Suboxone, Subutex, Buprenex Info (The Big Q&A Post)

Sub Sucks and if you havent figured that out yet.. please read a few posts

Suboxone, Subutex, Buprenex Info (The Big Q&A Post)

Postby ratch » Sun Jan 30, 2011 7:54 pm

The following is a bunch of information I have extracted from numerous posts and resources. I hope this post will help anyone make an informed decision about detox, maintenance, and tapering.

Listed below is a Frequently asked Questions section.

Summary of Suboxone, Subutex, and Buprenex.

Buprenorphine is the active ingredient in Suboxone, Subutex, and Buprenex. Suboxone has a added ingredient called Naloxone. This was added to prevent abuse, and the Naloxone in Suboxone will allegedly cause immediate withdrawal if the Suboxone is injected or possibly snorted. Naloxone has also been known to induce withdrawal (wd) symptoms when some people are initially starting treatment, therefore some Drs will initially induct patients with Subutex which is just Buprenorphine without any additives.

Due to the fact that Sub has only been available for a couple of years in the United States there are a lot of questions that arise. Doctors are very misinformed about proper dosages, discontinuation of use, the existence of withdrawal symptoms, and length of withdrawal. This is due in part that most documentation pertaining to treatment, has conveniently been written to promote this medication as a harmless, pain-free way of detoxification and treatment for addiction. Most people are unaware that buprenorphine is a potent opioid with a strength 50 times greater than morphine (dose-dependent). The only reason it is considered safe is because of its partial agonist abilities, a partial agonist will only get you high or stimulate your receptors to a certain point, then it actually blocks itself out... so in actuality, taking more or high doses will do nothing but get you sick. A normal dose after you are stable for is around 6mg to 8mg. If your Dr is prescribing you amounts much higher than that (like 24mg to 96mg) then you Dr. does not have much practical experience with this medication.

So many questions have been asked regarding quitting sub, and dealing with the shockingly miserable and lengthy withdrawal symptoms that I have compiled a list of some of the frequently asked questions regarding this subject.

Prior to reading the FAQ section of this post please be aware that this stuff is NOT GOSPEL/ or written in stone there is always a chance that you have a fast metabolism, or just the right combination of brain chemistry to heal quicker. Everyone is different so please dont get discouraged no matter what you are doing, these figures are a compilation of many people that discontinued Suboxone -buprenorphine and posted their experience.

Question- How long should I stay on sub for?
Answer- This is a really tough decision, at least if you are armed with information you can make a informed choice, and be aware of potential pitfalls. The general rule of thumb seems to be that the shorter you are on sub the shorter the wds and recovery time.....However, if you are a chronic relapser, coming off years of MMT, or you just know that you are not prepared for sobriety then perhaps a longer stay might be in your best interest. Just remember that the wds from sub could last over a year if you stay on it for too long. A quick (less than 21 day stay on sub) always seems like the best/easiest option. Once you begin treatment with sub its best to get a sobriety plan in place right away. A plan can be any type of support that will help you stay away from the drugs that got you on the sub to begin with. Some people go to NA/AA meetings, some folks use alternative programs, support groups, or simply coming to this board for support. The posts that always seem to get the quickest responses around here, are from people that have cravings and need some help ASAP. People are almost always here if you need them for support.

When you hand a bottle of any type of opioids to a addict for self-administration, regardless of the partial-agonist properties (The inability to get higher) they will generally abuse them. Or in the very least try to feel "better than normal", this type of behavior is common in most addicts, and you could potentially run into trouble if, or when they decide to stop due to "behavioral dependance". Its better to think of this med as a treatment rather than a cure. Just try to be careful and remember that this is just another drug and not some magic pill or cure for addiction.

I am sure your Dr. Seems like a great/supportive/understanding person. But if they tell you that the wds from sub are going to be mild, or tell you to stay on it as long as you like, then they are misinformed. Sub wds are rarely mild and due to the extremely long half-life among other reasons, they will last for a very long time. Most of the literature and research done on sub seem to promote this miracle pill mentality. Buprenorphine is just another opioid, and no matter what excuses you can come up with or rationalizations, this is still drug replacement therapy just like methadone. Sub has been nicknamed methadone-lite or the lesser of two evils. It is addictive and a real bitch to get off, just be aware of these factors when making a decision.

