the Naloxone in Suboxone is active!

[Hammilton]

I had read about TLR's before but never thought much about them. I can't find any evidence that stimulation of TLR's has any measurable effect on the brain. I see documentation for their involvement in inflammation in the brain, but that's hardly the same thing, is it?

On a more interesting subject, how does naloxone's effect on TLR4 contribute to its pharmacological properties? I imagine very little, but I don't really have a clue.

Personally, I'm far more inclined to accept raybeez comments- seemingly all factual (I find nothing out there that contradicts anything he says), intelligently constructed and just so sciency sounding, than the statements of anyone whose claim to knowledge is having read a lot of PDF's.

I'm open to changing my opinion, but all you're giving is your say-so, which is pretty weak.

How about any sources which indicate a role for TLR mediated psychoactivity? Even one would make me reconsider, but I'm not seeing it.

 

[raybeez]

I had read about TLR's before but never thought much about them. I can't find any evidence that stimulation of TLR's has any measurable effect on the brain. I see documentation for their involvement in inflammation in the brain, but that's hardly the same thing, is it?

On a more interesting subject, how does naloxone's effect on TLR4 contribute to its pharmacological properties? I imagine very little, but I don't really have a clue.

Personally, I'm far more inclined to accept raybeez comments- seemingly all factual (I find nothing out there that contradicts anything he says), intelligently constructed and just so sciency sounding, than the statements of anyone whose claim to knowledge is having read a lot of PDF's.

Although there's a bit of data showing that cells killed by bacteria release proteins that bind TLR4, the general consensus is that there are no endogenous ligands for these receptors. This makes sense since their whole purpose is to act as the first-line detection systems against infection.

The only remote connection I can think of between TLRs and pain is that activation of some TLRs in some cell types causes upregulation of COX-2. But if naloxone is antagonizing TLR4 that would actually make it analgesic (if administered in the setting of infection-mediated inflammation).

 

[P A]

the Naloxone in Suboxone is active!

Not orally, due to it's poor bioavailability. And, as mentioned by someone already, far lower Mu-opioid affinity relative to its ultra-potent agonistic competitor buprenorphine precludes any substantial inhibition of effect either way you dice that turnip. No need to get our panties in a twist.

[bracing for PDFs]

 

[cj]

My question is if nalaxone will absorb in your mouth? I make it a point to never swallow any sub when I use sublingually anyone got an answer to that?

 

[Slapdragonx]

Swallowing it is bad because naloxone is an opiate antagonist.

Opiate agonists (Mu) cause constipation, guess what, naloxone does the opposite. There is mu receptors spread out through your GI tract.

 

[P A]

Opiate agonists (Mu) cause constipation, guess what, naloxone does the opposite

This has actually been considered by some as a convenient benefit to add-on oral naloxone, such as in the case of Suboxone-type formulations. It's expected that much of the constipation resulting from chronic use can be effectively antagonized by the presumably higher naloxone/bupe ratio in the GI tract following buprenorphine's outward diffusion and blood transport to the CNS. The remaining molecular stragglers may well be effectively outmatched by the very poorly bioavailable naloxone, the majority of which remains in the digestive system following administration.

 

[Dr. Beat]

Ok, I have finally got enough time to show you the PDF's that clearly prove that the Naloxone in Suboxone is active.

"Buprenorphine and Naloxone combinations: the effects of three dose ratios in morphine-stabilized, opiate-dependent volunteers" (1999)

This PDF clearly proves that the Naloxone is active, but as some of the people in the "Naloxone is inactive cult" (or religion), are not too bright, so I will post a few more.

"Abuse liability of intravenous Buprenorphine/Naloxone and Buprenorphine alone in Buprenorphine-maintained intravenous heroin abusers" (2010)

This PDF clearly shows differences between Suboxone and Subutex.

"effects of Buprenorphine and Naloxone in morphine-stabilized opined addicts" (1998)

"Self-administration of intravenous Buprenorphine and the Buprenorphine/Naloxone combination by recently detoxified heroin abusers" (2002)

"REVIEW - Clinical and pharmacological evaluation of Buprenorphine and Naloxone combinations: why the 4:1 ratio for treatment" (2003)

All these PDF's clearly show that the Naloxone is active in the Suboxone, so stop saying it has no effect.

I think I know why you dummies got it wrong. Because most doctors say that you cannot I.V. Suboxone, (due to the Naloxone) which most people on Bluelight know is false, some of the less intelligent people then jumped to the wrong conclusion that the Naloxone is innactive! That is clearly seeing the world in black and white terms , when in fact the world is rather grey scale.

And to answer Crimsonjunk, i read on PUBMED that Naloxone is absorbed in the mouth sublingually. The amount absorbed is dependent on the pH of your mouth, just like Buprenorphine.

Infact, it takes at least an hour (or more) for all the Buprenorphine to pass through mouth lining, and as a guess, Naloxone passes through a bit quicker.

