Killing the Suboxone Gift Horse with Naltrexone

First Posted 11/14/2013
I received an email update today with important news from the world of psychiatry and addiction.  The email highlighted a study from the October issue of Jama Psychiatry, entitled ‘A Randomized, Double-blind Evaluation of Buprenorphine Taper Duration in Primary Prescription Opioid Abusers’.  The study compared relapse rates in opioid addicts who were tapered off buprenorphine at different rates.  The study considered success as being free of opioid use and taking naltrexone, an orally-active opioid antagonist, after 12 weeks.  The study found that 50% of the people tapered off buprenorphine over 4 weeks were abstinent and taking naltrexone.  That compared to 21% and 17% of success in patients tapered over 1 or 2 weeks, respectively.
I’m sorry, but who cares?
Regular readers of my blog know my opinion about buprenorphine.  (Newcomers please note that by buprenorphine I mean buprenorphine, Suboxone, or Zubsolv, since they all work in identical fashion).  Most people who work in the addiction field agree that addiction is a life-long illness.  Most people who have worked in the field for a few years or more know that relapse is a common feature of opioid dependence.  I believe that anyone claiming to ‘cure’ opioid dependence through use of a plant, root, amino acid, vitamin, hypnosis, accu-pressure point, or 90-day program is either misinformed, pathologically optimistic, lying, or blinded by profit motives.
Opioid dependence is associated with a high rate of death and morbidity. Beyond buprenorphine, the only reliable intervention for treating opioid dependence is methadone maintenance, if ‘reliable’ is defined as ‘likely to be successful.’  I realize there are hundreds if not thousands of residential treatment facilities throughout the US that advertise ‘freedom from addiction’; some even offering freedom from ‘addiction’ to buprenorphine.  These claims are made, and apparently believed, even with one-year relapse rates greater than 90% in opioid addicts treated without medication.  In the real world of ‘Suboxone Talk Zone’, I have to burst a few bubbles about ‘sending someone to treatment.’    For opioid dependence, treatment without medication yields long-term sobriety in only a small minority of patients.
Yet many healthcare professionals continue to chase after the golden goose of abstinent recovery.  Makes me wonder if laetrile would still be around with better marketing!
Before buprenorphine, opioid dependence was an oft-fatal illness that in most people responded only to the administration of opioid agonists at frequent intervals, with no patient autonomy and the threat of discharge if anything prevented on-time arrival at the early-morning line-up.  In 2003, along came buprenorphine— a prescription medication with a reasonable generic cost (finally), with few or no long-term risks and tolerable side effects, that eliminates cravings and prevents illicit opioid use in 50% of an average study population of opioid addicts who are allowed to continue their medication.  So why, exactly, are we excited by the prospect of changing from buprenorphine to a medication that carries the risk of hepatic necrosis?
Are people on naltrexone better off than people taking buprenorphine?  One would hope so, given that 50%-83% of people in the current study went back to active using while trying to make the switch!  Patients on naltrexone still have the problem of blocked mu receptors during emergency surgery.  Having blocked opioid receptors is an even larger problem for many educated addicts than their doctors realize, that goes something like this: ‘I stopped opioid agonists, but now I have to block my endorphins too?!
Why not just keep stable buprenorphine patients on buprenorphine?
The argument for naltrexone over buprenorphine comes down to two issues.  The first is the quasi-spiritual attitude that people are in an inferior form of treatment if their mu receptors are bound by even a partial agonist—no matter that those receptors have developed complete tolerance to the agonist effects of the drug.
