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Bupe Suboxone/Buprenorphine Mega Thread and FAQ v16.0

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I don't have the background to prove anything..yet. So back to the pharmacist.

Yea, thats absurd. It seems like a conversation that would be semi insulting even behind closed doors with your P.C.P.

Not surprising tho, most of us on sub experience some form of misguided discrimination. I went to the ER a while ago because I was worried about a tooth infection. To be taken seriously, I have to make it completely obvious that I am there for antibiotics and don't even want the p.k's.

Guess it would save time if I brought a sign with me that says "Not looking for pain pills"...might cover up the "junky" tag I have acquired without my permission.
 
I am really excited right now!!!
I posted a few question this past month about the effects of Naloxone on Bupe (Suboxone). I was always skeptical of the general opinion that Naloxone has no effect on the Bupe. Very skeptical. I know many people on BL are very educated and experienced with Suboxone and I was not discounting their educated opinions and the information they generously share. Rather, I had a hard time believing that the pharmaceutical company B&R would seriously put Naloxone in the Suboxone if it doesnt have any effect. I am stubborn and I wanted some facts or studies or whatever that could prove this either way.
So here it is. And Its pretty cool what the results of this study are and the information that is given. Granted, this is one study, one conclusion. But I am still very excited to read this and I thought I would share.

http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a96619d8-5c87-4adc-9446-b6d3cb3d04aa

I hope someone else is excited and maybe this information can help someone some how. I hope you are all well. And no matter what anyone says, YOU are the only person that can decide what is best for YOU. Do not let judgmental, biased, cynical, argumentative people question what you feel is best for you. Until we find a way to literally walk in another's shoes, let's try to be more understanding and empathetic. We all struggle, we all hurt, and we all could use some help and compassion.

Peace. Scarlet
 
can u plz explain further??? im lost on that one.

the naloxone has no effect on BUPE itself. i know that for a fact. it took me a couple years to even understand that.

and if u look into it... there is no other reason they added it except for reasons that have been debunked for the most part. it was just a way to push it thru the FDA and get $$$ FUCK R&B and FUCK that stupid idiot at the pharmacy. shes lucky i have anxiety meds i was able to take to calm down... i was really planning on going up there and telling her whats up with a little paperwork to back it up.

i plan on discussing this with my DR as well, i mean i pay him. not the other way around. he needs to at least listen to me and give me a better explanation than , o thats a different med... no its not. ive been on it before and ive shot both subutex and suboxone Iv there isnt a damn bit of difference... ugh i get a little mad about this now.

people like her and my Dr make america look stupid as all hell... and greedy.
 
Yea sorry about the link, it works for me but I'm sorry it doesn't for you. Here is the part I was speaking of. It comes from a more reputable source than say, a Suboxone "patient information" site. But it is still the internet. It was just nice to see the results of a non partial parties study on the topic of the effects of Naloxone on Bupe.
I know this won't work but ill past the link to "site" my source.

http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a96619d8-5c87-4adc-9446-b6d3cb3d04aa
 
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Dang. Please disregard the above text I copied- I didn't copy the correct paragraph. Really sorry folks that was stupid!! Ok here is the paragraph I was talking about.

Physiologic and subjective effects following acute sublingual administration of SUBOXONE and SUBUTEX tablets were similar at equivalent dose levels of buprenorphine. Naloxone, in the SUBOXONE formulation, had no clinically significant effect when administered by the sublingual route, although blood levels of the drug were measurable. SUBOXONE, when administered sublingually even to an opioid-dependent population, was recognized as an opioid agonist, whereas when administered intramuscularly, combinations of buprenorphine with naloxone produced opioid antagonist actions similar to naloxone. In methadone-maintained patients and heroin-dependent subjects, intravenous administration of buprenorphine/naloxone combinations precipitated opioid withdrawal and was perceived as unpleasant and dysphoric. In morphine-stabilized subjects, intravenously administered combinations of buprenorphine with naloxone produced opioid antagonist and withdrawal effects that were ratio-dependent; the most intense withdrawal effects were produced by 2:1 and 4:1 ratios, less intense by an 8:1 ratio. SUBOXONE tablets contain buprenorphine with naloxone at a ratio of 4:1.
 
Well, fuck. I need some advice.

First things first, I'm on 10mg a day of Suboxone, scripting for ORT. I have a very fast metabolism, and the 10mg lasts until I'm asleep.

