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

It seems far more likely to me that the naloxone was originally included to pull a fast one and convince the FDA and medical community that suboxone is less abusable, then it is that it was included to "trick" users into thinking it is not injectable.

Somehow I doubt that those prone to shooting pills would simply believe that shooting suboxone doesn't work. People will try shooting anything. I just don't see people taking R&B at their word.
 
The patent for bupe-only medications was running out, so they figured out a way to make a new formulation with a new patent to make more money from drug addicts. They succesfully managed to convince lots of authorities that suboxone is somehow "less abusable" so now the clinics in some places have no choice but to use the more expensive suboxone, instead of generic buprenorphine medications. And guess who benefits from that.
 
I'm with the "Naloxone is bad" side, myself. Subutex made the beginning part of the detox process so much more tolerable than suboxone. But thats a different subject, i suppose.

Anyway, there is a fairly standard warning that one should wait 12-24 hours or longer if possible, because the bupe won't be able to activate the receptors as effectively as any opiod agonist still present. So you're might not receive as much or possibly any, benefit/relief if you take it too soon.

Regarding naloxone, my understanding of the happenings is that injected naloxone will be active, and sublingual will not. I have no idea about the outcome of other roas... I don't see why they'd be administered as I don't believe there's enough pharmacokinetic benefit to be had with suboxone. Subutex may be a slightly different story. Active naloxone is very bad as it will clear the opiod receptors while also preventing the bupe (an opioid partial agonist) from attaching as well. I always waited till I was pretty miserable before starting maintenance... although that also had something to do with my less than ideal sub-supply available.

Regarding injecting subs. I'd definitely say injecting subs is a very fiend-like behavior... but however fiendish it might be, as far as I can tell, it's really not uncommon. I imagine the thought at least occurs in every person thats used needles and is involved with bupe. There are a good number of postings on supposed easy ways to separate the bupe and the naloxone, which I'll admit to having fiendishly tried myself when I was detoxing and desperate to satisfy my needle fixation (I found (find) the injection process of it all to be somewhat meditative). I don't know how effective the effort really was as I only took 2mg "doses" in this manner. Which might not be enough to cause full precipitated withdrawal, even if it had been left as it was. Since there's no rush or euphoria when injected, the pharmacokinetic advantage is far from outweighing the risks whether it's going into withdrawal or losing your limb to infection. Oh, and injecting pills is as bad of an idea as everyone says it is... reinforcement for those with needle-fixation reading this thread.

Excuse the drawn out information that is already very widely known by many. I figure there may always be someone who's finding the infor for the first time here, so...
 
Active naloxone is very bad as it will clear the opiod receptors while also preventing the bupe (an opioid partial agonist) from attaching as well.
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This is untrue but a bit later on it...

Any composition of buprenorphine and naloxone will cause absorption of both drugs, it doesn't matter if it's a sublingual or an intravenous route (even orally, here's another catch - bioavailability and efficiency of certain ROA are 2 different things, buprenorphine is said to have ~5% bioavailability orally, that's not true, the bioavailability is much much higher but it's metabolized right away in the gut; both buprenorphine and naloxone will be taken up from stomach quite good but they'll go through first-pass metabolism).

Anyway, one might take into account that a few drugs injected i.v. at the same time may have different lipophilicity and that could make one drug or another cross BBB faster and in higher quantity. Anyway, it's not a matter of concern here. Imagine you're on buprenorphine/naloxone for some time. Levels of buprenorphine is stable at some point in blood due to its long half-life; with naloxone's very short half-life levels of it in blood doesn't build up.

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).

Buprenorphine has a very high affinity to mu-opioid receptors. Naloxone is a good antidote for morphine-like drugs and synthetic opioids overdoses. But naloxone affinity is a lot lower than buprenorphine's. Buprenorphine easily forces naloxone out of mu-opioid receptors (I'm writing about mu receptors as they're crucial). A person with no tolerance is injected with 100mg of morphine HCl and overdoses, overdose is treated with 0.5-1.0mg of naloxone HCl, then 0.3mg of buprenorphine HCl is injected - it forces naloxone out of receptors.

Now my subjective view on using buprenorphine/naloxone preparations intravenously. I wouldn't inject even a solution of lab grade buprenorphine and naloxone both at once starting buprenorphine or buprenorphine/naloxone treatment. Some trials suggest that some amount of people feel some effects from naloxone (s.l. intake). Even if it's subjective I wouldn't risk as withdrawals have always been extremely hard for me, there were times I even went paranoid after 1 day. But I wouldn't fear injecting buprenorphine and naloxone both preceded by buprenorphine-only injection.

Anyway, as I believe buprenorphine s.l. bioavailability is at most 25% (source: UCSF Drug Dependence Research Center and The General Clinical Research Center). To feel alright I had to take minimum of 16mg of buprenorphine s.l. (not buprenorphine/naloxone!). This doesn't qualify me for Suboxone treatment, I guess. I wouldn't be given two 8mg/2mg tablets a day IMO. In such circumstances methadone has been found superior to buprenorphine (edited ;)).
 
