How Suboxone Works

Morphine was first isolated from opium in 1805 by a German pharmacist, Wilhelm Serturner (1783-1841).  Serturner described it as the Principium Somniferum.  He named it morphium - after Morpheus, the Greek God of Dreams. 

Buprenorphine as a medication,and the circumstances under which it can be used, together provide a new means to treat opioid addiction in the United States.  Buprenorphine's usefulness stems from its unique pharmacological and safety profile, which encourages treatment adherence, and reduces the possibilities for both abuse and overdose.

Because buprenorphine has unusual pharmacological properties, physicians may want to consult with addiction specialists to understand more fully the partial opioid agonist effects of buprenorphine and how these properties are useful in opioid addiction treatment.

Although buprenorphine offers special advantages to many patients, it is not for everyone.  Care must be taken to assess each patient fully and to develop a realistic treatment plan for each patient accepted for buprenorphine treatment.

How Suboxone Works 

1.  When opioids attach to the mu receptors, dopamine is released, causing  pleasurable feelings to be produced.

2.  As opioids leave the receptors, pleasurable feelings fade and withdrawal symptoms (and possibly cravings) begin.

3.  Opioids continue leaving the mu receptors until a person is in a mild-to-moderate state of  withdrawal .  At this point, SUBOXONE therapy can begin.

4.  The primary active ingredient in SUBOXONE-buprenorphine-attaches to the empty opioid receptors, suppressing withdrawal symptoms and reducing cravings. 

            

5. Buprenorphine attaches firmly to the receptors.  At adequate  maintenance, buprenorphine fills most receptors and blocks other opioids from attaching.  Buprenorphine has a long duration of action, so its effects do not work off so quickly.

References: (1) Johnson RE. Strain EC. Amass L. Buprenorphine:how to use it right. Drug Alcohol Dependence 2003; 70(suppl 2) S59-S77. (2) Walsh SL. Eissenberg T. The clinical pharmacology of buprenorphine; extrapolating from the laboratory to the clinic. Drug Alcohol Dependence 2003; 70(suppl 2) S13-S27

 

The Opiate Receptor System and Opiate Dependence

Visualize a rectangular green meadow about the size of a football field with, thick grass and soft earth.  This represents an area of the brain in which the morphine  (also known as opiate or narcotic) receptors are found.  The meadow is mildy sloped with the left side being higher.  At the left edge there is a box about the size of a hockey goal.  This is the endorphin factory from which a steady stream of low weight green slippery bowling balls (the endorphins in this example) is emerging.  Endorphins are natural compounds which we all produce.  They act as the body's own morphine and pain killer and fill the same receptor sites that narcotic drugs stimulate.
  stimulate. stimulate
.

There are bowling size indentations in the meadow which are the sites of the morphine receptors.  We all need a significant percentage of these holes (receptor sites) to be filled to be comfortable.  Since the balls are low in weight they do not cause their own new indentations and because they are slippery they do not stay in the indentations for long before they slide out of the holes and then off the right edge of the meadow.

There are no sensors under the meadow, which measure the weight and number of balls on the meadow and how many of the receptor site holes are filled. When they are more balls the sensors slow down the production and release of the green endorphin balls and visa versa, thereby maintaining the number of receptor sites containing balls.

Under normal circumstances, if there is pain, there is an increase in endorphin production. There is also an increase in production with exercise and pleasure or with pain.  When many receptor sites are filled, one may fill a "natural high." 

If one person is given or takes an opiate drug, such as heroin, morphine, methadone, oxycodone (Oxycontin), hydrocodone (Vicodin), hydromorphone (Dilaudid), or fentanyl (Duragesic) a large number of heavy black slippery bowling balls is released on the left edge of the meadow. (Visualize a dump truck which dumps its load at the left edge of the meadow.)These cover almost all the receptor sites holes. 

This fights the pain and can give the high associated with drug use. Because they are so heavy they stop endorphin production  and the factory at the left edge of the meadow becomes dormant. In addition because they are so heavy they make new holes, which now have to be filled for the person to stay out of drug withdrawal. If drug use persists the factory is "dismantled" and can lose its ability to produce any green balls. It may take a very long period of time for it to regenerate and in some cases it may never be able to function at its former level.

If the supply of "black balls"stops the now increased number of receptor sites rapidly become bare and the person starts  to feel the symptoms of opiate withdrawal .  (Remember  that not only does there have to be enough balls on the meadow, but there also must be a signficant percentage of the holes filled as well to be comfortable.)  These include muscle and joint aches , tremors, nausea, diarrhea, sweating, severe anxiety and insomnia.  This sensation is very painful and most people will do almost anything to stop it...This is why addicts will steal, prostitute themselves, or even kill to get their "fix."

Eventually since there are no longer heavy black balls on the meadow's surface the grass can regrow and the top soil can reaccumulate.  The new holes will shrink and the number of holes that need to be filled for comfort will decrease. The endorphin factory will start producing green balls again and the system will get back into balance.This process usually takes a few days to at least start to normalize, but it may take weeks to fully stabilize.  Sometimes, however, this may take quite a bit longer and as stated above, for some individuals it may never be normal again. 