I'm travelling, and have lost most of one dose somewhere. Thankfully it's just 8mg, so I've got 2mg left. I'll be flying though, and am not looking forward to being in withdrawals on the plane...

I also have 600mg of pure (no APAP or Ibuprofen) Codeine, in pill form. Now, I want to stress that my body clears Suboxone out quickly (it's made life difficult when I was trying to stabilise a year and a half ago); for example, if I don't make sure I keep the subs in my mouth for long enough and spit out undissolved strips, I'm in withdrawals within about 8 hours or so.

I took my last dose of 10mg at 12pm today. This should hold me until late tomorrow morning, but I'd rather not spend my flight in withdrawals.

I want to stress that I don't want to get high -- I just want to hold myself over on the flight until I can get home and go to bed, then go to clinic as usual tomorrow morning.

What is my best course of action here? I was thinking I'll take the codeine tomorrow morning (unsure of dose, I just want to not be in withdrawals if I can help it as I'm seeing and ex-girlfriend when I get back!), then once that has worn off and the WD's start tomorrow eveninig I'll take the 2mg (possibly snort it? or would orally be better here) to tide me over and let me sleep.

Or is it better to try and reverse that? The only issue is I really don't want to take the codeine out of the country if I can help it; I have a letter for customs for my Suboxone, but not the codeine.

Any help is greatly appreciated!
 
Interesting read, thank you! Its cool to see bupe in action.

Naloxone did not affect the pharmacokinetics of buprenorphine and both SUBUTEX and SUBOXONE deliver similar plasma concentrations of buprenorphine. The levels of naloxone were too low to assess dose-proportionality. At the three naloxone doses of 1 mg, 2 mg, and 4 mg, levels above the limit of quantitation (0.05 ng/mL) were not detected beyond 2 hours in seven of eight subjects. In one individual, at the 4mg dose, the last measurable concentration was at 8 hours. Within each subject (for most of the subjects), across the doses there was a trend toward an increase in naloxone concentrations with increase in dose. Mean peak naloxone levels ranged from 0.11 to 0.28ng/mL in the dsose range of 1-4 mg.

Naloxone did not affect the pharmacokinetics of buprenorphine and both SUBUTEX and SUBOXONE deliver similar plasma concentrations of buprenorphine.

So, naloxone did not affect the Absorption of buprenorphine in either drug.

Since they didn't ask about euphoria or side effects, this doesn't help us figure out what is going on in the receptors though, correct? I was told the receptors are invisible. (by an M.D)

Mean peak naloxone levels ranged from 0.11 to 0.28ng/mL in the dsose range of 1-4 mg.

It does help me understand how much naloxone is being absorbed in the bloodstream.

Within each subject (for most of the subjects), across the doses there was a trend toward an increase in naloxone concentrations with increase in dose.

As expected naloxone was detected in at least 7 of the 8 patients and the levels increased with dosage.

RECEPTORVILLE WALL THEORY

The bupe/norbupe reaches the receptors first, therefore making the naloxone ineffective. So, bupe wins the race to receptorville and builds a wall that the naloxone cannot penetrate.

UNIQUE OVERRIDE THEORY

I am starting to think the override theory might be more accurate. Meaning the naloxone does get to the receptors but the bupe whips its ass so fast its hard to notice. How fast the bupe does this would be dependent on the dose, person, and the bupe/naloxone ratio in the bloodstream.
The higher % of naloxone vs bupe, the harder it would be to override.

speculation ofc..

The study seems to add credence to the idea that the naloxone would become more difficult to override for some people depending on the dose and the bupe vs naloxone ratio in the bloodstream. Therefore unique override theory is still a possibility...(I Hope) :sus:
 
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UNIQUE OVERRIDE THEORY



The study seems to add credence to the idea that the naloxone would become more difficult to override for some people depending on the bupe/naloxone ratio. Therefore unique override theory is still a possibility..

What part of the article did you get that from. I saw the ratio thing mentioned, but I interpreted it differently.

In morphine-stabilized subjects, intravenously administered combinations of buprenorphine with naloxone produced opioid antagonist and withdrawal effects that were ratio-dependent; the most intense withdrawal effects were produced by 2:1 and 4:1 ratios, less intense by an 8:1 ratio. SUBOXONE tablets contain buprenorphine with naloxone at a ratio of 4:1 (source).


