Apr 28, 2025
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What is buprenorphine used for officially? How about off label? And what’s the coolest thing about it?
Buprenorphine is an opioid. But, like, a special kind of opioid.
There was a time, the 1920s through the 1970s, when opioids just... weren't prescribed outpatient. If you were getting opioids, you were either recovering from surgery in a hospital, in the final stages of dying of cancer, or you were getting them illegally as heroin.
Full stop.
The reason? Fear of opioid addiction (which had been a major problem in the decades leading up to this de facto prohibition) was firmly instilled in the medical psyche.
But options for pain management were a lot more limited than they are today, and opioids? Well, they're useful.
So in the 1960s UK researchers John Lewis and Kenneth Bentley set out to create an opioid with a lower risk of addiction (and side effects in general). And in 1969 they largely succeeded with buprenorphine. About a decade later, in 1978, buprenorphine was approved to treat severe pain in the UK.
In the 1990s, it would be approved to treat pain in the US, and in 2002 it would be approved for what it is probably most well known for today- treating opioid use disorder.
There are several things that make buprenorphine different from other opioids. One, it has a pretty long half life. A half life is how long it takes for half of the drug to be eliminated from the body, and gives an indication of how long the drug works. Buprenorphine's half life is 38 hours, and its effects generally last a little over 24 hours (though it can be dosed multiple times a day in small doses for acute pain).
A long half life means steadier control over pain and potentially a lower risk for abuse because people aren't getting cycles of highs and lows like they might with other opioids.
Two, it has a relatively low risk of euphoria. Euphoria is name for the "good" feeling people get from opioids. While it's not impossible to get mild euphoria from buprenorphine, it is pretty unlikely compared to other opioids and typically doesn't last with repeated doses, meaning there's a lot fewer people who would seek it out as a way to get high, leading again to lower rates of abuse.
Three, very low rates of hyperalgesia. Opioids do a thing where, if taken consistently over time for pain, the pain actually gets worse. This is called opioid hyperalgesia, and it's separate from just building a tolerance to the opioid itself. The pain the person experiences literally gets worse, which sucks if you're trying to treat that pain.
It is fairly rare to get opioid hyperalgesia from buprenorphine.
Four, and potentially the coolest, it has a ceiling effect.
We have opioid receptors in our brains and throughout our bodies, which are how opioids, which bind to those receptors, treat pain and cause side effects. Generally, the effect of an opioid is modulated by how many of our receptors are bound at one time. For example, more bound receptors means more pain control, but also more side effects, like sedation and respiratory depression (slowed breathing).
If too many receptors have opioid molecules sitting on them, we die of an overdose.
Buprenorphine binds to these receptors too (in fact, it will knock other opioids off the receptors so it can bind to them), but instead of fully binding, it kind of "half-binds". It's sitting there so nothing else can sit there, but it's not causing the same level of sedation and respiratory depression common with other opioids.
That also means that after a certain dose (about 32mg), every opioid receptor is bound to buprenorphine. But unlike, say, oxycodone, where if every receptor was bound the person would be dead, if every receptor is bound to buprenorphine, the person would be getting very good pain control but markedly less sedation and respiratory depression.
Meaning it is almost impossible to overdose on.
Not only that, but because buprenorphine binds so strongly to opioid receptors, if a person who was taking a high enough dose of buprenorphine took a different opioid, they would not be able to overdose (or get a euphoric effect) on that opioid either because the other opioid wouldn't be able to bind to the receptors. This is part of why it is so useful for treating opioid use disorder- it manages the physical dependence/prevents withdrawal by sitting on those receptors, but it doesn't allow effects from non-buprenorphine opioids.
I'm a little rusty at explaining things so I hope this all was understandable. But I just think that buprenorphine should really be used more for acute and chronic pain. It's markedly safer, has lower rates of abuse (it's been tested for years in people with opioid use disorder), and has lower rates of opioid hyperalgesia than more common opioids.
How many drugs from drugs.com's top 100 drugs have you taken?
0
1-5
6-10
11-15
16-20
21-25
26-49
50-100
Czyżby nowy rozdział w moim uzależnieniu? Może się nie wykoleje i jakoś wyjdę z tego .. :/
Learn about the government’s plan to provide addiction treatment to people in prison, an underserved population.
Thanks to @gardening-tea-lesbian for posting about this and bringing it to my attention!
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The Biden-Harris Administration wants to make substance abuse treatment more accessible for all prisoners in the U.S. Addiction is common among people in prison, and treatment helps fight recidivism and reduce overdose rates.
From Federal Prisons To State Prisons
By this summer, all federal prisons will offer addiction treatment, Dr. Rahul Gupta, director of the White House Office of National Drug Control Policy, said last week.
Federal officials want states to follow suit. Starting this spring, Medicaid funds will be set aside for states to use in their own jails and prisons to provide mental health services, including SUD treatment.
Approximately 25% of all Americans received Medicaid benefits in 2022. For people with low incomes, Medicaid is the largest provider of funds for healthcare services.
The Biden-Harris Administration has shown a commitment to helping underserved communities receive addiction prevention, treatment, and recovery services.
This includes services for rural populations and Tribal populations along with people who are incarcerated.
Addiction In Our Prisons
It’s hard to know precisely how many incarcerated people have an SUD, but the National Institute on Drug Abuse (NIDA) estimates that about 65% of all inmates do.
NIDA estimates that another 20%, who didn’t meet the official criteria for an SUD, were under the influence of drugs or alcohol when they committed a crime.
Overall in America, about 40 million people ages 13 and over are living with addiction, or about 12% of the population, according to the 2020 National Survey on Drug Use and Health.
How Treatment Helps Prison Populations
Drug abuse treatment is effective. For people in prison, receiving treatment can mean the difference between staying out of jail once released or returning behind bars.
It can also provide them with the mental clarity and tools to meet the challenges of life, improve their mental health, and succeed in their relationships and work.
Aids Long-Term Recovery
The Biden-Harris Administration is focusing on evidence-based treatment methods to help people who are incarcerated get and stay on the path to addiction recovery.
This includes medication-assisted treatment (MAT), which combines the use of medications like buprenorphine with behavioral therapy to treat opioid abuse.
Buprenorphine, the first medication that could be prescribed by physicians to treat opioid use disorders, helps people overcome addiction in a few ways.
Using buprenorphine helps with recovery by:
reducing cravings
diminishing opioid withdrawal symptoms, which include flu-like symptoms and severe anxiety
improving safety, if overdose occurs
lessening the chance of misuse
One study in support of buprenorphine’s effectiveness showed that participants receiving the medication were almost twice as likely to remain in treatment and not relapse.
Prevents Overdose Deaths
According to U.S. News and World Report, the leading cause of death among people newly released from prison is drug overdose.
This is partly due to the fact that their tolerance levels decrease while incarcerated, so they aren’t able to tolerate the same amount of the drug as before they were in prison.
The buprenorphine study mentioned above also revealed that people not receiving the treatment had a 20% mortality rate."
-via Addiction Resources.net, 3/9/23
🎀