Pharmacology - Opioid Tolerance: Reversing Receptor Sensitivity

[fiveleggedrat]

Swim just spent about the past several days on the net looking for both naloxone and naltrexone, in both pharm form and pure chemical form; Swim can find a supplier of neither (Swim must either A) have a script B) Chem licenses or C) Have assorted medical licenses)

Looks like Swim can't even do this study now. Fuck this stupid fucking nonsense on a substance that saves lives on it's own.

Swim does not have money to see some bloated fucking doctor for a prescription, and what's the chance a doctor would script anyways

I'm so furious. I've done so much research, and once again, the law is the only thing stopping it's completion.

And, I can't even ask for help finding a source. Lovely.

I hate this country. /endrant

[Cakes]

It's a darn shame no one else even bothers helping me out with this.

hell, I'd take it for you but I can't afford it either .

if you're needing help with money, our idea for this week is dog poo. We saw it on King of theHill. Like people may not pay for lawnmowing but they could feel real different if SWIM would save them from picking up dogpoo. a shop vac on battery might be just the thing.

our idea last week was custom guitar picks; real easy to make from shrinky plastic and a computer printer but hella expensive to order. if I was SWIM i might SPAM every band on myspace and offer to do a set from their logo; makes great swag to toss to the crowd.

[Richard_smoker]

i'm sure you can find naltrexalone from an online pharmacy... i assume you're looking for a US supplier. I can tell ya that it's in the very least-controlled substance category. one step away from over the counter. -DICK

[fiveleggedrat]

Dude, I swear, I spent 12 hours internet binging looking for it in US and international pharmacies. They all want me to fax in a script, and I'm not getting a felony for forging a script, that's nuts. I don't have the money to see a damn doctor either.

The chem supply companies either A) dont service individuals B) want med/chem licenses or C) Wont sell less than huge bulk orders over 500 bucks.

I never have luck sourcing anything; everyone here is always like "Google!" and I have sold my soul to google, and still have nothin'. Swim has only ever been able to get tramadol online.

I'm trying to find a heroin clinic; I plan on going and pretending I'm a junkie worried about overdose to get a script for naloxone, or pray they give me a free ampule/loaded syringe. I even contemplated going to a hospital pretending I'm ODing on heroin. I don't even have a single track mark either, and def. don't look like one. Darn, once again.

Edit: I'm an idiot when it comes to sources, I guess. So often gold members and up say "Oh, sources forum is useless to us, we can find what's in their on our own, etc", But I'm the dummy it would do wonders for, lol.

[Richard_smoker]

no no... i apologize. i've done my own google search, and you're telling the truth.

sorry. this is an example of supply vs. DEMAND in action.

you're probably the only the 2nd individual in the history of the internet to actually SEEK OUT this drug from non-convential prescriber. notice how prevalent ultram, soma, flexeril, viagra are? they're all equal or more-controlled than naltrexalone.

Personally, I 'get' what you're trying to do here, but I honestly believe that the risk-to-reward ratio here makes this experiment not really worth carrying out... if you're not sure what i mean by this, then go ahead and block out your opiate receptors with a very small dose of buprenorphine. you will see that ANY attempt to self-medicate with other opiates is virtually impossible for 2 to 4 days following the bupe...then, when your opiate receptors are finally cleared-out, it still will take several days AFTERWARD in order to achieve the "high" you previously got off any reasonable dose PRIOR to the bupe.

I hate to interject my own opinion in this kind of scenario, but in this case, i just couldn't help myself...if swim could go back in time, he would try to talk himself out of any and all experimentation with opiates. Borrowing a comedian's reference to his dad's quote: "Son, you're playing with fire."

but that's a different issue entirely. And in some ways my opinion regarding the dangers of opiates & their unusually powerful addictive properties goes against the very fiber of this forum. So again, I'm sorry for throwing in my $0.02.

However, regarding my wholehearted belief that naltrexalone will not reduce your opiate tolerance in REALITY (maybe theoretically, but not in reality)...I stand by this statement. True, it demonstrates that you're thinking heavily and probably in the correct direction on this subject, but from reading/hearing about experiences of others, i gotta say this is a pretty empty arena. you'd probably be better served spending the $$ on something else. -DICK

p.s. regarding your original post, and the NMDA theory--this is a much stronger argument...I'm pretty sure that in practice, DXM is not much different than MK-801...you can mix low-dose dxm with a regimented opiate dose to decrease overall tolerance, but in practice many people find that the DXM 'robs' them of the natural euphoriant properties of the opiate itself. correct me if i'm wrong, but it's the euphoriant that you're seeking. to clarify: as the dose of dxm is escalated, the euphoriant properties of the opiate tend to DECREASE.