Here they are talking about precipitated withdrawals and how different bupe/naloxone ratios effected it. I wish that they said what the doses were instead of just the ratios, because we don't know if the bupe doses were increased while the naloxone dosage remained the same, or vice versa. If think it's the former, and the withdrawals may not have been as intense at the higher dose since the bupe is able to fill the receptors after ripping the other opiate off, compared to lower doses that may just be enough to rip the other opiates off but not enough to take their place to relive the withdrawals.

That's my interpretation of it. I still don't think the naloxone does anything in that case, and probably only would if the ratios were reversed. That's seen in cases of bupe overdoses when 4-8x the normal dose of naloxone is needed to remove the bupe from the receptors.
 
Here is more of that article. It is really interesting information- its also great to find information like this. Like I said above this group is not associated with the brand Suboxone. I know this is long but since my link didnt work here it is. Thanks for dissecting some of this! The chart at the bottom didnt copy correctly so FYI (im sure you all can figure it out but just in case) the dosing goes information is in increasing order.

CLINICAL PHARMACOLOGY
Subjective Effects:
Comparisons of buprenorphine with full agonists such as methadone and hydromorphone suggest that sublingual buprenorphine produces typical opioid agonist effects which are limited by a ceiling effect.
In non-dependent subjects, acute sublingual doses of SUBOXONE tablets produced opioid agonist effects, which reached a maximum between doses of 8 mg and 16mg of SUBUTEX. The effects of 16mg SUBOXONE were similar to those produced by 16mg SUBUTEX (buprenorphine alone).
Opioid agonist ceiling effects were also observed in a double-blind, parallel group, dose ranging comparison of single doses of buprenorphine sublingual solution (1, 2, 4, 8, 16, or 32 mg), placebo, and a full agonist control at various doses. The treatments were given in ascending dose order at intervals of at least one week to 16 opioid-experienced, non-dependent subjects. Both drugs produced typical opioid agonist effects. For all the measures for which the drugs produced an effect, buprenorphine produced a dose-related response but, in each case, there was a dose that produced no further effect. In contrast, the highest dose of the full agonist control always produced the greatest effects. Agonist objective rating scores remained elevated for the higher doses of buprenorphine (8-32 mg) longer than for the lower doses and did not return to baseline until 48 hours after drug administrations. The onset of effects appeared more rapidly with buprenorphine than with the full agonist control, with most doses nearing peak effect after 100 minutes for buprenorphine compared to 150 minutes for the full agonist control.
Physiologic Effects:
Buprenorphine in intravenous (2mg, 4mg, 8mg, 12mg and 16 mg) and sublingual (12mg) doses has been administered to non-dependent subjects to examine cardiovascular, respiratory and subjective effects at doses comparable to those used for treatment of opioid dependence. Compared with placebo, there were no statistically significant differences among any of the treatment conditions for blood pressure, heart rate, respiratory rate, O2 saturation or skin temperature across time. Systolic BP was higher in the 8 mg group than placebo (3 hour AUC values). Minimum and maximum effects were similar across all treatments. Subjects remained responsive to low voice and responded to computer prompts. Some subjects showed irritability, but no other changes were observed.
The respiratory effects of sublingual buprenorphine were compared with the effects of methadone in a double-blind, parallel group, dose ranging comparison of single doses of buprenorphine sublingual solution (1, 2, 4, 8, 16, or 32 mg) and oral methadone (15, 30, 45, or 60 mg) in non-dependent, opioid-experienced volunteers. In this study, hypoventilation not requiring medical intervention was reported more frequently after buprenorphine doses of 4 mg and higher than after methadone. Both drugs decreased O2 saturation to the same degree.
Effect of Naloxone:
Physiologic and subjective effects following acute sublingual administration of SUBOXONE and SUBUTEX tablets were similar at equivalent dose levels of buprenorphine. Naloxone, in the SUBOXONE formulation, had no clinically significant effect when administered by the sublingual route, although blood levels of the drug were measurable. SUBOXONE, when administered sublingually even to an opioid-dependent population, was recognized as an opioid agonist, whereas when administered intramuscularly, combinations of buprenorphine with naloxone produced opioid antagonist actions similar to naloxone. In methadone-maintained patients and heroin-dependent subjects, intravenous administration of buprenorphine/naloxone combinations precipitated opioid withdrawal and was perceived as unpleasant and dysphoric. In morphine-stabilized subjects, intravenously administered combinations of buprenorphine with naloxone produced opioid antagonist and withdrawal effects that were ratio-dependent; the most intense withdrawal effects were produced by 2:1 and 4:1 ratios, less intense by an 8:1 ratio. SUBOXONE tablets contain buprenorphine with naloxone at a ratio of 4:1.
Pharmacokinetics:Absorption:
Plasma levels of buprenorphine increased with the sublingual dose of SUBUTEX and SUBOXONE, and plasma levels of naloxone increased with the sublingual dose of SUBOXONE (Table 1). There was a wide inter-patient variability in the sublingual absorption of buprenorphine and naloxone, but within subjects the variability was low. Both Cmax and AUC of buprenorphine increased in a linear fashion with the increase in dose (in the range of 4 to 16 mg), although the increase was not directly dose-proportional.
Naloxone did not affect the pharmacokinetics of buprenorphine and both SUBUTEX and SUBOXONE deliver similar plasma concentrations of buprenorphine. The levels of naloxone were too low to assess dose-proportionality. At the three naloxone doses of 1 mg, 2 mg, and 4 mg, levels above the limit of quantitation (0.05 ng/mL) were not detected beyond 2 hours in seven of eight subjects. In one individual, at the 4mg dose, the last measurable concentration was at 8 hours. Within each subject (for most of the subjects), across the doses there was a trend toward an increase in naloxone concentrations with increase in dose. Mean peak naloxone levels ranged from 0.11 to 0.28ng/mL in the dsose range of 1-4 mg.
Table 1. Pharmacokinetic parameters of buprenorphine after the administration of 4 mg, 8mg, and 16 mg Suboxone® doses and 16mg Subutex® dose (mean (%CV)).
Pharmacokinetic Parameter Suboxone®
4 mg Suboxone®
8 mg Suboxone®
16 mg Subutex®
16 mg
Cmax, ng/mL 1.84(39) 3.0(51) 5.95(38 ) 5.47(23)
AUC0-48,
hour. ng/mL 12.52(35) 20.22 (43) 34.89 (33) 32.63 (25)
 