The second argument focuses on diversion.  Buprenorphine is sold on the street, particularly in areas where there are no doctors certified to prescribe the medication.  People divert buprenorphine in a number of ways, ranging from efforts to get high, to use ‘in between’, to attempts at self-treatment.  But should risk of diversion reduce the legitimate use of a medication that has saved thousands of lives? Is it logical to throw the bupe-baby out with the bath water when deaths from buprenorphine are less common than deaths from acetaminophen?
I expect that the risk of diversion decreases over time in patients treated with buprenorphine.  Patients in long-term, stable treatment are more likely  employed and insured, with less financial incentive to sell controlled substances and more to lose for doing so.  Most of my stable patients develop insight into the damage caused by addiction, and have no interest in getting someone else caught in the same trap.  Most of the patients I’ve treated over time have severed their connections with the using world.  And most of them are grateful for a second (or tenth) chance at life; grateful enough to avoid risking everything by selling drugs.
Even if diversion could be blamed, in part, on stable buprenorphine patients, why is addiction treated differently than other diseases?  Diversion of opioid agonists is a greater problem than diversion of buprenorphine, both by sheer volume and by the damage from diversion, yet the FDA just approved another potent mu agonist in Zohydro—a drug with far greater diversion potential than buprenorphine or Suboxone.  If diversion doesn’t disqualify the pain meds used for strained backs, bumps, and bruises, why should diversion derail one of the only effective treatments for a disease that is killing thousands of young people?  Heck, pseudoephedrine is sold from pharmacies with a signature; the dangers of methamphetamine didn’t eliminate our collective concern for people with stuffy noses!
If we take diversion out of the argument—for example by deciding that the 300-odd deaths from buprenorphine diversion don’t warrant removing an effective treatment for a disease that has become the leading cause of death in young adults— the push off buprenorphine makes little sense.  I suspect that the people advocating ‘progressing’ from buprenorphine to naltrexone do not envision patients treated indefinitely with naltrexone either, but rather see naltrexone patients as somehow ‘closer’ to abstinence than buprenorphine patients.  From a neurochemical standpoint, what is the difference between being fully tolerant to a partial agonist vs. taking an antagonist?  For relapse-prevention, advantage goes to buprenorphine, since ‘effective relapse’ to opioid agonists requires buprenorphine patients to first go through days of withdrawal.  Naltrexone patients on the other hand can miss the morning’s naltrexone, and later that night relapse using mu receptors that are even hyper-sensitive to agonists.
As for arguments that patients on buprenorphine are impaired, I would love to see my attorney-patients take part in THAT debate.  Concerns of impairment have come from poorly designed studies where buprenorphine groups consisted of patients with no tolerance to the medication. I suspect that medical reporters too often read the abstract and skim the ‘materials and methods’—let alone the statistics!
If ‘success’ consists of moving to naltrexone—a medication that many real-world addicts reject–   how long is naltrexone continued, and what happens when it is stopped?  Do people go back to heroin again?  If not, why not? The cycle of ‘use, treat, cease treatment, use, and repeat’ should be a black box warning on naltrexone— as soon as they finish stamping the warning on the steps of every residential treatment center.
I’ve been accused of being too long-winded.  The short version for those who skipped to the bottom:  buprenorphine-based medications offer an effective, tolerable, long-term treatment for a chronic, life-long disorder.  How many people will die in their quest—or their doctor’s quest—for ‘abstinent recovery’ with or without naltrexone?  Emphasis on naltrexone is just one more example of looking the gift horse of buprenorphine treatment in the mouth.
Sigmon SC, Dunn KE, Saulsgiver K, Patrick ME, Badger GJ, Heil SH, et al. A Randomized, Double-blind Evaluation of Buprenorphine Taper Duration in Primary Prescription Opioid Abusers. JAMA Psychiatry. Oct 23 2013;

