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Discussion => Drug safety => Topic started by: malacath on October 22, 2012, 09:12 pm

Title: Opiate Addiciton- "Miracle Drug" to end your addiciton.
Post by: malacath on October 22, 2012, 09:12 pm
Hi, this is a thread I am starting about the drug that saved me from my opiate addiction, but is unfortunately (due to big pharma greed and the FDA) not widely used in addiction treatment. The drug is called naltrexone and the brand name for the form I will be speaking about is Vivitrol.

NALTREXONE:

Naltrexone is a mu-opioid receptor antagonist, which means it binds to mu-opioiod receptors in the brain but does not stimulate them. Conversely, opiate drugs like heroin and painkillers bind to the same receptors and stimulate them, causing the euphoric effects associated with these drugs, they are opioid receptor agonists. When you take naltrexone, all your opiate receptors are occupied with the non-stimulating naltrexone molecules so that when you take an opiate drug, the effect is blocked.

Naloxone, also known as Narcan (the drug paramedics give when you OD on opiates) is also an opiate antagonist, closely related to naltrexone, but it only works for a few hours. Naltrexone works for 24 hours.


VIVITROL:

Vivitrol is a brand name for a once-monthly IM injection of naltrexone. You get a shot every 4 weeks and the shot blocks all opiate drugs for those 4 weeks, so you can get high even if you wanted to. Oral naltrexone does the same thing, but you must take a pill every 24 hours so if you wanted to get high you would only need to skip a dose. Its much easier to commit to one injection a month than taking a pill every day. This is the drug that saved me from my addiction.

The reason this works so well is complicated, but I will try to explain it. When you become addicted to a drug, you develop special circuits in your brain related to the addiction. These circuits grow and are reinforced every time you use an opiate drug, which is one of the reasons addictions get progressively worse. When you stop using, you would think that these circuits would diminish over time but they dont- the reason being because your bodies natural endorphins stimulate the same receptors in the brain an although they are normally not strong enough to make you feel any euphoria, they are enough to keep the circuits active. This is why you can stop using for years but as soon as you start again your addiction is back to where it was in a manner of weeks when initially it took years to develop. By talking Vivitrol for a period of about 2 years, you have 24/7 blockage of these receptors and the circuits are allowed to diminish themselves. This is an important difference and is the reason why abstinence alone is not enough to "cure" an addiction.

CONS:

The main con with Vivitrol is its price. If it weren't for big pharmaceutical companies, the effectiveness of this drug would be more well known and more people would produce it and the government would probably subsidize the cost, but that is not the case. Only 1 FDA approved version exists right now and its about $1000 a shot (so 1000 a month for 2 years is $24,000). Insurance helps but it was still expensive for me.

Also, your doctor cannot force you to get the shot every month so it does require a certain amount of will power, but its a lot easier to do than taking a pill every day.

MY EXPERIENCE:

I was first started on methadone, then buprenorphine (subutex) but I was able to get high on both these drugs by saving my doses and using sparingly. Also, there is a "loophole" with buprenorphine where you can take small doses and get a goo high because one of buprenorphine's metabolites is a strong opiate. Anyway, eventually I was switched to Vivitrol with a new doctor, was on the shots for 2 years, and now I am over my addiction enough to be able to take the pills every day.

SUBUTEX AND METHADONE:

These are highly ineffective, both are stimulating opiates (subutex is half antagonist half agonist, but still has euphoric potential and can easily be abused). They are effective short term for keeping you off more dangerous drugs like heroin and painkillers but they only reinforce your addiction, just more slowly. The reason they are so popular is because big pharma companies shell out millions to promote their product and bias scientific studies, bribe doctors, etc... My doctor has been approached numerous times at pharmaceutical conferences by these companies and been offered all expense paid vacations etc.. to prescribe x drug. Fortunately he is a good doctor and never gave in. If you are on subutex, suboxone, or methadone I am NOT suggesting you throw them out and leave your doctor, but talk to him about naltrexone, specifically vivitrol.

TRANSITIONING FROM OPIATES TO NALTREXONE:

This is the hardest part, you need to ween off the opiates and onto the naltrexone. If you take the naltrexone while there are still opiates in your system, you will go into immediate and several withdrawal. What I did (under advisement of my doctor) was over the course of a month, take a lower and lower dose of subutex and a larger and larger dose of naltrexone everyday. For example day one was 8mg suboxone and a tiny tiny scraping of pill powder from a crushed naltrexone pill, probably less than one mg. Every day I took a lower dose of suboxone and a larger dose of naltrexone. The symptoms were mild and managed with a mild muscle relaxant and anti-nausea medication. The end was the hardest, when I was down to about 1/4mg suboxone I said "fuck it" and I took half a tablet of naltrexone. That night was rough, but not as bad as normal withdrawals. I was able to handle the symptoms by talking periodic walks in the cold outside air it was winter) and with my muscle relaxant. After that, I was able to take a full tablet without any problems for the next few days, then I got my first shot.