Naloxone did not affect the pharmacokinetics of buprenorphine and both SUBUTEX and SUBOXONE deliver similar plasma concentrations of buprenorphine. The levels of naloxone were too low to assess dose-proportionality. At the three naloxone doses of 1 mg, 2 mg, and 4 mg, levels above the limit of quantitation (0.05 ng/mL) were not detected beyond 2 hours in seven of eight subjects. In one individual, at the 4mg dose, the last measurable concentration was at 8 hours. Within each subject (for most of the subjects), across the doses there was a trend toward an increase in naloxone concentrations with increase in dose. Mean peak naloxone levels ranged from 0.11 to 0.28ng/mL in the dsose range of 1-4 mg.

This shows that the naloxone had a very minimal impact on 7 of the 8 subjects.

In one individual, at the 4mg dose, the last measurable concentration was at 8 hours.
I assumed if he still had naloxone in his system after 8 hours, a higher concentration must have entered his system.

Even if its a slow metabolism thing, this shows the naloxone effects some people very differently.

So in this instance the bupe/naloxone ratio would be dependent on the individual and not the numbers on the package.

Within each subject (for most of the subjects), across the doses there was a trend toward an increase in naloxone concentrations with increase in dose. Mean peak naloxone levels ranged from 0.11 to 0.28ng/mL in the dsose range of 1-4 mg.

Its logical that an increase in dose would cause a higher concentration of naloxone in the blood, which is seemingly supported here.

My overall conclusion would be:

95-99% of people experience the receptorville theory (Theory #1)
(or the "override" happens so fast you wouldn't really notice)

People have reported a delayed onset from IV suboxone vs IV subutex.

1-5% of people are very sensitive to naloxone and might react in a way closer to the Override Theory (Theory #2)

Resulting in a longer duration before the bupe infiltrates and saturates all the receptors.