The Other Opioid Dependence Medication

Today I met with representatives from Alkermes who were promoting Vivitrol, a long-acting mu opioid antagonist that is indicated for treatment of alcoholism and opioid dependence.

Naltrexone
Naltrexone

I admit to some pre-existing bias against the medication.  I’m not certain, to be honest, whether that bias was based upon sound clinical reasoning, or whether it was based on personal, negative reactions to naltrexone in my past.  Or maybe, as a recovering opioid addict, I have negative feelings about anything that blocks mu receptors!
Vivitrol consists of naltrexone in a long-acting matrix that is injected into the gluteal muscle each month. The medication is expensive, costing about $1000 per dose (!)  That cost is usually covered by insurance, and like with Suboxone, Wisconsin Medicaid picks up the tab save for a $3 copay.  Alkermes, the company that makes Vivitrol, also has a number of discounts available to reduce or even eliminate any copays required by insurance companies.
I’ll leave the indication of Vivitrol for alcoholism for another post.  The indication for opioid dependence came more recently, and appears more obvious, given the actions of naltrexone at the mu opioid receptor.
In short, naltrexone blocks the site where opioids—drugs like oxycodone, heroin, and methadone—have the majority of their actions.  Blockade of that site prevents opioids from having any clinical effect.  There is some dose, of course, where an agonist would regain actions— an important feature in the case of surgery or injury.  But even in those high doses, the euphoric effects of addictive opioids would be muted.  People on Vivitrol, essentially, are prevented from getting high from opioids.
Back in my using days, I took naltrexone, thinking that doing so would help me get ‘clean.’  I didn’t wait long enough, however, and so I became very sick with precipitated w/d.  The makers of Vivitrol recommend waiting at least a week, after stopping opioids, before getting an injection of Vivitrol.  I suspect that a week is not long enough to prevent w/d, but I realize that it would be very difficult to expect patients to last longer, without using anything.  I would expect that any precipitated w/d could be reduced through use of comfort medications, at least for a day or two until the symptoms are mostly gone. This requirement, though, to be clean for a week or more is one of my problems with the medication.
As an aside, I was also prescribed naltrexone (oral tabs) at the end of my three months in residential treatment, and I took the medication for another three months.  I had no withdrawal or other side effects to naltrexone at that time.
Another issue was the concern that naltrexone has been connected to hepatic toxicity.  We discussed that issue today, including the studies that led to that connection—which are not compelling.  The discussion allayed most of my concerns about liver problems from Vivitrol.
Finally, I have always recommended buprenorphine over naltrexone because of the anti-craving effects of buprenorphine that result from the ‘ceiling effect’ of the medication.  I worried that naltrexone, by blocking the actions of endorphins, would actually increase cravings.  But that is not what the data shows.  In the studies with Vivitrol, cravings for opioids were dramatically reduced by the medication.  The mechanism of that effect is not entirely clear;  some of the anti-craving effect may be psychological, as addicts stop wanting something when they know there is no way to get it.  But there may be other complicated neurochemical effects at presynaptic opioid receptors that are not fully understood.
The bottom line is the result of treatment;  the very sick opioid addicts treated in the studies used by Vivitrol to gain FDA approval showed a profound reduction in opioid-positive urines, over a span of 6 months.
I suspect that I will continue to favor buprenorphine.  I do not buy into the ‘need’ some people describe to ‘get of buprenorphine as fast as possible.’  Buprenorphine is a very effective, safe, long-term treatment for inducing remission of opioid dependence.  But because of the cap, I am glad that another option is available to treat this potentially-fatal condition.  And I admit to perhaps being too quick to judge Vivitrol, which appears to be a safe alternative—particularly for people who have a lower opioid tolerance that do not want to push it higher, or for people who have been free of opioids for a week or two.
I would invite local people who are on my buprenorphine waiting list to consider Vivitrol as an option.
 

New Formulation of Oxycontin– Will it make a difference?

