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the Naloxone in Suboxone is active!

D

Dr. Beat

Bluelighter
Joined
Apr 1, 2002
Messages
511
please stop saying the Naloxone in Suboxone is innert or inactive.

Goggle "BupPharm" and read the power point at the top. It clearly shows Naloxone is active in Suboxone.

I also have 2 other PDF's that clearly show that a small amount of Naloxone gets through in most people, and even a small amount has an effect on your CNS for an hour or two.

So from reading that power point, if you take Buprenorphine alone (Subutex), you will be high very quickly (15 to 30 min), but if you take Suboxone sublinguly it will take a few hours to get to the max high.

Even if your argument was true that all the receptors were "full" of Buprenorphine (saturated) so no Naloxone can find a free opiate receptor, (which is not true in most cases), Naloxone will go and find TLR4 receptors, and that has an effect on your CNS.

Goggle "Naloxone TLR4" if you want to know more.

I must explain something: there are millions of opiate receptors in your brain, so when you take Suboxone, depending on dose, and frequency, a lot of receptors will have Buprenorphine on them, and a few will have Naloxone on them, for a few hours. It is not one big on/off switch in your brain, as a few people seem to think.

Some lucky people seem to get no Naloxone from Suboxone. It depends on the amount of enzymes in your liver and gut. It also depends on what you ate before taking Suboxone - if I eat a blood red grape fruit an hour before taking my Suboxone, I feel the Naloxone more.

If I take Amitriptyline 10mg the night before, and eat a blood red grapefruit for breakfast, then have my Suboxone an hour later, I massively feel the Naloxone, and my pupils dilate massively, (normally very small), I have to run to the toilet for a massive shit, I start sweating like crazy, and I get lots of pain. I get all this symptoms or an hour or two, then the Buprenorphine kicks in, and I feel great the rest of the day.

So there are many factors determining if the Naloxone gets to your brain, or is broken down before then. It is very complicated.

I hope this cleared things up for a few people.
 
Why not reply to the other thread of creating a new one - if you get the meaning of thread and post mixed up we're gonna have a serious meltdown of thread numbers here :D

Otherwise, thanks for being informative - if not posted in the most ideal tone to learn something from it.
Ok cool, I'm done criticizing. Lets take a breath and chill.

For the record I wouldn't have thought that agonists and antagonists together would be such a good idea, but clearly its full of win for some situations.
 
never under any circumstance inject suboxone and when injecting subutex make sure you use a thick filter
 
seep said:
noob
Click to expand...

Well, his advice for using good filtering is a decent one. On the other hand, I inject suboxone all the time. It works just fine.

For the record, I've never said that the naloxone has no effects in the suboxone. But the naloxone will not prevent the buprenorphine from having an effect.

I have noticed the effects of naloxone most clearly when I have taken suboxones sublingually. At those times I noticed a very pronounced laxative effect, which I never had from sublingual subutex... now this is just a hunch, but I figure it might have something to do with opioid receptors in the gut getting antagonized when you swallow the rest of the suboxone after holding it under your tongue.

there are millions of opiate receptors in your brain, so when you take Suboxone, depending on dose, and frequency, a lot of receptors will have Buprenorphine on them, and a few will have Naloxone on them, for a few hours. It is not one big on/off switch in your brain, as a few people seem to think.
Click to expand...

Uh... there are millions of receptors, sure, but there are quadrillions of molecules of buprenorphine in every milligram. It only takes one molecule to activate one receptor.
 
dread said:
Uh... there are millions of receptors, sure, but there are quadrillions of molecules of buprenorphine in every milligram. It only takes one molecule to activate one receptor.
Click to expand...

Good point. There are 10 quintillion buprenorphine molecules in an 8 mg hexagon, but more importantly, buprenorphine has a higher mu affinity than naloxone.

That's the rub. Bupe has a higher affinity than naloxone.

