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Bupe No effect from 16mg suboxone snorted

bluecollartweeker

bluecollartweeker

Bluelighter
Joined
Nov 7, 2023
Messages
224
Location
Canada
I decided to abuse my script today because i was getting extreme heroin cravings and wanted to snuff thosd out, but after railing all the powderd generic pills its been ebough time that i should be feeling high but im not. Is it because the naloxone in it is that strong it can kill the high from a 16mg dose?
 
It's because buprenorphine has a ceiling effect.

After enough is built up in your system, taking more doesn't do anything or cause any increase in effects.

Honestly after about 4-8mg, subs aren't going to really produce any more or better effects.
By 16mg, all of your opioid receptors are completely covered & no more bupe can attach to anything.
It builds up with daily use too, so if your taking it every day, then you have a bunch built up in your system.

Not only does it have a ceiling effect but it's also only a partial agonist, so it's not going to activate your receptors all the way.
Think of your receptors as locks & the drug molecules are the keys. Full agonists like heroin fit perfectly into the lock & open it up. Partial agonists fit but are the wrong shape, so they don't fit all the way & can only open the lock ever so slightly.

I can explain the whole way buprenorphine works but that's basically the gist of it. Taking more subs doesn't do anything.
 
Im on 16mg daily for maintnence after a morphine and heroin addiction, where my tolerence to morphine reached 600mg at its peak. So does that mean i can take 8mg and stay in successful maintnence while pocketing the rest of the dose?
 
bluecollartweeker said:
Im on 16mg daily for maintnence after a morphine and heroin addiction, where my tolerence to morphine reached 600mg at its peak. So does that mean i can take 8mg and stay in successful maintnence while pocketing the rest of the dose?
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Yeah probably.

Buprenorphine is incredibly potent.
In Europe, buprenorphine gets used for pain in doses as low as 0.02mcg.

So as long as you aren't still withdrawing from morphine & heroin, you could easily drop your dose & probably be fine.
I do think the higher doses can some times help with cravings psychologically, but in reality, yeah anything over 8mg is pretty much overkill (unless you're coming off of a full agonist).

Most doctors also don't want people to discover that at around 2mg & under, you actually start to get a buzz from your bupe (although not a very good one). This is because the lower doses allow for your blood levels to drop sooner & to have receptors open to receive your next dose, which causes a mild buzz. So I think they keep people on ridiculously high doses so that their blood levels are constantly maxed out & they never feel their bupe. I think this is super counter-productive if the goal of maintenance is to help with cravings, but I digress. I could complain about how our healthcare is run all day. lol
 
bluecollartweeker said:
Fascinating, thanks for informing me
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No problem!

And yeah the naloxone in subs is basically pointless.

Back in the day it use to be Subutex (straight buprenorphine). But the makers of Suboxone came up with the buprenorphine/naloxone combo & patented it as "Suboxone", claimed their product was "less abuse-able" due to the naloxone. Except bupenorphine is so strong at your opioid receptors that not even naloxone can displace it.

Many people think the naloxone is what causes withdrawals when they take bupe on a full agonist too, but that's not the case. It's actually the bupe that causes withdrawals because it's so strong that it rips other opioids off your receptor & replaces it with itself, leading to less receptor activation.

So yeah, the naloxone is useless.
 
Wow that explains alot! Thanks.

Im going to over share here, but its cuz im spun on ritalin.

The receptor fighting explains why i got so sick after injecting a micture of 10mg oxymorphone and whatever half a pill of hydrocodone was while on 8mg of subs, it was a bad idea but i was emotional because my ex girlfriend made sure to remind me she was lying everytime she said she loved me, i was hoping id get high enough to atleast forget the pain but it wasnt a suicide attempt. (I only ever made a suicide attempt once with an OD if aripiprizole and i survived and the aftermath completely ruined my life but now 9 months later ive neve been happier to be alive!) If it wasnt for the subs maybe it wouldve been an OD. Its been 5 weeks since that day and i havnt touched a needle,
 
bluecollartweeker said:
Wow that explains alot! Thanks.

Im going to over share here, but its cuz im spun on ritalin.