This is entirely based on my own experience, others experience, and info I have access to.
(grain of salt perhaps)

Its a work in progress.. :\

EDIT:
(I might have missed this part)

Naloxone, in the SUBOXONE formulation, had no clinically significant effect when administered by the sublingual route, although blood levels of the drug were measurable. SUBOXONE, when administered sublingually even to an opioid-dependent population, was recognized as an opioid agonist, whereas when administered intramuscularly, combinations of buprenorphine with naloxone produced opioid antagonist actions similar to naloxone

SL roa = recognized as an opioid agonist

IM roa = produced opioid antagonist actions similar to naloxone

In methadone-maintained patients and heroin-dependent subjects, intravenous administration of buprenorphine/naloxone combinations precipitated opioid withdrawal and was perceived as unpleasant and dysphoric. In morphine-stabilized subjects, intravenously administered combinations of buprenorphine with naloxone produced opioid antagonist and withdrawal effects that were ratio-dependent; the most intense withdrawal effects were produced by 2:1 and 4:1 ratios, less intense by an 8:1 ratio. SUBOXONE tablets contain buprenorphine with naloxone at a ratio of 4:1.

IV roa = produced opioid antagonist and withdrawal effects that were ratio-dependent

:?
 
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i feel what tommyboy said. there is some holes in that situation for testing the naloxone/bupe. what dosages of what opiate were the subjects that were tested on? ya know what i mean??

either way WTF does the naloxone accomplish that Dr's and pharmacies need to push suboxone over subutex?? nothing that i can see...

look ive had PW's from IV suboxone. and ive had it from subutex. it felt the same. also it goes for the other way too... ive IV'd both while dependant on bupe, or at least in full w/d from full agonists, they give the same delayed, extremely dull rush and effect.

so either theory... whats the point of the naloxone?? am i over reading something???

i got so upset about this yesterday. im still shaking mad about it really. im so tempted to go get that womans name... there were people lining up behind us so i didnt have as much time as i needed to remember to grab her name.

she thinks that naloxone reverses bupe just like other opiates... she even said all sarcastic like: you know what they give people when they OD on opiates?? i said yes... narcan, or NALOXONE!! she turned red and didnt want to listen to that.

i even told her what tommyboy said (kinda). i said something like watch an "OD on bupe" patient get a big ol shot of naloxone. it wont do the trick. u would have to use a LOT of it. and it still may not be totally effective. kinda like fentanyl in a way. i think. i cant say i know as much about that side of it...
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but i used to have both subutex and suboxone tablets on hand at any given time. using one or the other, subL or IV, it made no difference in how it felt. IF anything... i was slightly partial to the suboxone tablets when using them subL, for some reason. IV it made no difference.

I havent been able to directly compare the film both IV and subL while having subutex and suboxone tabs on hand as well. that being said i have IV'd and subL'd the films many many times and am taking them currently. subL w/alcohol to be exact, about 2mg a day right now.
 
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out of curiosity, how much water do people use when they iv the films? like is there a suggested # units per mg ( or .25 mg or whatever)?
 
as much as possible for more filtration. like i never used .5cc/ml rigs for subs. only 1ml. and tried to use at least 70-80 units of water. capt heroin could answer this one best, as he is very experienced here in this.
 
out of curiosity, how much water do people use when they iv the films? like is there a suggested # units per mg ( or .25 mg or whatever)?

I generally put one 8mg film into 30ml of water including 27 units of benzyl alcohol.
 
whats the point of the naloxone?? am i over reading something???

It clearly shouldn't be in the med.

I was trying to figure out how naloxone works and the overall effect it may have.

In the end its probably pretty staightforward.

The bupe vs naloxone ratio in the blood will determine the effect naloxone has on an individual.
 
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I just remembered, remember a couple years back i tappered of the subs. I ended up putting them in capsules numberedsomething like 1-30. Started with 2mg chunks.. then 1mg.. then Imade a small pile that weighed contained about 1mg of sub and make smaller and smaller amounts to put into each capsule for the last 10 or so. Must have been doing around .1 at a time or less at the end. I would open the capsule and snort. Sometimes i iv'd. Was able to stop completely, but I believe i started doing H again a couple months later.

Do you think the effects are more short lived when you snort bupe, or not ?

I mean its a convenient way of taking smaller and smaller doses, but could easily lead to fiending if theres a sudden buzz that goes on to wear off just as suddenly.
 
The two theories are not very important I was just trying to understand what happens. (precise action)
I have not used either via IV so my opinions were all based on SL and the information I have been able to attain.

When considering suboxone vs subutex my main question is:

Is the naloxone diminishing the euphoria you get from buprenorphine?
Honestly curious if the naloxone could grab a receptor, multiple receptors, resulting in diminished euphoria.

Is this even possible?

(I don't know much about this stuff from a science perspective)
 
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