Regarding iNOS and Nitric Oxide Synthesis--again, very interesting post; definitely shows that you're thinking along the right tracks and that you're comprehending the medical/biological literature--but realize that we this is an enzyme/transmitter that is virtually universally used by many different tissues in the body. one example is with erectile dysfunction treatment. This is how Viagra (and cialis/levitra) effect the localized vasculature of the penis/corpus cavernosa. as you probably already know, these drugs are very new and thus, not much is known or understood about how to affect the iNOS system (outside of using viagra et al).

-DICK

[fiveleggedrat]

Swim refuses to accept that opioids don't work anymore. Never. They are Swim's only drug he really ever enjoyed; he only had about 8-10 months of actual usage, on and off, before his tolerance developed.

I don't think you see what Swim is getting at:

Swim lost ALL the euphoria, and his doses, just to get PHYSICALLY sedated, as in CNS depression and pupil contraction ONLY, went up 4-7 TIMES what they were. WHY? NO REASON.

Swim used to take 4mg hydromorphone intranasal and nod out, hardcore. He can now RECTAL 16mg all at once, with promethazine, and get a ONE HOUR buzz.

Why? Swim NEVER abused opiates, NEVER used more than 2x a week, and even then took breaks. Swim is fucking furious because he ALWAYS had self control, and not even a SLIGHT tinge of addiction or ANY physical tolerance develop, until a 3 month break when he moved and had money to do opioids again.

I refuse to acknowledge that Swim cannot enjoy the only drug he ever truly enjoyed, and lost for NO GOOD REASON.

Swim HATES people who can get high all they want, and build up little to no tolerance, but Swim followed the rules and was a good boy, but still got hit with a stick in the face. Fuck that.

Plus, besides Swim's selfish, whiny self, this has potential to help other people.

Richard_Smoker, did you see the paper Psych0naut linked to a few posts up? It's that kinda thing. And there is at least some hope. I have several theories, including lesser ones not mentioned here, but the naloxone/naltrexone thing is my main idea, and the most feasible

Risk to reward? What is the risk? Swim sees no risk here.

1) I can't get bupe and 2) It's an agonist, and I want to test a pure antagonist, with high affinity for Mu receptor, because I believe that is the one that lost effects.

Yeah, I can get Fioricet, Soma, and Tramadol, but not a fucking opioid overdose antidote. WHY?! Because the government WANTS all the users to die.

And Swim has read about this happening with benzos and being fixed.

I will not stop researching and spending 6 hours a day reading old medical papers until I answer this question. I will solve this, I am determined

Feel free to share any and all opinions man, this is why I live on this forum and make threads.

Swim did the DXM test, and it failed. And, Swim refuses to be seeing crosseyed and being unable to function just to get a buzz. Swim is extremely sensitive to DXM as well, and it makes Swim extremely paranoid and such. In the past, when opioids did work, Swim also tried mixing DXM with opioids to potentiate doses; it did nothing back then too, causing just a disjointed, spacey, undesirable high.

Check out my last post about CCK and Proglumide: This sounds VERY realistic too IMO.

Edit: Swim's only alternative to figuring out reversal of permatolerance is IV. Swim sees IV as a big risk, a danger, something he is only half ready to handle, and one he wants to put off for years; If Swim can figure this out, he would not even consider IV ever again; the satisfaction from opioids orally is plenty. Even then, IV would eventually stop working too, the same things will happen with IV, and then Swim will only turn to other, more risky, desperate ways to get a high.

Seriously, Swim is content with tramadol and pot. That's ALL Swim wants. Tramadol has no effect now.

Swim has not had euphoria since he had some meth, and Swim hates Stims, and they make him fiend and act crazy, and WILL get him addicted, whereas with opioids, he just gets controllable cravings.

[Club Head]

Swim has heard that Dextromethorphan is actually the same as the opioid molecule, however reversed in a mirror-image so it retains some of the characteristics of opioids (cough control) while not behaving as an opioid in the opioid receptors in the body. Can anybody confirm my statement? Swim is not certain, this is something Swim learned from a science teacher in school, and it could be wrong. Can anything be done chemically to enhance these similarities to opioids? Swim would imagine that it is a synthetic or semi-synthetic copy hence the name "meth(orphan) <similar to morphine> and "Dextro" meaning left side or other side. Comments please. Swim needs to know this. C

Reputation Comments on this post:

	make your own thread for it
	Thread hijacking.

[fiveleggedrat]

First, post in the right area. This thread has nothing to do with that.

Second, all the information you seek is on the internet, and we aren't going to find it all for you.

