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Suboxone and Subutex – How Are They Used? Part Two
THREE TYPES OF OPIOID DRUG–RECEPTOR INTERACTIONS
Not all opioids are the same. There are three types of opioids that are classified by the effect that they have on the endorphin receptors. They are the full agonist, the partial agonist and the antagonist.
As used here, an agonist is something that stimulates or produces an effect. Agonist is derived from the Late Latin agnista which means contender, which is derived from the Greek agonists which also means contestant which came from agon meaning contest. An agonist is a chemical contestant or contender.
Full agonists are drugs that bind to endorphin receptors in the brain and cause them to produce endorphins which give analgesic (pain) relief and, depending on the dose and frequency, addictive effects and feelings of euphoria. Unless an individual’s metabolism and DNA prevent it, the larger the dose of a full agonist, the more receptors are activated and the larger the effects. Examples of full agonists are oxycodone, methadone, codeine, heroin and morphine.
Partial agonists are drugs that bind primarily to endorphin opioid receptors and cause them to produce endorphins but to a much lesser extent than full agonists. Buprenorphine, Suboxone and Subutex are partial agonists. When the dosage of a full agonist is increased, the opioids will activate more receptors and create more endorphins. When the dosage of a partial agonist is increased, there is only a small increase, if any, in the production of endorphins.
COMPARING EFFECTS OF FULL AGONIST AND PARTIAL AGONIST
One way of viewing the difference between a full agonist and a partial agonist is to compare it to the operation of an elevator that requires a code that must be entered for someone to use the elevator to reach a specific floor.
Each time a person takes a full agonist it contains a code, unless significantly modified by the DNA and the way the full agonist is metabolized, which will allow the elevator to reach a certain floor. In low doses, the elevator code (number of endorphins created) may only allow the elevator to reach the second floor. However, as the full agonist dosage increases, the elevator code can now rise to higher floors and eventually to the tenth floor.
A partial agonist, like buprenorphine, will only stimulate the receptors to produce a certain amount of endorphins. Using our elevator example, when an individual takes a partial agonist in small doses it may contain a code that allows the elevator to rise to the second floor. However, no matter how much the dosage of the partial agonist increases, the code in the partial agonist will not allow the elevator to rise above the fourth floor.
This is why it is much harder to abuse a partial agonist than a full agonist, but this is also why a partial agonist like burprenorphine is very helpful as we medically detox someone from opioids.
For our purposes here, an antagonist is something that blocks an effect. Antagonist is derived from antagonize which is derived from the Greek antagonizesthal which means to struggle against, which is derived from agonizesthal which means to struggle which is derived from agon (contest).
Antagonists are drugs that bind to the same endorphin receptors but don’t stimulate the production of endorphins. What they do is occupy the receptors and prevent the receptors from being stimulated and reduce the amount of endorphins being created. This is why someone who is taking oxycodone (the active ingredient in OxyContin) to stimulate endorphin production can go into withdrawal if they take an antagonist. The antagonist blocks the receptors and does not allow the oxycodone to stimulate the receptors to produce endorphins. Naloxone and naltrexone are antagonists.
Antagonists are used in emergency rooms to try to counteract the effects of opioid overdose by causing the receptors to immediately give up the opioids.
HOW PARTIAL AGONISTS CAN TRIGGER WITHDRAWAL
Many of our patients have heard, or even experienced, taking a partial agonist like buprenorphine and immediately going into withdrawal and getting very sick.
The answer is simple. Endorphin receptors prefer buprenorphine to other full agonist opioids. When you take buprenorphine, it goes to the receptors and literally kicks out any other full agonists that were there and still activating the receptors, and then it effectively seals that receptor off and will commence to partially activate it to produce endorphins but at a much lower level.
This lowering of endorphin production continues longer because Suboxone is slower- acting than many other opioids and stays on the receptor for a longer period of time.
Using our elevator analogy, if the full agonist was still stimulating some of the receptors before the introduction of the partial agonist and causing our elevator to rise to the eighth floor, buprenorphine evicts the full agonist but only produces enough endorphins for the elevator to go to the fourth floor. This is like suddenly being dropped from the eighth floor to the fourth floor. It isn’t as bad as being dropped all the way to the first floor, but the person is going to get very sick as the body reacts to the sudden lowering of the amount of endorphins available—similar to trying to withdraw at home from opioids by just not taking them.