Question- What is a good taper plan?
Answer- For a quick, less than 21 day detox a 1mg reduction every other day seems to work for most people. The less than 21 days time frame is assuming that your body has not yet become thoroughly re-addicted to the sub. People that stay on sub roughly past the 21 day mark seem to report a much more difficult time discontinuing sub when they try.
The first few days of sub induction its important to stay at the highest doses that don't make you sick. Most people start out between 8mg or 12mg, and after about 3 to 5 days the wds from your previous drug will begin to fade and that is when its best to start reducing your dose. Everybody is different, so if you really begin to feel wd symptoms when trying to taper, just take a little bit more to make yourself comfortable. For most people initially taking sub, a dramatic reduction will rarely be felt at all, and like previously mentioned..if it does, just take a little more!

A pill cutter or razor can be used to achieve the lower dosages, sub is also available in 2mg pils.

Day 1 (8mg to 12mg) - If all you needed was less than simply find your dose and reduce a little slower or in 1mg doses.
Day 2 (8mg to 12mg) Once a day.. or split into (2) 4mg or 6mg doses
Day 3 (8mg to 12mg)
Day 4 (6mg to 10mg)
Day 5 (6mg to 10mg)
Day 6 (6mg to 8mg)
Day 7 (4mg to 8mg)
Day 8 (4mg to 6mg)
Day 9 (4mg to 6mg)
Day 10 (2mg to 4mg)
Day 11 (2mg to 4mg)
Day 12 (2mg to 3mg)
Day 13 (1mg to 2mg) (at around this point you may start to feel the reductions)
Day 14 (1mg to 2mg)
Day 15 (1mg to 2mg)
Day 16 (.5mg to 1mg) (you can stop at this point if you are ready)
Day 17 (.5mg to 1mg)
Day 18 (.5mg to 1mg)
Days 19 to 21- (.25mg to .5mg) if you can break/cut the pills this small, this low amount will make the wds as mild as possible. A long drawn out taper is not really needed if you are not yet physically addicted to the sub, so feel free to make up your own plan, just try to jump at around the 1mg mark for the easiest overall time. (Short term sub detoxes only)

FOR LONGER TERM USE TAPERS- You can follow the same schedule as above, due to the long half life sometimes it takes up to three days to feel dose reductions. Also try to drag out the .25 and .50 mg as long as you can, if you can get away with every other day dosing that would be even better. The reason for such a long drawn out taper towards the end is to reduce the amount of sub you have in your body when you do finally stop. People have reported much milder wd symptoms that have used sub for longer periods of time if they paid their dues with a long drawn out partially painful/uncomfortable taper at extremely low doses. These low tapers lasted weeks up to a month at .5mg doses. For a lot of us addicts, this method for controlling our dosages is pretty difficult. If you just jump when you get down to .5mg your acute wds probably wont really be too bad. The problem with stopping sub is usually not really the severity of the wds, but the length of time they last for. And then there is always a very good chance that the PAWS (Post Acute Withdrawal Symptoms) will follow after the acute wds have subsided or stopped.

Most people report little difficulties tapering down to 2-4mg and then a much harder time from there down. This is the dose range where the drug operates more like a full-agonist (any regular opiate.)

Question- What happens if I jump off at a higher dose?
Answer- Most people that have jumped off at higher doses that have been on sub for long term have reported extremely severe acute WD symptoms. Its best to get as low as possible, if you are a risk taker or just have have a extremely high tolerance for wds then just going for broke without a taper will be rough. We all started sub to reduce wds, so this method wouldnt be any easier than going cold turkey off our DOC (Drug of choice) and even if you were able to handle it, the PAWS would not be any shorter.

