Suboxone is made up of buprenorphine and naloxone. Buprenorphine is the parent compound in Suboxone. Buprenorphine was originally discovered as a synthetic pain medication and was first used in the vein (IV) in the 1960s to treat pain related to cardiac arrest. Today buprenorphine is used to treat pain as well as opioid addiction and opioid use disorder (OUD). The dynamism of buprenorphine lies in its ability to provide pain relief akin to morphine without the risk of resulting side effects such as respiratory depression. Its analgesic properties are unique; buprenorphine provides relief from chronic pain as well as pain associated with the use of opioids, i.e., nausea, constipation, vomiting, etc. Importantly, different brand name versions of buprenorphine correspond to these different uses.

In 2002 buprenorphine was approved as an office-based treatment for OUD. Initially the medication had to be administered under direct medical observation, but now home induction is common.

The presence of naloxone in Suboxone acts to block stimulation of the brain’s opiate receptors if the drug is injected or misused, preventing diversion of the medication. Naloxone is absorbed negligibly from the gastrointestinal tract when absorbed sublingually (under the tongue). If the combination medicine is injected, the full hindering effect of naloxone is released, this stops the opioid effect of the buprenorphine.

What does Suboxone do to Your Brain?

Suboxone works in the brain to combat the effects of full opioid agonist consumption. Opioids such as heroin, oxycodone, and fentanyl function in the brain to alter how a person feels and responds to pain. See Suboxone Ingredients: All You Need to Know for more on the effects of full opioid agonists.

Opioids fundamentally target and block your body’s pain receptors to alleviate pain; however, the body builds tolerance over time, and more and more opioid is needed to manage the same quantities of pain. As a result, opioid doses escalate, tolerance builds, addiction ensues, and the risk of overdose increases. While buprenorphine is also an opioid, it is a partial opioid agonist that possesses a ‘ceiling effect.’ Meaning buprenorphine does not necessitate dosage escalation and does not build tolerance.

This combined with Suboxone’s sublingual delivery system controls the distribution of the opioid in the body to avert full opioid cause and effect. If the drug is injected, a full opioid effect is established. This is when the naloxone will activate to antagonize the buprenorphine, as discussed in the paragraph above, meaning there is no opioid effect and instead this may cause withdrawal.

Suboxone Pain Management

Suboxone is not approved for the treatment of pain. Buprenorphine, which is the active ingredient in Suboxone, can be used to treat pain in other formulations. 

The brain has two pain corridors: pain and the perception of pain. The perception of pain is the belief that you have more pain than you do. The more opioids you consume, the further desensitized these pathways of pain become. This is the hyperalgesia side effect of opiates. Hyperalgesia occurs as a result of the chemical changes to the nerves linked with pain detection. 

Suboxone does not occupy these pathways; therefore, the perception of pain does not become desensitized. Instead, Suboxone promotes recovery and the reestablishment of pain sensitivity. When under the influence of opioids, the connection between the brain’s executive function (the frontal cortex) and the middle brain where the opiate receptors live and addiction builds enters a state of disarray. Suboxone does not interfere with the brain’s frontal cortex, while the ‘ceiling effect’ of the buprenorphine reduces feelings of euphoria associated with other opioids.

What is Suboxone used for?

Suboxone is used for medication-assisted treatment of opioid addiction Suboxone should be used in conjunction with behavioral change support such as psychotherapy.

Suboxone Dosage

If you take buprenorphine too soon after consuming an opioid, the buprenorphine can cause precipitated withdrawal. Incidents of precipitated withdrawal are more common in patients transitioning from methadone or other full opioid agonists such as fentanyl. To reduce this risk, it is imperative that withdrawal has commenced before starting a course of buprenorphine-based treatment, i.e., Suboxone. Before taking Suboxone, it is recommended to wait at least 12 hours since the last use of a short-acting opioid and 24 hours since the last use of a long-acting opioid - this may be longer depending on the drug and should be discussed with your provider. This allows the patient to enter a reasonable state of withdrawal which is measured by the Subjective Opioid Withdrawal Scale (SOWS). 

When it comes time to end treatment and remove the buprenorphine from the equation, relapse and overdose become a major risk. The body’s tolerance is much lower as a result of time spent in recovery; therefore, the risk of overdose is much greater. The responsible approach to the prescription of Suboxone is to continue treatment for as long as the patient is benefiting from the treatment. Suboxone can be tapered (reduced) under the direction of your prescriber if that is the right plan for you. Speak to our team at Confidant to see if Suboxone is the right treatment for your opioid dependence or addiction.