[Club Head]

Swim doesn't think swiy speaks for everyone in the forum and since swim thought that since it was an opioid related question and as it was similar enough to fit in the thread it wouldn't bother anyone but I guess I was wrong, it annoyed the heck out of swiYOU, and dang, just because swiy doesn't know the answer to this, no need to get rude, does swiy have a problem with swim personally? Swim is sorry for what ever swim did. Last of all, everything in these threads is probably on the internet somewhere, but swiwe all have similar interests and some of swius probably know more than others, so swiwe learn from each other, & swim thought that was the purpose of this forum. Swim was making a comment and asking a question that is NOT on the internet if swiy read it carefully. Do swiy think that "a way to enhance the molecule" would be on the internet? Swim doesn't.

Club Head added 3 Minutes and 57 Seconds later...

BTW Swim never asked anyone to research this for swim. swim only asked for comments.

Club Head added 9 Minutes and 47 Seconds later...

[QUOTE=imyourlittlebare;494633]tolerance can occur very quickly especially in certain individuals. Its just the nature of the beast. NMDA antagonists, while they seemed promising, offer little hope. I have a compiled chart of the effects of certain nmda antagonists on opiate tolerance and addiction from a neuropharm book. Ill try and get that up. As for anything else, I cant go in depth. But there is other forces at work. Not the receptors themselves, but something refered to as norepinephrine. And there are transporters for certain neurotransmitters effected by addiction and tolerance along with certain changes that can be changed back by ibogaine. Aside from ibogaine, the idea is flawed. Tolerance comes back quickly, bupe is a partial agonist/antagonist meaning it agonizes partially the mu receptor and antagonizes the kappa opiod receptor. Theres a ceiling effect. One thing i remember about methadone is its notorious effect to raise tolerance to a point where its useless trying to abuse opiods anymore. Ill let you know more later.

imyourlittlebare added 3 Minutes and 39 Seconds later...



ketamine, while an NMDA antagonist, esp nr2b which is a subunit, also effects GABAergic, Seritonergic, Opiate, and muscarinic pathways. It has a synergic effect. Thats why its being tested for certain types of depression and other things. They found that those who had one i.v. administeration of a low dose of ketamine required lower amounts of opiates for ANALGESIA. this is not the same as EUPHORIA. Or else everyone would be abusing 7 hydroxymitygaine since its 25 times more potent than morphine. I have these cited on various portions of the website.

imyourlittlebare added 2 Minutes and 35 Seconds later...

Originally Posted by stupidorange

DXM is indeed a synthetic opioid, although it's not "the" opioid molecule (there are many different ones!).

I thought your etymology sounded pretty shaky, but as it turns out you're right:

while it is a mirror molecule, this does not mean it would have any effects of opiods. In fact, its effect to reduce cough is questioned. Shapes of molecules can be very close and have very different effects. Take MPPP, a strong opiod, if one thing in synthesis goes wrong as it has in the past it is called mptp and can cause brain damage and parkinsons disease like symptoms that are not reversable.

imyourlittlebare, swim wants to thank you for not being rude & patiently answering swim's query & for being so generous with swiy's knowledge & obvious intelligence. Swiy is what these forums are all about and swim wants to make it known how much swim appreciates people like swiy. Thank swiy. Swiy is awesome. Swiy is so brilliant. Swim is not worthy. Lol.

[stupidorange]

Originally Posted by Club Head

Swim has heard that Dextromethorphan is actually the same as the opioid molecule, however reversed in a mirror-image so it retains some of the characteristics of opioids (cough control) while not behaving as an opioid in the opioid receptors in the body. Can anybody confirm my statement? Swim is not certain, this is something Swim learned from a science teacher in school, and it could be wrong. Can anything be done chemically to enhance these similarities to opioids? Swim would imagine that it is a synthetic or semi-synthetic copy hence the name "meth(orphan) <similar to morphine> and "Dextro" meaning left side or other side. Comments please. Swim needs to know this. C

DXM is indeed a synthetic opioid, although it's not "the" opioid molecule (there are many different ones!).

I thought your etymology sounded pretty shaky, but as it turns out you're right:
[quote=Merrian Webster]Etymology:dextr- + methyl + morphinan parent substance of morphine alkaloids, from morphine + 3-an[/qoute]I can't comment on the chemistry though, unfortunately.

stupidorange added 0 Minutes and 51 Seconds later...

Damn I wish I could edit my post!

Originally Posted by Merrian Webster

Etymology:dextr- + methyl + morphinan parent substance of morphine alkaloids, from morphine + 3-an

Reputation Comments on this post:

dont incourage off-topic discussion, especially not in this thread, please, thank you.