Question- Once I stop how long will it take before I feel any symptoms?
Answer- The average half life of sub is about 37.5 hours, this means that it will take your body about a day and a half to expel 50% of whatever you took 37.5 hours prior. { If you took a 8mg dose at 8am you will still have about 4mg of sub in your body at 9:30pm the next day} You also have to take into consideration all the doses you took prior, they also stack up. So a 8mg dose you took almost 5 days ago will still be equal to around 1mg still in your body, plus add the amounts of all the doses after that together. This is why a low long taper is so important once you decide to quit. Especially if you are physically addicted to the sub. A lot of this half-life stuff has to do with how fast your metabolism works, but you will normally start feeling actual wd symptoms 24 to 72 hours after your last dose..The onset of the ACTUAL wds are watering eyes, yawning constantly, feeling tired and sluggish, about 12 hrs later the more harsher symptoms begin to appear.

How long the sub wd's will last, depends on two very crucial factors.
1) How long have you been on the sub for?
2) Did you taper? What stabilized dose did you jump off at?

Question-What are some of the wd symptoms I can expect?
Answer- Aches, pains, chills, jimmy legs (similar to Restless legs (RLS)), sneezing, diarrhea, and sleep difficulties (insomnia)... these symptoms and severity range a lot on the individual and the taper. These acute physical symptoms last a week to four weeks, and then by 4 to 6 weeks the individual is feeling pretty good physically again//(everybody is different, but these are the general times)
If you were on sub for a very long time, the chills and sleep difficulties seem to take a lot longer to feel ok again.
With a long drawn out taper most of the abovementioned symptoms are non- existent or mild . However these types of mild results seem to achieved by people that have actually suffered through many of the above symptoms during their long drawn out low dose taper for over 30 days. Meaning that they felt crappy and felt wd like symptoms during their entire taper (slight chills,fatigue,sleep trouble). A long drawn out taper may reduce or eliminate the acute wds, however anyone that has tried this method has still reported the inevitable PAWS. (A detailed description of PAWS is written below)

A less than 21 day detox usually yields a 3 week recovery period ( a week or more of PAWS)
A 21 day to 3 month stay on sub yields about a 4 to 6 week recovery period, some PAWS
A 3 to 6 month stay on sub yields about a 4 to 8 week recovery period, PAWS
A 6 month and longer stay on sub yields about a 6 to 10 week recovery period, and 3mos to 2 years of PAWS
The Actual wds from sub are really not that bad if you are jumping off at a low dose, however the biggest problem with sub wds is duration of wd's, not the intensity. It is similar to a REALLY bad flu.

Question- How long will these symptoms last?
Answer- This depends a lot on the taper, and how long you were actually on the sub for. The real strong acute stuff and sleeplessness only lasts for about 2 or 3 weeks, but the chills and just feeling crappy overall could last up to 12 weeks if you are a longer term user. And then just as you are beginning to feel a little better, a lot of people report a wave of extreme fatigue suddenly hits them. It feels like you are wearing a 500lb lead suit, and at this stage it is hard to complete almost any task, wiping your nose will take extreme effort! This massive fatigue lasts around 5 days and then partial energy slowly starts to restore over the upcoming days/weeks. Once this severe fatigue stage is over, it is usually followed by the PAWS. Which in the case of buprenorphine/sub wd's ... PAWS is the worst part of them all.

Question- What can I take to reduce/alleviate these symptoms?
Answer- Without getting into a huge explanation involving neuroscience. A lot of people report that a short acting opioid helps ease a good portion of the acute symptoms, the problem with this method is in a lot of cases, you are basically going back to the exact same drug that got you on the sub to begin with, which brings up the question..why not try tapering off your DOC instead of ever starting this treatment to begin with? As mentioned above, there are always good reasons for both sides of this argument.. Your tolerance for other opioids will also be a lot higher due to blocking abilities of buprenorphine (it sticks to your receptors and prevents other opioids from doing their job), and the half life of bup/sub is so high that your receptors are used to getting a constant flood of opioids from the sub. Taking another opioid before allowing your receptors a chance to clean off a bit (3 to 5 days) is like feeding a crumb to a lion, nothing will happen..But if you get a GIANT pile of crumbs (other opioids) you risk the chance for OD or just a HUGE waste of money.