As for never injecting suboxone under any circumstances:

NSFW:
I am a micron-filtered vial of suboxone solution and I am fun in the vein:
NSFW:
step6.jpg
thread here
 
i have a question regarding when it is safe to inject multiple 15mg oxycodone after taking suboxone. i will give some back ground on my use. the last 3 days i have been dramatically lowering my doses in preparation for getting high. prior to my suboxone use i used to inject 40-60mg of oxycodone 3 to 6 times a day. Or i would 8-16mg of dilaudid the same number of times per day. here is the background of my use of suboxone so anyone responding will have a better idea of when i will be able to get high :

Suboxone use
Last 18 months : 8-16mg per day, average 12mg per day
The last 3 days i started weening so i could get high again. i have a prescription of thirty 15mg Oxycodone pills i plan to inject like the good old days and then go back on my bupe. this is what i have taken in preparation of this the past 3 days:

Day 1 at 7 a.m. - 8mgs

Day 2 at 2:30 p.m. - 4mgs

Day 3 at 2:30 a.m. 2mgs
at 6:30 p.m. 2mgs
at 8:30 p.m. 1mgs

I know the standard answer is 24 hours, but i have been taking an average of 12mg per day since March of 2009, and i dont know if bupe is cummulative but if it is id bet i have quite a build up and that my time of waiting would be longer than someone who randomly took a suboxone to get well one time and just waited 24 hours. i figured the wait would be more than i could take all at once ( as in just waiting like 50 or 60 hours with no subs without feeling really sick ) so i decided to stagger down so i can wait a lesser amount of time after taking reduced doses for a few days instead of having to wait a full 2 or 3 days with no opiates in my system. anyone have a good idea of when id be fully in the clear to bang after my last dose of 1mg at 8:30p.m. on day 3? any info on this would be greatly appreciate. also this is my second ever bluelight post, i just joined today, so i dont know if this is the right place for a new sub question and im not sure how to start my own thread. im also not sure if i can private message people yet. thanks for reading
 
i have a question regarding when it is safe to inject multiple 15mg oxycodone after taking suboxone.
Click to expand...

The oxycodone will probably not work too well until you've been at least 3 days without suboxone.

Alternatively, you can do massive dosages, but that's just stupid.
 
I don't think that's necessarily true. Even after 24 hours I can feel hydrocodone administered orally. That was when I was on 16mg daily, and a dose of 40mg of hydrocodone. Oh well.
 
I guess it depends on the individual somewhat, but I've found buprenorphine usage to create a massive tolerance towards opioid agonists.

Many years ago, I tried being without buprenorphine for 24 hours and then did heroin, which had basically no effects... same with oxycodone. YMMV I guess.
 
OP, again - why didn't you post in the other thread?

I've already referred to the PowerPoint presentation you're referring to there...

myself said:
Anyway, as I believe buprenorphine s.l. bioavailability is at most 25% (source: UCSF Drug Dependence Research Center and The General Clinical Research Center).
Click to expand...

This information you can also find in that presentation, I believe. Also, this example was inspired by the trial described there (I just didn't have it at hand to write it the same as it is there):

myself said:
A simple trail explains it better than talk in theory. Buprenorphine is given at 4mg for 8 days (i.v.), for another 4 days 4mg of naloxone (i.v.) are added to buprenorphine (no change in subjective withdrawal feelings), then buprenorphine is stopped and for another 4 days naloxone (i.v.) is only given (change in subjective withdrawal feelings minimal, may be even placebo). After buprenorphine is cleared out of body, continuation of naloxone injections will mean true withdrawal (but actually naloxone won't have any impact on severing it, naloxone is also an antidote for loperamide overdoses - no whole system withdrawal begins).
Click to expand...

From what I remember, there's only written here that some patients feel antagonist activity of naloxone. I think this may be subjective as:

1) both drugs cross BBB
2) even if Suboxone is injected and naloxone gets first to receptors buprenorphine forces it out in miliseconds...
3) naloxone can't access any opioid receptors from then on as in any Suboxone formulation there is more molecules of buprenorphine than of naloxone; 2mg vs. 0.5mg and 8mg vs. 2mg is enough to be a proof (drugs don't differ much in molecular mass) but to make sure, I'll do the math for you:

Code: 
1 mol buprenorphine HCl ------- 504.1g
x ----------------------------- 0.008g (=8mg)

x = 1,587*10^-5 mol

N = 1,587*10^-5 * 6.022*10^23 = 9.5568 * 10^18 [molecules of buprenorphine HCl

1 mol buprenorphine freebase = 467.64g
% = (467.64g/504.1g) * 100% = 92.77% => You have 92.77% of buprenorphine in hydrochloride salt

N = 9.5568 * 10^18 * 92.77% = 8.8668 * 10^18 [molecules of buprenorphine freebase]