Oxycontin was not my drug of choice so I don’t know the ins and outs of abusing the medication. But I suppose anything that makes the drug harder to abuse is a good thing. The other things that are being looked at for approval are combinations of agonist with antagonist in small doses– for example Embeda is morphine plus little beads of naltrexone, and orally-active form of naloxone. The naltrexone is only released if the pill is crushed, and there is not enough naltrexone to cause withdrawal, but only enough to reduce the ‘high’. I guess my thought is why limit to a small amount of naltrexone? The drug is not to be injected or snorted, so why not put enough naltrexone in it to make any tampering a very serious downer?
I thought I’d share the article below with you, so you can see how thrilled the FDA is with the new formulation.  Read on…
FDA Panel Recommends Approval of New Oxycodone Formulation
By Emily P. Walker
Published: September 24, 2009
Reviewed by Zalman S. Agus, MD; Emeritus Professor University of Pennsylvania School of Medicine.
GAITHERSBURG, Md. — An FDA advisory panel voted to recommend approval of a new formulation of oxycodone hydrochloride (OxyContin) that is more difficult to crush or dissolve, and which may deter drug abuse.
By a 14-4 margin, with one abstention, the panel recommended that the FDA approve Purdue Pharma’s application for a new, resin-coated formulation that it hopes will eventually replace the original version, which has been on the market since 1996.
The FDA does not have to follow the advice of its advisory committees, but it usually does.
The advisory panel’s endorsement was less-than-enthusiastic in this case, and members complained that there’s no proof the new version of the drug is any safer than regular oxycodone hydrochloride — one of the few drugs on the market that can be deadly in a single dose.
Purdue’s current pill is meant to be swallowed whole, but abusers can easily chew it or crush it and then snort it, smoke it, or dissolve it in liquid and inject it to achieve a heroin-like high.
Although there is no proof that the new formulation is safer, the panel agreed that making the pills harder to crush, chew, or dissolve into liquid may deter abusers. When the new version of the drug is dissolved into water, it produces a gel, which makes snorting the drug more difficult.
“Clearly the old [formulation] is worse than the new, although I think the difference is relatively small,” said panelist Randall Flick, MD, an anesthesiologist at the Mayo Clinic who voted to recommend approval of the drug.
“My feeling is that there would at least be some incremental improvement in the safety profile,” said panelist Stephanie Crawford, PhD, a pharmacist at the University of Illinois in Chicago.
Some 1.2 million people age 12 and older used OxyContin in 2006 for nonmedical purposes, according to the Department of Health and Human Service’s National Survey on Drug Use and Health.
Purdue originally sought FDA approval for low-dose versions of the new product in 2008, but the agency told the company to develop more clinical data and to apply the technology to all dosages of the drug.
Also, it took until 2008 for the company to convince the advisory panel in 2008 that the drug was any more difficult to tamper with than the original formulation, said panelist Ruth Day, PhD, director of the Medical Cognition Laboratory at Duke University.
This time around, the company convinced the panel that new tablet is harder to dissolve or crush and that the resin excipient might make it harder to take the drug in an unprescribed manner, said Day, who was also a member of last year’s panel.
In one lab test, Purdue researchers used 16 household tools to attempt to crush the tablet into small particles. All 16 tools handily crushed the original OxyContin tablets to a fine powder. Although four of the tools managed to break down the new tablet into shavings or particles, none could turn it into powder.
Even so, FDA staff reviewers concluded that the technology does not make a huge difference in OxyContin’s abuse potential.
Hardcore abusers are likely to devise new ways to break down the harder tablet or figure out which solvents will dissolve it fastest, within “day or weeks of the product’s release on the market,” Flick predicted.
The panelists who voted for approval said they were concerned that Purdue had not developed an adequate Risk Evaluation and Mitigation Strategy for the drug.
The new formulation will keep the name “OxyContin” and be used in seven available doses. Purdue said it will not market the reformulation as a “safer” version.
If it’s approved, Purdue will produce only the newer version and stop shipping the old one.
“Within six to eight weeks [of production] roughly 90% of drug in the supply chain will be the new product,” said Craig Landau, MD, Purdue’s chief medical officer.

Naltrexone Implant vs Suboxone: Mano a Mano!