A lot of people use imodium (loperamide) to help ease the acute wd symptoms of the sub wds (or any other opioid). IMODIUM IS NOT JUST TAKEN TO REDUCE/ELIMINATE DIARRHEA . Imodium/loperamide was actually formulated with synthetic molecules similar to demerol which is a VERY powerful synthetic opioid. Loperamide is a member of the same class of drug as is meperidine. Imodium has all the properties of an opioid without the ability to effect your brain receptors to a point of getting high. It is so strong that it will partially overide your receptors in the early stages of wd. It has been reported by plenty of people suffering from sub wds that it actually reduces the severity of most symptoms dramatically. A 8mg to 10 mg dose of lopermide should help ease wds, it sometimes takes up to 4hr to work. The liquid Imodium is allegedly faster acting. It may take a little more (12mg to 20mg), just please check all meds for interactions prior to taking them.

Please be warned- Since Imodium/Loperamide is an opioid it is physically addictive. Please keep your Imodium use limited and spaced out. The last thing you want to do is switch one addiction for another.. This rule goes for any other opioid as well. A 7 to 10 day stretch is about as close to the "getting re-addicted" safety zone as you want to get. Alternating/skipping days/weeks is also another way to avoid addiction.

Question- What if I switch or use another opioid to help with wds?
Answer- If you tapered low enough you may not need anything else. Switching to another full agonist opioid (a drug that gets you high) is like playing with fire. There is a good chance everything will work out ok, but there is also a chance that you can just get started on your old habits all over again. And this once again raises the question, why did you ever bother getting on the sub in the first place if you could control your opioid habit to begin with.

Question-What is PAWS (rebound)?
Answer- Post Acute Withdrawal Syndrome (PAWS) is a set of impairments that occur immediately after withdrawal from alcohol or other substances. The condition lasts from six to eighteen months after the last use and is marked by a fluctuating but incrementally improving course.

PAWS/Rebound-Many substances can cause rebound effects (significant return of the original symptom in absence of the original cause) when discontinued, regardless of their tendency to cause other withdrawal symptoms.. Occasionally light users of opiates that would otherwise not experience much in the way of withdrawals will notice some rebound depression as well. Extended use of drugs that increase the amount of serotonin or other neurotransmitters in the brain (opioids including buprenorphine) can cause some receptors to 'turn off' temporarily or become desensitized, so, when the amount of the neurotransmitter available in the synapse returns to an otherwise normal state after wd's, there are still fewer receptors to attach to, causing feelings of depression/fatigue until the brain re-adjusts (Receptors turn on again).

Buprenorphine PAWS/rebound seem to differ a bit from the typical/textbook definition of PAWS. The lingering effects from bup/sub seem to be more of fatigue, lack of motivation, or lack of energy that slowly restores over the course of months. Sometimes you feel ok, and a week later you will feel crappy again. Its VERY frustrating and unpredictable, and its almost impossible to gauge improvement on a day to day basis, some entire weeks/months are better than others. One thing that does appear to hold some validity, the longer you were on sub, the longer the PAWS will last. I would not state that you are feeling depression initially. However, feeling exausted, fatigued, and lazy for months is certainly a cause for depression all on its own.

Question- What can I take to reduce PAWS?
Answer- There are many supplements you can take to increase neurotransmitter production, but without many active or desensitized receptor sites there is no way to produce the proper balance of endorphins (as well as other neurotransmitters like dopamine, norepinephrine, and epinephrine) naturally to get absorbed by enough receptors to feel good. Time seems to be the best way to combat PAWS, and that is the most frustrating part of the whole ordeal.

Department of Biological Pharmaceutical Sciences, College of Pharmacy, Nihon University, Chiba, Japan.

