John Wayne once said, “Courage is being scared to death and saddling up anyway.” - Novusdetox

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John Wayne once said, “Courage is being scared to death and saddling up anyway.”

There are few things that can make one scared than being trapped by drugs or alcohol. Many of our Novus Medical Detox Center patients come to us because they want help escaping from this horrible trap. In almost every case, our patients have tried to detox on their own. In almost every case, they were unsuccessful because of the pain and severe discomfort they experienced and resumed taking the drug or drinking alcohol.

What type of discomfort? Probably the best description we have heard from our patients is that it is like the worst case of the flu they’ve ever had but ten times worse than that. Chills, sweating, diarrhea, vomiting, fever, cramps, insomnia, and the list goes on and on. You don’t feel like eating or drinking and as you become more dehydrated the discomfort increases. Some people have told us about this state continuing for weeks and not being able to sleep more than a hour at a time and seldom more than a total of a couple of hours a day.

It is frightening to decide that you are going to do something even if there is the type of discomfort described above associated with it. Logically, someone else’s experience may not be their experience. I think it is true that all of us believe that minor surgery is somebody else’s surgery because any surgery on you is major surgery. This is the same perception felt by most of our patient about withdrawing from drugs at a medical detox facility—no matter what other people experienced.

Quite often the concern of our patients about the discomfort they will feel while detoxing from opioids like OxyContin, methadone, heroin, Vicodin or Percocet is increased when they learn that we use buprenorphine in our protocol. Why? They have heard, or in some cases personally experienced, a bad reaction after taking Suboxone or Subutex–two drugs whose principal ingredient is buprenorphine.

We tell them that our patients uniformly don’t have bad reactions to Suboxone. Then our nurses and counselors explain why and, like in all other aspects of their lives, once they understand the way buprenorphine should be and is used at Novus Medical Detox Center, they relax a bit. However, until they actually see the process work on them—they are still skeptical. Again, what may work for someone else may not work for them.

The purpose of this page is to explain how buprenorphine works and why, in the hands of skilled medical personnel, it is a powerful tool to reduce the discomfort of opioid withdrawal.

ENDORPHINS, ENDOPHIN DOWNLOADS AND OPIOID DRUGS

Before understanding how buprenorphine works, it is necessary to understand the way that opioids (OxyContin, methadone and Vicodin) primarily work in our bodies. Opioids activate receptors in the brain that increase endorphin production.

DEFINE ENDORPHINS

Endorphins are protein molecules that bind with receptors located in your brain, spinal cord, and other nerve endings. Simply put, endorphins block pain signals from reaching the brain. Were it not for endorphins, many of the normal acts of life—breathing, walking, talking–would be uncomfortable or even painful.

The body naturally produces endorphins by sending chemicals to activate endorphin- producing receptors. For our normal activities, the body normally does a good job of keeping us from feeling pain. However, if we experience unusual pain, like from a bad fall, the body may not create enough endorphins to block the pain signals and we will feel the pain. If at that time we were to take an opioid, the drug would activate endorphin-producing receptors and block the pain signals by increasing the endorphin production in the body.

Taking one or two of these pills to block the pain signals while the body is healing is not going to create dependence or addiction. You are still taking drugs that disrupt your body’s normal functions, but much more serious problems can and do arise when the pain blockers are taken for longer periods of time which can lead to dependence or addiction.

ENDORPHIN DOWNLOADS

When the person feels more pain than the body can handle with natural endorphin production, endorphin downloads are accomplished by taking an opioid like OxyContin, Vicodin, oxycodone, Lortab, Lorcet, Percocet and methadone. These drugs accomplish the endorphin download by activating endorphin-producing receptors and the resulting endorphins block the pain signals by increasing the endorphin production in the body.

Taking one or two of these pills to block the pain signals while the body is healing is not going to create dependence or addiction. You are still taking drugs that disrupt your body’s normal functions, but much more serious problems can and do arise when the pain blockers are taken for longer periods of time which can lead to dependence or addiction.

DEPENDENCE AND ADDICTION

There is a great deal of confusion about the difference between dependence and addiction. You are said to be dependent on any substance from which you experience uncomfortable symptoms when you stop taking the substance.