I am going to share an interaction with a person who wrote to me about using the Naltrexone implant. I am always a bit suspicious about the motivations of people who want comments posted about a different type of treatment, or who come with pot-shots against Suboxone. I don’t go to methadone clinic sites or ads for rapid opiate detox and hound people for their choice of treatment—even though I don’t agree with their choices. But the point of my blog is to educate people (that better be the point, as it certainly isn’t a money-maker!), so I will share the material and let people decide what is right for themselves. I did make some comments at the end of the discussion—the owner of the blog gets the last word!– because there were some things written about Suboxone and Naltrexone that I don’t agree with, based in some cases on the literature, and in other cases on personal experience.
The message about Naltrexone:
I just wanted to add a thought to the doctor’s paragraph about Naltrexone and how it could be used as a tool to help in recovery but it can’t because it doesn’t last in the body for long. I want to tell everyone about the Naltrexone implant. It has been around for a long time but not many doctors have the knowledge of it. I detoxed off heroin six years ago and went onto the Naltrexone implant for twelve months. The implant lasts about 8 weeks and then you have to go back for another. I have to tell you that it was the best twelve months in my whole life. I wish everyone knew about it. I had a great doctor that was a recovering addict and really understood what it takes to be clean and stay clean. I would suggest ANYONE that wants to really be clean…STOP hiding behind Suboxone and get to a doctor that knows how to detox you and put you on something NON ADDICTING like the implant.

Naltrexone vs Suboxone
Naltrexone vs Suboxone

My Reply to the Writer:
Thank you for your comments. I will add your perspective, but will also discuss the problems with the Naltrexone implant that have kept it from becoming more popular.  I’m glad it worked for you, but for many who have it implanted (usually as part of a rapid opiate detox weekend) there have been significant complications.  There is the liver damage from Naltrexone of course, but that is not the only issue.  I have met addicts who dug the implants from their belly or arm out of desperation to get ‘high’; there also have been several documented suicides in patients after rapid opiate detox and Naltrexone implantation.
As a board certified anesthesiologist, one of my initial plans after getting clean was to set up a rapid opiate detox place with a friend who was an internist.  After research of the literature I learned that the medical community sees rapid detox mostly as a gimmick that pays well but that does little to ease the suffering of addicts.
I also take issue with your comment about ‘hiding behind Suboxone’.   Most people would see the implantation of Naltrexone to be at least as significant an undertaking as taking a Suboxone tablet once per day. I’m not sure which person is actually ‘hiding’.

The Writer’s Response:

I completely understand your thoughts about the implant.  I do know about these types of cases and they are unfortunate.  However, because I took that step and did my best to use it correctly as a tool in my recovery, while working VERY VERY hard with a counselor, it worked for me.  Since then, I have devoted a lot of time to speak with other addicts about it and have “sponsored” hundreds and hundreds through this option and I have seen more people stay in recovery longer because of it.  I also was part of a Naltrexone implant study over the course of 12 months to see if people on the implant really achieve longer sobriety than someone on the oral form and even the injectable.  As far as liver damage, case studies show no liver damage within the first 12 months of staying on Naltrexone.  If that was the case, then I truly believe Vivitrol would not have been FDA approved for alcoholism (and they are more prone to have liver damage than an opiate addict).
I went through a rapid detox but with sedation….no anesthesia.  I have been through both and the sedation detox was SO much easier and more comfortable process to go through.  The doctor was great (he too was a board certified anesthesiologist) and I was awake through most of it to learn a lot about the process of which my brain and body was going through.
However…there are still several addiction specialists that can offer a detox (no anesthesia or sedation) on an outpatient basis and still complete it with the Naltrexone implant on the last day.  There are usually several options to offer a patient to help them even get through the tough time.
And with the Suboxone…there are truly people who need to be on it; pain management, people who are NOT ready to be clean, etc.  But there are some who did NOT know enough information about it, took the advice of their “MD” and then now are having a hard time getting off it and have no idea what to do.  I am “sponsoring” a woman now who is a school teacher in AZ….she called me this week and is so upset that her MD keeps writing her scripts for Suboxone, then she talked with him and told him she wanted to stop, and he doesn’t know how to get her through it…..because is in NOT an addiction specialist.  She is only on 2mg per day but she cannot get off of it.  I sent her to a specialist who will detox her in 5-8 days comfortably and then put her on the Naltrexone implant……it will take away her cravings, temptations, and provide her that “safety net” during the first 2 months of her recovery.  She knows it won’t be easy to be dependent for 2 years and all of a sudden not be dependent, but she is so excited to have the “opportunity” that she was never offered before.
I hope you will consider posting my blog…..it may help some and it may not.  But, addiction is non-predictable anyway and there is never a guarantee.  Thanks for the good work you are doing…..look forward to reading more stories.

