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Why is Naloxone in Suboxone if it is 'inactive'?

N

nogills

Greenlighter
Joined
Nov 16, 2010
Messages
8
Hi, I have been reading a lot about suboxone on BL and have seen countless times that naloxone is actually inactive in the suboxone preparation. My question then is why is naloxone even in suboxone if it doesn't do anything...? I know that if you take suboxone while on another opiate (before going into w/d's) you will go into immediate w/d's because of the BUPE, not the naloxone. so...why is it there. Just to trick suboxone users into thinking you can't abuse it because of the naloxone?
 
to make you think that it's active.

and actually they thought it was originally. Apparently something about having subjects injecting these tablets for a study that couldn't pass ethical muster...
 
i think they could abuse-proof oral opiates by putting in a hefty dose of DMT or Salvinorin A....

all gravy if you just eat it as directed, but if you try to shoot or smoke it, you're in for a nasty surprise
 
nogills said:
I know that if you take suboxone while on another opiate (before going into w/d's) you will go into immediate w/d's because of the BUPE, not the naloxone.
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The precipitated w/d isn't immediate. You'll be ok for about a half hour (oral)
 
bupe has a much higher binding affinity to the MOR than the naloxone in the pill. Making the naloxone pretty much useless at those doses.
 
wungchow said:
i think they could abuse-proof oral opiates by putting in a hefty dose of DMT or Salvinorin A....

all gravy if you just eat it as directed, but if you try to shoot or smoke it, you're in for a nasty surprise
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I think if they put DMT into pills I'd have to start smoking pills. =D
 
nogills said:
Hi, I have been reading a lot about suboxone on BL and have seen countless times that naloxone is actually inactive in the suboxone preparation. My question then is why is naloxone even in suboxone if it doesn't do anything...? I know that if you take suboxone while on another opiate (before going into w/d's) you will go into immediate w/d's because of the BUPE, not the naloxone. so...why is it there. Just to trick suboxone users into thinking you can't abuse it because of the naloxone?
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It's to discourage injection. Not only does Buprenorphine have a higher affinity for mu receptors, naloxone's bioavailablity is very low when used sublingually. Thus, unless Suboxone is injected - the naloxone has no effect.

At least this is how I've always understood it.
 
Mudeltakappa said:
It's to discourage injection. Not only does Buprenorphine have a higher affinity for mu receptors, naloxone's bioavailablity is very low when used sublingually. Thus, unless Suboxone is injected - the naloxone has no effect.

At least this is how I've always understood it.
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Did you bother to read the thread? Bupe has a higher affinity whether its injected or sublingually thus the naloxone has no effect either way. YOU WILL NOT GO INTO WITHDRAWL FROM SHOOTING SUBOXONE. jesus
 
crimsonjunk said:
Did you bother to read the thread? Bupe has a higher affinity whether its injected or sublingually thus the naloxone has no effect either way. YOU WILL NOT GO INTO WITHDRAWL FROM SHOOTING SUBOXONE. jesus
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Yes, you will. But this is due to the bupe, not the naloxone. The guy you're quoting has the idea behind putting naloxone in it correct. It just didn't work out that way in practice.
 
^^
You can go into precipatated withdrawl if you have other opiates on your receptors but that doesnt have to do with shooting as it will happen whether you snort it or use sublingualy.
 
crimsonjunk said:
^^
You can go into precipatated withdrawl if you have other opiates on your receptors but that doesnt have to do with shooting as it will happen whether you snort it or use sublingualy.
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I didn't say it only happened if you shot them.
 
^^
Its cool we agree I think. I mean we both know about suboxone shit im prescribed to it and I can see you know your stuff we are just arguing semantics.
 
crimsonjunk said:
Did you bother to read the thread? Bupe has a higher affinity whether its injected or sublingually thus the naloxone has no effect either way. YOU WILL NOT GO INTO WITHDRAWL FROM SHOOTING SUBOXONE. jesus
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A) Congrats on being a jerk for no reason.

B) I specifically stated in my post that Buprenorphine has a higher affinity for mu receptors... so I'm not sure why you are telling me that. I was under the impression that the naloxone can still have some effect... guess I was wrong about that. It happens.

C) Jesus.
 
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Rest easy Ham, they got nothing on you;)

And yeah, the naloxone isnt totally inert, just overpowered. I believe they thought it had more of an effect than it does, and possibly it was a deal to achieve Suboxones CIII status. Pure speculation though. And the myths that it wont work in the case of a buprenorphine overdose aren't quite true either....it can, just in much higher doses. I am convinced that it does have a small, though not perceivable, effect when injected in conjuction with buprenorphine. The RB trials are interesting reading, esp the reports of different ratios of naloxone to bupe. Incredibly potent stuff, hundreds of micrograms can reverse a heroin overdose. And it is active orally, just very poor bioavailability. In trials around a 1000 mgs orally was found to be effective at blocking agonists actions.

Funny how a topic on bupe immediately starts to turn ADD into OD.:) If we really wanna get crazy it lets talk about the much vaunted Bupe-Norbupe idea that is so frequently passed off as truth as over there.

Actually, lets not.

Cheers
 
Naloxone is active in Suboxone. But this medication contains 2 drugs. And in presence of buprenorphine naloxone just can't bind receptors to block them because buprenorphine has higher affinity to them. But it's in no way that naloxone is inactive. It spends its time in synapses being unable to do a thing and then it's cleared fast as it's T1/2 is really short.

I don't know why it was originally put into Suboxone. Now it's still there to prevent addicts from injecting it as most of them don't know what's potency, what's affinity, and what's internal activity... So they see a blocker inside and they can be easily lied to by their doctors it's going to make them withdraw if they inject it.

I gave this as an example in my "Guide to Morphine and its Semi-synthetic Analogs":

Potency and affinity for receptors are two different things that doesn’t always go hand in hand. There is a lot of misinformation on this in the internet. The problem can be best described by a few examples:

- (-)-pentazocine is half as potent as morphine but has a greater affinity for receptors which
means pentazocine binds stronger but a larger dose is necessary for the equipotent
analgesic effect
- heroin itself has a very low affinity vs. morphine but due to its lipophilicity it is more
potent as an analgesic (the drug gets to the brain easier – crosses the blood-brain barrier
easier and a lower dose is needed, actual active metabolites are 6-acetylmorphine, morphine
and its further metabolites, heroin itself is a very weak agonist on opioid receptors)

Another thing is internal activity. Partial agonists don’t activate receptors as much as full agonists. Buprenorphine has a high affinity for receptors and can force out strong opioids such as morphine. However, it is only a partial agonist and doesn’t fully activate receptors. This is the cause of possible withdrawal symptoms when buprenorphine is given to an addict in a binge.
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