It doesn’t have to be an opioid like OxyContin or methadone to create dependence. Many of us have become dependent on sugar or caffeine. When we tried to stop eating sugar or drinking coffee or caffeinated beverages, we experienced uncomfortable symptoms—headaches, cramps or others, for example.

However, for the person becoming dependent on opioids, the withdrawal symptoms can be much more uncomfortable and can continue for longer periods of time. In fact, many people who have become dependent on these drugs no longer take them because they need them to block pain signals but because they don’t want to go through the painful withdrawal that will occur when they stop taking the drug.

Addiction is the condition where a person will modify their behavior and even do destructive things to satisfy the craving created by a drug. They may have originally taken the drug to block pain signals but they continued taking the drug because it allowed them to “feel” a certain way or avoid feeling a certain way. People who become addicted to these drugs are also dependent on the drugs and will experience not only the pain of withdrawal but also the emotional pain of no longer having the drug modify the way they feel.

HOW DO THESE DRUGS CREATE DEPENDENCY AND ADDICTION?

Our bodies are incredibly sophisticated at doing things for us. If the body senses that a particular chemical is needed, unless there is some structural problem, it will try to produce the chemical. If someone is using a chemical, like OxyContin for example, to download endorphins by stimulating endorphin activity, their brain senses that it doesn’t need to produce the natural chemicals to make endorphins. The brain decreases its own endorphin production and relies on the drugs.

You need endorphins to keep from getting very sick—the worst flu only ten times worse. If the brain is not creating endorphins but relying on the opioid, then if you stop taking the opioids you will not have enough endorphin production and will get very sick.

PAIN HAS A PURPOSE

Like all sensations in our body, such as thirst or hunger for example, pain serves a useful purpose for us. (This is extensively discussed in our earlier newsletter about Pain.) Pain is used by the body to indicate that there is a problem that needs to be handled.

We have had a number of patients come to Novus to detox from opioids who began to experience a toothache as they were withdrawing. The toothache got worse and we took them to a dentist. What the dentist found was that they needed not just a cavity filled, but the decay had progressed to the point where a root canal or even an extraction was required. The opioids had flooded the brain with endorphins and prevented the early signs of tooth decay from reaching the brain. Had they not been on the opioids, they would have felt the pain, gone to the dentist and had the cavity filled.

Other patients on opioids relate how they permanently damaged their backs because they were working in construction and lifted too much. Without the opioids, when you lift too much you will feel the pain or discomfort in your back and know that you need to stop. However, because of the opioids the pain warnings never reached the brain so they just kept hurting their backs until the damage was irreversible.

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.

FULL ENDORPHIN AGONIST

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

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.

ANTAGONISTS

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.

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. (Frank, moved this here from below.)

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. They believe that this is Suboxone withdrawal but it is not. It is withdrawal caused by taking Suboxone too soon.

The answer is simple. Endorphin receptors prefer buprenorphine, the opioid in Suboxone, 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 and this creates the symptoms of withdrawal.

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 (SUBOXONE)

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.

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.

HALF-LIFE OF SUBOXONE AND SUBUTEX

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 for half 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.

SUBOXONE SIDE EFFECTS

According to its label, Suboxone has the following side effects:

  • Chills
  • Headache
  • Anxiety
  • Depression
  • Dizziness
  • Weakness
  • Constipation
  • Diarrhea
  • Nausea
  • Vomiting
  • Insomnia
  • Runny Nose

SUBOXONE WITHDRAWAL

While the use of Suboxone to assist in the detox and withdrawal from other opioids and opiates is beneficial to many. Done properly at a medical detox like Novus Medical Detox Center, Suboxone withdrawal is normally very easy.

However, Suboxone is an opioid and people can become both dependent and addicted to it. Withdrawal from Suboxone is similar to withdrawal from other opioids and can be very uncomfortable if not not properly. Some of the Suboxone withdrawal symptoms are:

  • Anxiety
  • Increased Respiratory Rate
  • Crying
  • Yawning
  • Goose bumps
  • Irritability
  • Dilated Pupils
  • Extreme Restlessness
  • Insomnia
  • Nausea
  • Vomiting
  • Diarrhea
  • Rapid Heartbeat
  • Cramps
  • High Blood Pressure
  • Aches
  • Tremors

There is hope for a new life. Call to speak to one of our experienced & caring detox advisors today!

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