it is only a partial agonist, you get a minimal euphoric effect, so patients have less of a compulsion to misuse it.  Tolerance is also less likely to develop than with full agonists.  Lastly, there is a ceiling effect.  After 16-20 mgs of medication/day there is no additional effects felt whether one take one extra pill or ten extra pills.  For these reasons, buprenorphine is the easiest opiate for an addict to control.   

Buprenorphine has the one of the highest affinities for the mu receptors (see pharmacology article) of any opiate medication.  It will displace any abused drug or pain medication from the opiod receptor.  That is why it is also said to be a blocker even though it has partial stimulatory effects. 

Unfortunately, when a person has a high tolerance from using other drugs (10-20 bags of heroin, >30-40 pills a day), withdrawal can be precipitated.  That is because you are replacing a stronger drug with a weaker one.  This precipitated withdrawal is relatively mild in most cases and resolves within 12-24 hours in most cases, although it occasionally last longer.  Patients using lower amounts usually do not have problems.   Occasionally, patients using higher amounts not have withdrawal.  Whether one will have withdrawal cannot be predicted; it seems to be related to an individual’s biology.

In addition to its effect at the mu receptor, it acts as a blocker at the kappa opiate receptor, another receptor that moderates pain.  Now, it takes more buprenorphine to block the kappa receptor than to stimulate the mu receptor.  So at lower doses, we stimulate the mu receptor and get pain relief; at higher doses, we begin to block pain relief.   This is one reason that there is a ceiling effect and that more medication may be less effective than less medication for pain control. 

The partial opiod  agonist effect is able to prevent withdrawal in most persons as well as treat chronic pain of a moderate nature.  However, it is not enough to cause intoxication or euphoria.  Most patients will feel clean and sober on the medication.   They can focus on what they need to do to get through a detox.   Many are able to work on the medication. 

Buprenorphine is a long acting drug and comes out of the body slowly.   This means that withdrawal will be less intense.  Some people may feel no withdrawal at all but they are in the minority.  Unfortunately, acute withdrawal often occurs and it will last longer than withdrawal from other opiates.  It often lasts last 5-10 days after the last day of using the medication (but up to 3 weeks).   However, the longer withdrawal period, combined with lower tolerance, results in a significant reduction in the intensity of physical withdrawal symptoms.

Buprenorphine represents a significant aid to persons who want to detox.  It is not a wonder drug.  The use of the medication will not avoid the emotional abstinence symptoms that can last a month or more.  Depression can be an issue.  Psychiatric medications do help.  Counseling is extremely important. 

Buprenorphine has been approved for maintenance.  Physicians, in the community, who have completed special training, can prescribe it.  A list of doctors who have such training can be found at the Samsha physician locator website.  However, there is wide variation in their experience and understanding in treating addiction.  Each doctor will have his own rules about how often a patient is seen and whether they need to be in counseling.  For most patients who require long-term maintenance, this represents an excellent treatment option

Still, I do have concerns.  The highly tolerant addicts will not have their cravings controlled with this regimen.  The drug will be easier to stop; that will allow more patients to become non-compliant with the medication and they may be more likely to pick up Heroin or their drug of choice.  Also, there is no requirement that a person on buprenorphine maintenance receive counseling.

One of the most common situations I encounter is with people who want maintenance for a period of several months and then undergo detox.  They say they want to detox slowly, but any stabilization at a dose for more than a week or two is in effect maintenance.  The rationale is that they need time to get control of a chaotic lifestyle.  They also need time for some of the drug associations they have developed (i.e. if its Friday night and my friends are partying, than I get cravings on Friday night) to weaken.  These are valid arguments.   

However, If your goal is to completely detoxify, I feel shorter episodes of use are more appropriate.  I have found that the prolonged use of the medication leads to greater degrees of abstinence symptoms compared shorter use.  This is especially true for emotional abstinence symptoms of fatigue, depression and cravings.

One mechanism underlying this emotional withdrawal may be related to kappa receptor activation.  Kappa receptor activity, a subset of opiate activity, serves to cause psychological distress.  Buprenorphine is a kappa receptor antagonist.  While this may be one reason that buprenorphine contributes to a good psychological state, it can be associated with an increase in the concentration of kappa receptors.  Now, when we try to wean off buprenorphine, we may be subject to kappa over-activity and a negative psychological state.

Early studies demonstrated that three days of buprenorphine are as effective as longer treatments.  I have seen very few people who have been on the medication 4 months or more successfully complete a detox.  My own experience suggests that up to 2-4 weeks of buprenorphine is optimal for most patients although some patients will require more time.  This is especially true for persons who have been on Methadone or high-dose delayed-release opiates for chronic pain.

Buprenorphine is also useful for treating pain.  It is particularly useful in persons with a history of substance misuse who need pain medications temporarily after an injury or operation. However, addiction and loss of control can and does occur.  It may prove to be to weak for treatment of severe pain especially since it antagonizes the kappa receptor. 

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