1 mol naloxone HCl------------- 347.836g
x ----------------------------- 0.002g (=2mg)

x = 5.75*10^-6 mol

N = 5.75*10^-6 * 6.022*10^23 = 3.462 * 10^18 [molecules of naloxone HCl]

1 mol naloxone freebase = 347.836g
% = (311.37g/347.836g) * 100% = 89.52% => You have 92.77% of naloxone in hydrochloride salt

N = 3.462 * 10^18 * 89.52% = 3.099 * 10^18 [molecules of naloxone freebase]

8.8668 * 10^18 > 3.099 * 10^18

Voila, after injecting a 8mg bupe/2mg naloxone pill, you've got 8.8668 * 10^18 molecules of buprenorphine when freed from the salt and 3.099 * 10^18 molecules of naloxone when freed from the salt.

- - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -

ADDED:
Also, I agree with you that buprenorphine in Suboxone formulation doesn't make naloxone inactive but actually makes it useless there. I've already explained why...

Buprenorphine's affinity for mu-opioid receptors >>>>>> naloxone's affinity for mu-opioid receptors

So there is no way, naloxone binds to any receptor as firstly, buprenorphine binds stronger, and secondly, there are more buprenorphine molecules than naloxone's once they both cross BBB.
 
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There's no need to account for the freebase/HCl difference. Suboxone and subutex both contain an amount of buprenorphine hcl that corresponds to 8mg buprenorphine freebase. It says so right on the package.
 
I wasn't sure, I've only seen French and Finnish Subutex but then one has:

1.03 * 10^19 molecules of buprenorphine
3.86 * 10^18 molecules of naloxone

in one 8mg/2mg tablet. :) (No, I didn't count it for the second time, I first counted it treating amounts in tablets as you wrote)
 
Slapdragonx said:
Is there a set ratio for any substance as a salt? Eg Bupe HCl with the 92.77% freebase.
Click to expand...

The ratio differs between substances and salts. It's the ratio between the weight of the freebase molecule and the weight of the acid molecule.

Therefore if we have

b = weight of the parent molecule (base)
a = weight of the acid molecule (eg. HCl, SO4H2, etc.)

Then the ratio of the salt vs. the freebase is (b+a) / b

(times 100 if you want to convert to percentages)



example:

buprenorphine freebase weight = 467.64
hydrochloric acid weight = 36.46

buprenorphine hcl weight = 467.64 + 36.46 = 504.1

ratio of hcl to freebase = 504.1 / 467.64 = 1,0779659567188435548712684971345 = ~107.8%

ratio of freebase to hcl = 467.64 / 504.1 = 0,92767308073794881967863519143027 = ~92.8%
 
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Dr. Beat said:
Even if your argument was true that all the receptors were "full" of Buprenorphine (saturated) so no Naloxone can find a free opiate receptor, (which is not true in most cases), Naloxone will go and find TLR4 receptors, and that has an effect on your CNS.

Goggle "Naloxone TLR4" if you want to know more.
Click to expand...

Toll-like receptor 4 (TLR4) has absolutely nothing to do with psychoactivity of opioids or any other drugs. TLR4 is an innate immune receptor that binds a component found in the cell walls of pathogenic bacteria (called lipopolysaccharide).

TLR4 actives inflammatory and immune pathways. When activated in most tissues it causes recruitment of immune cells to those tissues. When activated in the blood it causes sepsis. When activated in the CNS it causes fever.

This speaks only to the immunomodulatory properties of naloxone.
 
Some of the people replying here sound like they know what they are talking about, but they are totally wrong in their assumptions about how drugs effect the human body and brain.

I have read hundreds, if not thousands of PDF's about how opiates work, and I could explain to you why you are wrong, but I am on a smart phone, so i will do it later, when I get access to a keyboard.

Also please tell me now if your not open to changing your point of view, as I don't want to waste my time (or your time) on pointless arguments. I got better things to do.
 
You don't tell what you mean and you ask if "some people" are open to changing their point of view. Well, it's now about changing someone's point of view here but getting to know things anyway. In politics you can have your point of view, in science you either accept that x = y or you can go stuff yourself. ;)
 
Hey, you guys are all so wrong. I could explain why but I'm currently writing with one hand and wanking with the other. But just trust me, I've read thousands of PDF:s about watching paint dry.
 
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