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Treatments : The Buprenorphine Hideaway
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 Message 1 of 14 in Discussion 
From: MSN NicknameSha_mtl  (Original Message)Sent: 6/17/2005 6:46 PM
I found this site called "The Buprenorphine Hideaway." A guy by the name of Nephalim worte a summary (information sheet) on his experience and knowledge of Buprenorphine, et al. Coming from the perspective of someone who was on Bup..I found it to be all the more informative..interesting and believable. He seems to be pretty well informed. If anyone cares  to comment after reading it I'd like an opinion.?


From the pages of :
 
The Buprenorphine Hideaway.

The Buprenorphine FAQ - Version 2.01 WIP

By Nephalim27

Introductory Notes:

(bupe = buprenorphine, 'done/mdone = methadone, as far as this document goes)

First and foremost:

Bupe is not a wonder drug! While I am writing this from a bupe advocate position generally speaking, I will keep the facts objective, and my goal is an easy to read compendium of relevant information. I have had mostly wonderful experiences with bupe and as such it is only natural that I would think it's a good drug for maintenance (not getting high, although that doesn't mean a maintance "buzz" isn't included, although it appears to happen rarely in most people.) Neither bupe nor mdone is better, period. It all depends on the person and their goals (not just their goals, however, as bupe can work wonderful in certain people as a lifelong maintenance drug.) In general, using the limited facts and studies we have at the current time, it appears that 'done “works�?on more people than bupe does, but by only a very small factor, and only at higher doses of 'done (90mg+).

 

Secondly, and most importantly:

Opioids are can be extremely individualized in their subjective, and even sometimes objective, effects. Some work for some, other work for others, all with different effects. With buprenorphine this is multiplied by infinity. Every aspect of the drug can be VERY individualized (even the science of opioids is poorly understood in a large regard, especially so in buprenorphine's case). One of the large reasons for this is the fact that the drug is a "partial agonist." These words ring fear into the ears of pharmacologists, as they try to this day understand the puzzle (progress has been made, which I will address, but in this layman’s humble opinion the science of bupe is still poorly understood). On top of that, one person's experience with bupe will likely vary from day to day. I will get into this further later. Nothing said in this FAQ can necessarily be true to you. Please keep this in mind.Note: All of the technical information in this FAQ is relevant only to the USA unless specifically stated otherwise.

Disclaimer:

I am not a doctor. I am not a pharmacist. I am not a scientist. I am not a licensed professional of any kind, nor do I possess any relevant degree. I have absolutely no qualifications to provide medical advice. This FAQ is for informational purposes and should not be treated as medical advice. All medical advice should come from your doctor, and if the case is that you doubt what he is saying for whatever reasons, then a second opinion is the next step, not disobeying his orders to follow anything in this FAQ. You may, however, discuss what you may have found in here with him/her, and I encourage you to try to find as much evidence of what you are trying to tell him/her as possible. Try to do this as gently as possible, as no doctor enjoys being told he is wrong.

What is Buprenorphine? What is the DATA?:

Buprenorphine, exactly like methadone, is a medication given to keep people off of heroin and improve their, and society in general's, quality of life. Buprenorphine's major clinical importance is as an agonist. Buprenorphine is *not* like naltrexone (in terms of a treatment for opioid addiction). It's antagonist/partial agonist nature is only important in the regard that it might effect how well it can do it's job as an agonist, and as a side bonus that it can blockade very effectively (at least as far as most medical literature says, however this has found to be not true (it being effective) by at least anecdotal evidence and at least at the lower end of the dose spectrum,) other opioids, much like ‘done. This IS like Naltrexone, but it is not the primary clinical importance of the drug. For the reason it's a "partial agonist," it's regarded with less abuse, addiction, and diversion potential, and is schedule III under the controlled substances act which allows it to be prescribed by qualified physicians out of their offices as per the Drug Addiction Treatment Act of 2000 (abbreviated as DATA, and called as such for the rest of this FAQ

What the DATA is, From SAMHSA (the Substance Abuse and Mental Health Services Administration):

[The Drug Addiction Treatment Act of 2000 (DATA 2000) expands the clinical context of medication-assisted opioid addiction treatment by allowing qualified office-based physicians to dispense or prescribe specially approved schedule III, IV, and V narcotic medications for the treatment of opioid addiction. In addition, DATA 2000 reduces the regulatory burden on physicians who choose to practice opioid addiction therapy by permitting qualified physicians to apply for and receive waivers of the special registration requirements defined in the Controlled Substances Act.]

What this means is that drugs approved for maintenance (which currently only included Methadone, LAAM, and Buprenorphine) that are in schedule III or above (which only includes Buprenorphine, in the Subutex and Suboxone formulations,) can be given by qualified physicians (usually psychiatrists and certain clinics) directly out of their office (via prescriptions that can be brought to your pharmacy of choice). This law was inacted (in 2000!) in order to help get more addicts into treatment by loosening some of the "klinik" restrictions, by eliminating the "klinik" completely in certain situations.

Eliminating the fat:

Can any doctor prescribe buprenorphine? What are the requirements?

No. Only doctors who meet the (simple) qualifications, and then apply to SAMHSA (who then follows through with the DEA, who issues the doctor a second, special DEA number) may prescribe maintenance medications. See the "Practical Information" section for more...practical information, including finding a doctor. The qualifications are more of a red tape then anything else. All that is necessary at minimum is an 8 hour course (if the doctor meets none of the other requirements) and a short application. If you have a doctor or psychiatrist you know and like whom isn't a part of this program, perhaps you can convince him to sign up. There is a short waiting period, which the doctor can waive by checking a box on the sign-up form. Finally, there currently is a 30 patient limit. There currently exists a bill in congress to remove this limit, due to the problems it has been causing (doctor’s using the limit as an excuse to scam patients into constant detox at high prices, and angry doctors that they have to follow such a rule they are unaccustomed to.) Stay tuned for more information on that.

Does this mean that qualified doctors can prescribe methadone or LAAM?

No. Both methadone and LAAM are in schedule II. Only Schedule III, IV, or V drugs may be prescribed by office physicians under the rules of the DATA. The drug must also be FDA approved for *opioid dependence*. Buprenorphine is the only drug that meets this criteria. There is no other drug your doctor may legally prescribe for maintenance.

UPDATE: LAAM is no longer available in the United States. Forget about LAAM. It’s bad news anyway, in this humble writers opinion, except in very very rare situations.

It is possible, and likely, that other drugs will come forth in the future that will meet this criteria, although most likely not anytime in the immediate future. Perhaps even methadone or LAAM will be rescheduled. That is fairly far out for the USA, however, although it is true of certain countries (Australia, for instance? - VERIFY). It is doubtful that mdone (or LAAM) will be rescheduled due to the highly profitable kliniks that will go out of business alone, despite the fact that both have very little abuse potential (although fairly high diversion/addiction potential.) They (the 'done lobby) are partially responsible for buprenorphine taking, what was it now, 10+ years to be FDA approved, despite it's already proven safety and it's efficiency in other countries for maintenance. They (the kliniks) were afraid of going out of business, with all their patients lining up for buprenorphine. The thought that might happen is laughable, and the possibility of them using buprenorphine in-house (as an option), without the stringent rules, would likely boost their revenues significantly.

Note: just as Methadone Maintenance Treatment is abbreviated MMT, Buprenorphine maintenance treatment is abbreviated BMT.

Bupe vs. Methadone:

A lot of heroin addicts or methadone maintenance patients have preconceived notions that bupe won't work. That is just not true. Bupe is not in general inferior to Methadone. That is a widely believed myth. It's different, but not generally inferior. It all depends on you, personally. For some people 'done will work better, for some 'bupe will work better, it's that simple. While the ceiling level for bupe is only equal to about 30mg 'done in potency, you can get it so that *you dose that twice a day or more*, and it reduces your tolerance! This mostly due to it's antagonistic/partial agonist nature. Because of this, it makes what would be equal to 30mg of 'done a hell of a lot more effective, in some people. *I am not saying bupe could ever be more potent than a full agonist. I am saying due to other factors it CAN in SOME cases work better, especially over time* Granted, it is likely very rare that bupe will get someone "higher" than 'done in general. It *can* work better though, if you give it time, and give you more flexibility. If you are on it long term and you are successful with it I am nearly positive you will get a buzz, given the fact that you were successful with it. This as always is individualized, and there are plenty of people who don't receive a buzz, but are usually on lower dosages. (UPDATE: It seems that there are a lot more people who don’t receive a buzz than I thought, but oddly enough they are happy with that, that was their aim (very little side-effects seem to go along with not getting a buzz). You shouldn’t rule out bupe because of this, but if getting a buzz is of #1 importance to you, then that should definitely effect your choice). I strongly believe either it'll work or it won't, once you give it time and find the right dose. Struggling on buprenorphine therapy is unlikely. If it doesn't work, it doesn't work, and switching to methadone is a fairly simple process, the klinik will probably be happy to have you.

Luckily there have been a lot of addicts in the community who have had good experiences with bupe and have shared those experiences, so that the community is more informed. Street addicts, however, are not, and bupe is still grossly underused. There is also the prevailing belief that bupe is for pill addicts not for heroin addicts, and this is totally bogus, minus the fact that I wouldn’t recommend a hydrocodone addict to get on methadone, of course,

A simple example of the possibilities of maintenance treatment: (4 possible scenarios of dependence, not including the guy who suceeds at abstinence the first go around. I don't think I've ever met him :P)

Person A has an "ordinary" opioid dependence. He needs a dose of agonist to keep him maintained. Methadone works, at doses most likely anywhere in the double digits, and he is happy. Buprenorphine works, and he is happy. He is the most likely to succeed with abstinence, but not necessarily so. Don't rule yourself out of this spot so quickly. This also includes the person who wants the least "opioid" necessary, he doesn’t want to get a buzz or get high, and he doesn’t want side effects. (If that’s the case, while it is totally possible bupe can give you a buzz and give you side effects equal to methadone, the chances of it not doing so warrant it being your first choice IMO).

Person B has an "ordinary" opioid dependence, but her tolerance and addiction level is sky high. She needs a high dose of agonist to keep her happy. Methadone at normal levels isn't enough. She needs a dose (most likely) of 100mg or more to be happy on methadone. Had she tried buprenorphine, it would have never reached her level of opioid dependence. She would have failed, and she would have relapsed or switched to methadone.

Person C has a "special" opioid dependence. Methadone at any dose doesn't work. Buprenorphine doesn't work. I feel bad for her. Let's hope she can get into Holland.

Person D has a "special" opioid dependence. He has a certain predisposition that makes him a good candidate for bupe. He is *likely* to have a high level of addiction, although this could depend on how long he has been using opioids, and which ones. He also is quite likely (but far from definitely, it's individualized like everything else) would have failed on methadone. Buprenorphine lowers his tolerance and addiction level, and seems to fit right, and gives him the proper maintenance that he needs.

Now, the Person A and Person B scenarios I gave you are very typical. It's what you would expect. Person C is less typical, but is still there. However, the Person D scenario tends to be overlooked. While I can't prove that certain people have a predisposition to having success on buprenorphine, I don't see how you could argue against it. Just look at how individualized opioid use is in general, and the responses people have to which drugs. What could be argued is just how often Person D comes strolling along.

Exactly what criteria Person D is likely to fall into I don't know for certain. It is entirely possible that they would have failed on methadone. Don't rule out bupe because 'done didn't work. Also, I strongly believe tolerance has nothing to do with it. I can say this from personal experience among other things. Hopefully future research will give us answers to these questions.

