"The Science of Suboxone (Buprenorphine)"

Here at Urban Peaks Rehab, we have patients everyday that are not quite sure about how Suboxone actually works. To make it easier to understand, we have found an awesome article that answers the most common questions regarding how Suboxone works from WorkIt Health.  Give it a read!

How does Suboxone treatment work, and what are its effects?

We’ve talked extensively about Suboxone, including its history and its role in medication assisted treatment for opioid addiction. If you’ve read some of these articles, you know that Suboxone is an opioid that eases withdrawal symptoms.

But what exactly is going on in your brain when you take Suboxone — is it different from what happens with other opioids? For those of you who want to delve a little more into the nitty gritty of why and how Suboxone works, here is some more information about its neurological effects.

First of all, what happens in your brain when you take opioids?

There are molecules in your brain called neurotransmitters that carry information between neurons (i.e. brain cells). Different types of neurotransmitters attach to different receptors on the neurons.

One type of receptors is called the opioid receptors. We have many of these opioid receptors in an area called the locus coeruleus in the brainstem. Whenever the right kind of molecules attach to the opioid receptors in this area and activate them, this prevents the release of noradrenaline – a neurotransmitter which stimulates alertness and blood pressure. Preventing noradrenaline from being released causes the opposite symptoms: drowsiness, slowed respiration (breathing), and analgesic (pain relieving) effects. Another effect of opioid receptor activation is the release of another neurotransmitter called dopamine into the nucleus accumbens, which is a brain region implicated in reward processes. This reaction causes feelings of pleasure.

The above process can occur with neurotransmitters that naturally exist in your body called endogenous opioids (like endorphins, which make you feel good when you exercise).

But chemicals that you ingest can also attach to the opioid receptors. When you take full agonist opioids like heroin and oxycodone, they copy the actions of endogenous opioids and attach to opioid receptors – causing even stronger pleasurable effects like euphoria.

However, if you take a lot of full agonist opioids for a long time, your brain notices the influx of opioids and “turns off” some receptors. This means that you eventually need more opioids to achieve the same effect (tolerance). In addition, when you stop taking opioids and there are not enough of them in the receptors, you release more noradrenaline than usual, causing highly unpleasant side effects like vomiting, anxiety, jitters, and pain (withdrawal). Although opioid use may be pleasurable at first, eventually these neurological changes induce physiological dependence – opioids become a necessity to function in daily life.

In the worst-case scenario, high levels of opioid use will slow down the respiratory system enough to dangerously lower the amount of oxygen reaching the brain, causing brain damage or even death (overdose).

What does Suboxone do to help?

Suboxone is the brand name for buprenorphine and naloxone.

Buprenorphine is also an opioid that attaches to opioid receptors. It has strong binding ability, replacing and blocking other opioids so that they become ineffective. It is a partial agonist instead of a full agonist, meaning that it causes limited pleasurable effects, just enough to stop withdrawal symptoms. People report feeling “normal” rather than high when on a regimen of buprenorphine. In addition, there is lower propensity for tolerance because buprenorphine takes longer to dissipate, creating a steadier effect on the receptors.

Essentially, taking buprenorphine substantially reduces one’s need to turn to other, more dangerous opioids in order to maintain the status quo of an opioid-dependent brain. It thus allows the individual to function on a day-to-day basis experiencing neither withdrawals nor highs. There is also the possibility of lowering dosage over time to return the brain to its pre-dependence state (tapering).

Suboxone has a few advantages over other medications used to treat opioid addiction, such as methadone. Buprenorphine is thought to have less respiratory effects (and even cause withdrawal symptoms) at high doses, reducing the risk of overdose. Like methadone, it can still be misused by being diverted (i.e. used to get high, although it is reportedly difficult), which is why naloxone is added. Naloxone, an antagonist, attaches extremely strongly to the receptors and completely blocks other opioids. However, it does not have any effects of its own, doing nothing to prevent withdrawal symptoms. If Suboxone is injected instead of taken orally, the naloxone kicks in, blocks the buprenorphine, and causes withdrawal. This combination helps ensure that people use Suboxone as directed.