[DonPeyote]

SWIM has tried ULDNx (ULTRA low dose Naltrexone), Proglumide, and Ketamine, to reduce tolerance and dependence on Opioids. The ULDNx and Proglumide were useless. Only Ketamine had any effect.
Ketamine substituted quite well for SWIM addiction to opioids, so well that he became addicted to the Ketamine too! Whilst high on K, SWIM noticed normally high (100mg Oxycodone) doses had almost no effect. The Ketamine stole the show. However, SWIM was taking low dose Ketamine (ie. 30mg IM) frequently throughout the day. Unfortunately, Ketamine used that often leads to a rapid tolerance build up, so shortly one is shooting 100mg per pop. So there are limits to the usefulness of NMDA antagonists unless one has an unlimited supply. And an unlimited supply of Ketamine would be what? Heaven?

Reputation Comments on this post:

Thanks for sharing dude.

[imyourlittlebare]

tolerance can occur very quickly especially in certain individuals. Its just the nature of the beast. NMDA antagonists, while they seemed promising, offer little hope. I have a compiled chart of the effects of certain nmda antagonists on opiate tolerance and addiction from a neuropharm book. Ill try and get that up. As for anything else, I cant go in depth. But there is other forces at work. Not the receptors themselves, but something refered to as norepinephrine. And there are transporters for certain neurotransmitters effected by addiction and tolerance along with certain changes that can be changed back by ibogaine. Aside from ibogaine, the idea is flawed. Tolerance comes back quickly, bupe is a partial agonist/antagonist meaning it agonizes partially the mu receptor and antagonizes the kappa opiod receptor. Theres a ceiling effect. One thing i remember about methadone is its notorious effect to raise tolerance to a point where its useless trying to abuse opiods anymore. Ill let you know more later.

imyourlittlebare added 3 Minutes and 39 Seconds later...

Originally Posted by DonPeyote

SWIM has tried ULDNx (ULTRA low dose Naltrexone), Proglumide, and Ketamine, to reduce tolerance and dependence on Opioids. The ULDNx and Proglumide were useless. Only Ketamine had any effect.
Ketamine substituted quite well for SWIM addiction to opioids, so well that he became addicted to the Ketamine too! Whilst high on K, SWIM noticed normally high (100mg Oxycodone) doses had almost no effect. The Ketamine stole the show. However, SWIM was taking low dose Ketamine (ie. 30mg IM) frequently throughout the day. Unfortunately, Ketamine used that often leads to a rapid tolerance build up, so shortly one is shooting 100mg per pop. So there are limits to the usefulness of NMDA antagonists unless one has an unlimited supply. And an unlimited supply of Ketamine would be what? Heaven?

ketamine, while an NMDA antagonist, esp nr2b which is a subunit, also effects GABAergic, Seritonergic, Opiate, and muscarinic pathways. It has a synergic effect. Thats why its being tested for certain types of depression and other things. They found that those who had one i.v. administeration of a low dose of ketamine required lower amounts of opiates for ANALGESIA. this is not the same as EUPHORIA. Or else everyone would be abusing 7 hydroxymitygaine since its 25 times more potent than morphine. I have these cited on various portions of the website.

imyourlittlebare added 2 Minutes and 35 Seconds later...

[quote=stupidorange;493621]DXM is indeed a synthetic opioid, although it's not "the" opioid molecule (there are many different ones!).

I thought your etymology sounded pretty shaky, but as it turns out you're right:

Originally Posted by Merrian Webster

Etymology:dextr- + methyl + morphinan parent substance of morphine alkaloids, from morphine + 3-an[/qoute]I can't comment on the chemistry though, unfortunately.

stupidorange added 0 Minutes and 51 Seconds later...

Damn I wish I could edit my post!

[/i]

while it is a mirror molecule, this does not mean it would have any effects of opiods. In fact, its effect to reduce cough is questioned. Shapes of molecules can be very close and have very different effects. Take MPPP, a strong opiod, if one thing in synthesis goes wrong as it has in the past it is called mptp and can cause brain damage and parkinsons disease like symptoms that are not reversable.

Reputation Comments on this post:

please get that up!! thank you!

[Richard_smoker]

wow. that was quite the post! seems i found myself lost a few times while you were running around, trying to hit every single base!