I will give reasons for my beliefs as to what people would fall into the "Person D" category throught this FAQ. See my personal experience and partial agonist (in pharmacology) sections especially for more information.

 Effectiveness of treatment:

In many studies done SL (sublingual) 8mg buprenorphine (a low-average maintenance dose) was shown to be slightly less effective as a maintenance drug than ~90mg 'done (keeping people in treatment and having clean urine). It was shown to be much more effective than low dose mdone (~20mg.) It was also, interestingly, shown to be more effective than LAAM, which is a full agonist. (PROVIDE REFERENCE.) Given that 8mg is basically the lowest line in terms of dose for maintenance (4mg for maintenance is possible, even lower is possible but not generally speaking,) it can be fairly safely assumed that bupe is generally as effective as 90mg of 'done in terms of effectiveness as a maintenance medication, and can also be somewhat assumed that bupe, once it your body adjusts to it, at an optimal dose, is equal to about 90mgs mdone in potency for you vs. potency for some guy on 90mgs 'done, however this is a major simplification.

The 48 hour rule:

There is one other difference to be noted. Bupe has an extremely high affinity for the opioid receptors, which means it “blockades�?them, not allowing other opioids to bind to them and forcing other opioids that do bind to them off pretty quickly and unpleasantly.

What I wrote previously was, �?I>This means (in this case) that within 48 hours of dosing, you won't be getting high on any other opioids. So if you still plan to get high "once in a while," then bupe isn't for you. It's fairly easy to do and i've done it before without much issue, but it's not "fun." It's like the 'done blockade, but stronger. The only case where this "48 hour" rule doesn't apply (generally) is in the case of doses under 8mg. However, this is, like everything else, individualized. Just don't expect to be the exception. Generally speaking, it can take up to a week before another opioid agonist can exert it's 100% full effects.�?/SPAN>

This has recently found to be largely untrue. If you are on a dose of 16mg or more, you really can’t get high for a solid 48 hours-72 hours, this is true as it was written. You get what is called an “attenuated rush�? You get a small rush, and then feel like crap. It’s like the ‘done blockade, but with an antagonistic backlash that is VERY unpleasant and I strongly recommend you don’t test the waters. However, if your dose is 12mg or less, more-so with 8mg or less, and extremely so with 4mg or less, you can get a solid 75% effect from stronger opioids, namely heroin or oxycontin, about 24 hours later. I do believe the reason this holds true is after being on buprenorphine for a long period of time, which the studies regarding this do not properly account for, your tolerance is lowered to such a large extent that you can get high easily. This is merely hypothetical, however.

If you do this however, there is the potential for an antagonistic backlash that must be mentioned. Even after those 24 hours, that bupe will be sitting there in your system for a solid week, even after taking other opioids. Occasionally it can decide “hey, get out of there, those receptors are mine!�?(not literally of course, drugs can’t “decide�?anything,) and push the other opioid off the receptors and retake it’s space. This causes nausea mainly, and other unpleasant symptoms, although they do NOT clearly resemble opioid withdrawal. This can easily be fixed by another dose of your drug of choice, even a tiny one (if you are going to do this, I strongly suggest a tiny one, opioids can kill you ESPECIALLY in the scenario I have just described! You are a prime risk for overdose, DO NOT FORGET IT).

Finally, I will mention that if you do this, which *I am not suggesting, I am merely providing information*, switching back to buprenorphine is fairly easy, if you binge for 2-3 days, just wait until you are sick (WAIT) and then take your bupe, and *hopefully* the transition back will be smooth, but there are no guarantees. I have personally found that quite ironically the higher your tolerance is, up to a point, the better bupe works.

Of course, this, again, is individualized, and your tolerance and metabolism will play a large role in all of this.

Less than daily dosing?:

With recent data, it seems that buprenorphine can be given with less than daily dosing, with every other day to tri-weekly (three times a week) still being effective in some people (PROVIDE REFERENCE). However, as always, this is very individualized, and with the recent laws in the US there seems to be no reason to attempt such a dosing schedule unless for some reason you want to (having a very slow metabolism for buprenorphine for instance, which could possibly *lower* your ability to be maintained on buprenorphine (more != better once you reach that ceiling level,) in which case less than daily dosing would be a good idea.) Discuss it with your doctor.

Continued in next post..not enough space left in this one. 

Next: Update

 Source and credit to:

Nephalim of

 
 Home:
 
He's also written something on it here:


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 Message 2 of 14 in Discussion 
From: MSN NicknameSha_mtlSent: 6/17/2005 6:56 PM

Continued from the above post:

UPDATE:

There is currently a depot formulation of bupe in clinical testing. It seems to be doing well, and you can expect it to be available in a few years. It is a little “pill�?that gets injected under your skin (like the naltrexone depot) and keeps you with a steady state of bupe for a month. No more sucking on that damn pill anymore! This, most certainly, is not for everyone, and we’ll have at the bare minimum a year to think about it.

 

Should I switch from 'done to bupe?:

Probably not. You WILL go through at least some withdrawals, and it won't be worth it, unless you really want out of the klinik or want to detox. If one klinik doesn't suit your needs, perhaps another will. If 'done isn't working for you though, then that doesn't mean 'bupe won't, and in that case also it's worth a try. However, a mdone -> bupe conversion can be tricky, and if bupe just doesn't work for you, you are in for a very rough week or so.

Should you switch from 'done to bupe if you are going to detox? Absolutely! I see absolutely no reason why this should not be done. Buprenorphine detox has been shown to be very effective. 'Done withdrawals are TERRIBLE. Bupe withdrawals are a joke in comparison. On top of that, it will work sort of like an UROD (bupe will force the 'done out of your system,) while giving you enough opioid stimulation in your brain to help the withdrawals, at the same time. If anyone knows any reason why this shouldn't be done, i'd love to hear it, as I can't think of a single thing (unless of course 'done withdrawals aren't that bad for you, but I don't think i've ever heard anyone say this.) See the withdrawals section for more information.

To further sum up:

If you want to get off H, and have not been in maintenance, should you try bupe? Of course! It's very likely to work just fine on you. And if it doesn't, there is always 'done. It's your call, of course, but it isn't something that should be ruled out without at least a full investigation.

Does bupe give you a "buzz"? YES, it does. (dependent on dose) Can you get high off of it? YES, you can (and if you say no, try telling that to the gigantic population in France that went from having a heroin problem to having a Subutex problem.) Is it as good for getting high as a full agonist? Of course not. As always, this is individualized, but not strictly linked to tolerance.

Bupe is a very individualized experience. I strongly believe that it works the best on people with a certain type of predisposition to heroin use. It seems to fix certain broken indogeneous opioid systems. Some people will LOVE bupe, and some people will find it ineffective. This is the way it goes.

One final thing to note - i'm not 100% positive, but if you are on mdone a long time generally speaking the dose has to go up once and a while, yes? (not everyone, but usually or sometimes, right?) Well with bupe, once you find that dose you will never have to increase it. (VERIFY)

General rules for starting buprenorphine:

Try to cut down as much as you can before starting bupe. If it's just for a day or two, it won't make that much of a difference.

You must wait until you are *in* withdrawals before taking your first dose of bupe. If you don't, you WILL be *in* withdrawals after taking it, and it will be much less pleasant than if you wait. In general, with the short acting opioids, including heroin, this means (from your last dose) waiting at minimum 8 hours, but 12-24 hours is strongly recommended (sleep some of it out). This is THE most important thing when starting bupe. The longer, the better. The only potential downside is the rare case where bupe doesn't work for you *at all,* then it'll be longer before you can get a working dose of another agonist.

When starting bupe, lower is better. Start with a dose of 4mg (SL), and work up slowly from there, with 2 additional doses of 2mg to a maximum first day dose of 8mg (just a general recommendation.) Exceeding 8mg during the first day will most likely just make you regret it, and is not recommended in any case. I am saying this for *your* well being, trust me.

Your doctor will be in control the first three days, and give you your doses. Be completely honest with him and do what he says.

In the case of methadone:

It is strongly recommended that you lower your dose to 30mg or less. I think this is a little on the conservative side, but until further data is available, you shouldn't stray from this number. Methadone has a nasty backlash, as you probably know, so it's much better safe then sorry.

It is strongly recommended that you wait 24 hours minimum (I STRONGLY recommend 48 hours in the case of 'done) before taking your first bupe dose.

What to expect:

This part is the most individualized. It depends on four things:

1. Your level of opioid addiction.

2. The current level (amount) and state (time since your last dose) of your opioid of choice in your body.

3. Your reaction to buprenorphine.

4. Dose of buprenorphine (remember, less is best).

Now, I honestly can't tell you what to expect. It varies far too much. Unfortunately since not only is it individualized it's weighing on a combination of four different things, it makes it nearly impossible to predict. I can promise you almost definetely you will go through at least some withdrawals, unless you really shouldn't be on buprenorphine in the first place. These withdrawals will either come before or after your first buprenorphine dose, depending on the above four things (see the guidelines for further info.) It most likely will be a mixture of both, but will weigh more to one side, and this will be mostly your choice.

These withdrawals could last anywhere from 4 hours to 4 days. It is possible that you could have mild lingering withdrawal after this period. It is also possible that you could decide to wait it out and keep trying, making the withdrawals last longer. I will make a rough estimate and say average withdrawal lasts about 24 hours. I will search for more information on this (for the next version).

How long should you wait it out if you are struggling? My opinion - if you are still having major withdrawal symptoms after 4 days since your first buprenorphine dose it's time to move on. It is unlikely that you will find buprenorphine to work for you if you are suffering *greatly* after 4 days. If you are still having mild symptoms, this is normal. This is my opinion, and I will search for more information on this as well (for the next version).

In the case of switching over from 'done the above is not necessarily true as was already pointed out earlier. Dose (and your level of addiction that comes along with that) weighs in much heavier than with short acting opioids, and withdrawal time could be longer. See the guidelines for more information.

Once again, this does not *strictly* depend on tolerance by any means.

Side effects of treatment:

There have only been 3 confirmed side effects from long term methadone maintenance treatment: Constipation, Sexual dysfunction, and Sweating. ( ) With buprenorphine, you can expect the same. The constipation is still there, but not as bad as heroin (can't compare to mdone, will try to find more information.) The sexual dysfunction is definetely still there, I can unfortunately say that personally. I have never experienced the sweating, but there is no reason to believe it is not part of buprenorphine maintenance. It's importance, however, is practically nothing. Unfortunately tolerance does not develop, or develops very little, to these three side effects of opioids. ( )

My Personal Experience:

I personally am fairly certain I would have failed on methadone. My tolerance was so high that ANY dose of anything other than good heroin (1 bag minimum) going straight into my *vein* did absolutely nothing. This was *good* quality dope, trust me. There was only one brand that I liked, the rest were no comparison. I took my last dose of H in the evening. The next morning I was sick as a dog (I smoked some opium later that night (the one before) to try hold the withdrawals longer. I didn't wait long enough. BAAAAD idea.) By the end of that day, I recieved my bupe dose and was a hell of a lot better. Those were the worst withdrawals I have ever experienced (before taking the bupe.) I was puking every 3-5 minutes, cramped so bad I couldn't hold a thought, kicking and screaming...it was actually like the movies. Anyway, the withdrawals were over by the end of day 2. In about a week, I started feeling *REALLY* high (I hadn't felt high in ages.) One night I was so high I nearly OD'ed (I was barely breathing and couldn't move,) it was the best high i've ever felt. Obviously, that ended fairly quickly, but it shows clearly that tolerance doesn't necessarily mean that bupe won't work for you. In fact IMO I think they will find it to be the opposite. I still get a buzz off 'bupe, and sometimes a fairly strong sedative effect, but rarely anything really nice, usually just a buzz. HOWEVER, it's different every day. It holds me every day, but some days are much better than others. That is my experience with bupe and my opinion.

