How Does Suboxone Work?

Suboxone (buprenorphine)

Suboxone (active ingredient buprenorphine) is a medication for treatment of opioid addiction. In simple terms, the drug prevents opioid withdrawal symptoms and cravings by replacing the effect of illegal drugs at opioid receptors in the brain. Suboxone does this without causing a high and with a much lower risk of opioid overdose.

How is this possible? To answer this, we need to discuss how opioids interact with the human body.

There are receptors for opioids on the outside of many cells within the human body. These receptors exist to detect hormones that the human body creates naturally (called endorphins), but opioid drugs exploit this system and activate the same receptors. Enorphins are used by the body to calm pain signals, among other functions. These endorphins are responsible for “runner's high” and naturally make people feel good.

Taking an opioid drug triggers these same receptors, which are called mu receptors. Heroin and fentanyl trigger these receptors stronger than natural endorphins and therefore cause strong positive emotions in most people. These strong positive emotions, known as euphoria, are the reason that some people begin to abuse opioid drugs.

Over time, constant triggering of the mu receptors causes the body to make less receptors and to respond less strongly when the receptors are triggered. This results in tolerance to the effects of opioid drugs, which causes people with opioid addiction to require larger amounts of opioid drugs for the same effect as they use for longer periods of time. Prolonged use of opioid drugs also forces the body to make less natural endorphins (as it senses that there is already too many mu receptors triggered).

If a person then stops using opioid drugs or reduces their intake drastically this will create a crisis in the body where there is a less stimulation of mu receptors. This crisis produces the symptoms of opioid withdrawal and will only resolve if the person takes additional opioids or if they wait long enough for their body to create more mu receptors and more natural endorphins.

As it takes the body a long time to create new receptors and turn endorphin production back on, it takes days to weeks for withdrawal symptoms to end. The exact duration of withdrawal symptoms depends on the length of opioid use and the amount of daily use; the longer the use and the higher the daily dose, the longer it will take for the body to reset these systems and the longer withdrawal will last.

Buprenorphine Stimulates Mu Receptors

Buprenorphine (the active ingredient in Suboxone) also stimulates the mu receptors in the body, just like drugs such as morphine, heroin, or fentanyl. For this reason, it prevents the symptoms of withdrawal and opioid craving. In that case, however, why is Suboxone used rather than another opioid drug for treatment of opioid addiction? To answer this question, we must learn more about how mu receptors themselves function.

Mu receptors are present on the outside of certain nerve cells. The receptor is built so that natural endorphins can bind to it. When a molecule of endorphin binds to the mu receptor, it changes the shape of the receptor and this change in shape triggers a reaction inside the cell that ultimately leads to the effects associated with opioid use. Opioid drugs bind at mu receptors similar to natural endorphin.

Effects of Opioid Drugs

To understand the effects of opioid drugs, we must consider two factors.

The first is how strong a certain drug binds to the mu receptor. Some bind stronger than others. Morphine binds well to mu receptors but a drug like fentanyl binds even stronger.

The second is how well the drug activates the mu receptor. Certain drugs bind strongly, but do not change the shape of the receptor and therefore do not have any effect. Narcan (naloxone) is an opioid drug that binds strongly to the mu receptor but does not activate it; think of a blank key that fits into a lock but cannot be turned to open the lock. Narcan can reverse an opioid overdose because it binds stronger to mu receptors than other opioid drugs such as morphine or heroin. When Narcan is injected into the body, it displaces the other opioids from receptors but does not trigger the receptors it binds to and the patient immediately experiences a reversal of the effect of opioids.

Most opioid drugs are classified as “agonists” if they activate mu receptors or “antagonists” if they do not activate mu receptors they bind to. Morphine is an agonist and it produces opioid effects. Narcan is an antagonist and it reverses opioid effects.

Some opioids have an action in-between, however. These drugs have some action when they bind the mu receptor but they do not activate it fully. These drugs are called “partial agonists” and buprenorphine is one such partial agonist drug. If a full agonist is the key that opens a lock and an antagonist is an uncut blank key that does not turn the lock, then think of a partial agonist as a bump key that can open the lock if you jiggle it.

Even though buprenorphine only partially activates the mu receptors, it binds much more strongly than most others. For this reason, it blocks the action of other opioid drugs which do not bind as strongly and can displace those drugs from mu receptors.

In most adults, buprenorphine does not activate the mu receptors enough to cause an opioid overdose. Since buprenorphine blocks other full agonist opioid drugs from binding, it prevents overdose. Unfortunately, this mechanism can also create sudden withdrawal symptoms when buprenorphine is taken by a patient who has other full agonist opioids in their system. This is called “precipitated withdrawal” and it occurs when a person goes from their mu receptors fully activated to a much lower state of activation.

Precipitated withdrawal can be avoided if the patient delays their first dose of Suboxone until after they are experiencing mild to moderate withdrawal symptoms and after at least 12 hours from their last dose of short acting opioid and at least 48 hours from their last dose of long-acting opioids. The procedure of transitioning from opioids of abuse to Suboxone is known as “induction.”

Once a patient has completed induction and is on a stable dose of Suboxone they take a regular dose once or twice daily. This is possible because Suboxone is a long acting opioid that can suppress withdrawal symptoms and cravings for up to 24 hours. Patients typically remain on Suboxone for months if not years as a daily medication for treatment of their opioid use disorder. If the patient remains stable and feels ready to stop taking Suboxone, they can slowly taper off by gradually reducing their daily dose over a period of 3-6 months in order to reduce opioid withdrawal symptoms. However, many patients keep taking Suboxone indefinitely as it is so effective in treating their addiction.

If you or someone you love is suffering from problematic drug or alcohol addiction use and is seeking treatment, contact the clinic by calling or clicking the “Get Started” button in order to schedule a discovery call and initial evaluation, both of which are free.

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North Tampa Executive Health Clinic is directed by Dr. Jack McGeachy. He provides confidential and comfortable addiction treatments and therapy for opioid and alcohol use disorder. Rather than a rehab or detox, meaning that each patient is cared for one-on-one by a medical doctor, in contrast to other treatment programs. Heed Help? Book your in office appointment in the Tampa office or via video conferencing today.

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