It may be possible to gradually reduce the opiate dose and allow a slow return to normalcy, but for many,  this is very uncomfortable or even unbearable. There are also those who either will never be able to produce the amount of endorphins they need to be comfortable or in whom the number of receptors is chronically increased.  Many of these persons will become drug seekers or will go back to using opiates with any stress, either physical or emotional.  Stress or pain potentiates the opiate receptors, causing them to require increased stimulation for the person to be comfortable.

Stress or pain potentiates the opiate receptors, causing them to require increased stimulation for the person to be comfortable. What does this mean to you?  If you are addicted, you need to try and remove any stress from your life. We all understand there is stress that cannot be removed and we must learn how to deal without letting it upset us. There is a lot of stress we can eliminate from our lives. If you understand what the above paragrap is saying, then you understand, it will take more medication to make you comfortable, depending upon the amount of stress you have in your life.  

If you have physical pain from an injury/or illness then it will increase the amount of medication you need.  If your pain is severe, then you should consult your physician. I have no doubt some of you are aware of the problem that exists if you are presently taking medication to curb your craving and withdrawal symptoms. If you are unaware then let me share the dilemma you will find yourself in.

 We have very few physicians educated enough in "Addiction" to realize that you need extra medication for pain.   You may need to locate the material on the Internet and print it out for your physician and try and educate Him /Her yourself. You may not succeed at this but it is important we try and educate as many physicians as we can.  I am asking you to try and attempt to educate your physician.  Be persistent and stay calm and just insist He read the material.

If you cannot persuade them,then you must try and find another physician. Sometimes it can be very difficult and many of us suffer with our pain, as do many of us needing a dose increase and cannot obtain it because of our physician's lack of knowledge or if we are taking methadone, because of their refusal to obey Federal Regulations. We must not give up and continue to fight for our rights.  I am here to inform you of your rights and tell you, we are discriminated against more than any group of people. If we want change then we must join together and demand it.  We must take a stand!  

We are here to educate you about "Addiction." We are here to educate you about what is available to you. There are medications available to you that will take away the craving and withdrawal symptoms. If these are the reason you are unable to stop using then you have no excuse.  They do work and I am here to educate you about them and help you locate what is right for you.

Buprenorphine

Buprenorphine is termed a partial agonist (stimulator) for the opiate receptor.  The opiates themselves are full agonists. This means they stimulate the receptor and fully occupy the receptor area.  The more that one takes, the more the receptor is stimulated, the stronger the drug effect and the more "holes" are created. on

A partial agonist occupies the receptor site, but only partially stimulates it. After a certain amount of buprenorphine is present adding more makes no difference and therefore taking more has no additional effect. This is called a "ceiling effect."  Buprenorphine eliminates the withdrawal sensations and treats pain, but only to a certain extent.

Picture light weight sticky blue bowling balls that fill the holes and eliminate the withdrawal symptoms.  Since they are sticky, they stay in the receptor holes  and therefore  the effect is long lasting.  Once a blue ball occupies the hole,  a dose of an opiate (black balls ) is blocked from getting into the receptor, thereby blocking  the action of any opiate that the person might take while on buprenorphine.  

If they are heavy black balls in the receptor holes, the blue sticky buprenorphine balls can displace them and since the blue balls are only partial agonists, they can induce drug withdrawal. This is why it is so important that starting buprenorphine be timed correctly.  This is why the first dose is always taken in the physician office so that any side effects can be handled correctly and safely.  The first dose should be taken just as withdrawal starts; too early and acute withdrawal can be induced, too late causes needless suffering. 

Since the blue balls are ligher in weight than the black balls, the meadow can slowly regenerate, although this is still a slow process. Since the blue balls stick in the receptors and "cover" the receptor holes drug craving is either markedly reduced or in most cases eliminated.

The buprenorphine dose can slowly be reduced, but as I noted earlier, there are many   individuals who will never completely regenerate their ability to make endorphins and whom the meadow is perpetually scarred (the holes do not disappear). For them it may be necessary to continue treatment indefintely.

Suboxone

Buprenorphine is used to treat opiate addicted persons who have the potential to relapse into drug abuse and addictive behavior. Many of these patients have been long time drug abusers.  A common method of "getting high" is to crush, dissolve and then inject an oral medication.  Suboxone  contains  buprenorphine  and naloxone, a  very   strong   opiate
antagonist. An antagonist is a medication which fits in to a receptor but which does not stimulate the  receptor  action. 
  It
blocks the ability of the agonist to enter and then stimulate the receptor. This blockades the usual action of the drug.  In this case it prevents an opiate from stimulating the opiate receptor.

If a person is currently taking opiates the antagonist can displace the narcotic  and by blocking its action it can precipitate withdrawal. Naloxone is not absorbed orally and therefore does not interfere with buprenorphine action when taken through the usual sublingual route. If it is injected, however, it blocks any opiate or buprenorphine effect. This dramatically decreases the risk of abuse.

Reference: (1) Richard I. Gracer, M.D. San Ramon, CA 94583 
                Mechanism of Buprenorphine

Gracer Medical Group
5401 Norris Canyon Rd. Ste. 102
San Ramon, California 94583
Phone (925) 277-1100   Facsimile (925) 277-1263  

 
Deborah Shrira,Editor                    Date: February 2007