In case you are wondering, i've cheated twice. (two small binges.)

I address my experience some more scattered throughout this document.

Bupe Pharmacology:

First of all i'd like to get something out of the way: there is alot of conflicting data about bupe. (Miller et al., 2001) I think it has to do with many factors, dose being #1. On top of that, the concept of a "partial agonist" is poorly understood. This further emphasizes how bupe can be very individualized, and work differently every time you take it. Alot of the pharmacological information you may find may be outdated and incorrect.

By the Textbook:

Buprenorphine is a semi-synthetic narcotic opioid, derivitave of thebaine. It is a mixed partial agonist-antagonist. It is a mu partial agonist and a kappa antagonist (Subutex full prescribing information). At low doses (~100mcg-1mg,) it works as a full agonist, and is slightly selective for mu. At higher doses, the antagonistic property becomes more dominate (and the partial-agonist as well) and it is competitive. (Buprenex full prescribing information, (1), (Miller et al., 2001)

Chemically, it is 1 7-(cyclopropylmethyl)-? -(1,1-dimethylethyl)-4, 5-epoxy- 18, 19-dihydro-3-hydroxy-6-methoxy- ? -methyl-6, 14-ethenomorphinan-7-methanol, hydrochloride [5?, 7?(S)]- **

It has a molecular formula of C29 H41 N04 HCl and the molecular weight is 504.10

Buprenorphine hcl is a white powder, weakly acidic with limited solubility in water (17mg/ML) (Subutex full prescribing information).

 

** Holy fuck, that's all i've got to say. (excuse my language) What's up with the ?'s? Is it different in each molecule? Could this mean, even if the chances are extremely slim, that some molecules are more effective than others? Further mystery surrounding bupe, or just simple, clinically insignificant, biochem information that I don't know, who knows. Look forward to the answer next version...

At the receptors:

Bupe has a high affinity at all 4 major opioid receptors (mu, delta, kappa, and ORL1) (Miller et al., 2001, (1))

Order of affinity (How much attraction to and how tightly it binds to each receptor):

mu > kappa > delta > ORL1 (Miller et al., 2001)

(delta has about 30 fold less affinty than mu) (Negus et al., 2002)

Bupe is a partial agonist at mu, delta, and ORL1. It is a full and potent antagonist at kappa*. (Miller et al., 2001) It's efficacy at the receptors is related to dose. The higher the dose, the less efficacious it works, (1) until it reaches a dose (~32mg SL) where increasing it any more would make it work less efficacious, although more data is necessary. (See Bupe and Dose)

Order of efficacy (how strong it works as an agonist):

ORL1 (34%) > mu > delta (Miller et al., 2001, )

The fact that it is efficient at ORL1 is very signinficant, as I don't think any other traditional opioids can stimulate ORL1 (this definetely includes morphine and heroin.) Unfortunately it has a very low affinity for it, which would require large doses to create a significant effect there.Fairly large doses have been attempted in limited studies with no interesting results, other than the apparent reversal of agonist effects. ( ) I Believe ORL1 has been shown to have similar effects to mu. Describing ORL1 is beyond the scope of this document and my knowledge.

* There is alot of conflicting studies in regards to kappa. Some say that it does indeed produce kappa agonism. This isn't the case, i'm fairly positive of it, but i'd like to know why this is. It possibly has something to do with in vitro testing, however the in vitro testing summary  (Miller et al., 2001) has determined bupe to be a kappa antagonist. I look forward to finding further information on this, as always, for the next version...

Bupe has an extremely long half-life at the receptors. It takes about a month for the drug to be completely removed from your system.

Finally, buprenorphine has a major active metabolite, norbuprenorphine, which has activity at the receptors. See metabolism for more information.

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From: MSN NicknameSha_mtlSent: 6/17/2005 7:05 PM
 
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General Pharmacological Information:

Bupe has a slow onset of action, with peak effects taking place in approximately 100 minutes. (Suboxone full prescribing information.) The peak effects for methadone take place in approximately 120 minutes (VERIFY.) The onset of action for bupe is approximately 30-60 minutes.

The duration of action depends heavily on the dosage. At a low dose (~<4mg), it is approximately 8-12 hours. At a high dose (~>16mg), it can last approximately 24-72 hours (and thus the reason less than daily dosing is possible.)

Bupe readily crosses the blood brain barrier, and is highly lipophilic.

Bupe is about 10x more potent IM than PO (oral), which is about the same ratio as morphine. You CAN eat bupe, although there is no reason to do so.

Sublingual absorption varies greatly, and can be anywhere from 25%-75%. ( ) The same percentages can be applied to an IM/SL potency comparison. However, in most people, their personal variation from one dose to another is low. (Subutex full prescribing information).

A comparison of bupe to 'done for respiratory effects found that bupe had a much higher incidence of respatory depression *not* requiring medical intervention. Bupe can cause respiratory depression, but *very* rarely anything resembling life threatening. Both drugs decreased 02 saturation to the same degree. The chances of severe respiratory depression are increased via the injection route. (Suboxone full prescribing information).

Bupe is a very safe drug for an opioid. Overdose is very difficult, even for opiate niave individuals. (Subutex full prescribing information).

See "Bupe and Dose" for further information on this topic.

Buprenorphine is approximately 96% plasma bound, primary to alpha and beta globulin (Subutex full prescribing information).

Bupe has a mean half-life plasma elimination of 37h (this can greatly vary between people) (see metabolism for further information) (Suboxone full prescribing information.) The half-life of methadone is 15-22 hours, although recent data suggested this could increase with repeated administration, and be as high as 150 hours.

Note about Suboxone: The Naloxone is present in a 4:1 ratio in both dosage strengths (8mg/2mg and 2mg/0.5mg). See "Subutex vs. Suboxone" for further information on the naloxone component.

Metabolism:

Buprenorphine undergoes N-dealkylation into norbuprenorphine and glucuronidation. This is done by the cytochrome P-450 3A4 isozyme (Subutex full prescribing information.) Norbuprenorphine is an active opioid. It is similar to bupe from what is known of it, which isn't much. From one in vitro test, it has a very similar affinities to bupe. Norbupe is a full agonist at delta and ORL1 with a low potency, but bupe antagonizes it's effects. This study also states that at the ?- (mu?) and Kappa- receptors, both bupe and norbupe are potent partial agonists, with bupe having a low effacacy and norbupe having a moderate effacacy, which we know is not true (in terms of kappa), and makes me doubt this study. (Huang et al., 2001) Further studies are necessary, or more access to information for me.

NOTE: Whether you take it orally or sublingually, approximately the same amount of norbuprenorphine is bioavailable. If, for some reason, you would want to maximize norbupe and minimize bupe, oral would be the way to go. This shows that the first-pass liver breakdown is responsible for the low oral availability of buprenorphine, quite similar to morphine. This also hints that *possibly* the reason for IV use resulting in a better high being the minimization of norbupe, but that is pure speculation.

Inhibiting/Inducing P450 3A4 will cause differences to you personally on how bupe works. What those changes would be are impossible to say without further investigation. Unfortunately, this includes HIV protease inhibitors, just like 'done. It is doubtful any significant differences/problems would arise that dose adjustment wouldn't solve.

NOTE TO CHEMISTS: There are several direct derivatives of bupe that are of much greater potential for use for pleasure, certaintly worth a try to *experienced* people. I imagine this could be difficult, due to bupe's complex structure. I'd like to find out more information about this.

Pregnancy:

Bupe is very similar to mdone when it comes to pregnancy. The good part, however, is that neo-natal withdrawals are less, for obvious reasons. (Fischer et al., 1998) Bupe also being the unique drug that it is that very rarely causes tolerance would be less likely to cause problems related to neo-natal addiction later in life if such problems do indeed exist. I have not backed this up, nor has problems later in life have been confirmed (making this impossible to back up,) this is mostly assumption and logic. I am fairly certain if you become pregnant or are planning on becoming pregnant it will be recommended you switch to bupe, if this didn't require a major dose reduction. This, however, is 150% better told to you by a doctor, and a decision made with his advice.

Partial Agonist?:

Buprenorphine best classified as a mixed partial agonist-antagonist. Does the fact that it's a mixed -antagonist make it weaker? Nope, in fact if anything it's a good thing (that it antagonizes, or rather doesn't agonize, kappa.)  Does the fact that it's a *partial*-agonist? Yes. They are two different things as far as Buprenorphine's classification is concerned. Bupe is a *very* bizarre drug, mostly due to the fact that it's a partial agonist.. I can't emphasize this enough. It has a ceiling for agonist effects (due to it's partial agonist nature), and, for example, 16mg is not twice as strong as 8mg.

Bupe can also be classified a mixed antagonist at mu because it has a very high affinity, which means it pushes whatever is there off of the receptor and takes it's place, and it's partial agonist nature (low efficacy, to put it simply) means it can't do the job that was just being done. This can cause it to be classified as having mixed -antagonistic effects, however partial agonist is a better classification as long as the dose is proper. It doesn't simply have a "low efficacy", it's better put as a "partial agonist." Read on for more theories on this.

Taking a large enough dose of bupe, out of proper clinical dosing, can be enough to do a UROD, as it pushes all the opioids out of your brain (VERIFY AND PROVIDE REFERENCE). This is what causes the problem with starting bupe. You have to go through some withdrawals. See the part on starting buprenorphine and methadone vs. buprenorphine for further information.

So what exactly does all this mean? It is easiest (and still largely accurate) to describe buprenorphine as a normal opioid agonist with a sliding ceiling (by sliding I mean different in every person, and dose and effects aren't linearly linked.)

See the section "Partial Agonist Theory" for more information on what exactly a partial agonist is, in theory (and in practice.)

Bupe and dose:

Bupe is a very weird in one regard when it comes to dose. As I already explained, double the dose doesn't equal double the effects. The reason for this is because as the dose goes up the efficiency goes down. (1) The reason for this is unknown, and related to partial agonist theory. I honestly wish I knew.

Dose for highest efficiency: 0.3mg (IM.) At this dose, it's effects are maximized and it behaves almost completely like a full agonist, acting equal to 10mg IM morphine in opiate nieve individuals. (Buprenex full prescribing information).

32mg is about the ceiling level. This ceiling level is different in every person (see bottom of this section.) For this reason, it is *possible* that in people who have a very low ceiling are those that would likely fail at buprenorphine, but further information is necessary. Increasing the dose higher than this will have the loss in efficacy overtake this increase in amount in your system. Taking doses higher than the ceiling will eventually lower it's effects, and taking very high doses will function as a straight up antagonist, (1) although again more information is necessary. (see below).

There is one study to this regard available, in rats a dose of about 1mg/kg caused an end to increase in agonist effects and a linear reversal in effacacy. In the average human this would be a dose of about 80mg, which is way more than ~32mg. Obviously, since it's a different species, the numbers can't be applied. It does seem however that this same mechanism happens in humans, but at a lower dose. Further studies are necessary. (VERIFY AND PROVIDE REFERENCE)

An 8mg-24mg dose is highly suggested for maintenance, depending on your personal reaction to the drug and dose. If you go over 16mg, I STRONGLY suggest you take it more than once a day.

It is also important to say that 32mg is the *GENERAL* ceiling. This depends on the individual, but in every individual a ceiling was reached, and usually above 8mg. (Subutex full prescribing information.) So please remember, more doesn't necessarily mean better with buprenorphine. If this is the drug for you, you will find the proper dose, and don't feel like you are getting gyped because you are only on 8-24mg.

