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Bupe What is and what is not true about swallowing buprenorphine?

B

black kat

Bluelighter
Joined
Nov 11, 2014
Messages
243
Hey guys ive been creeping around this forum for while
and since there seem to be alot of helpful people
around i decided to try to find an answer for this one that has been bothering
me for awhile now..


I recently joined a recovery program that gives you Subutex every day
(increasing doses) and "take home" Suboxone for weekends.Its been just
a couple of weeks since i joined and before that i was preety clueless
regarding bupe and the way its working,and still after searching the
internet i feel unsure of a couple of things,especially since most of the posts
regarding this matter are relatively old.


So here it goes:


If someone(addicted to opiates) takes the Subutex INCORRECTLY and swallows it instead of using it
sublingually,will the buprenorphine lose most of its effect INCLUDING
the part that "antagonizes" other opiates?
In other words,will he be able to use other opiates on top/after and feel them/get high?


Moreover,is the above considered safe(swallowing instead of placing under tongue)?
Ive heard and read stories of how it will make you sick and the agonist part weakens
but the antagonist is still in effect, to other people saying that they are swallowing
it daily for months and they are completely fine,except that they can still use and feel
other opiates on top on a daily basis.


Please if you can help from either knowledge or experience it'll be highly appreciated!
 
If you swallow bupe it's going to be quite significantly less effective, and (this is dose dependent) would most likely not have any blocking effect. Now I say blocking not antagonizing because it doesn't antagonize other opiates. It's completely safe it's just going to be weaker. The antagonist in bupe is NEVER active, the blocking effect is a result of buprenorphine having a high affinity to opioid receptors (think of it as the bupe holding on to your receptors tight so other opioids can't get on).
 
Just be straight up, dude. You're asking if you can just swallow your dose so you can still get high on your DOC. It's okay to be honest. Just curious, is this a mandatory program or is this a one time thing?

I swallowed my medication in rehab and snuck out at night and got high the first week. I had the best results just spitting out the medication but swallowing worked too. It just took a few days of doing that because bupe lasts so long in your system. Even if your body absorbs some of the bupe, the blocking effect is not present in low doses.
 
Thanx alot for the info :) Looks like im still a big noob on bupe and the program certainly doesnt seems to care to change that(apart from some really basic info).

So in a highly monitored environment where some days they crush the pill before they give it and sometimes even have to show your mouth after,
is swallowing the bupe the preferred or maybe the only way to get a decent high on other opiates later that day?
 
rhun said:
Just be straight up, dude. You're asking if you can just swallow your dose so you can still get high on your DOC. It's okay to be honest. Just curious, is this a mandatory program or is this a one time thing?

I swallowed my medication in rehab and snuck out at night and got high the first week. I had the best results just spitting out the medication but swallowing worked too. It just took a few days of doing that because bupe lasts so long in your system. Even if your body absorbs some of the bupe, the blocking effect is not present in low doses.
Click to expand...
Its the biggest program in a certain European country with a huge waiting list of about 3-4 years.You can reapply for another location of service but you gotta
attend at least a couple of weeks first at the clinic they fist assigned you,or else youll be kicked out and wait for another 3 years.

Spitting directly is not an option as you are being watched somewhat closely
by 3 nurses the time youre given the bupe and usually youre not allowed to leave until 10-15 minutes pass and show your mouth.
When the pill is cut in 2 or 3 pieces its easy to hide it in the mouth somewhere but that doesnt really work when its crushed to 10 small pieces or even worse,powdered!

Btw,the current dose is 8mgs,is that qualified as small?
 
It will still block in high enough doses if swallowed its just when swallowed the bupe is only partially absorbed meaning you need to swallow at more than you would have taking it under the tounge to get the effects you want. If you are swallowing the dose not enough of the opioid you need is being absorbed. It wont even satisfy your cravings or block other opiates so whats the point of even taking it? your only going to absorb maybe 1mg of bupe at most with swallowing a 8mg tablet. More naloxone will be absorbed through the stomach too.