And some of the posts in this thread by Added and Dread made me laugh out loud, they were so dumb! Lots of big numbers to confuse the less educated, but as long as it make you feel better, keep posting them, to keep your little cult happy. The blind leading the blind

 

[P A]

^^Doesn't know the meaning of the words "bioavailability" and "affinity." Also incapable of critical thinking.

And some of the posts in this thread by Added and Dread made me laugh out loud, they were so dumb! Lots of big numbers to confuse the less educated, but as long as it make you feel better, keep posting them, to keep your little cult happy

Now, now. No need to be so butthurt because you're too much of a fucking moron to independently research and comprehend the posted data.

 

[seep]

"Buprenorphine and Naloxone combinations: the effects of three dose ratios in morphine-stabilized, opiate-dependent volunteers" (1999)

This PDF clearly proves that the Naloxone is active

Ah, one simply has to be in awe of a paper that states:

Buprenorphine alone did not precipitate withdrawal . . .

 

[dread]

Lots of big numbers to confuse the less educated, but as long as it make you feel better, keep posting them, to keep your little cult happy. The blind leading the blind

I'm very sorry you're incapable of comprehending large numbers.

 

[Dr. Beat]

Ah, one simply has to be in awe of a paper that states:

Are you guys really that dumb?

I never said that Suboxone causes opiate withdrawal, I said the Naloxone has an effect for the first hour (or two) after taking Suboxone in some people - at minimum it reduces the Buprenorphine high for the hour (or two) as all 5 PDF's show.

Wow, I am staggered at how big some of your egos are, and how you cannot understand basic science.

Good luck on the rest of life!

 

[seep]

I never said that Suboxone causes opiate withdrawal

it does, because of the buprenorphine. The studies you are referencing are flawed.

 

[Dr. Beat]

^^Doesn't know the meaning of the words "bioavailability" and "affinity." Also incapable of critical thinking.

Now, now. No need to be so butthurt because you're too much of a fucking moron to independently research and comprehend the posted data.

Wow, put downs because I proved you wrong. So intelligent.

Stop been a pompous tool and grow up.

 

[Dr. Beat]

it does, because of the buprenorphine. The studies you are referencing are flawed.

I trust those studies more than a bunch of brain damaged drug addicts, me included

 

[Dr. Beat]

All though some of the guys here are (in reality) not that dumb, I can see from the responses that they have low emotional intelligence. So there is not much point in me trying to convince you that Naloxone is active, no matter what evidence I show, as it is like a religion on Bluelight that Naloxone is inactive.

Good luck in life!
Peace out

 

[seep]

I trust those studies more than a bunch of brain damaged drug addicts, me included

way back in Bush's 1st term I happily ate a Subutex (8 mg of naloxone-free buprenorphine) after deciding to skip the methadone clinic that day. I thought because there was no Narcan in it, it wouldn't cause me to go into withdrawal. I thought this because instead of Bluelight, I relied on Hunter College's online database. After the pill dissolved I bought a pack of Newports and walked to Central Park to listen to the birds chirp.

I think I was on my 3rd cigarette when I started praying that God's fist strike me down

 

[dread]

Ouch seep. Methadone + buprenorphine is not a nice combo.

 

[P A]

put downs

pompous tool

put downs

pompous tool

put downs

pompous tool

And you're apparently still unwilling to meet any among the multitude of contributers to this thread (most of which are clearly considerably better-educated than yourself regarding psychoactive drugs) halfway to discuss the issue intelligently. Instead, you prefer your certainty and complete lack of regard for/comprehension of the raw data, which directly conflicts with the poor, outdated conclusions drawn by your 'PDFs.' Excuse me and everyone else for our mounting disagreement based upon scientific data that could be easily invalidated (if untrue) by posting conflicting results from other sources. Instead of engaging in discussion and argument, you didactically make poorly supported claims that are demonstrably false, then proceed to bitch, sneer, and gripe when they're quickly controverted. Aside from being antisocial and unproductive, this makes you look like a raging asshat.

tl;dr - You're still a fucking moron.

 

[Hammilton]

funny... you're relying on nonscientific anecdotal reports instead of looking at actual research...

how about everyone look at the actual research and then comment on it? If you're going to say it's invalid for some reason, you had better find a flaw in design, because otherwise your objects are based on personal opinion, which is stupid.

 

[Subliminal*420]

was reading over some these posts and i have a question for you all.. I saw u said its a bad idea to Sublingually take suboxone and then use any opiate. (you're supposed to wait until a full withdrawal, 24hrs correct?)... but how long after u take ur last dose of suboxone can u take an opiate without enducing a withdrawal??

Its been about 40hrs for me since the last time I took a 4mg suboxone, and im curious if eating 2, 10mg methadone and a 2mg klonopin would help me out a bit..

Ive heard from over the site people use Benzo's to get through opiate withdrawals. But im 40hrs now w/o and Suboxones , just curious. Thanks.