The receptor fighting explains why i got so sick after injecting a micture of 10mg oxymorphone and whatever half a pill of hydrocodone was while on 8mg of subs, it was a bad idea but i was emotional because my ex girlfriend made sure to remind me she was lying everytime she said she loved me, i was hoping id get high enough to atleast forget the pain but it wasnt a suicide attempt. (I only ever made a suicide attempt once with an OD if aripiprizole and i survived and the aftermath completely ruined my life but now 9 months later ive neve been happier to be alive!) If it wasnt for the subs maybe it wouldve been an OD. Its been 5 weeks since that day and i havnt touched a needle,
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Hmm,
Well technically you can use full agonists on top of bupe.
It's only when you take bupe after a full agonist is in effect that it should cause problems.
For example if you're taking hydrocodone every day for a week & then you take 8mg of subs before it's worn off, then it will throw you into what is known as "precipitated withdrawal". But if you take hydrocodone on top of buprenorphine, it'll either do nothing (because bupe is blocking it) or just cause added effects (depending on how many receptors you have open for the hydrocodone to attach to).

I've used full agonists on top of my bupe many times in the past & have been fine.

So I'm not quite sure why you got sick.

I hope I don't sound preachy here, but shooting pills is pretty bad for you. If you're going to do this, it's best to have micron filters. Because some of the binders & fillers in the pills can get lodged in your circulatory system if they're not water soluble. It's possible you either just got sick from taking too many opioids or possibly from the injection itself.

I personally am pro-legalizing heroin & opioids, but I'm against using needles, as they can cause problems that you wouldn't have otherwise had to worry about if you had done the drug any other route. It can lead to infections, heart problems, loss of limbs, circulatory damage, etc..

So it might not mean much coming from a total stranger on the internet, but I'm proud of you for putting the needle down & leaving it down! Nothing wrong with getting high, as long as you're doing it in the safest possible way!
 
bluecollartweeker said:
Im on 16mg daily for maintnence after a morphine and heroin addiction, where my tolerence to morphine reached 600mg at its peak. So does that mean i can take 8mg and stay in successful maintnence while pocketing the rest of the dose?
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You can take even less. They prescribe such insane dosages to block the receptors so you won't take heroin or morphine.
And like another person said, bupe indeed feels better in lower dosages. When I was using bupe, I felt the best on 2-4mg max. Anything more - and you are getting all the side effects, without any positive effects.
In a place where I live, drug addicts on substitution program use 1/2-1/3 of their prescribed dose, and save the rest.
 
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DeathIndustrial88 said:
It's because buprenorphine has a ceiling effect.

After enough is built up in your system, taking more doesn't do anything or cause any increase in effects.

Honestly after about 4-8mg, subs aren't going to really produce any more or better effects.
By 16mg, all of your opioid receptors are completely covered & no more bupe can attach to anything.
It builds up with daily use too, so if your taking it every day, then you have a bunch built up in your system.

Not only does it have a ceiling effect but it's also only a partial agonist, so it's not going to activate your receptors all the way.
Think of your receptors as locks & the drug molecules are the keys. Full agonists like heroin fit perfectly into the lock & open it up. Partial agonists fit but are the wrong shape, so they don't fit all the way & can only open the lock ever so slightly.

I can explain the whole way buprenorphine works but that's basically the gist of it. Taking more subs doesn't do anything.
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I usually take the name brand Suboxone strips (2mg ones), but when given the 2mg Hikma pills they barely covered me. If I tried to do more I’d feel pretty awful.

I’m genuinely curious if there is more Nalaxone in generics than the name brand. Obviously, if you’re used to taking generics you’ll be fine and won’t notice the difference, but going from Suboxone to generic bupe was a no go for me.
 
neversickanymore said:
How is narcan administered? Nasally.

The bioavailability of naloxone orally is only 1 to 2 % It’s mixed with it in an attempt to prevent injection and insufilatiin misuse.

journals.lww.com

917: EFFECT OF ORAL NALOXONE ON OPIOID REQUIREMENTS IN... : Critical Care Medicine

An abstract is unavailable.
journals.lww.com journals.lww.com

If it actually works is still up for discussion, but from your report it seems to.

Did you go into withdrawal?
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Right, but I can snort the strips and be fine, yet if I do the same with the tablets I feel pretty bad. Nowhere near full-blown withdrawal, but cold sweats, heightened insecurity/fear, irritability (the mental withdrawal aspects).

I thought I was crazy until I googled the issue and apparently some other folks have experience some version of this too.
 
