Are you considering your options when it comes to pain relief? If so, you may have heard of buprenorphine. Buprenorphine is an opioid medication used for both the treatment of Opioid Use Disorder and the relief of chronic and severe pain.

In this article, we’ll delve into the specifics of how buprenorphine works in the treatment of pain, and who it may be best suited for.

This guide will cover:

  • Understanding Buprenorphine and how it works
  • Using Buprenorphine for pain
  • The benefits of using buprenorphine for pain
  • Side effects and risks of buprenorphine
  • Who can use buprenorphine for pain.

Let’s get started.

Understanding Buprenorphine: How Does It Work?

To understand how buprenorphine works to relieve pain, let’s take a look at the properties of buprenorphine and how it works in the body.

Buprenorphine is a synthetic opioid, derived from alkaloid compounds of the poppy flower. As buprenorphine is an opioid, it produces effects of opioids such as euphoria, pain relief, sedation, decreased breathing, and other symptoms.

However, buprenorphine is also a partial opioid agonist, meaning that it only partially activates opioid receptors.

As a result, taking higher doses of buprenorphine does not create larger reactions at a certain point. This is referred to as a ‘ceiling effect’.

For this reason, buprenorphine is perceived to be a safer drug than other full opioid agonists, as dangerous side effects such as respiratory depression are unlikely to occur even at high doses.

Using Buprenorphine for Pain

So how does buprenorphine work to alleviate pain?

Once taken, buprenorphine activates mu-opioid receptors in the brain which then release large amounts of dopamine.

This dopamine in the brain then causes the euphoria experienced by the individual. In addition to releasing dopamine, buprenorphine also prevents the release of noradrenaline, which is responsible for increasing focus and stimulation.

Therefore, buprenorphine has the opposite effect of making the individual feel relaxed and sleepy, as well as experiencing a decreased breathing rate.

The two factors together induced euphoria and increased sedation function to create the pain relief effects experienced after taking buprenorphine.

 

The Benefits of Using Buprenorphine for Pain

Now that we understand how buprenorphine works, let’s take a look at some of the benefits associated with using buprenorphine for pain:

Effective pain relief

If you are experiencing severe and chronic pain that is difficult to manage, then buprenorphine may be a great option for you. Buprenorphine is a strong drug that is effective in providing relief for more serious pain.

Lower risk of respiratory depression

Due to buprenorphine being a partial opioid agonist, it produces what is referred to as a ceiling effect.

This means that even if taken at high doses, the risk of dangerous effects is low. One of the main concerns when taking opioids is that there is a risk of respiratory depression and risk of overdose. With buprenorphine, this risk is significantly lowered.

Reduced risk of addiction

In addition to the lowered risk of respiratory depression, the fact that buprenorphine is a partial opioid agonist means that the risk of addiction for the user is greatly reduced.

This is because even at high doses of the drug, effects such as euphoria do not reach significant highs.

As the receptors are only partially activated, the brain is not exposed to the full effects and is less susceptible to opioid dependence as a result.

Longer duration of action compared to some opioids

Another benefit of buprenorphine is that it has a larger duration of effect than many other opioids.

At larger doses, buprenorphine effects may last up to 72 hours. This longer effect is due to the fact that buprenorphine leaves receptors at a slower rate than other opioids.

Can be administered in various forms (tablets, patches, injections)

Buprenorphine treatment can also be administered in a number of different forms.

These include tablets or buccal films taken orally under the tongue or cheek, via patches that are placed on the skin, and extended-release injections which provide long-lasting pain relief.

These different forms of administration are a benefit of the drug as it provides options for patients to suit their specific needs and lifestyles.

Lower abuse potential compared to other opioids

Due to the ceiling effect of buprenorphine, it has a lower abuse potential in comparison to many other opioids.

This is due to the fact that even if taken at a dose higher than prescribed, desired effects such as euphoria and sedation will not be experienced to a large degree.

There is therefore less risk of abuse in prescribing buprenorphine than other opioids such as morphine that do not have this ceiling effect.

Suitable for chronic pain management

An important benefit of buprenorphine is that it is suitable for use in the management of chronic pain patients.

This is due to the drug having a lower level of risk of abuse and opioid overdose compared to other opioid drugs.

Buprenorphine is also easier to stop taking after a longer period of time in terms of withdrawal effects and physical dependence.

Fewer withdrawal symptoms when discontinuing

Due to the fact that buprenorphine is a partial agonist and does not fully activate opioid receptors, there are fewer changes in the brain when administered in comparison to full opioid agonists such as morphine or fentanyl.

This means less physical dependence on the drug. As a result, when the drug is stopped, the individual will experience fewer withdrawal symptoms from buprenorphine than they would from other opioids.

Opioid withdrawal symptoms include things such as cravings, sweating, mood swings, tremors, vomiting, and nausea.

The Side Effects and Risks

Like all drugs, there are potential adverse effects and risks that may occur from taking buprenorphine.

Common side effects associated with buprenorphine include gastrointestinal symptoms such as vomiting, nausea and constipation, difficulty sleeping, loss of appetite, headaches, body aches, and sweats.

More serious adverse effects may include chest pain, difficulty breathing, slowed pulse, dizziness, hallucinations, blurred vision, and signs of liver issues such as jaundice and upper stomach pain.

Seek urgent medical attention in the case of any of these symptoms.

It’s also important to only take the prescribed dose from your physician and to carefully follow the administration instructions.

Who Can Use Buprenorphine for Pain?

Good candidates for buprenorphine for pain relief are individuals who are suffering from severe and chronic pain. If you are only experiencing transient or mild pain then buprenorphine is likely not suitable for you.

Examples of individuals who may be a good candidate for buprenorphine include individuals with chronic cancer pain or other severe illness, or those recovering from a major surgery.

However, it’s essential to discuss your options with your medical provider. They can assist you in finding the best solution to your specific needs.

Conclusion

As we’ve seen, buprenorphine is a powerful synthetic opioid medication that is used in the treatment of patients with more severe and chronic pain.

Due to the ceiling effect of buprenorphine, this makes the drug less inclined to cause dangerous effects such as respiratory depression.

It also makes the drug less susceptible to misuse and well-suited for long-term use in the management of pain.

As buprenorphine is a strong drug it is typically not used for mild or acute pain but is more suited to severe and chronic pain patients.

It’s also important to be aware of the potential adverse effects and risks associated with this drug. Talk to your healthcare provider today if you think buprenorphine treatment may be able to help you.

Sources

  1. https://www.ncbi.nlm.nih.gov/books/NBK459126/
  2. https://psychopharmacologyinstitute.com/section/buprenorphine-for-opioid-use-disorder-mechanism-of-action-2037-4002
  3. https://ophelia.com/blog/brain-on-suboxone
  4. https://www.drugs.com/buprenorphine.html

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