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I believe the Naloxone is present in suboxone to make the drug less abusable (naloxone makes many people feel sick) and to make full agonist opiates less effective as to further help recovering addicts.
 
adder 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). To feel alright I had to take minimum of 16mg of buprenorphine s.l. (not buprenorphine/naloxone!). This doesn't qualify me for Suboxone treatment, I guess. I wouldn't be given two 8mg/2mg tablets a day IMO. In such circumstances methadone has been found superior to methadone.
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You wouldn't be given two 8 mg tablets a day? Sure you would. That's exactly what I am prescribed.
 
I get four :( heh

I was once prescribed 32, so good for me though.

Anyway, someone said in this thread that methadone is superior to methadone, and I liked that.
 
Oh dear, it was me. %)

I meant that at some dosage comparing methadone maintenance treatment (MMT from now on) and buprenorphine maintenance treatment (BMT), MMT proves to be superior to buprenorphine at >80mg methadone. This happens when doses of 12mg buprenorphine don't work as they should (clinical trials compare 8-12mg buprenorphine to 40-80mg of methadone) BUT I've seen no randomized clinical trails for ≥16mg buprenorphine. So it's still worth nothing.

I didn't write that it's impossible to maintain people at 16mg or even at 32mg but anything beyond 16mg should light a bump if one shouldn't be switched to methadone as buprenorphine is only a partial agonist at mu receptors so at some point it won't do anything better.

I just know what is practiced here in country. There's no Subutex available (unless illegally from Ukraine to where it comes from the West, e.g. Italy), only Suboxone. After over 3 months spent on buprenorphine (no naloxone, just buprenorphine, it wasn't Suboxone) and with my first plans to zero myself with it proved impossible I switched to methadone as I could hardly call being at 16mg a state in which I could focus on my life not thinking something is wrong with me. It did the job with withdrawal generally but there were times I was still finding myself sweating (anyway, it worked great for any pain, better than methadone, no boneache, furthermore I could take even take more pain). Now I've been on methadone since February and I feel alright even though buprenorphine presents less problems with dosing in my case, after a few doses I could go on for more than 24 hours without starting to feel bad, methadone doesn't cover one day for me. I'm not against buprenorphine. If there was Subutex here, I would be keen on trying again if the dose could be worked up just a little bit from 16mg but I know it's impossible. Although a few years have passed since Suboxone is available as maintenance it's still too early, those programs supervisors often don't even know how to adjust the dose properly, that's a sad truth. And methadone has been here since first maintenance program started. And that wasn't until 1999 for sure as my friend addicted to morphine (then heroin) sought help since '97 (IIRC, it might have been even earlier). He wasn't helped, they just kept prescribing him antidepressants, sedatives, and neuroleptics. And one day he passed away, I guess that released him from misery he got into. :X

This is Poland, it's not like I go to a clinic and I'm welcomed there, and a free place at maintenance program waits for me. Getting on the program is like winning in a lottery, still after all those years. Besides I'm cross with the physician who's a supervisor of herein program.

I believe the Naloxone is present in suboxone to make the drug less abusable (naloxone makes many people feel sick) and to make full agonist opiates less effective as to further help recovering addicts.
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One more "no". Buprenorphine is enough to keep morphine, heroin etc. away from receptors as it's got a higher affinity to them than naloxone. So in that way it also helps.
 
I know first hand that you can go into precipitated withdrawals from taking suboxone to soon after taking opiates.
 
adder, Are you saying even with a dose of 16mg of bupe your withdrawals were not taken away? hmm, now i wonder what you were on... I was addicted to opiates for about 4yrs and 5 of 7 days i was snorting around 400-500mg of oxycodone a day, and the other 2 days probably 150-200mg due to lack of money.. then i switched to heroin for about 3 months and was shooting up anywhere from 25-35bags a day.. when i started suboxone i was in serious withdrawl and 8mg did the trick for me, now im presribed 12mg a day and i rarely ever feel any sort of withdrawl symptoms.. as long as i take my subs at the right time.. just dont see why anyone would chose Methadone over suboxone, unless there still trying to get high one way of another.. Methadone is horrible for your body aswell, and much more addicting than suboxone.

Basically if anyone is trying to actually kick the habbit of using prescription drugs (percocet, oxycodone, hydrocodone).. and obviously the list goes on and on.. then SUBOXONE is the choice over METHADONE.
 
I can positively tell you that even doctors lie about this. Nalaxone is completely inert in bupepe nalaxone mixes such as suboxone.
 
Not even a question. Bioafinity of bupe far out weighs nalaxone. It's an extra drug you don't need in your body. It does not block opiods or give any reaction at all bupe does. I'm not advising injection. But this is fact. Tried and true.
 
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