Given the possible variability of bioavailability of diffrent forms and different roas we have see the mystery. Also we need to look at what if any effect naloxone has in comparison to buepe. Naloxone is touted to have a stronger affinity to bind then other agonists.

Very strong agonists like methadone and bupe can overide the affinity of naloxone.

My Father is an ER dock retired and encountered a methadone suicide attempt that required ALL of the Narcan for multiple hospitals to reverse the methadone OD attempt. She made it, but literally took almost all the narcan from four whole hospitals to push through.


I know the ROA fixation. Is this the reason you are choosing to administer this rout despite negative results?
 
neversickanymore said:
Given the possible variability of bioavailability of diffrent forms and different roas we have see the mystery. Also we need to look at what if any effect naloxone has in comparison to buepe. Naloxone is touted to have a stronger affinity to bind then other agonists.

Very strong agonists like methadone and bupe can overide the affinity of naloxone.

My Father is an ER dock retired and encountered a methadone suicide attempt that required ALL of the Narcan for multiple hospitals to reverse the methadone OD attempt. She made it, but literally took almost all the narcan from four whole hospitals to push through.


I know the ROA fixation. Is this the reason you are choosing to administer this rout despite negative results?
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Nah not true. Naloxone affinity is def higher than methadone’s

Only reason she needed all that is cause the narcan wore off but the methadone is still going strong cause of the super long half life

Bupe yeah got a stronger affinity than narcan but a way lower activation and isn’t even possible to fatally overdose on cause of the dose ceiling at least on its own
 
buprenorphine exhibits 6-fold higher MOR affinity than naloxone - bridgetotreatment.com

buprenorphine has a 10-fold greater binding affinity for the µ opioid receptor compared to naloxone - ^ article I liked above
Voxide said:
Only reason she needed all that is cause the narcan wore off but the methadone is still going strong cause of the super long half life
Click to expand...

Please correct me if I’m wrong, but if naloxone had a higher affinity than methadone… then wouldn’t that mean less narcan would have been needed?

I understand a very low understanding of pharmacology in general. Embarrassingly so.
 
pixies+ said:
Please correct me if I’m wrong, but if naloxone had a higher affinity than methadone… then wouldn’t that mean less narcan would have been needed
Click to expand...

No. That’s not how it works it’s not just affinity it’s activation
 
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There is pre-clinical evidence to support the claim that naloxone has very limited effects when buprenorphine is present. First, though naloxone can displace most opioids due to its relatively high binding affinity, buprenorphine has a 10-fold greater binding affinity for the µ opioid receptor compared to naloxone (3–5). The slow receptor dissociation kinetics of buprenorphine in conjunction with the rapid elimination kinetics of naloxone further suggests that buprenorphine would largely supplant co-administered naloxone from µ opioid receptors, thus effectively rendering naloxone inert (6). Furthermore, the half-life of naloxone is only 30–40 min. Buprenorphine has a half-life of 24–60 h with other clinical effects such as analgesia and euphoria lasting at least 6 h. Any attenuation of buprenorphine’s effects by co-administered naloxone would therefore likely be short-lived.
 
Voxide said:
Naloxone does have a higher affinity than methadone so idk what you’re askin
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Narcan lasts maybe 2 hours methadone lasts 30 so that answers why this person needed more doses of narcan


This story also doesn’t sound right not saying it’s made up but when this situation occurs you’re supposed to be just be hooked up to a continuous narcan drip

I saw bupe as being incorrectly characterized as being as a strong agonist in a previous post when it’s not; it’s a partial agonist with a stronger binding affinity than Naloxone but low activation
 
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Naltrexone is an orally active opioid antagonist, with an effective duration of action of 24–48 hours, making it suitable for use once a day. It has a very high affinity for opioid receptors and will displace heroin and methadone in minutes, and buprenorphine in 1–4 hours. It is used clinically after opioid withdrawal to prevent relapse to opioid dependence.

Naloxone​

Naloxone is a short-acting injectable opioid antagonist used in the management of opioid overdose to reverse the effects of opioids. It is poorly absorbed orally and so is used either intramuscularly or intravenously. It has a half-life of approximately one hour but continues to have 50% receptor occupancy at 2 hours after injection due to its receptor binding [273].

I was trying to find this… I was mistaken when I thought I had seen that methadone had a higher affinity… something similar to suboxone. My bad.
 
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