Most of it sounds about right, from memory anyways. but there is one thing that i was very unclear on:

Originally Posted by imyourlittlebare

ketamine, while an NMDA antagonist, esp nr2b which is a subunit, also effects GABAergic, Seritonergic, Opiate, and muscarinic pathways. It has a synergic effect. Thats why its being tested for certain types of depression and other things. They found that those who had one i.v. administeration of a low dose of ketamine required lower amounts of opiates for ANALGESIA. this is not the same as EUPHORIA. Or else everyone would be abusing 7 hydroxymitygaine since its 25 times more potent than morphine.

maybe you're just thinking too fast for me to keep up. are you saying that if ketamine decreased the dose required for euphoric threshold, then everyone would be abusing 7-OH-mitragine??

did you mean to insert something about how that IF this were true, then people would be injecting low-dose ketamine mixed with their opiates? and then, people would change their opiates-of-choice into a 7-OH-mitragine/ketamine mixture???

perhaps i'm focusing too much on this one part of your post, but it seems quite the leap in logic...please clarify your position. -DICK

Reputation Comments on this post:

Thanks for sticking around on this thread.

[fiveleggedrat]

I think he means that everyone would munch weaker/more common opioids with ketamine as a booster. I think he is saying also that IF it did increase euphoria (and not just analgesia) everyone would be doing it too. But that's me.

And bah for ketamine being rare in the United States.

Damn, sad Swiy didnt get much from proglumide or ULD naltrexone, first person Swim ever heard from that did not get help from proglumide. Everyone else was raving about it.

Great posts everyone, great info for Swim. Damn kratom needs to be here soon! Swim will be testing the kratom extract between him and his friend, comparing the differences in dose and effects for reference. Swim had maybe 250-300mg propoxyphene a week or more ago which gave no effects, but that was it opioid wise in a bit.

But yeah, guys, let me try to sum up the issue again, it might help. In Swim:

ANALGESIA can STILL be present, although in reduced amounts.
EUPHORIA is absent, 100%, and it stays that way.

Someone told me analgesia is the way medical people measure tolerance. Well god save Swim if he's ever in serious pain or an accident; it's gonna HURT.

[10001110101]

lot of misinformation on here.

Naltrexone (pure opiate antagonist) will RAPIDLY reduce tolerance, and will also RAPIDLY bring about w/d symptoms in opiate tolerant users.

you could lower your tolerance in 24 hours with naltrexone.

you could dramatically lower it in 3 days.

ever heard of the 24 hour detox they use for heroin addicts, they essentially knock them out for 24 hours and give them IV naltrexone for the duration.

they wake up clean, no W/D's, and then all they have to deal with are addiction issues.

ULDN (Ultra Low Dose Naltrexone) is being used in combination with opiate receptor agonists (morphine, hydro, oxy, diamorphine, etc) as a means to both enhance analgesia and prevent tolerance.

please google this. it's pretty cool because not only does it enhance the effect of the opiates you're using, it also prevents tolerance accumulation.
the dosages are in the Nanogram range, so it may be difficult (although you could do serial dilutions to make an oral solution from naltrexone)


DXM will prevent or reduce further tolerance accumulation but will do nothing to reverse tolerance.

so let's say you get your tolerance down, 30-60mg (i think 60 is the effective dose but that seems high) along with your opiate dose will reduce the tolerance building effect of the drug, this study however was only referring to tolerance to analgesic effects so may have no effect on euphoria.

Melatonin will prevent or reduce further tolerance accumulation but will do nothing to reverse tolerance.
Melatonin acts on peripheral benzodiazepine receptors to prevent tolerance accumulation in the same manner as NMDA antagonists (DXM)

Buprenorphine is an opioid agonist/antagonist so it does 2 things:

1) it works like any other conventional opiate to provide analgesia through stimulation of the mu-opioid receptor
2) it works similar to naltrexone at the same time to block the mu-opioid receptor

so bupe is given to addicts a la methadone as an opiate substitution therapy, but it also has the added benefit of blocking the effect of any additional opiate. so you take the bupe like you'd take 'done it will suppress cravings and WD's but will also block the effect of anything else. so let's say you are on bupe maintenance and you try to IV heroin, no high because although the receptor is being moderately stimulated by the bupe it is also blocking the diacetylmorphine from further stimulating the receptor, therefore blocking the high!


it ain't rocket science.

onzero added 12 Minutes and 32 Seconds later...

but yeah all that being said.


even if you lower your tolerance to an opiate naive persons tolerance the euphoria will probably not be the same.

the mind is quite intricate in its adaptive processes, your mind has built in certain expectations on how it is "supposed" to feel based on your frequent opiate use. it is not the mu opioid receptors that you should be primarily concerned with as you could simply take a higher dose and get the same euphoria.

the real issue here has to do with the neural pathways between the Ventral Tegmental Area and the Nucleus Accumbens. Dopaminergic pathways from the VTA to the NA are the ones primarily involved in addiction and produce the feelings of euphoria and familiarity provided by drugs of abuse.

it is these pathways that must be changed in order to achieve a higher level of euphoria.


honestly i think several years off of moderate opiate use will allow SWIY to get back to that "virginal" state. but i'm talking several years completely opiate abstinent. even a few small incidences of opiate use (prescribed or otherwise) would drastically change the outcome of this experiment. your mind has to "forget" what it's like to be high on opiates. if the addiction is deep enough you may never be able to get back there. i doubt many addicts ever truly go long enough to find out!