Suboxone vs Naltrexone
Suboxone vs Naltrexone

My Last Word:

I appreciate the writer sticking with the discussion; too often a discussion will degenerate into name-calling, as I mentioned in my prior post.
I am not aware of anyone using the Naltrexone implant in my part of the country (the upper Midwest). I know that there are places in Florida that advertise heavily on the internet, and I do have one current patient who had rapid detox in Florida and the implant several years ago. He now takes Suboxone.  I will admit to some real stupid behavior on my part, borne from desperation:  on three occasions during my active using days I performed unmedicated rapid opiate detox… on myself!  On one of the occasions I injected the contents of an unlabelled syringe– something that often results in a dead anesthesiologist– but which in this case resulted in an anesthesiologist who only felt dead.  The unlabelled material turned out to be naloxone.  It was when I recognized this level of addiction– and this level of dangerousness– that I decided to leave anesthesiology behind and do another residency.
The other two occasions were equally stupid.  Again, understand that I hated being addicted to opiates from day one;  I took naltrexone tablets (which unlike naloxone are active orally) thinking that the block would set me free.  The first time, I was in a meeting with my partners after I took about 100 mg of naltrexone;  by 60 minutes I had to run from the meeting, much like a disgusting scene in the movie Trainspotting (I won’t say more, but those of you who have seen the film likely know the scene I am referring to).  The last time was late in my active addiction at a time when I was truly going crazy, and I don’t remember the event very well. Yuck.
Back to the writer’s comments– I don’t agree with the idea that Suboxone is for ‘pain patients’ and ‘people who are not ready to be clean’. People taking Suboxone are as ‘clean’ as a person on Naltrexone in my opinion; in both cases the person feels ‘normal’. There is no ‘high’ or any other subjective opiate effect associated with proper use of Suboxone. In fact, I have concerns when I start Suboxone in a patient having significant pain, knowing that the use of opiate agonists will be impossible on Suboxone and that tolerance develops to the agonist effects of buprenorphine.
As I have said in other posts, I see buprenorphine to be in line with Naltrexone, but an improvement upon it. I have not seen evidence that buprenorphine reduces opiate cravings; in my experience the cravings on Naltrexone were if anything more severe. Yes, Naltrexone reduces cravings for alcohol, but that is a completely separate effect. On the other hand, buprenorphine clearly does reduce opiate cravings, very effectively.
Everyone will have his/her own way of seeing things. Here is mine: Naltrexone provides assistance with sobriety by assuring the addict that use would not result in intoxication; the addict therefore can tell himself, as a last-resort measure to avoid use, that ‘even if I did use, nothing would happen’. In my model, ‘addiction’ consists of the mental obsession to use. Since Naltrexone doesn’t treat cravings, it doesn’t treat the ‘obsession’—it doesn’t treat ‘addiction’. So a person taking Naltrexone is truly in a ‘dry drunk’; the obsession to use is STILL there, and so active involvement in a 12-step program is necessary to regain a sense of freedom from substances. I think this is why rapid opiate detox and Naltrexone implantation has sometimes resulted in disaster; an addict stumbles out of a hotel after rapid detox, blocked from using, but still obsessed with opiates—without any exposure or experience with a recovery program (again, the steps are the ‘gold standard’ here). So the blocked addict is miserable—and sometimes digs out the implant, or worse.
ON THE OTHER HAND… and as I have written about many times, buprenorphine gets to the heart of addiction—the obsession to use. A person taking buprenorphine (in Suboxone) is relieved of the obsession, and so in my mind is not in a ‘dry drunk’. For that reason I see twelve step meetings as less of an issue in patients taking buprenorphine. This is a tough point, so I will word it another way: the meetings are necessary with Naltrexone implants in order to stop the obsession (which meetings stop through the adoption of powerlessness and a higher power); Buprenorphine ITSELF stops the obsession in patients taking Suboxone. This leads to my frequent caveat– if a person stops buprenorphine, he needs to take up meetings—or the cravings and obsession will eventually return.
One final comment: there are currently trials underway for a buprenorphine implant, Probuphine, owned by Titan Pharmaceuticals. I have tried to make contact with people at that company on a number of occasions but cannot get a response; if you have contacts with anyone there, please contact me at [email protected]