PREVENTING SEVERE WITHDRAWAL FROM BUPRENORPHINE
At Novus Medical Detox Center, we have a medical protocol that we follow to ensure that our patients don’t experience the precipitated withdrawal that is a problem with taking buprenorphine too early. Using vital signs, observation of the person in front of them and communication with the patient, our patients receive buprenorphine only when it is going to help them with their medical detox and not make them sick.
SUBOXONE AND SUBUTEX
Suboxone and Subutex are manufactured by Reckitt Benckiser Pharmaceuticals, Inc. These opioid drugs were approved by the Food and Drug Administration in 2002. Only doctors approved by the Substance Abuse and Mental Health Services Administration, a department in the United States Department of Health and Human Services, are allowed to dispense Suboxone and Subutex in medical detox facilities or for outpatient Suboxone maintenance.
Suboxone contains buprenorphine, a partial agonist, and naloxone, an antagonist. The proportion is four parts of buprenorphine and one part naloxone. Suboxone comes in two dosage forms: two milligrams buprenorphine and 0.5 milligrams of naloxone and eight milligrams of buprenorphine and two milligrams of naloxone.
WHY COMBINE A PARTIAL AGONIST AND AN ANTAGONIST?
When people learn that Suboxone contains an antagonist, there is a reluctance to take something that could throw them into withdrawal. The naloxone is included in the Suboxone to prevent it from being crushed and snorted or injected.
The reason is bioavailability. Bioavailability is a term used to define how effectively a drug can be absorbed and used by the body. Buprenorphine has poor bioavailability if just swallowed and moderate bioavailability if placed under the tongue (sublingual) and allowed to dissolve. What this means is that normally a person will get the effects of approximately 40-60% of the buprenorphine when taken sublingually and allowed to dissolve but this will activate, partially, the endorphin producing receptors and provide the extra stimulation needed to make the withdrawal more comfortable. If administered sublingually, naloxone has low bioavailability and the person will receive only about 10% of the drug. This means that a person taking Suboxone sublingually will receive mostly the effects of the partial agonist and very little of the antagonist.
On the other hand, if Suboxone is crushed and injected into the bloodstream, the effect of the buprenorphine will be increased but only by about twice as much as if it were taken sublingually. However, the effect of the naloxone will be increased by 15 times and will dominate. The naloxone will bind to the receptors and block the buprenorphine from activating the receptors and this will precipitate the painful withdrawal which can occur if Suboxone is misused.
Subutex contains just buprenorphine. In order for it to be effective, It is taken sublingually like Suboxone. Subutex is often used in some of our medical protocols for a short time if someone has been taking heavy doses of opioids. Then the person completes their medical detox using Suboxone.
It is important also to remember that one of the reasons that buprenorphine is so effective in medical detox is that it has a half-life (the time it takes forhalf of a drug to leave the body) of between 24–60 hours. Opioids are generally classified as Schedule II drugs, but because they have less ability to be abused, Suboxone and Subutex are classified as Schedule III drugs.
We believe that our patients are among the bravest people in society. They come to Novus Medical Detox Center fully expecting that they will have to endure discomfort or pain. They don’t really know how they will feel at the end of their withdrawal but, as John Wayne said, they saddle up anyway. They come because they have concluded that being drug-free is worth it. They come because they want to be there for their spouse or child. They come because it is the right thing to do. We are proud that we are able to help these brave people and love to see the butterfly that emerges from the cocoon woven by drug use. It is even better that this transformation doesn’t take months but literally seven to fourteen days and with far less discomfort that the patients ever dreamed.
If you know of anyone who is ready to be free of drugs or alcohol, please have them look at our website or contact us directly. Remember, each person that we help get free from drugs is literally a new person with unlimited potential to help others.
NOTE: This information is provided for general educational purposes only and is not intended to constitute (i) medical advice or counseling, (ii) the practice of medicine, health care diagnosis or treatment, or (iii) the creation of a physician patient or clinical relationship. If you have or suspect that you have a medical problem or that this information may be useful to you or others, please consult with your health care provider before applying any information from our articles to your personal situation or to the personal situation of others.
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