Tips for getting the most out of bupe: (This is one of the reasons I kept emphasizing this. I wanted to make sure people knew how to get the most out of it.)

1. First and foremost, see "bupe and dose" in the above section.

2. Cut your dose in half, and take it twice a day. This is because of efficacy as I just explained. By taking it twice, you get more bang for your buck, and it's long half-life makes sure that it's effects are cumulative the second time you take it. I strongly believe this makes a big difference. However, for you, as always, it could be different. Certaintly worth a try, and definetely if your dose is over 16mg daily, or if it's just not working and you've reached the ceiling.

3. Take your dose in the evening. I have personally found that when I take it in the morning, it leaves me wanting more and having very little effect. If I wait it out and take it later in the day, it works great. Granted, I have to be a *little* sick for about an hour or two, but it's nothing really, for me at least.

4. Hold it under your tounge for longer than 15 minutes. At first it didn't take as long as it does now, it took about a half hour (to ABSORB, not to DISSOLVE.) Nowadays it takes at least an hour for it to absorb as best as it will. SL absorption varies greatly from individual to individual, which is one possible reason why bupe works for some people and not for others.

How can I tell that it's absorbing and how long it takes? I have been taking this drug for several years. I can feel it tingle on my tounge. I can taste the drug in my mouth. If my tounge is in it, it will tingle. If I take my tounge out before it's done, it will stop tingling to some extent. This is how I can tell.

You have nothing to lose by trying.

I will add more as I think of them and find out about them.

Partial Agonist Theory:

A very fascinating section coming soon. This may help to explain the reasons bupe works the way it does, and may even in the future help to find a way to maximize the drug's effacacy. (Not my summary, the theory itself).

Buprenorphine, Withdrawals, and Detox:

There are two aspects to this, withdrawals when switching to bupe and withdrawals from quitting bupe.

Withdrawals from switching to bupe:

You do have to go through at least a little withdrawals if you are addicted to opiates. This is unavoidable. Now, if you are switching from heroin, it really isn't that bad. See "General rules for starting buprenorphine" for further information.

Buprenorphine withdrawals:

Bupe withdrawals are mild at best (in comparison to other opioids.) For this reason, it is a great thing for people wanting to get off 'done but unable to deal with the withdrawals. Unfortunately, due to it's long receptor half-life like 'done, the withdrawals will last at least a month (although this too is individualized, and can be shorter.) Bupe has one major unique symptom of withdrawal that will be the centerpiece: this unbeatable fatique that will outlast all the other symptoms. All of the other symptoms, except a few minor and not worth mentioning unique ones such as stomach grumbling, are similar to other opioids. I have been told that the withdrawals are the worst during the first week and then proceed to lighten up alot. Once again, individualized.

It is strongly recommended you do NOT taper your dose really low before quitting. It doesn't work, and doesn't help. It'll make the withdrawals linger much longer. It is not a good idea. Reports of withdrawals cold turkey have been much more positive than taper attempts. (PROVIDE REFERENCE) The suggested dose to go cold turkey from is 4mg. Your body will take care of the rest (via the slow dissassociation of the drug from the receptor, lasting quite a long time, creating an auto-taper.)

I must say however, as I have in just about every other section, this is individualized. There have been people who have had bad withdrawals from buprenorphine. In this case, a different strategy is warranted, *possibly* involving a longer and lower taper.

Treatment with Naltrexone (although strongly frowned upon by myself) is possible very early after the cessation of low-dose buprenorphine treatment, within days, and does not cause severe withdrawal symptoms. (Bell et al., 1999) This certaintly is individualized, and if you are in the rare situation of having bad withdrawals after stopping low-dose buprenorphine, it is a very bad idea. (ADD BELL)

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From: MSN NicknameSha_mtlSent: 6/17/2005 7:15 PM

Continued from 4th post: (yep...this is a loong one)

Buprenorphine withdrawals:

Bupe withdrawals are mild at best (in comparison to other opioids.) For this reason, it is a great thing for people wanting to get off 'done but unable to deal with the withdrawals. Unfortunately, due to it's long receptor half-life like 'done, the withdrawals will last at least a month (although this too is individualized, and can be shorter.) Bupe has one major unique symptom of withdrawal that will be the centerpiece: this unbeatable fatique that will outlast all the other symptoms. All of the other symptoms, except a few minor and not worth mentioning unique ones such as stomach grumbling, are similar to other opioids. I have been told that the withdrawals are the worst during the first week and then proceed to lighten up alot. Once again, individualized.

It is strongly recommended you do NOT taper your dose really low before quitting. It doesn't work, and doesn't help. It'll make the withdrawals linger much longer. It is not a good idea. Reports of withdrawals cold turkey have been much more positive than taper attempts. (PROVIDE REFERENCE) The suggested dose to go cold turkey from is 4mg. Your body will take care of the rest (via the slow dissassociation of the drug from the receptor, lasting quite a long time, creating an auto-taper).

I must say however, as I have in just about every other section, this is individualized. There have been people who have had bad withdrawals from buprenorphine. In this case, a different strategy is warranted, *possibly* involving a longer and lower taper.

Treatment with Naltrexone (although strongly frowned upon by myself) is possible very early after the cessation of low-dose buprenorphine treatment, within days, and does not cause severe withdrawal symptoms. (Bell et al., 1999) This certaintly is individualized, and if you are in the rare situation of having bad withdrawals after stopping low-dose buprenorphine, it is a very bad idea. (ADD BELL)

Buprenorphine for detox:

Coming soon.

 

Subutex vs. Suboxone:

OK, alot of you hear "naloxone" and get scared. The fact of the matter is that naloxone is not absorbed sublingually. It is added so that people don't bang it. If you bang Suboxone, you will get very sick and will deeply regret it. There is no clinical difference between sublingual Subutex and sublingual Suboxone.

OK, now to get a little more technical. A tiny tiny amount of naloxone is absorbed. So little in fact, it wouldn't even qualify for ULD antagonist therapy (as told by my doctor, and Mike Strates, "inventor" of ULD Naloxone therapy, as I can't personally make sense of the numbers.) So, you ask, if it does nothing why are there two formulations? Quite honestly it's because the company wants more money. Supposedly the Subutex is supposed to be used for initiation so the naloxone doesn't cause withdrawals. Quite honestly, this is a crock of shit. The picograms you are absorbing is not going to make a difference to your withdrawals, it is downright silly. Doses of Naloxone at much higher levels have been shown not to cause withdrawals, so why would this ridiculously tiny amount do so? (PROVIDE REFERENCE)

The company decided to push to get Subutex approved sometime in the middle of the clinical trials. This is one of the reasons FDA approval took so long! It was the company that pushed for Subutex - no one else.

The difference in maintenance between Suboxone and Subutex is absolutely nothing. As someone who has taken both formulations for long periods of time at least twice each, I can personally say that from experience.

Now, the fact that you are getting a drug that has another drug merely in there to prevent you from shooting it IS insulting. It shows a real lack of trust. But it's not really up to the doctor. This is the way the USA is, and there is no way around it. So try not to think about it, and just take comfort in the fact that there is no difference, even though, alas, you cannot try and shoot it (you were thinking about it, weren't you? See, a lack of trust is warranted :P)

 

Practical information:

First and foremost - SUBOXONE IS 100% AVAILABLE. We are still waiting for the Subutex, with no promise of a date from the company.

Not every doctor is authorized to prescribe bupe. Any doctor who wishes to be only needs to take an 8 hour course, or meet any of the other easily meetable requirements. For this reason, I am positive bupe will be very easy to come by (in the near future.) When a doctor is "authorized" (s)he gets a second DEA number to be used for this purpose, which the pharmacy quite honestly has no way to verify unless they physically call up samhsa or the DEA.

Here is a link to the doctor locator: (Note: Not every doctor authorized is listed here. Not every doctor listed here is competent).

http://buprenorphine.samhsa.gov/bwns_locator/index.html

Sadly, even though Suboxone is available, and the DEA numbers are issued, that doesn't mean getting into the program will be easy. Doctors have little clue of what they are doing, nevermind what is going on. Pharmacies are skeptical of catering to heroin addicts. Let me address some of this.

SAMHSA has been spreading misinformation. They have been telling doctors that Subutex/Suboxone won't be available for three months. If your doctor doesn't know the drug (Suboxone, not Subutex yet) is available, have him call 1-877-SUBOXONE. This is the company's helpline, and they will tell him all about it.

Doctors are under the impression, thanks to Reckitt Benckiser (the company who makes Subutex/Suboxone,) that they should use Subutex for induction. There is no reason for this other than to be cautious for extreme hypersensitivity/allergy to naloxone. (See Subutex vs. Suboxone for more information on this.) Be sure to tell him that you are not afraid to be inducted with Suboxone. For this reason, and for many others, doctors do not have their induction doses, and probably won't for several months. This will delay the majority of buprenorphine maintenance a great deal.

There is a solution, and Reckitt suggests it themselves: have your doctor write a script for 3 8mg tablets or so, and then you can bring it back to the office for induction or the pharmacy could deliver it. (Suboxone full prescribing information.) If he is willing or prefers to do inductions with Suboxone, have him/her call 1-877-SUBOXONE. They will connect him to warehouses in order for him to get his induction doses.

Pharmacies are not going to have Suboxone in stock. They will most likely order it on a per prescription basis. This is even more the case because of it's price, nevermind it's use. Be sure to keep this in mind. Almost all pharmacies have next day delivery, provided that it's not backordered (which it's not at the current time.) You should have your doctor call in this induction dose the day before so it will be available. Then we come to the next problem. Pharmacies don't want to cater to junkies. Most will be very skeptical. In major cities, this really isn't an issue, but in rich/suburban communities, this can pose quite a problem. Be sure to call around and try to find a good pharmacy. A good pharmacy will make your life a whole lot better, and you should not quit until you find one. I suggest you try and find one before finding a doctor, as he may bring this up.

Moving on, here is a list of *approximate* prices. I have no idea whether your insurance will cover it, call them and ask. As of my last (and only) script for 'bupe, it came up as drug not found on my insurance. When further information is available regarding information I will provide it.

(These prices are for a month supply (30 days) at the specified daily dose. I have *roughly* extrapolated these numbers from the price of the 8mg daily monthly supply, and as such the other numbers are far from perfect. This can also vary regionally, and by pharmacy. Some pharmacies offer discounts, 10% for such a large cost is not uncommon.)

8mg  - $175

12mg - $250

16mg - $340

24mg - $510

32mg - $650

The average daily dose is 16mg. 32mg is NOT *necessarily* the best dose, due to pharmacological reasons, regardless of whatever your tolerance may be. (See "Bupe and dose" in the "Bupe Pharmacology" section.

Bupe comes in bottles of 30 and is available in 2 strengths: 8mg and 2mg, in both Subutex and Suboxone formulations. They will likely come in the original bottle for as much as your dose is divisible by 30.

The procedure for switching to bupe is simple. You go to the doctor's office the first 3 days where he administers a dose of most likely Suboxone. (S)he will likely have you in the office for 2 hours during the first dosing. The second and third days will be shorter. You will then go once or twice a week for the first month, and it is unknown how large a script you will be given. After the first month is up, you will get monthly supply scripts, once a month (obviously,) and will see your doctor (most likely) once a month for maintenance and once a week if you are recieving psychotherapy. Psychiatric fees are usually in the $200-300 range for one visit, at least in New York.