The active ingredient, buprenorphine, is lipid soluble meaning that it is more like a ‘fatty’ molecule than a ‘watery’ molecule. Cell membranes are made of fats or ‘lipids’. Buprenorphine sticks to the cell membranes in the mouth, an area where the surfaces are called mucous membranes. That type of surface has a thin layer of cells which the buprenorphine crosses before eventually entering small blood vessels and capillaries where it then enters the bloodstream, eventually transported to the brain. In the brain the buprenorphine leaves the capillaries and binds to receptors on neurons that recognize endorphins and opiate medications.

Buprenorphine will not diffuse as easily across other surfaces, such as the skin on your body the cells are layered more deeply, so there is more to cross to get to a capillary. This is why buprenorphine is only made in IV solutions, skin patches and sublingual tablets

If you swallow the tablet, the buprenorphine will pass through the stomach and into the intestine. There it will be taken up by the bloodstream, into the ‘portal vein’, which goes straight into the liver. The liver is a big detoxifier; it destroys many chemicals before they have the chance to get further into the body. This is called ‘first pass metabolism’. Some drugs are broken down so efficiently that almost none of the amount taken will get to the brain. This is the case with buprenorphine. It is also the case with naloxone, the other ingredient in Suboxone naloxone doesn’t dissolve in lipids though, so it does not get into the bloodstream through the mouth lining either.
 
Last edited:
black kat said:
Its the biggest program in a certain European country with a huge waiting list of about 3-4 years.You can reapply for another location of service but you gotta
attend at least a couple of weeks first at the clinic they fist assigned you,or else youll be kicked out and wait for another 3 years.

Spitting directly is not an option as you are being watched somewhat closely
by 3 nurses the time youre given the bupe and usually youre not allowed to leave until 10-15 minutes pass and show your mouth.
When the pill is cut in 2 or 3 pieces its easy to hide it in the mouth somewhere but that doesnt really work when its crushed to 10 small pieces or even worse,powdered!

Btw,the current dose is 8mgs,is that qualified as small?
Click to expand...

If you're taking 8mg SL daily, it should be a blocking dose yes. And for many, it raises tolerance to your DOC because bupe is more potent than people think. But if you're able to swallow the medication immediately, any small amount absorbed shouldn't be enough to block. If you can't swallow immediately, holding the pill above instead of below your tongue should lessen absorption.

I don't feel like giving you this information is exactly harm reduction, though. Are you not wanting to quit right now but want to keep it open as an option? This will catch up to you eventually... at my clinic they drug test (just warning you, we can't answer any questions on drug testing).
 
It defo is harm reduction man cause you know what stupid things someone is capable of doing if he is fiending to get high.
Knowing theres a safe and tried way to bypass the Sub while youre under strict supervision is relieving and nice to know.

Yes they drug test you randomly in my program as well but ive admitted that im still using H on top and thats fine with them
for the first week or 2,as long as youre taking your bupe correctly(so even if ure using its going to waste).
 
black kat said:
It defo is harm reduction man cause you know what stupid things someone is capable of doing if he is fiending to get high.
Knowing theres a safe and tried way to bypass the Sub while youre under strict supervision is relieving and nice to know.

Yes they drug test you randomly in my program as well but ive admitted that im still using H on top and thats fine with them
for the first week or 2,as long as youre taking your bupe correctly(so even if ure using its going to waste).
Click to expand...

They're probably counting on that you will realise that you can live a happy life without heroin if Suboxone keeps your withdrawal away. But if you don't want to quit heroin, then sooner or later you're likely going to stop taking Suboxone because it will take away most of heroin effects if not all of them unless you're obliged to be on the program for some reason. My program has few Suboxone patients and given that Suboxone is not as readily available as methadone, most of the patients on Suboxone take it because it works out for them. However, I met a few people who had been on Suboxone and one who was and they complained Suboxone was garbage. Well, it is garbage when you expect a high, but it's the best option out there if you want to get off opioids but are unable to having been long and/or severely addicted. I couldn't really feel fine if I knew that I was taking place at a maintenance program not getting anything out of it but keeping it just in case and there were people out there who wanted to quit because they'd realised their life on heroin was miserable but they couldn't because the program was full. If you've been given a chance, then at least think carefully what you potentially have to gain and what you have to lose. Even if you wasn't 100% sure that you wanted to quit when you arrived at the clinic, perhaps that's what you really need. People often have a problem with quitting addictions because they're simply used to them and they're afraid of changes.
 