You can also do a "rapid detox" where they sedate you and inject you with naloxone and naltrexone, but this is expensive. Use it as a last resort and remember you will be saving a lot when you are no longer buying drugs.

I would suggest getting some Valium to help deal with the symptoms, my doc would not prescribe it because its addictive but it does help and you would only be taking it when you really need to, probably not more than a day or two.

DO NOT try rapid detox by yourself, you can die from withdrawal this way.

ME NOW:

I still think about the feeling of opiates, but I am in enough control to be able to take my naltrexone pill every day and not go any buy any opiates. The naltrexone therapy also cause me to cut back on drinking and other drug use (Google "the sinclair method"). Addiction is a lifelong disease, but it is manageable. I now only use speed for studying and getting things done (never more than once a week) and smoke cigarettes when I'm stressed (2 packs a year on average). Its a lot better than a bag a day heroin habit!

DRUGS THERAPY IS NOT ENOUGH:

I've been saying great things about naltrexone, but it alone is not the best method of getting over an addiciont. On of the most important  things you need to do during your naltrexone treatment is get out and find activities you enjoy. I picked up windsurfing, its great and I get a bigger rush from windsurfing now than I did from drug use. Exercise is important, which is why I suggest finding a sport you like. Learning a new language also has clinically proven benefits for addiction (use the Pimsleur method), it has to do with your brain focusing on forming new circuits other than those formed in your addiction. Try to make new friends, get a new job is possible, the goal is to create a new life that is different than you life as an addict because if you don't change anything in your life it will be very easy to fall back into your addiction.



Thats all I have now, I will be back to edit and update this thread if it seems people are reading it. Feel free to post your concerns, if you agree or disagree, have a better method, have tried this, etc... Anything goes just please be respectful, we are all just trying to help here.

Title: Re: Opiate Addiciton- "Miracle Drug" to end your addiciton.
Post by: microRNA on October 22, 2012, 09:28 pm
thanks for sharing your story and what worked for you. that is GREAT to hear you beat your addiction. congrats! keep it up and hopefully you will even be free of the antagonist

i am currently in the processing of slowly decreasing my dosage, with plans to get off eventually but its a very difficult process especially with medical conditions that are helped more by opiates than anything else. i am just tired of being a slave to the drugs
Title: Re: Opiate Addiciton- "Miracle Drug" to end your addiciton.
Post by: malacath on October 23, 2012, 12:08 am
thanks for sharing your story and what worked for you. that is GREAT to hear you beat your addiction. congrats! keep it up and hopefully you will even be free of the antagonist

i am currently in the processing of slowly decreasing my dosage, with plans to get off eventually but its a very difficult process especially with medical conditions that are helped more by opiates than anything else. i am just tired of being a slave to the drugs

Good luck to you as well, weening off is tough, my advice is go as slow as you need to even if it takes a year to go from your normal dose to nothing that's still progress. Just never go back up more than a step if you are having withdrawal problems stick with the same dose for a week or so before lowering more rather than going back up.  I wish naltrexone was available here its great even in pill form because every time you feel like using (after you detox) you can just pop a naltrexone and have another 24 hours of safety.

Another thing I forgot to mention that is helpful is once you are clean get a jar and everyday put the amount of money you would usually spend on drugs in a day in the jar every morning so you can visualize how much you are saving, this helped me quit my pack a day cig habit, by the time I was not smoking anymore I was saving around $60 a week. For my dope habit it was closer to $140 a week.
Title: Re: Opiate Addiciton- "Miracle Drug" to end your addiciton.
Post by: ZenAndTheArt on October 23, 2012, 12:41 am
You bring up some very good points there Malacath, especially the 'Drugs therapy is not enough' section.

I was prescribed Naltrexone, when it had 'built up' enough in your system the blocking effects would last for three days. In the EU you can get Naltrexone implants, which I believe can last up to six months!
Title: Re: Opiate Addiciton- "Miracle Drug" to end your addiciton.
Post by: Ben on October 23, 2012, 01:27 am
It's a great thing if drugs like these help you kick a habit.

I would not take then lightly however, they do mess with the natural opioid system in the brain as well, and will cause adverse effects accordingly.

The development of drugs or even vaccines that render some substances ineffective is still in its infancy, with a nicotine blocking treatments on its way.

This may seem to be a good development at first sight, but it also poses problems: what if you are taking long lasting opioid blockers, but you really need opiates to treat pain after trauma? You could find yourself in a situation where you break a leg and usual pain management is not effective because of the preventative medication you have been taking. Chances of that coinciding may not seem that large, but if you happen to be one of the unlucky few, you're in for a hell of an experience.
Title: Re: Opiate Addiciton- "Miracle Drug" to end your addiciton.
Post by: malacath on October 23, 2012, 07:02 pm
It's a great thing if drugs like these help you kick a habit.

I would not take then lightly however, they do mess with the natural opioid system in the brain as well, and will cause adverse effects accordingly.

The development of drugs or even vaccines that render some substances ineffective is still in its infancy, with a nicotine blocking treatments on its way.