Buprenorphine is a schedule *III* (not V) narcotic under the controlled substances act. This was changed recently. Bupe most definetely deserves to be a CIII, and I believe the prior scheduling (via Buprenex) was automatic due to it's relation to thebaine, and has not been examined directly. (VERIFY)

There is one other formulation that exists: Buprenex. (as was just mentioned) They come in 0.3mg injection vials (possibly 0.6mg but i'm not sure.) They are very expensive I hear. It is important to note that Buprenex is NOT FDA approved for maintenance, it is approved for pain, and it IS illegal for that use (for your doctor (Special rules apply to opioid maintenance, see the first section). If you had a legit script, it's not illegal for you.) People have used it in desperation in the past, with mixed results, although generally the results are surprizingly favorable for such a small dose.

Overseas:

In some countries Subutex comes in an 0.4mg strength as well. This has no practical use except for PRN (as needed) use during induction. This will not be happening in the USA (the doctor will personally induct you for the first three days, making this dosage unnecessary.) It could possibly be used for tapering purposes, however the only reason why one should taper so low is if they are having unusually strong withdrawals from buprenorphine, which is uncommon. See the withdrawals section for more information.

There is also another formulation, Temgesic, but it isn't available in the USA. It's generally useless, and comes in 0.2mg and 0.4mg SL tablets. It's only use is for the same reasons listed above for the 0.4mg Subutex, and for pain, which is what it is approved for in the countries it's approved. It is interesting to note that Temgesic contains no listed inactive ingredients. I find it hard to believe it's nothing but buprenorphine, however, as 0.2mg is barely visible to the naked eye if it is at all (VERIFY), and on top of that handling the tablets could easily cause destruction of the drug. The reason why this would be worth mentioning is because it is almost asking you to inject it. There is also Temgesic-NX, which contains Naloxone just like Suboxone. You do NOT want to inject that under any circumstances.

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From: MSN NicknameSha_mtlSent: 6/17/2005 7:25 PM
Continued from above (4th) post:
 

And this leads us to our final topic, getting high..

Getting high:

YES, it IS possible to get high off of bupe. In France they have a HUGE problem with bupe being used illicitly, where they use bupe in abundance. Heroin has virtually dissapeared and bupe has become the street opioid you are likely to find. Heroin does exist there, don't get me wrong, but Subutex seems to be far more popular (VERIFY.) I can't tell you exactly how they do it, I wish I knew myself. I can tell you that they sniff or bang it. Do NOT sniff or bang Suboxone, you will get very sick.

There have been 120-something or so deaths from bupe in France. Almost always the bupe was banged, and also almost always mixed with another drug, usually a benzo.

It should be noted that respiratory depression is increased when the drug is injected. This shows that injection probably increases the euphoria aspect of buprenorphine.

The euphoric aspect of Buprenorphine appears to be increased by injection/sniffing. The drug IS highly lipophillic, which means it rushes the brain like heroin (and theoretically should provide a rush if not for it's partial agonist nature,) however, and also due to it's partial agonist nature (?), it has a very long onset of action, of approximately 100 minutes to peak effects.

I feel 100% confident in saying that bupe works just fine for getting opioid nieve individuals high. It's quite potent in that case, actually. The downside is it's long onset of action, which can take 1-2 hours if taken SL. In this case, a dose from 0.2mg to 1mg SL works wonders, however even in opioid nieve individuals overdose is difficult. Don't try it out, though! People HAVE died, and it will most likely be unpleasant at an extremely high dose. If you don't have a tolerance, 0.2mg SL should be your first dose. And give it time!

I am *NOT*, nor will I *EVER*, say bupe is superior to a full agonist for getting high.

A personal report of getting high on 0.3mg via IV in an opioid tolerant/non-dependent individual: http://www.erowid.org/experiences/exp.php3?

He compares it to Vicodin and Xanax all rolled into one, mild (without the rush, nod, or intense euphoria), yet glorious. This is just one account, however, and is far from what you will experience if you try.

Another one:

http://www.erowid.org/experiences/exp.php3?ID=13581

This one uses Temgesic 0.2mg SL tabs. He had a very strong reaction to the 1mg he took the first time, and enjoyed the rest of the bottle of 30, taking only one at a time. He takes them SL, as they are designed for.

Getting high while on buprenorphine is difficult to say the least. The drug can work with a fairly similar efficacy to oral Naltexone in blocking opioid agonists. See the "48 hour rule" in Buprenorphine vs. Methadone for further information.

This FAQ, while comprehensive for buprenorphine (USA), is meant to focus on maintenance, not recreation.

Bibliography:

G Fischer, P Etzersdorfer, H Eder, R Jagsch, M Langer, M Weninger (1998). Buprenorphine Maintenance in Pregnant Opioid Addicts. European Addiction Research;4(suppl 1):32-36

Miller W; Hussain F; Shan S; Hachicha M; Kyle D; Valenzano K J (2001). In Vitro pharmacological profile of buprenorphine at mu, kappa, delta, and ORL-1 receptors.

(1) Dum JE, Herz A. In vivo receptor binding of the opiate partial agonist, buprenorphine, correlated with its agonistic and antagonistic actions. Br J Pharmacol. 1981; 74:627-33.Heel RC, Brogden RN, Speight TM et al. Buprenorphine: a review of its pharmacological properties and therapeutic efficacy. Drugs. 1979; 17:81-110. (IDIS 121541)Kareti S, Moreton JE, Khazan N. Effects of buprenorphine, a new narcotic agonist-antagonist analgesic on the EEG, power spectrum and behavior of the rat. Neuropharmacology. 1980; 19:195-201.Sadée W, Richards ML, Grevel J et al. In vivo characterization of four types of opioid binding sites in rat brain. Life Sci. 1983; 33:187-9.

Negus SS, Bidlack JM, Mello NK, Furness MS, Rice KC, Brandt MR. (2002?) Delta opioid antagonist effects of buprenorphine in rhesus monkeys.

Huang P, Kehner GB, Cowan A, Liu-Chen LY (2001) Comparison of Pharmacological Activities of Buprenorphine and Norbuprenorphine: Norbuprenorphine Is a Potent Opioid Agonist J Pharmacol Exp Ther 2001 May 1; 297(2):688-695

Buprenex full prescribing information (USA)

Subutex/Suboxone full prescribing information (USA)

To be continued...

Copyright 2002 Nephalim

This document may be distributed only with permission from the author

 Contact Information: Email: [email protected]

Feel free to email with any (non-insulting) comments at all. I'd love to hear from you. Also feel free to share your experiences. I am looking forward to making a more complete collection of personal experiences with BMT.

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From: MSN NicknameSha_mtlSent: 6/17/2005 7:31 PM
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Treatment for heroin/opiate addiction: a primer.
by nephalim
Sat Jan 8th, 2005 at 14:42:04 PDT

At the suggestion of georgia10, I am writing this diary. I didn't think there would be much interest, but hopefully there will be, we shall see. I shall try to focus on the legal and political aspects and implications.

As a few people know, I am a former heroin addict. I have been in maintenance for 4 1/2 years - but not with methadone. There has been an alternative around for about 2 years now [in America], yet few people know of it. It's called buprenorphine, a drug that has been around for many many years, but now is available for maintenance purposes in a high-dose form under the brand names of Subutex and Suboxone. If you don't know what maintenance is, keep reading.

First of all, a plug: The Drug Reform Coordination Network (DRCNET)
They were founded in 1993 and have both a lobbying arm and a non-profit arm, similar to the ACLU. They release a weekly newsletter, and at the least I suggest you subscribe - you will learn alot about something that has fallen to the back burner in recent years with the massive issues created by the Bush Administration.

Much more below the fold

Diaries :: nephalim's diary :: :: Trackback ::

Let me provide a link to the ACLU for ease here: American Civil Liberties Union
I strongly urge anyone who isn't a member to join the ACLU, it is of my opinion that nothing is more important than our civil liberties, and I am worried that the "PATRIOT" Act has barely a mention at all - nevermind "PATRIOT II", which is downright disgusting. It's THESE things that could destroy this country - not the end of Social Security [although that is certainly not something to be ignored, don't get me wrong.]

Finally, one last shameless plug. A FAQ I wrote on buprenorphine, the maintenance medication I am taking Buprenorphine FAQ (in need of updating) by Nephalim(27)
It contains just about anything you would want to know about buprenorphine, a large amount of info on methadone, and the current law. I will reiterate much of it here. It also contains a bit about me, as well. If you read this and want more info, that's where to go. It's written as a FAQ - a format that is much more readable.

Anyways, enough with the plugs. Onwards and upwards.

There is another reason I am writing this, and that is because heroin, as well as other hard drugs, are about to become a major problem again. I will get into this later.

Everything I will say here will be as much in layman's terms as possible as opposed to technical terms, so don't jump on me for not getting something "technically" correct. This isn't the place for such things.

Let me end by saying this will hopefully be part of a series, assuming there is enough interest. Tell me what you want to see, and I will deliver.

UPDATE (day 2): (sorry, haven't figured out how to use update tags yet.) I have written this from the perspective of someone who is an advocate of maintenance treatment. Let me make it as clear as possible: there are people who feel this is not the best way to deal with heroin addiction. And while I strongly disagree, and am not going to un-bias my diary, as it is my personal opinion, I am going to show you the other side of the coin. Look towards the bottom of this diary to see what I am speaking of.

A Personal Statement

Let me get one thing out of the way: heroin has been stigmatized to no end, largely due to the needle use involved. However, due to the great increase of potency that heroin has had in the past decade or two, needle use is no longer necessary for those who aren't hardcore addicts. There is large growth in suburban sniffers and smokers, as well as large growth in use of prescription opiates (properly known as opioids, except for codeine and morphine, but I will use opiates anyway,) especially Oxycontin [generic name oxycodone], which spreads out to rural areas as well as suburban areas, and it's a HUGE problem. It's even hitting the rich - just look at Rush!

Now, back to what I was saying: is heroin (and other opiates) bad? Hell yes! I am not, nor will I EVER, advocate heroin use. But it's bad for one reason and one reason alone: the addiction/tolerance. Every single other reason is due to the drug war. Every last one. This is my opinion, and you are free to disagree. Let me also make clear that I am not downplaying the problem of addiction and tolerance: it's a HUGE, HUGE problem - as you will soon learn about. Now, a large group of street addicts are worthy of the stigma - there is no doubt there - just go to a crummy methadone clinic if you have any doubts. But there are also large groups of opiate addicts you have no idea existed. If you are so inclined, visit alt.drugs.hard [where mostly current users are], on usenet, and speak to some of these people. They are intelligent, thoughtful, friendly, and to some extent, as much as is possible, in control. Unfortunately that's still very little.

If you limit heroin to sniffing and smoking, let's just say that I would rather that than be an alcoholic. Alcohol causes permanent bodily harm, and even death. Heroin does not [overdose is a problem but could largely be controlled with legalization(at least for addicts) - by knowing what you are getting, and giving the cure for overdose out freely - and doesn't occur very often in those who aren't shooting. Yes, there is a CURE for overdose. The most common is naloxone, an opiate ANTagonist, which means it blocks opiates from working. You will feel like the worse kind of shit imaginable after getting a shot of that - but your life will be spared.] What else does alcohol do? It causes violent and other nasty behavior, for one. Opiates do not, except perhaps to those desperate to get what they need to feel normal. It causes far more deaths in car crashes, heroin doesn't impair your driving ability to THAT much of an extent - although it surely does - unless you are "nodding" (falling asleep.) It also has life threatening withdrawals - as do tranquilizers - heroin does not. It's just as addictive as smoked or sniffed heroin, and ALMOST as hard to get off of, in the long term. I just want to make the point that just because something is legal, doesn't mean it's "OK".

