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  #1  
Old 01-22-2012, 11:03 AM
ilovechronic ilovechronic is offline
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Default Suboxone/Subutex (Buprenorphine V.2)

Buprenorphine

Buprenorphine is a partial mu-opioid agonist otherwise known as a mixed agonist-antagonist. For the purposes of this thread the substance called buprenorphine will be referred to as "Bupe." Bupe is derived from the alkaloid of the opium poppy called Thebaine which is not an opioid it self. Examples of Thebaine derivatives include
-Full antagonists Naloxone and Naltrexone
-Semi/synthetic full agonists Oxycodone,Oxymorphone, Hydrocodone, Hyrdromorphone
-Partial agonists Nalbuphine and Buprenorphine

Pharmacology

Buprenorphine has a unique pharmacological profile with activation of the mu-opioid receptor compared to full agonist activation induced by morphine. once converted to norbuprenorphine. Though bupe has a higher affinity for the mu-opioid receptor compared to morphine. Buprenorphine is a partial agonist but a pretty potent analgesic itself without even being converted to norbupe.

Buprenorphine has also now been shown to act as an epsilon-opioid antagonist. Buprenorphine is also a κappa-opioid receptor antagonist, and partial/full agonist at the recombinant human ORL1 nociceptin receptor.

Metabolization of buprenorphine occurs in the liver and metabolized into the full mu opioid agonist nor-buprenorphine by the liver enzyme/s CYP3A4 (CYP2C8 enzyme involved)

Norbuprenorphine is a full mu opioid receptor agonist but also an agonist at the delta opioid receptor. This is what the stimulatory perceived effects may be largely attributed to and explained by bupes' thebaine based structure.
Warning: Precipitated Withdrawal.
Because buprenorphine has partial agonist activity it causes Precipitated withdrawal syndrome where buprenorphine itself(Not naloxone) causes displacement of full agonists like morphine due to the higher affinity for the opioid receptors compared to most conventional opioid agonists.

Bioavailability:
-sublingual: 40-50%(Ethanol Solution)
-sublingual: 35-40% (Tablets)
-transdermal:~50%
-intranasal: ~50-60%

Suboxone
Suboxone is a orange flavored sublingual formula consisting of Buprenorphine and Naloxone.


Dosages formulated in: 2mgBupe/.05mgs Naloxone and 8mg Bupe/2mg naloxone.

Note: The naloxone contained in suboxone is mostly inactive when suboxone is used as intended(sublingual). Some people do experience naloxone sensitivity and irritation. Since the bupe is absorbed in the mocous membranes it is likely that when bupe is used intranasally the naloxone is probably not active in that situation either or mostly inert.

Subutex (Buprenorphine)
Subutex is a chalky white flavored tablet formulated to just contain buprenorphine but has the same precipitated withdrawal associations as suboxone. Because bupe is a partial agonist it also has antagonist activity. Buprenorphine is responsible for the the precipitated withdrawal syndrome not bupes active metabolite norbuprenorphine which is a full agonist.

Note: Precipitated withdrawal is only likely to occur in those individuals who are dependent on full agonist substances like morphine, oxycodone, methadone, diacetylmorphine, hydrocodone, hydromorphone, oxymorphone etc. The dependent individual should wait until the full agonist is completely out of their system and they are in full withdrawal before switching to a buprenorphine containing formulation. For short acting full agonists like morphine, oxycodone, etc it is recommended to wait atleast 24 hours.

Longer acting full agonists especially methadone are more tricky. Considering methadone potency it is recommended that the opioid dependent individual should wean down to at least or less than 30mgs of methadone. Also it is of great importance if the person has been on a chronic daily dose(1 month or more) of methadone that they should wait at least 72 hours before switching but 5-8 days is a more reasonable wait for those who metabolize and eliminate methadone slower or have been on it for a very long time.

The naloxone contained within suboxone is commonly attributed by buprenorphine user and even the doctor as the sole cause of precipitated withdrawal; however. it is more likely that buprenorphine itself is culprit for precipitated withdrawal especially when no injection type use is occurring.

Naloxone is known to antagonize buprenorphine and even given in the event of a buprenorphine overdose; however; naloxone has a very short half life lasting about 60 minutes.
Some have said buprenorphine may have a higher affinity for the mu opioid receptor compared to naloxone anyways but more recent studies show that it is likely the half life of naloxone that results in the bupe eventually winning out in the system.

To be continued

Last edited by ilovechronic; 01-23-2012 at 01:29 AM.
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  #2  
Old 01-22-2012, 12:28 PM
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Default Re: Suboxone/Subutex (Buprenorphine V.2)

Good post, very informative. I look forward to the continuation.
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Old 01-23-2012, 12:40 AM
Gun Lover Gun Lover is offline
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Default Re: Suboxone/Subutex (Buprenorphine V.2)

It's great to see some solid contributions!

This is the first time I've heard of the epsilon opioid receptor; got anymore info on that?
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Old 01-23-2012, 01:04 AM
SuicidalPonce SuicidalPonce is offline
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Default Re: Suboxone/Subutex (Buprenorphine V.2)

I was on Suboxone replacement therapy for a couple years. It's a great thing.

When I was on Suboxone I generally ground it up and railed it, as this has slightly higher availability. It's fairly unpleasant, but tolerable...unless you're trying to rail multiple pills at a time, in that case don't.