Well, i'm no scientist, or bupe afficianado, but I've been copping the stuff from a pal to keep me functioning, been so broke lately I can't afford my usual fix...but I digress..

I believe what you mean by saying "people who swallow their bupe instead of SL or whatever can still get high" is probably sort of a paradox....in that, from what common sense would tell me, the ORAL BIOAVAILIBILITY of Bupeprenorphine is what?? like 25% give or take??
The SUBLINGUAL B.A. is around 40-50% if i'm not mistaken, right folks???

The so-called "blocking effect" does not start to become an issue until you reach a dose of around 3-4 mg give or take, is that correct anybody???

Therefore, the patients swallowing their sub will absorb appx. 20-25% LESS BUPRENORPHINE VS. SUBLINGUAL ADMINISTRATION....Therefore, people who swallow their dose, are actually getting QUITE A BIT less bupe, therefore the "blockade effect" does not actually take effect, because their ORAL DOSE is not high enough to cause it....
HOWEVER, if the same patients began taking their sub SUBLINGUALLY, they will receive their full dose, usually enough to really nurture the blockade effect and have your receptors completely saturated with bupe.

So basically the less bupe you take, the more likely other opioids will still work for you..(I've mixed stronger opioids with LOW doses of bupe < 2mg, with really good results..but not vice versa ya dig??)
The more bupe you take, the less you will feel any other opiates....

Just the other day I took 6mg sub and ate 8 10mg hydros with nil effects...next day I plugged 90mg MScontin and I was feelin pretty groovy there for a minute!

But in short....wait until you have only a tiny amnt of sub in you to use other opiates, or they will be wasted..
 
I think its different for different people.
Bupe has a really strong blocking effect on me personally. Even if I take just 1mg of Bupe theres no point in me doing any other opiates fo at least 12 hours, they just wont work. Even 150ml of Methadone didn't get past the Bupe. A lot of people I know say the blocking effect doesn't happen until 3-4mg so who knows.
 
I believe what you mean by saying "people who swallow their bupe instead of SL or whatever can still get high" is probably sort of a paradox....in that, from what common sense would tell me, the ORAL BIOAVAILIBILITY of Bupeprenorphine is what?? like 25% give or take??
The SUBLINGUAL B.A. is around 40-50% if i'm not mistaken, right folks??
Click to expand...

Oral bioavailability of buprenorphine is only around 10%, it's because once it's absorbed from small intestine, it's transported to liver where it undergoes extensive first-pass metabolism.
 
^^^ but without the benefit of a liquid solution, sublingual can be as low as 13% :)

i don't understand the point of swallowing bupe, unless you're in a mandatory program or something. Even then, it will just be like taking roughly half a dose sunlingually(maybe less, you get the point).

One thing I'm surprised no on has mentioned is the fact that oral administration gives you more of the full agonist metabolite, norbuprenorphine. Granted I don't really buy into the whole norbupe thing, but interesting nonetheless.
 
If your only getting 14 percent sublingual your doing something wrong. If you keep it in your mouth for 10-15 mins and you haven't drank caffeine or smoked nicotine before your dose it should be more like 40 percent.

Where did you hear oral bupe converts more to nor bupe? It would be good to see the study it sounds like bullshit to me your better off doing it sublingual and absorbing the whole dose.
 
I found that the sublingual bioavailability of suboxone is about 55%, oral comes in between 10-22% (I found varying numbers so those are the lowest and highest I found) and intranasal is approx. 85%.
 
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