Let me say something again: I am not advocating opiate use! You WILL regret it! I promise you. You will be chasing that "virgin" high for the rest of your life, and might wind up unable to experience the pleasure you were once able to. It's not a fun life, and it's surely not glamorous. Let me also make it clear that there is no "soft" opiate (except, perhaps, opium.) Everyone starts, that is the people who aren't on the street, with "soft" opiates. It doesn't last - and even if it does, the differences between them and heroin are minimal at best. The thing that makes heroin so much different than other opiates is the so-called "rush" - it rushes your brain faster than any other opioid, and causes great feelings of pleasure, even after your tolerance is sky-high. Maintenance meds are different, and I will explain.

Alright, let's start with the basics.

The Basics

Well, in that personal statement, I have explained very much about the non-legal and non-political aspects of this, so I will largely try to keep this on topic. But there are many concepts I need to explain, first. I hope I am not boring you too much, and thank you for taking the time to read it. I promise I will get into something interesting.

I didn't tell you what maintenance is, for those who don't know, and it's a very fundamental concept to all of this. Maintenance is when you take another opioid instead of heroin, "maintaining" your addiction. At face value, that doesn't sound very productive. But it is, and I will now tell you why. At the current time, there are two maintenance medications: methadone, and buprenorphine[Subutex/Suboxone]. There was a third, LAAM, legally no different than methadone, which worked for a whopping three days, but it was pulled from the market (in the USA) because of lack of interest and the potential for heart attacks it causes (one of the few opiates, if not the only, to have such problems.)

So why is maintenance important, and a very necessary option for heroin and opioid addiction treatment? Why isn't it "trading one addiction for another"? Because depending on the study you are looking at, nevermind anecdotal evidence, your chances of success at long-term abstinence are anywhere from 5-15%. No one knows why this is, at least not yet, but even after the withdrawals are over, "the easy part" according to just about anyone, the hard part begins - long term abstinence. "Willing it" just doesn't seem to work - believe me, I have tried. Your brain seemingly gets rewired to treat heroin like the most basic of your biological needs, lasting anywhere from 6-12 months to the rest of your life. It's like trying to "will" yourself not so sleep, or eat, or fuck. Over the long term.

So that's why it's important, because your chances of abstinence are so low, and people just want to live normal lives (and buprenorphine is a HUGE step towards that goal, as opposed to methadone, I will explain.) The important question many must be asking themselves is what makes it any different than heroin? There is a world of difference between methadone/buprenorphine and heroin/other opiates. The first and foremost is the duration of action and the time to peak effects. They both prevent withdrawals for 24 hours (or more), meaning you will not be constantly running around looking for a fix, and you won't have the ups and downs of heroin - once stablized, you will essentially just feel normal - not high, not low. Your body will adjust to the drug and make itself work as if it wasn't there. Ideally, at least, there are some very unique people out there. The fact that it takes nearly 2 hours to reach peak effects means you just simply don't get high from these drugs - unless you are "niave" to opiates, that is, in which case you wouldn't be going into maintenance. As I said, it let's people live normal lives - people on methadone, undetectable, are lawyers, engineers, even doctors. You would be amazed.

Buprenorphine is different than methadone, and it's vital. I will get into the legal differences and implications in a minute, but let me get the final bit of basics out of the way. Buprenorphine is a "mixed opiate agonist/antagonist," well, actually, it's better described as a "partial opioid agonist." Describing this is beyond the scope of this diary. Let's just say there are several things about buprenophine that make it very different pharmacologically than methadone, which I will describe:

#1 - It is a much weaker drug. It won't leave you with a sky-high tolerance to opioids.
#2 - Following that, even though it's weaker, it has an antagonist effect - meaning it blocks other opioids from working (i.e. heroin.) - quite well in fact, but not as well as was originally believed
#3 - Following THAT, It seems to fix what heroin broke, and anecdotal evidence clearly implies that you are often more sucessful getting off buprenorphine than methadone.
#4 - Finally, the withdrawals of buprenorphine are mild at best in relative comparison to other opiates, especially methadone. Methadone withdrawals are a month of utter, utter hell.

There are two major downsides to buprenorphine, which I will also list for you.
#1 - As I said, it's, simply put, "weaker." This means that it can't satisfy all addicts - although the specific tolerance and level of addiction of the addict seems to play only a small role in this.
#2 - Due to it's opioid-blocking effects, the transition of getting on to buprenorphine from heroin or other opiates can be quite painful, especially if it's not done properly - and most doctors have no idea what the hell they are doing in this regard.

One final thing to say about buprenorphine - poorly understood, but it seems that it helps greatly with cocaine addicts. Getting into this is beyond the scope of this diary.

Well, I hope that's about it for the technical mumbo-jumbo. I hope you are sticking with it. On to some more relevant stuff.

The Law

So what is the law regarding maintenance treatment, and how has it evolved? When and how did buprenorphine come into the picture, and how is it different?
Let me start by saying methadone maintenance treatment has been around since the 1960s. It has very much proof as to it's effectiveness, as well as something very important: it is far cheaper, for society, to have an addict on methadone than on the streets on heroin. That's some food for thought for conservatives.

Methadone has some very strict laws regarding it's use. These laws vary from state to state, but under the Federal CSA (Controlled Substances Act, as amended, which is the federal law controlling almost all of prescription and illegal drugs,) only doctors with special certification, working in special clinics, can prescribe methadone. In most cases, "prescribe" isn't really the word. The users need to show up, every day, sometimes within as little as a one hour period, to get their methadone. Most clinics have a ridiculous rule that you must piss heroin positive in order to get on heroin - causing people who have been clean a few days but just can't take it to go out and get high needlessly. Only after testing clean and going every day for 6 months or more do you get any "takehomes." These takehomes start for weekends and work there way up, after several years, to monthly (in some cases.) Usually two weeks is about all you can expect. I don't know exactly how much of this is federal law, state law, or not law at all, unfortunately. I will look further into it if there is interest.

So the laws regarding methadone (and LAAM before it was discontinued,) are pretty harsh. It's hard to imagine anyone making it through that instead of just scoring a bag. Or getting screwed because of a momentary lapse of judgement. That brings us to buprenorphine, which comes in two forms - Subutex, which is just buprenorphine, and Suboxone, what is commonly used, which contains an extra ingredient - naloxone. This is added to prevent abuse. If taken normally, it does nothing. If injected, it causes massive withdrawals. This is what I am taking.

So what makes buprenorphine different? In 2000, under Clinton, the 106th Congress passed the Drug Addiction Treatment Act of 2000, otherwise known as the DATA. You can search Thomas for info on this, including the full text of the bill and the Yea's and Nay's. Unfortunately I can't link it, as it only keeps what is generated temporarily. The DATA amended the CSA (Controlled Substances Act) to allow normal doctors, who either meet certain qualifications or take an 8 hour class, and apply to the DEA and SAMHSA (Substance Abuse and Mental Health Services Administration), to prescribe Schedule III opiate agonists (opiate drugs), that are FDA approved for opiate addiction treatment (methadone is Schedule II - meaning this act doesn't apply to it.) You can get a regular prescription from a qualified physician, and fill it at your local pharmacy (alas, most local pharmacies, especially chains, are very reluctant to fill these prescriptions and in many cases will make up blatant lies.) The doctor is in full control of your treatment, and you can take home up to a month's supply as soon as he sees fit. This is a major step forward. Unfortunately, it has yet to spread to the streets, and only the upper-class drug addicts have been able to make use of the drug, and it's a real shame.

Methadone clinics are afraid to be put out of business, and have done everything they could to stonewall this and the FDA Approval of Buprenorphine for Opiate Addiction every step of the way. Now, even though this law was passed in 2000, there were no opiates that were Schedule III or above that were FDA approved for opiate addiction. Buprenorphine was in clinical trials for nearly two decades, being stonewalled every step of the way by everyone who had an interest in seeing addicts suffer or keeping the cash in the methadone lobby's pockets. It finally was approved by the FDA in October 2002, and available in pharmacies next January, 2 and a half years after the DATA was passed, despite ample evidence of it's effectiveness. Buprenorphine has been used in other countries with great success (although some abuse has been reported when heroin supplies ran dry, like in France,) for a long time. It is currently used in dozens of countries, including much of Europe, Canada, and Australia.

It's interesting to note that immediately before the FDA approved it, the DEA rescheduled it to Schedule III from Schedule V (the lowest.) Reading the petitions to the DEA was both fascinating and frightening, hearing misguided assholes demanding it be in Schedule II with things like Hydromorphone (Dilaudid) or Morphine. Luckily they decided not to put a stop to the whole thing by doing so, and they put it in Schedule III. They put both Subutex and Suboxone in Schedule III, which makes little sense, as Suboxone is specially formulated to greatly reduce any potential for abuse.

Now, let me finish this part off by saying that congress did something blatantly illegal when they passed this law - they delegated their powers to the executive branch, putting it into the law that the DEA can pull the plug at any time. While I find this unlikely at this time because this drug is used mainly for upper- and middle-class drug addicts, such as Rush I am sure (eventually at least,) it is still a scary thought. Even if they didn't put this little disclaimer in there, it would matter not, as the DEA could reschedule the drug at any time to Schedule II, putting it with methadone, and then the special provisions of the DATA would no longer apply.

Why this is important

Well first of all, we are going to see a huge resurgance in hard drug use - if we haven't already. Poor economic times lead to this - nevermind the HUGE crop in Afghanistan, which, luckily (for US,) will flood Europe and Russia and very little will wind up in the USA. The Heroin in the USA comes from Columbia (East Coast) and Mexico (West Coast,) and small amounts from East Asia, mostly on the East Coast. But it's still a matter of supply and demand, and I can tell you that scoring heroin on the streets of New York has never been easier.

So with a resurgance in drug problems, we have two issues - the first being getting the people that need help, help. The second being the "war on drugs" might return as it started - and that won't be pretty. With drug laws being toned down or outright decriminalized in many places, I am afraid of a backlash. The homosexual "acceptance" has had a backlash - that's for sure.

In fact, the drug war bears a great resemblence to the evolution of homosexual rights, only the drug war is further behind. First, it was a crime. Then, it was a disease. Now, (for homosexuality,) it is a right - yet still viewed as a problem by most in society. I am waiting for drug users to reach the next step.

Drug law reform needs to be properly framed, and treatment as opposed to incarnation needs to be the only option. Sending low-level non-violent drug users to jail is not only counterproductive, but a huge waste of money, and ruins many, many lives. Here in New York the Rockefeller Drug Laws were laxed - which is a big step for us here, but it is far from what can be deemed "reform."  Somehow we need drug laws that will discourage new users, even though I personally believe it to be a civil right, many others do not. I think what I do with MY body is MY right. And if you disagree, I wonder why most feel that people can do what they want with their body when it comes to abortion, but not with drugs. If proper heroin maintenance is given to addicts, the problems of heroin addict to society would virtually dissapear.

Besides that, the drug war is a complete and utter failure. It causes crime, causes people to become homeless and poor, causes needless deaths, the repercussions are endless - and this is blatantly obvious. We cannot continue such a fundamentally flawed policy, whether you believe drug use is a right or not (the founding fathers seemed to think so, I might add.)

Why else is this important? Because as I said way up at the top, there is nothing more important in my mind than our civil liberties - and it is something that must be defended - it is the last door to full-blown tyranical fascism that needs to be crossed. We must fight tooth and nail to stop any futher incursions into our liberties as Americans. (BTW, look up "liberty" in the dictionary. Tell me if you can honestly say to me that currently applies to America.)