Suboxone vs Subutex: Where did the high go?

I encourage addicts doing the work of staying clean to ‘bring the memory full circle’; with every pleasant recollection, be sure to think about where the use took you, and where the pleasant sensations ended.

A bit of confusion over how Suboxone and Subutex work:
Subutex gave me a strong buzz during detox…After a year of being on suboxone (which completely suppressed any high the buprenorphine might give, which it did) and being switched back to subutex, one might think subutex would give me that feeling again, with the naloxone being out of my body and all. Is it a matter of tolerance? I’ve been told that tolerance is reset by naloxone…I just don’t know what the real cause is here. I’m on straight subutex, 8mg and the magic is gone. perhaps…forever? Let me know if you have any clue, or if it is just tolerance. (email me at [email protected]
My Response:
Suboxone and Subutex are interchangable;  there is no difference between the subjective experiences of them, save for the lack of flavoring in Subutex and the ‘fruity flavor’ of Suboxone.  The naloxone in Suboxone is not absorbed from the mouth, and the naloxone that is absorbed from the intestine is broken down very efficiently by the liver, so that very little gets into the systemic circulation.
The effect one has to the initial dose of buprenorphine, whether it comes from Suboxone or from Subutex, depends on the person’s level of tolerance.  If a person has a very high tolerance, he will feel withdrawal.  If the tolerance is very low, the person will feel a ‘high’.  In either case, they will adjust to the dose of buprenorphine within a few days and feel normal.  In the case of the person who initially felt a buzz, the person becomes tolerant to the buprenorphine;  in the case of the person who felt withdrawal, the person ‘recovers’ from withdrawal as his opiate receptors adjust to the reduced level of opiate stimulation.he
To answer your question, the tolerance is what took away the ‘high’ you got from the initial dose of Subutex.  It had nothing to do with changing to Suboxone, and would have occured in the exact same way had you stayed on Subutex.  A person who is not opiate-tolerant will get a significant opiate effect (I hate to use the term ‘high’, but I guess the term is correct) from the initial dose of Suboxone or Subutex– but it will only last for a day, or maybe two at the most.  Buprenorphine has a very long half-life, so there is no significant drop in the blood level from that first dose to the next– and the constant opiate stimulation from a drug with a long half-life results in the very fast development of tolerance.
I have had a number of patients switch from Suboxone to Subutex and vice versa, sometimes a couple times (in the case of women who take Suboxone, but who change to Subutex during pregnancy to avoid the naloxone).  They have no change in how they feel;  in both cases the buprenorphine is the active substance, and since the dose is the same I would not expect them to feel any difference between the two medications.