This may seem to be a good development at first sight, but it also poses problems: what if you are taking long lasting opioid blockers, but you really need opiates to treat pain after trauma? You could find yourself in a situation where you break a leg and usual pain management is not effective because of the preventative medication you have been taking. Chances of that coinciding may not seem that large, but if you happen to be one of the unlucky few, you're in for a hell of an experience.

Thank you for bringing this up, I meant to say a few words on this.

As far as long lasting effects go, there have been several studies done on long term use of naltrexone and it has not yet been found to cause any negative long term effects. This is probably due to the fact that naltrexone only binds to mu-opiate receptors which are primarily associated with feeling of pleasures and pain management. Your body has other opiate receptors that remain open which also play a role in natural pain relief among other things.  Additionally you body does several other things to relieve pain in the event of serious trauma. In the end, you will probably experience a good amount more of pain if you are in an accident while taking naltrexone but it wont be like you have no natural defense against pain, there are also non-opiate painkillers and reversal drugs that the hospital can give you once you get there so you would only experience the more intense pain until you are treated.

It is something to consider, but I can't think of a situation where this risk is not justified, its a lot more dangerous to continue using.

It is for this reason that many people taking naltrexone carry a medication ID bracelet or wallet card, in case opiates need to be given.
Title: Re: Opiate Addiciton- "Miracle Drug" to end your addiciton.
Post by: Ben on October 24, 2012, 01:08 am
It is something to consider, but I can't think of a situation where this risk is not justified, its a lot more dangerous to continue using.

It is for this reason that many people taking naltrexone carry a medication ID bracelet or wallet card, in case opiates need to be given.

Whether the risk is justified is hard to tell, that's something that really varies for each person. I'm just pointing out that in some situations the implications can be quite severe. If you were to suffer trauma from a mechanical accident, the first cause of action in pain management would probably administering morphine in the ambulance. A bracelet or something similar would be very useful to notify emergency response staff that opiates will not have much of an effect, but it will also leave them with a problem: perhaps there are other substances that can still be effective in managing pain, but those may not be available in an ambulance since it's not a pharmacological wholesale supply on wheels.

The 'natural' response to unbearable pain is basically passing out, which is not something you want when dealing with a trauma victim under most circumstances. Being rendered unconscious from pain despite being given opiates could be mis-interpreted as a sign of a different condition (such as head trauma)  leading to improper treatment.

That said i'm not saying you should never take these medications to kick a habit, just to be aware that there are some risks involved when the things you least expect happen just at that time. Besides that naltrexone has a pretty good safety record as it has been used for a few decades to treat alcohol dependence (quite successfully).

There is a big difference between taking it against alcohol dependence vs opiate dependence though: in treating alcohol dependence it still allows you to get as drunk as you like, but limits the addictive properties of alcohol. In opiate dependence it simply blocks the substance from having any effect,  but not limiting withdrawal problems at all. It would be comparable to taking something like disulfiram against alcohol addiction, making it impossible to use rather then interfering with the mechanism responsible for addiction.
 
Title: Re: Opiate Addiciton- "Miracle Drug" to end your addiciton.
Post by: microRNA on October 24, 2012, 01:24 am
i dont know if ambulances do, but if they have bup for analgesia that would at least still be partly active because of its activity and the NOP receptor which promotes anti-nociception

plus it binds so strongly it may rip the naltrexone off, not sure though cause i didnt check the binding affinities. does nal block bup as well at mu?
Title: Re: Opiate Addiciton- "Miracle Drug" to end your addiciton.
Post by: BobSacamano1 on October 24, 2012, 09:13 pm
My friend is prescribed that for alcoholism.  Definitely no recreational value, and definitely blocks opiates.  You would really need to want to quit to have that be effective so 'miracle drug' is a little strong.  Also, I'm not sure how it deals with withdrawal effects, but that is usually the hardest part of breaking the opiate addiction cycle.
Title: Re: Opiate Addiciton- "Miracle Drug" to end your addiciton.
Post by: Ben on October 25, 2012, 01:28 am
i dont know if ambulances do, but if they have bup for analgesia that would at least still be partly active because of its activity and the NOP receptor which promotes anti-nociception

plus it binds so strongly it may rip the naltrexone off, not sure though cause i didnt check the binding affinities. does nal block bup as well at mu?

It might, or might not. The problem with substances like naltrexone is that they bind very strongly to the receptors, despite not activating them. There is no magic potion that simply clears these bindings instantly, so it may simply be a matter of time before opiates are effective again.

The mechanism of action of these compounds requires them to bind very strongly to the receptors, up to the point where even large doses of opiates cannot displace them anymore. This renders you insensitive to both the addictive/negative effects as well as the analgesic/positive effects in equal degrees.

Obviously these substances have no recreational effects at all, the only effect i would expect is negative since it also disturbs the natural opiod system. I have no personal experience with these substances, but i'd reckon side effects include apathy and possibly depression. I suppose the latter would then be treated with SSRI's, resulting in an odball cocktail of medication that overall does more harm then good.