I switched to Subutex and I often IV'd that. It gives a nice buzz, even a little nod. There's not much of a rush unless you haven't used in awhile. One thing is you adjust very quickly...so if you bang Subutex, after a couple times you stop noticing the effect and just feel normal. It's very easy to just keep banging more chasing a high, but it never comes. You have to take a break.

You can IV Suboxone as well. The industry likes to perpetuate the myth that the Naloxone prevents IV abuse, but it's not true. It only prevents you from abusing WITH ANOTHER OPIOID. IF YOU HAVE ANOTHER OPIOID IN YOUR SYSTEM DO NOT IV SUBOXONE OR SUBUTEX.

In reality you shouldn't bang either, but especially Suboxone because the pills are full of nasty crap that can cause problems if you miss (or even if you hit). Subutex pills aren't much better, but are a definite improvement much less crap and no sugary flavorings and whatnot. If you do go this route, invest in some wheel filters and keep all your shit clean as hell.

Banging and railing subs is a double edged sword. One thing is in my experience it decreases the amount of time you have to wait to use another Opioid. When I took it sub-lingually I'd have to wait several days to be able to use with a noticable effect.

With banging and railing, it goes down to a day or two.

However, it will make your Suboxone WD set in more quickly and severely.

Overall this drug offers excellent help for addicts like myself. I suggest if you get on it you take it seriously and make an effort to follow the program with your MD.

However, addicts as they are...it's hard to resist the urge to have some fun. So if you find yourself on the program, IMHO it's better that you cop a buzz from your subs than run out and cop some dope or what not. Try taking a day or two off then railing some.

Also note, R&B (the manufacturer of Suboxone) has an excellent program where you can get your script for free. Just call Doctors in your area to see if they participate, and then all you have to do is cover visits.

I'd also note that Subutex is generally cheaper and available as a generic, so you may be able to convince your MD to write for that instead. You could also say the Suboxone gives you headaches.

Try drinking some white grapefruit juice to get your liver to trash less of the bupe.
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Old 01-23-2012, 01:04 AM
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Thumbs Up Re: Suboxone/Subutex (Buprenorphine V.2)

Thanks, there is so much misinformation on bupe even amoung experienced junkies. Maybe this will keep the seemingly daily stupid bupe question from being posted.
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Old 01-23-2012, 01:18 AM
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Default Re: Suboxone/Subutex (Buprenorphine V.2)

I actually do get a headache from suboxone which is why I shyed away from suboxone maintenence. My doc wouldn't prescribe subutex because of abuse potential. No done clinics close by either. Still searching for a doc for subutex...
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Old 01-23-2012, 01:24 AM
ilovechronic ilovechronic is offline
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Default Re: Suboxone/Subutex (Buprenorphine V.2)

Quote:
Originally Posted by funkatron54 View Post
I actually do get a headache from suboxone which is why I shyed away from suboxone maintenence. My doc wouldn't prescribe subutex because of abuse potential. No done clinics close by either. Still searching for a doc for subutex...
This is why I switched to subutex. But even just opioids in general just give me headaches sometimes. Even buprenorphine does.
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Old 01-23-2012, 03:08 AM
Strange Daze Strange Daze is offline
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Default Re: Suboxone/Subutex (Buprenorphine V.2)

Is there a feasible way to convert bupe (partial mu-agonist) into nor-bupe(full mu-agonist)? This would effectively place it in the leagues of other full agonists like oxycodone/morphone and hydrocodone/morphone amirite? What about enhancing the CYP3A4 enzyme which breaks down bupe into norbupe?
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Last edited by Strange Daze; 01-23-2012 at 03:22 AM.
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Old 01-27-2012, 09:37 PM
ilovechronic ilovechronic is offline
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Default Re: Suboxone/Subutex (Buprenorphine V.2)

Quote:
Originally Posted by Strange Daze View Post
Is there a feasible way to convert bupe (partial mu-agonist) into nor-bupe(full mu-agonist)? This would effectively place it in the leagues of other full agonists like oxycodone/morphone and hydrocodone/morphone amirite? What about enhancing the CYP3A4 enzyme which breaks down bupe into norbupe?
Yeah they call it the liver, I am not sure if nor bupe is up to par with other full agonists. I know that it is a pretty potent analgesic and that is probably due to the full agonist activity of nor bupe. It takes a good hour to a few hours for the effects of buprenorphine to peak which probably has to do with the metabolism of bupe into nor bupe.

It may be a risky situation to alter the natural enzymatic processes that metabolize buprenorphine because they require testing to check for enzyme levels because buprenorphine can cause elevated enzymes.

Last edited by ilovechronic; 01-27-2012 at 09:40 PM.
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Old 01-27-2012, 09:54 PM
funkatron54 funkatron54 is offline
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Default Re: Suboxone/Subutex (Buprenorphine V.2)

Quote:
Originally Posted by ilovechronic View Post
This is why I switched to subutex. But even just opioids in general just give me headaches sometimes. Even buprenorphine does.
Did you have any issues with your doc when switching to subutex? I imagine when I find a doc they will want to start me on suboxone even with the headaches. I've really cut down my heroin use but I still go on massive binges every month or so and end up figjting off the sickness or hanging around outside the done clinic. I love my dope nut am tired of the cycle.
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