Perhaps in another edition I will write the history of the drug war and drug use in America - and how, seemingly, drug use wasn't really a problem until the government propagandized it and created prohibition, the correct word for the current situation. Alcohol prohibition didn't work, and drug prohibition is working far less. Ending drug prohibition would go a long way towards curbing crime on all levels.

Here are some links to wet your whistle with on the drug war, and why this is important:
An Open Letter to Judge Rufus G. King III - A nice summary on the problems with the drug war.
The current DRCNET "chronicle" (newsletter)

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Thank you for reading this. I know it was long and contained lots of boring info you probably don't care about. Tell me where you want me to take this and it will be done, assuming the interest is there. I can talk about other drugs, or (/and) talk about prohibition and the drug war throughout American History.

UPDATE: It seems I have finally made the recommended diary list. I want to thank everyone for their very kind words, and let them know it's a pleasure to be able to write something that people find interesting or helpful.

Finally, I have decided to continue this into a series, with the next diary being on the history of drug prohibition and where we are now in the "war on drugs," and how exactly it's a problem. I will continue with what should be done in the future - a topic for debate - and then write some diaries on other drugs as I have done with heroin here. Please give me your input, this certainly isn't set in stone.

UPDATE (day 2): Here's what I promised, the other side of the coin. Here is a very well written post by glibfidget, who is also a former heroin addict, along with my rebuttal, to someone who feels very strongly that maintenance is not a good thing, and that abstinence via NA/AA is the way to go. I strongly disagree, and you will see both his and my arguements.

I want to say first that both he and someone down below stated that there is virtually no success rate with methadone or buprenorphine, and that it has little proven value. This is simply completely bogus, and I will provide the statistics to back up my claims.

I also want to say something very important I should have said in the first place: methadone and buprenorphine are VERY different medications, and there are strong downsides to methadone which don't exist with buprenorphine. I will make a list of the downsides of methadone that I didn't mention. And this is the reason I feel very strongly about buprenorphine as opposed to methadone - but for some people methadone is the only option - and I can say with absolute certainty that I *HAVE* met these people.

Downsides to Methadone (and compared to buprenorphine)

#1 - You have to go to a clinic every day for a long time at the beginning, which I did mention, but I didn't mention the fact that you are surrounded by drug addicts while doing so, and there are usually drug dealers parked outside (especially the lower-class clinics, there are many different "types" of methadone clinics, some for street addicts, some for upper-class addicts, and the latter is far superior.) Buprenorphine doesn't have this problem.

#2 - It is extremely difficult to get off of methadone. You have, in most cases, withdrawals worse than heroin, and lasting over a month (as opposed to a week with heroin.) Buprenorphine has extremely mild withdrawals in most cases, but they are long lasting like methadone, about a month (compared to about a week with short-acting opiates.)

Well, that's really it. I think I mentioned everything else. But these two things are very important. Let me know if I am missing anything.

Finally I want to say that this diary has been misinterpreted that I was suggesting lifelong maintenance. I was not. While that is certainly a possibility, especially with certain individuals, the goal of maintenance treatment is that you will get off of it eventually, and that should be very clear.

The Post by glibfidget including my Response

You said alot, and I hope I do your post justice in the response...

Let me say first of all that it's fine that you disagree, and I realize that I wrote the diary from one specific perspective, and I even added an update at the bottom that I needed to make it less biased, even though I AM biased in this regard. I have to say though quite honestly I disagree with alot of what you said, and I do find it "disgusting" to a large extent - but much like you, I am not going to attack you, and respect your views. You had success with a certain route, and that is important. Everyone is very different when it comes to this, and anecdotes should not be ignored. But neither should the scientific statistics. Anyway, let me get to what you said.

I gave you a 4 for the diary. Politically, I agree with most of what you said. Personally, it was well written and thought provoking; however, I find the mindset you subscribe to disgusting. I don't mean that as a personal attack on you, though I suppose by nature it is, but keep in mind I certainly don't know you. And, perhaps disgusting is a strong choice of words. And while I try not to be judgmental on this topic when I run into guys like you, that sort of mindset evokes some fairly strong gut reactions for me. Your way of thinking kept me (and people like me, ergo you) sick for a long, long time.

It did? Most of the people I know that tried to go clean tried being clean many many times, always going back to heroin. (I don't know many real-life junkies, well...not very well. Most of the people I know have been in online forums, I was alone in my habit, at least for the most part.)

Continued in next post:

http://www.dailykos.com/story/2005/1/8/17424/52761


Reply
 Message 7 of 14 in Discussion 
From: MSN NicknameSha_mtlSent: 6/17/2005 7:33 PM

Continued from above post:

What I personally agree with is that people need to try being clean, if they feel it's their place. What I don't agree with with is that they should try it right off the bat.

Have you ever seen the look in a junkie's eyes, one who has tried to be clean over and over again and just keeps failing? I have seen it many times, and it's one of the most horrible things you can see. To have these people keep trying to get clean in futile attempts is nothing short of inhumane.

I did take pot-shots at NA/AA, and I do NOT subscribe to their "faith-based" approach. I think it's a solution, but I think that accepting god as a solution to a problem is nothing short of a "cheap way out" as I believe you put it. That doesn't mean that I don't believe in any type of counselling period. I don't believe in group therapy with other junkies - it's a ridiculous idea. If it worked for you, great, but I think overall it is so ineffective and it puts people in a position they shouldn't be in that I wouldn't recommend it for ANYONE...

I am getting ahead of myself. Let me try and address them as you say them.

So, while I can't say it without it coming off as a personal attack (as it's a personal topic for the both of us), I mean it generally. Again, I don't know you.

What I do know something about is addiction, and addicts of all stripes. Background on me, some of it anyway, I'm a recovering addict myself. It's pretty much ruled my life from adolescence on (I'm in my late 20s now, so say 15+ years). I've been in numerous inpatients, outpatients, detox wards, mental hospitals, jails, etc over the years. Believe me when I say I understand the issues involved intimately.

I see that your history is littered with the most horrible of places. What is so great about buprenorphine is it lets you go to your doctor, take home a script, and return to a normal life. Then, and only then, when you are completely into a normal life and a normal mindset removed from drugs does anyone really have a chance at success with abstinence that I feel they should try. I think the chances of abstinence right off the bat are so low, and the chances of severe harm with relapse - guilt, further self-doubt, even death from overdose which happens most often with the relapsing junkie, that it simply doesn't even warrant trying at that point - unless there is simply no other option. But that is my opinion, and everyone is different, and there are always unique situations.

I also know, for me, what works and what doesn't.

I also want to make it clear what works for you doesn't necessarily work for other and vice versa. I think I already made this clear. In this world, everyone is very unique, and there is no one solution for everyone. Your story is but one anecdote. I know several thousand. I am sure you know plenty as well.

Indeed, in the recent history of addiction treatment (last 100 years or so), psychiatry, psychology, criminal justice, certainly pharmacology, have all failed in providing effective and holistic treatment for the addict.

Agreed.

AA and NA have been, consistently and unequivocally, the constant form of treatment that has proven most effective for long-term sobriety. What's more, any psychiatrist, psychologist, parole officer, or even pharmacist who knows anything about this and isn't trying to sell you something, will absolutely tell you the same thing.

Sorry, I disagree. My first doctor, a doctor from overseas in France who was personally responsible to a large degree for helping Paris get off heroin (at that time) and bringing buprenorphine here, understood many of the things I said, and I was so lucky to have had him. He thought leaving yourself on your own was the worst thing you could do - but surrounding yourself with other junkies was the second worst.

I DO agree that AA/NA is the most effective group therapy available - period, and that's an important thing to say. It is a well-designed program that works well for alot of people - especially alcoholics where in their case alcohol isn't illegal and the situation is very different from a junkie. But as I said a while back, a large hunk of their success is due to people giving themselves to god, and doing so for convenience. I am an atheist, and I find it disgusting, for personal reasons. People need to learn that they have the power over themselves, not some invisible force has the power over them.

I don't want to turn this into a discussion on god. I will address the issues of group therapy (alone) vs. medical treatment with therapy (of any kind.)

In your diary, you stated simply that long-term abstinence isn't for you because...the odds aren't good.

I should have made it clear that I meant that it isn't for me right off the bat. It isn't for just about anyone right off the bat, unless they are extremely special. The potential benefits don't outweigh the risks, and their chances of success are the lowest of all. Your mind is simply too fucked up to just go cold turkey and be clean - it just doesn't work in 99% of people.

I will likely have a go at abstinence sometime this year. I am afraid, but I am ready. It took me longer than most wait, but I didn't want an exercize in futility, it simply wasn't worth it. Methadone has many hardcore downsides (including the most severe withdrawals imaginable), buprenorphine has virtually none, and I am going to make this clear in the diary.

What you don't mention are the odds of people getting "better" by any measure on maintenance drugs. If you look at methadone, the "success" rate is astronomically small. The success rate with buprenorphine is simply non-existent, as we have no measure of its long-term effects.< You're betting the farm on 0% or 5% (buprenorphine and methadone respectively) against 5-15% (the % you put to abstinence, which I promise is A. wrong and B. doesn't tell the whole story).

What in gods name are you talking about (no offense)? Your numbers are just plain wrong. The numbers are upwards of 50%, IIRC, in keeping people off of heroin and keeping people safe from AIDS and other related problems. I will find the studies to prove it to you. The fact that you would quote such totally bogus numbers makes me question the the objectivity of your information.

Even based on your logic, you're playing the wrong numbers. But the other question you have to ask yourself is: how do you define success? If "success" on buprenorphine's terms means taking a narcotic daily for the rest of your life because you can't live without it, versus the "success" of say a 12 step program--which is abstinence and living a better life--well, I'd say the pot of gold at the end of the rainbow for abstinence is a heckuva lot richer than with maintenance pharms.

Hell no. While I feel that lifelong maintenance IS a valid option, and one that works for many people - I have seen them - they are professionals in many cases. My trip to the upscale methadone clinic absolutely boggled my mind.

But as I said, hell no. The goal of buprenorphine is NOT lifelong maintenance, even though *I* feel that's a valid option. The goal is treatment through medication until you are ready to become clean. And with buprenorphine, getting clean is a heck of a lot easier than with heroin or methadone. It's about being able to get your life in order. You are incorrect, whoever has told you this information does not know their facts. Any clinical trial of methadone or buprenorphine has the people go clean at the end, and that is the stated goal.

The bottom line though, and why BOTH maintenance pharms and long-term abstinence have low success rates, is because it's hard. Simply put. If it was easy to get off drugs, everybody who had a problem would do it. It isn't, it's going to be tough no matter how you try to do it, and most people won't make it (remember, this goes for maintenance pharms also).

Absolutely! But being on a maintenance med is no comparison to abstinence, and if you think it is, no offense, you are simply misguided. Either way it is hard, and no matter what abstinence is going to be super hard. But it is my strong opinion that abstinence after maintenance is a far better shot, and really the only one worth taking in almost any case, than abstinence cold turkey from heroin.