Reputation Comments on this post:

Fantastic summary of information. Saves me from wasting time digging through information. Very nice to have it all here ...

[Richard_smoker]

actually, and i can't believe no one has chimed in with this yet...

actually, i think your problem is with the specific opiate of choice. yes, i believe that it's the hydromorphone.

swim can say from countless tales of experience that this drug can be a very seductive 'gateway' opiate...yes, it is capable of showing the novice opiophile the greatest, most euphoric rush, buzz, nod. But, after a while, it really begins to lose its luster.

now, the way i see it swiy has 3 options.

1. mainline the dilaudid. yes, iv application will probably be better than rectal admin. swiy will get a 'rush' from iv use. but, i'm secretly hoping that swiy're not going to try this...after all, swiy must realize that simply changing administration tek's will only result (eventually) in the same situation swiy're in right now. dissatisfaction.

2. stop taking any and all opiates now while swiy is still ahead. remember, no matter how much swiy can rationalize that he doesn't have a problem, he is still playing with fire...why? because his tolerance has skyrocketed. is this how he expected addiction to rear its ugly head? OF COURSE NOT! Do you really think that most addicts TRIED to become addicted??? OF COURSE NOT!!! it was through seemingly innocent little bursts of intelligence, much like your realization that you cannot achieve the same level of gratification that you once could.

3. swiy's final veritable option... change opiates. for most people who take opiates for pain relief or fun, they generally use a longer-lasting, more 'run-of-the-mill' opiate as their primary drug of choice. Then, when they want to 'top-off' their experience with a stronger opiate effect, they will THEN take the rectal or nasal dilaudid. see?

swiy're not the only person in the world whom dilaudid only affects for 1 hour. that's a pretty common scenario--once people get accustomed to the drug effects.

Knowing swiy, i think that option #3 is probably going to bring the most noticeable short-term gratification. The only real problem that comes to mind (aside from addiction) with option #3 is overdosing on tylenol. Many people in this situation will take something like lortabs/vicoden/percoset/percodan/tylox as their primary drug of choice. in order to get the euphoria that you describe, most people will need to take more and more of the drug to find their 'sweet spot' (at first).

unfortunately, the high swiy is chasing is extremely elusive. Most people will get a crazy high AT FIRST from opiates (especially a high-dollar one like hydromorphone). The 'addiction' sneaks in while the person is 'making other plans.'

-DICK

[Matt The Funk]

Originally Posted by Richard_smoker

actually, and i can't believe no one has chimed in with this yet...

actually, i think your problem is with the specific opiate of choice. yes, i believe that it's the hydromorphone.

swim can say from countless tales of experience that this drug can be a very seductive 'gateway' opiate...yes, it is capable of showing the novice opiophile the greatest, most euphoric rush, buzz, nod. But, after a while, it really begins to lose its luster.

now, the way i see it swiy has 3 options.

1. mainline the dilaudid. yes, iv application will probably be better than rectal admin. swiy will get a 'rush' from iv use. but, i'm secretly hoping that swiy're not going to try this...after all, swiy must realize that simply changing administration tek's will only result (eventually) in the same situation swiy're in right now. dissatisfaction.

2. stop taking any and all opiates now while swiy is still ahead. remember, no matter how much swiy can rationalize that he doesn't have a problem, he is still playing with fire...why? because his tolerance has skyrocketed. is this how he expected addiction to rear its ugly head? OF COURSE NOT! Do you really think that most addicts TRIED to become addicted??? OF COURSE NOT!!! it was through seemingly innocent little bursts of intelligence, much like your realization that you cannot achieve the same level of gratification that you once could.

3. swiy's final veritable option... change opiates. for most people who take opiates for pain relief or fun, they generally use a longer-lasting, more 'run-of-the-mill' opiate as their primary drug of choice. Then, when they want to 'top-off' their experience with a stronger opiate effect, they will THEN take the rectal or nasal dilaudid. see?

swiy're not the only person in the world whom dilaudid only affects for 1 hour. that's a pretty common scenario--once people get accustomed to the drug effects.

