How Is Suboxone An Agonist and Antagonist Of The Opioid Receptor?

What is an agonist?

By definition, an agonist activates a receptor on the surface of a cell in the body, causing a physiological response. There are many different types of receptors. Each of these receptor types has a particular molecule, an agonist, that can activate it, like a key in a lock.

What is an antagonist?

An antagonist is a molecule that can bind to a receptor, but it does not activate it. It is like when you put the wrong key in a lock, and it fits, but cannot turn to open the lock.

A drug antagonist also blocks access to the receptor by other drug molecules. As long as the antagonist occupies the receptor, agonist molecules are prevented from binding and activating it.

What is Suboxone film?

Suboxone is available as a sublingual film or a sublingual tablet. In the United States, it is one of a limited set of medications that doctors can prescribe for opioid addiction.

Does Suboxone contain an antagonist drug and an agonist drug?

Suboxone’s ingredients can be a minor point of confusion. Suboxone contains buprenorphine /naloxone. Naloxone is an opioid receptor antagonist.

The naloxone in Suboxone is there as an abuse-deterrent. When a patient takes Suboxone correctly, the naloxone is minimally absorbed and does not affect the patient.

If a patient attempts to abuse Suboxone and inject it with a syringe and needle, seeking a buprenorphine high, the naloxone will make that patient feel sick. Most patients do not abuse Suboxone, so they do not ever feel the effects of the naloxone ingredient.

What is buprenorphine?

The other ingredient of Suboxone is buprenorphine. Buprenorphine is the drug in Suboxone that treats opiate addiction. Buprenorphine is both agonist and antagonist.

What is a partial agonist?

Remember that an agonist is a molecule that activates a receptor. When an agonist works on a receptor, it is like a finger pushing down on a button. What if the finger only pushes the button half-way down?

While this is an imperfect analogy, this is one way to think of a partial agonist. It activates the receptor, but only partially, like pushing the button down just a little. A partial agonist causes only a partial response.

Buprenorphine is a partial agonist and antagonist.

The fact that buprenorphine activates the opioid receptor at all puts it in the category of opioids. Yet, it only causes a partial activation. Buprenorphine is a partial opioid agonist.

The fact that buprenorphine is also an opioid antagonist is what makes it so fascinating. Buprenorphine happens to be a potent antagonist. It is not only a partial receptor activator but a blocker as well.

When it binds to an opioid receptor, it stays on the receptor, blocking agonist molecules, opioids, and endorphins, from binding and activating the receptor. Scientists believe that it is such a potent blocker, that it never comes off the receptor.

Receptors in the body do not last forever. There is constant turnover. The cell generates new receptors, and old ones are degraded and reabsorbed. An opioid receptor has a life span of about 72 hours.

Imagine buprenorphine latching on to a receptor and blocking it for the remainder of its short existence. During that time, it blocks opioids from binding, and it also continuously, partially activates the receptor.

If buprenorphine is an opioid, is Suboxone addiction a problem?

Suboxone addiction is rare compared to other types of drug abuse. Suboxone helps a patient to stop thinking in an addictive manner. It is part of a long-term treatment plan for opioid addiction.

Patients may develop a physical dependence on treatment medication. Dependence is not the same as addiction.

Physical dependence means that the patient may experience a withdrawal syndrome if they stop taking Suboxone suddenly against medical advice.

The reason that Suboxone is not addicting for most patients is because of the unique mechanism of action. It is because it is an agonist and antagonist.

Subutex vs. Suboxone: What is the difference?

These two drugs are nearly identical in that they both contain buprenorphine as the active ingredient. The difference is that Suboxone also contains naloxone as an abuse-deterrent.

Patients sometimes believe that Subutex works differently from Suboxone because it does not have the “blocker.” The fact is that, for most patients, there is no difference at all because naloxone does not have any significant effect when taking Suboxone as directed.

How do opioids work?

An opioid is a drug that is related to one of the active components of opium. There are opiates, synthetic opioids, and semi-synthetic opioids.

These drugs are agonists of the opioid receptors. When opioids activate opioid receptors in the central nervous system, the patient experiences pain relief and possibly euphoria.

There are also possible side effects. For example, constipation is a significant side effect due to opioid receptor activity in the intestines.

How long does Suboxone last?

While Suboxone has a half-life of nearly 40 hours, the length of its effects vary. Suboxone helps patients by blocking opioid cravings and withdrawal symptoms.

If a patient takes Suboxone once daily, it will prevent opioid withdrawal symptoms for at least 24 hours. However, it may not block cravings adequately for that same period.

To correct this issue, doctors may adjust the dosage, split it into twice-daily dosing, or convert the patient to a monthly subcutaneous buprenorphine injection. On the other hand, as a patient completes their MAT program, the doctor may prescribe alternate-day dosing. To answer the question about how long buprenorphine lasts, it depends on the patient and their treatment.

What is a typical Suboxone dosage?

The most commonly used dosage is 8mg/2mg. What this means is that it contains 8mg of buprenorphine and 2mg of naloxone. Patients take Suboxone by placing it under their tongue to dissolve.

Interestingly, the patient does not absorb the full 8mg of buprenorphine. Experts estimate that about one-third of the drug dosage absorbs under the tongue.

What about methadone vs. Suboxone? Is methadone an opiate?

Methadone is not a partial agonist like buprenorphine; it is a very potent agonist. Methadone is a much more dangerous opioid treatment medication compared to Suboxone.

That’s why patients on methadone have to go to the clinic every day to take their dose. It’s too dangerous to send them home with a bottle of methadone pills.

Methadone vs. buprenorphine: Which is safer?

A stated above; methadone is a dangerous drug. Buprenorphine is not nearly as dangerous. It is safer because it has a ceiling effect.

If a patient takes too much buprenorphine, it is rare to overdose on it. Buprenorphine has a protective ceiling effect. However, it is possible to overdose on buprenorphine in some cases, especially when combined with other drugs.

Suboxone and methadone are both effective treatment drugs, but methadone is more likely to lead to life-threatening breathing problems if a patient accidentally takes too much.

Why does buprenorphine have the ceiling effect?

Again, this is an advantage of the unique nature of the buprenorphine molecule and its effects on the human body. It is because buprenorphine is both an agonist and antagonist.

How can I start Suboxone treatment?

First, you must see a doctor who is certified to prescribe Suboxone as part of a medication-assisted treatment program. Talk to your doctor to see if Suboxone medication-assisted treatment is right for you.

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