As far as ‘naloxone resetting tolerance’, for naloxone to have an effect on human opiate receptors it would need to be given IV or IM, where it can be absorbed sufficiently.  The medication ‘Naltrexone’, on the other hand, is an opiate antagonist similar to Naloxone except for being active when taken orally.  When a person takes Naltrexone, the opiate receptors are blocked;  the neurons with the opiate receptors therefore react as if they are not receiving any input through the receptors.  In response to the lack of input the neurons up-regulate the receptors so that they are more sensitive to stimulation by opiates, which translates into a decrease in tolerance.
I understand your comment about the ‘magic’, but I don’t agree with it.  The ‘magic’, in my opinion, is the ‘normal’ feelings induced by buprenorphine.  After that first couple days patients taking Suboxone feel like non-addicts, and that is what makes it such a ‘magical’ medication.  That other feeling– the high from opiates– is only a small part of the true feelings induced by opiates– and you can’t have one without all the others.  In other words, yes, opiates give a warm, euphoric feeling… but also give an equal or greater amount of depression, fatigue, and bone-chilling coldness.  In the balance, there is no net ‘good feeling’– there is as much or more misery for every amount of ‘magic’.  Addicts stuck in a using pattern tend to see the OC or other opiate with ‘euphoric recall’, remembering only the tiny pleasant part of using, and ignoring the huge amount of misery associated with using.  I encourage addicts doing the work of staying clean to ‘bring the memory full circle’; with every pleasant recollection, be sure to think about where the use took you, and where the pleasant sensations ended.  Keep the memories attached to each other, because in reality they are not separable.

Precipitated Withdrawal

thank you anyway for replying.. So when i do get into seeing a doctor, i must be in withdrawal? I am so confused on this issue.  I am taking suboxone, but most likely have to take the lortab when it is out of my system because of the pain i do have. The lortabs are a prescription that i have been on for over a year.  I just know that i can’t stop taking them on my own, thats why i tried the suboxone.  I researched how to take it and it works wonders for me.
My Answer:
The primary issue with precipitated withdrawal isn’t so much being in withdrawal, but instead has to do with your level of tolerance.  Tolerance goes up with every dose of an agonist, and plummets when a person is in withdrawal.  In predicting precipitated withdrawal one looks at whether a person’s tolerance is higher or lower than it would be taking 30 mg of methadone per day.  A person taking 100 mg of methadone per day who didn’t start withdrawal will have severe withdrawal during Suboxone induction;  A person taking 10 mg of methadone per day who didn’t start withdrawal may actually get a mild ‘high’ during methadone induction.  Lortab includes hydrocodone, the active ingredient in Vicodin.  Hydrocodone is metabolized to a more potent drug—hydromorphone or Dilaudid—to varying degrees in different people (I am about to post something about that), so it is hard to predict the tolerance level in a person on hydrocodone.  The tolerance depends on how their genetics make them metabolize the drug.  For that reason one cannot simply say that 50 mg of vicodin per day won’t result in precipitated withdrawal.  These metabolic relationships occur with other opiates as well and explain why some people say they have never had precipitated withdrawal, and other people do have it, despite taking the same doses of the same opiate.


It is impossible to guarantee that precipitated withdrawal won’t occur, but one can make it exceedingly unlikely by reducing their use of opiates a bit as the induction approaches and then getting good and miserable before starting the induction by discontinuing use for 24 hours or so.  People on super-high doses of a drug like methadone (which tends to stay around in the body for awhile) have the highest risk for precipitated withdrawal, but can make it unlikely by stopping use for 3-4 days, as tolerance drops the fastest in a person who completely stops using.  For what it’s worth, I had precipitated withdrawal myself back in my using days on at least 3 occasions;  twice, in desperation, I took oral naltrexone (an opiate blocker) thinking it would help me stop using;  a third time I injected IV narcan by accident.  The naltrexone incidents were the worst, as that drug lasts for 24 hours or so.  It was pretty horrible, but I did live through it, and the experiences certainly gave me a stronger desire to stay clean!
SD
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