The thing is, you can't decide what you're going to do based on what seems easiest, which is essentially what you're doing. You need to decide based on asking yourself the question "What do I need to do to be the person I want to be?" I tell you what, dieting and exercise regularly for life is pretty tough too, but if you have a weight problem and want to change, that's the best way to go, versus putting your faith in every new miracle pill that comes on the market promising to make you thinner. It was easy(er) for me to quit shooting dope if I just drank a case of beer and smoked a few joints every night, but guess what, that was pretty shitty too. The thing is, I might have even been able to live like that, long-term, and I could tell myself I was living a reasonable life (getting to work on time, maintaining a relationship, not getting arrested, etc). But I'd ultimately be lying to myself. I know, I've tried it. If that's what some people choose to do, hey more power to them, but I have a hard time believing that they're much self-actualized that way, just based on my own personal experiences and the personal experiences of pretty much every single person I've ever met that's tried to stop using drugs by substituting with other drugs.

I am sorry, but I have to strongly disagree with you here, and I have already outlined my case. Your analogy is very flawed.

That's the general stuff. Specifically on this post, you say that it's not an ideal situation for a person trying to get clean to surround themselves with other addicts or alcoholics. And yet, it's consistently the most tired and true method we know over the last 70+ years.

Not so. That would likely be methadone. It's been used since the early 60s with great success.

Look at every person in that room that's more sober than you; that's exactly what worked for them when nothing else did it. You're acting like it's a drug party you're walking into: what it is is group therapy and a fellowship of people who have struggled with the exact same problems you're struggling with and have come out the other side. Your psychiatrist who is prescribing you drugs has no idea what you're going through or even what works for the problem. He hasn't faced the same demons you've faced and prevailed. The guys in the rooms of NA have.

That's just the thing. In most cases they haven't. They are trying to prevail against the demons, but in most cases they haven't. If there was group therapy where everyone was verifiably clean, that would be another story.

But this is what gets me most:

What if I believe in empowerment instead of helplessness? Teaching helplessness as a drug treatment strategy is poor to say the least, IMHO.

You believe in empowerment and not helplessness, by deciding that you are absolutely incapable of abstinence and the only way you can live a productive life is by ingesting a narcotic daily? How is that empowering? You've already decided you're helpless, it seems to me.

I have already addressed this for the most part. I am, for the most part, helpless. But for me to change that, empowerment is the only option. I am not going to give myself up to a higher power - and that simply won't work for me - period. As I said, everyone is unique in this case.

But, you share that with the folks in NA and AA. You said it yourself, you already know that trying to "will" or "empower" yourself clean doesn't cut it; the folks in AA and NA know it too. So instead of giving into that and saying "So fuck it, I'm helpless so I'll just keep taking drugs the rest of my life", the folks in those programs say "I'm helpless, I can't do it alone, but I know people who can help me and as long as I admit that I'm incapable of getting high anymore, I can figure out a way of life where getting high is no longer required."

I find it hard to believe you have ever been in NA, no offense, I am not questioning your truthfulness merely suggesting that your case is not like most. I have been to several NA meetings, though never have attended fully. I have scored heroin at NA meetings. Does that sound like it's going to work for anyone struggling to deal with their demons, as you put it?

I am not going to respond to the rest of your post. It is your personal experience, and your defense of NA, and I am not going to question it. In fact, I am going to put this entire post into the diary, to give people a full look at the options available - and hopefully find the studies to back up my claims of methadone and buprenorphine's success.

It was nice speaking to you, and even though we disagree - pretty strongly at that - I am glad we can keep it civilized.

Best of luck to you, and I am sure I will hear from you again soon.

The folks in AA and NA admit that they're powerless over drugs and alcohol so they're done trying to get on top of it. You admit you're powerless, but you`re embracing that helplessness and sitting in it. When you say the folks in NA and AA are trying to force a higher power on you, what they're essentially saying is "You are not God. You cannot control everything. Realize that and learn how to build a life around that very plain and self-evident truth."

And you're right, if you're just a statistic, you probably won't make it no matter WHAT you try. But I just can't imagine trying to live my life like that anymore, constantly trying to right myself with chemicals. If that's success, I want no part of it. I'd rather admit defeat and instead focus on being the person I truly want to be than wallow in my helplessness for the rest of my life. What's the longest you've been abstinent since you've been addicted? If you've just gone from one drug for another, are you sure you're giving it a fair shake? Shouldn't you try it first before passing judgement?

Finally, everybody has AA and NA horror stories. When you go in there looking for things to object to, more than likely you'll find them (guess what, that goes for anything else in life also). There are also more people for whom AA and NA has saved their lives than you'll ever find in line at the pharmacy or clinic. I know, on this site, Maryscott O'Connor is pretty open about her own experiences there, and I`ve heard a few others as well.

Finally, I hate how this post sounds. I hate coming off high and mighty and judgmental. So, my apologies, this is off the cuff and dreadfully early in the AM. But I just read a lot of posts about people who have family members struggling with addiction, and I can tell you based on what I know now that if my son or daughter is ever struggling with the problems I have, I will surely not recommend that they find a "better" narcotic to become addicted to. I've known people that have tried it both ways. I've never met somebody who long term has found a successful life by substituting one drug for another; I`d reckon that you haven`t either. Maybe it's possible, I don't know, but I've never seen a success story myself, and I've been around literally thousands of addicts. On the other hand, in my experiences in AA and NA, I've found some of the best, most self-actualized, and empowered people I've ever run across, anywhere, period, and nearly every person I've ever run into who has tried, HONESTLY tried, with willingness and an open mind, to work the NA or AA program, I've seen succeed, time and time again. REAL success.

Anyway, sorry for the rant. Like I said, it's a personal subject.

-----------------------

Thank you, glibfidget, even if I disagree with you. I sincerely apologize for not making it clear that not everyone believes the same as I do, although with all honesty most people in the heroin recovery community (who are addicts themselves) feel pretty strongly about maintenance. I can provide references to, for instance, the Advocates of Recovery through Medicine, who's hard work has been invaluable to people like me.

Update (day 2/part 2): I just realized this is a little unfair, my rebuttal without him being able to respond to my comments. If you want to see his response, as I am sure he will respond, as well as a post from someone who agrees with him, here is a link to his original comment:

glibfidget's post

Update (day 2): I promised to include other treatment options (besides maintenance and abstinence) and certain "harm reduction" policies (the current strategy today), and I am going to deliver.

Besides abstinence and maintenance, there are essentially two other treatment options. One is called "Rapid Detox." It is nothing new, and I have never heard a positive word about this method except from those trying to sell it to you. This is what I had to say about Rapid Detox, as well as a mention about the other new potential option, ibogaine:

"It's absolute quackery"

It's for people looking for miracle cures - and it just plain doesn't work. It's been around for quite some time now, it's no "breaking" treatment. It also costs ridiculous amounts of money. [Thousands of dollars]

Someone coming out of rapid detox has the lowest chance of success at abstinence of all - 5% at best. You just can't close your eyes and wake up cured. It DOES work in that you don't experience withdrawals - but if you ever see one of these things, up close or filmed, you wouldn't even consider it. It's downright horrible. They put you to sleep and force your body to go through what it needs to to be clean compressed into a 6 hour period. There have been deaths, and I wouldn't be surprized if it's shut down eventually. On top of that, you have protracted withdrawal symptoms, more minor nagging symptoms that continue longer than they should.

I have yet to meet anyone in the "loop" that had anything positive to say about rapid detox.

The only other treatment they have is this stuff called ibogaine. Well, that's not exactly true - they have plain symptomatic treatment for withdrawals, but NOTHING works to cure heroin withdrawals. Nothing - save one exception. There is a blood pressure med called Clonidine that depresses one area of the brain that heroin does - but far from all. So it does help - in some people - but others report no help or worsening of symptoms.

Back to ibogaine...it's this stuff that makes you have something resembling an unpleasant acid trip. Apparently some people think that when you take it, it does something to you that makes you look at your life and no longer want drugs. It has had mixed reviews, but there are some reports of success in clinical studies, which I need to catch up on.

------------------

I will look for some further info on Ibogaine, including a link to a site possibly with info about it, and hopefully provide that. My opinion on it is it might be worth a try, but it's no miracle cure. I think we are mostly seeing the power of placebo here. But I will investigate further, it's overdue on my part.

Harm Reduction

The current stragegy of the government, after much lobbying, is called "harm reduction." This means that while we still send people to jail, while they are using we will do what we need to reduce harm (to everyone involved.) This mostly includes:

#1 - Education and Addict Outreach

#2 - Needle Exchanges

Needle Exchanges have done extroadinarily well, at least here in New York (I am positive there are places that need to catch up on this.) They essentially allow addicts to trade used needles for old ones. The goal is preventing the spread of HIV - and there is plenty of evidence of it's effectiveness in this regard. Guiliani opposed the first needle exchange tooth and nail, but eventually relented. The other important thing needle exchanges do is take used needles - thus preventing, to a certain extent, spent needles in places they shouldn't be.

Many states, including now New York, have also taken the step of making needles over-the-counter, meaning you can just buy them without a prescription. They are fairly cheap, and this is an important step for the type of junkie who would rather not go to a needle exchange - or where there are none available (or available at the time the junkie needs the needle.) I hope the other states that haven't implemented this follow the lead.

As for addict outreach, it's not nearly what it should be. Street addicts, most homeless and have HIV, need to be hit on the head with a stick to really get through to them, and many are very fearful of going to jail. I hope to see improvement here in the coming years.

Well, that's it for now. Hope I have given you what you have wanted.

UPDATE: future additions to my series on the drug war

Drug Prohibition: a Primer on Drugs from my vantage point - This is an opinion piece about drugs, and an overall introduction and background information for the future.

Next to come: Drug Prohibition: Where we Stand [tentative]

Source:

http://www.dailykos.com/story/2005/1/8/17424/52761


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 Message 8 of 14 in Discussion 
From: MSN NicknameSha_mtlSent: 6/17/2005 7:37 PM
If anyone got through these long posts and is interested..there are many comments to his Drug War commentary here:
 
 
 

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 Message 9 of 14 in Discussion 
From: MSN NicknamebindymeSent: 6/23/2005 1:59 PM
Sha,
I thought that was brilliant, i found it so interesting what he had to say about bupe, cause i was on it for 3 and a half years. But in australia we get subutex and we dont get to take it home like a normal prescription. Its given out exactly like methadone here. So thanks for finding this and posting it.
Linda

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 Message 10 of 14 in Discussion 
From: MSN Nicknamebestbargirl-38Sent: 12/1/2006 12:03 PM
is it available in canada
 

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 Message 11 of 14 in Discussion 
From: MSN NicknameLovingmom2433Sent: 12/1/2006 1:45 PM
Sha,  thank you, thank you, thank you, for posting this.
I try to absorb everything i can on any kind of treatment and this is the best INFO I have seen this far.
 
How you doing girl?????
I think of you so often and hope your life is going good.
Write me when you have a chance, OK???
 
Much Love Karen

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 Message 12 of 14 in Discussion 
From: MSN NicknameLovingmom2433Sent: 9/22/2007 2:33 PM
BUMP..........
Sha, ive never seen this before but i found it incredibly interesting.
where have you been sweet lady??
I miss you SO much,
love karen

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 Message 13 of 14 in Discussion 
From: MSN NicknameLovingmom2433Sent: 9/24/2007 1:26 AM
My memory is good, its just very short lived LOL...
See, i bumped this up because i wanted to say how great this post is, even though i dont remember reading it in December, lol.
Love Karen

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 Message 14 of 14 in Discussion 
From: MSN Nickname©ShaSent: 9/24/2007 5:00 AM
lol I hear ya Karen..memory..what is that???
 
Ye Gads..mine is gone with yesterday..truly. Miss you too...will email and catch you up soon..mine is [email protected]
 
Yes this is a great info sheat on Bup..I know the guy z(Nephalim)..who wrote it and he speaks from experience..those are usually the best kind.
 
Sending you much love

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