Knowing swiy, i think that option #3 is probably going to bring the most noticeable short-term gratification. The only real problem that comes to mind (aside from addiction) with option #3 is overdosing on tylenol. Many people in this situation will take something like lortabs/vicoden/percoset/percodan/tylox as their primary drug of choice. in order to get the euphoria that you describe, most people will need to take more and more of the drug to find their 'sweet spot' (at first).

unfortunately, the high swiy is chasing is extremely elusive. Most people will get a crazy high AT FIRST from opiates (especially a high-dollar one like hydromorphone). The 'addiction' sneaks in while the person is 'making other plans.'

-DICK

So will SWIM never find this euphoria again?
I guess this is better for him as he got "clean" (non daily, or even weekly/monthly) a little while ago. SWIM recently tried with Oxycodone and went through about 500mg in 4 days (working his way up in dosages), highest dose ended up being 170mg. He actually did manage to squeeze a LITTLE of that different kind of opiate euphoria, but got all other effects to the full effect. SWIM supposes he's had his fun and can still enjoy them to relax once in a blue moon. SWIM's opiate of choice always has, and always will be hydrocodone (since it provides him the most euphoria) but he is thinking about actively seeking out tramadol...would this maybe work? SWIM hasn't tried tar or fent since breaking the addiction and probably won't, but would these substances maybe help bring back the euphoria?

[fiveleggedrat]

Swim has changed opioids, of course. All, same thing: Tramadol, hydromorphone, hydrocodone, morphine, heroin, etc. It is NOT the drug. It is NOT the substance; it is something else.

Swim never uses. Swim has used less than 6 times in the past 2 months.

I never searched naltrexalone, but naltrexone. I check spelling, trust me. I have searched by both all brand names and substance name, as well as CAS number.

Any and all opioids used to rock. Now they do nothing, but CNS sedation. I don't think anyone is getting what I'm saying here; this is not the same type of tolerance from using all the time. Swim did not get tolerant until Swim moved and took a break for a few months.

I know plenty of people who got clean from being full blown, several year addicts on opioids; they can use now whenever they want and get full nodding euphoria, but Swim who never was addicted at all and never uses can't get anything; explain why.

Swim is aware that chasing the drug is negative for behavior; this is irrelevant to Swim. Swim's logic is once things go back to at least close to how they were, Swim will be content. Swim was content with tramadol every now and then, and that was plenty to make him happy. Swim wants his occasional usage in his life to improve quality of life.

Swim definately realized IV is not the answer; Swim might get something for a little bit, but it will stop just as everything else did. Effects will cease; admim is now pointless too. Rectal was great the first 2 times he did it; now, same thing, no effects.

The high Swim wants is what it used to be after the original "opioid honeymoon" wore off. Swim did NOT "abuse", only use, proper use like everyone here preaches, and the Swim got tolerant anyway. Swim took what people said he was the way to prevent tolerance, by using rarely and taking breaks often, even taking more precautions than anyone suggested, and Swim still got tolerant as someone using every single day for weeks on end, just with no addiction component.

Tramadol is very weak, this stuff only really works for those with no tolerance; this is why Swim used this stuff when he first started so often; people with any tolerance coming to this drug will likely get no effect at all.

Swim is the most paranoid, over cautious user, and is not abusing any drugs, nor has he; Swim USED them. Swim STILL got tolerant. This is like telling someone smoking pot once a week who had it stop working it was from tolerance, that smoking once a week was too much, and that even quitting for a few months would do nothing, that pot would just not work anymore ever, because they smoked a few times a month; it just makes no sense.

Swim does not have normal tolerance, Swim's tolerance is over reacting here, it's acting like he uses all day every day.

Swim does not exagerate at all here, he uses rarely. Swim has consulted every single user he knows, current and former addicts included, and his story does not match anyone; they can all still get euphoria, at least when they take a break for a few days to a week, and Swim breaks for months with nothing. Explain this.

And on expanding: Simple enough, Swim has no access to any other drugs. Swim also does not WANT other drugs. Swim does not enjoy stimulants of any type, and Swim cannot get MDMA or K, the only other things he really wants. Swim has too many problems right now, and using psychedelics, even if he could get this, would not be smart. Swim is stressed and upset lately; they would aggravate this.

Swim really enjoys opioids, and by far they are the most interesting drug to him.

Swim'll continue to figure out how to get his receptors sensitive again.

What if Swim was in pain? What if Swim really needed opioids for medical purposes? He would be fucked. Figuring this out has big implications.

[Cakes]

but he is thinking about actively seeking out tramadol...would this maybe work?