A morphine alkaloid derivative, buprenorphine hydrochloride, induces apoptosis in NG108-15 cells. Apoptosis was detected mainly by apoptosis-specific DNA fragmentation and morphological changes. This apoptosis was dose-dependent and the time-course experiment indicated that DNA fragmentation occurred within 4 h after administration of buprenorphine hydrochloride. Specific inhibitors of the previously characterized apoptotic signal cascade as well as antagonists for opioid receptors were tested. Zn2+, herbimycin A, caspase inhibitors YVAD (Ac-Tyr-Val-Ala-Asp-CHO) and DEVD (Ac-Asp-Glu-Val-Asp-CHO), naloxone and naltrindole had no effect on apoptosis-specific DNA fragmentation. The serine protease inhibitor TPCK (N-tosyl-L-phenylalanyl chloromethyl ketone) specifically inhibited apoptosis-specific DNA fragmentation induced by buprenorphine hydrochloride; however, cell viability measurements revealed that cell death still occurred in NG108-15 cells. Thus TPCK pretreatment before buprenorphine hydrochloride administration induced apoptosis-independent cell death, presumably necrosis, in NG108-15 cells. This suggests that an unidentified serine protease, presumably functioning in the buprenorphine hydrochloride-specific death-signal cascade, could be pivotal for the rapid apoptosis observed in NG108-15 cells upon treatment with buprenorphine hydrochloride.

Repeated exposure to buprenorphine may eventually lead to changes in nuclear function and to altered rates of transcription of particular target genes by causing repeated perturbation of intracellular signal transduction pathways. Altered _expression of these genes would lead to altered activity of the neurons in which those changes occur and, ultimately, to changes
in the neural circuits in which those neurons operate. The result would be stable changes in behavior and mood. Whereas neural genes are probably regulated by hundreds of distinct types of transcription factor, two transcription factors in particular have so far been implicated in long term buprenorphine exposure: the cyclic-AMP response-element-binding protein (CREB)
and .FosB.CREB and upregulation of the cAMP pathway. CREB regulates the transcription of genes that contain a CRE site (cAMP response element; consensus sequence
(TGACGTCA) within their regulatory regions. These are only two of the many, novel and as-yet undiscovered transcriptional pathways that influence neural network modulation in cases of long-term opioid administration.
This modulation can be explained further by the fact that longer ½ life opioids, despite their many distinct actions in the brain, converge in acting upon some common systems. Prominent among these actions is the constant activation of the mesolimbic dopamine system. This
activation involves increased firing of dopamine neurons in the ventral tegmental area (VTA) of the
midbrain, and a subsequent increase of dopamine released into the nucleus accumbens (NAc) (also called the ventral striatum) and other regions of the limbic forebrain (for example the prefrontal cortex). Even after discontinuation of buprenorphine or methadone, protracted abstinence describes these various changes in drug reward and the persistent dysregulation of the
reward circuitry that underlies them. Excessive buprenorphine exposure may create changes in many
brain structures in addition to the VTA and NAc. In particular prolonged exposure, although partly
mediated by the VTA–NAc pathway, seem to involve plasticity in structures that mediate learned or conditioned responses, such as the amygdala, the hippocampus and the cerebral.
Chronic exposure to buprenorphine also reduces the birth of new neurons in the adult, newly born neurons and their integration within existing hippocampal circuits might As mentioned earlier, upregulation of the cAMP pathway within neurons is an important mechanism of tolerance and dependence regardless of the partial agonist properties of buprenorphine. A key part of this upregulation is the increased amount of PKA within certain types of neuron,which is due to the induction of particular catalytic and regulatory subunits of the kinase. Several lines of evidence indicate that induction of PKA subunits might not be achieved at the transcriptional level. For instance, upregulation of PKA immunoreactivity is not associated with detectable changes in subunit mRNA levels in certain brain areas. Similarly, alterations in CREB and .FosB do not lead to changes in PKA subunit expression, and the promoters of the PKA subunit genes do not contain identifiable response elements for these or other regulated transcription factors. Instead, work in cell culture indicates that induction of PKA might occur through reduced degradation of the subunits According to this scheme, inhibition of adenylyl cyclase by buprenorphine, for example, causes reduced levels of cAMP.As a result, more PKA molecules exist in the inactive holoenzyme form,which is less vulnerable to degradation within PROTEASOMES.Consequently, PKA subunits accumulate until a new equilibrium is achieved.
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