It is my understanding that this is different from the pain killer. it is a muscle relaxer. And if you are in pain, the thing to do is take them both together<that part i can confirm from experience.

honestly, since we like SWIM, we will go ahead and say that we are agreeing that it appears SWIM is getting a bit fixated on this opiate business. SWAN seriously suggests that he branch out. It sounds like he needs a fat tab of LSD to be truthful. and she further suggests that he make a list of at least three other new ones besides the acid and he go and do them before he goes back to the opiates.

Cakes added 21 Minutes and 1 Seconds later...

I will not stop researching and spending 6 hours a day reading old medical papers until I answer this question. I will solve this, I am determined

Feel free to share any and all opinions man, this is why I live on this forum and make threads.

Two things..first, congratulations on discovering independently what is now a very hot drug and research area.

second..the above quote illustrates my previous point about getting a little fixated. And we want to mention that behavioural training can be a very real thing. like if SWIM keeps beating himself into chasing after this drug, what is he teaching his subroutines really?

for people who plan to take these drugs, we found this sample medical card to carry with you:

TO MEDICAL PERSONNEL TREATING SWIM IN AN EMERGENCY: This patient is taking the oral opioid antagonist reVia , formerly known as Trexan (naltrexone hydrochloride).

In an emergency situation in patients receiving fully blocking doses of reVia, a suggested plan of management is regional anesthesia, conscious sedation with a benzodiapine, use of non-opioid analgesics, or general anesthesia.

In a situation requiring opioid analgesia, the amount of opioid required may be greater than usual, and the resulting respiratory depression may be deeper and more prolonged. A rapidly acting opioid analgesic that minimizes the curation of respiratory depression is preferred. The amount of analgesia administered should be titrated to the needs of the patient. Non-receptor mediated actions may occur and should be expected (e.g., facial swelling, itching, generalized erythemia, or bronchoconstriction), presumably due to histamine release. Irrespective of the drug chosen to reverse reVia (naltrexone hydrochloride) blockade, the patient should be monitored closely by appropriately trained personnel in a setting equipped and staffed for cardiopulmonary resuscitation.

For medical emergencies, call your regional Poison Control Center.
Further information may be obtained by calling: 1-800-4PHARMA.


Side 2

The name and telephone number of physician who prescribed reVia (naltrexone hydrochloride).

Physician's name:
__________________________________________________ _________________
Physician's telephone:
__________________________________________________ _____________
Patient's name:
__________________________________________________ ___________________
Patient's telephone:
__________________________________________________ _______________
Date treatment was initiated:
__________________________________________________ _______

from here:
http://quantumunitsed.com/materials/3508_Naltrexone.txt

[Richard_smoker]

yo 5-legs,

try searching for "Naltrexone" (generic for Revia).

I think "naltrexalone" is a common misspelling. -DICK

[Richard_smoker]

ok. well done.

so, with all that behind us, do tell how many mg of hydrocodone has swiy attempted without success? 20mg? 40? 60mg???

until one arrives at 'full blown' addiction (i.e. physical opiate dependence), it is virtually impossible to get happy off a small or even moderate dose of opiates.

that's why i said that at swiy's level, the most worrisome side effect might just be od'ing on tylenol. i once knew a particularly shady asshole (not the best role-model in the world). but he did "show me" how one could totally wrap their lives up around hydrocodone. This guy would take 4, 5, 6 10mg pills at a time. and he would gobble them up, proclaiming his wonderful self-indulgence as "peaceful", "wonderful", "the best", etc.

as always, continue to exercise caution and common sense. hope you find what you're looking for. -DICK

Reputation Comments on this post:

thank you for all the info.

[fiveleggedrat]

100mg hydrocodone causes a buzz. That's with 50mg promethazine, and with AND without CYP2D6 inhibitors. 16mg hydromorphone rectal gives a buzz. Swim can snort 2x the heroin his junkie friend shoots and get a buzz, what they call good shit. 400mg tramadol causes vomiting and mild buzz. At Swim's peak, 300mg was plenty for a nodding high, about 8 months into using on and off, meaning a day here a day there, per month. A buzz means a mild, weak, joke of stimulation, and complete lack of euphoria and no good mood/social anything. 300mg codeine causes a buzz. 40mg methadone, a buzz. 20 used to have Swim nodding. Swim has watched, very carefully all this happen, but it took a while to click; tolerance was going up quickly, even with Swim using rarely and breaking lots.

That;s the entire fucking insanity of it; Swim HAS no addiction but can't get happy off a big dose of anything. It's totally nuts. Swim can't find any answer except receptor inversion.

Swim is not even picky about opioids, he just wants decent effects from ANY one. Even kratom would make Swim happy.

[Richard_smoker]

hmmm maybe you need naloxone just to get high! lol -DICK

[fiveleggedrat]

Srsly!

Swim's going to try to obtain naloxone the legit route now, by visiting all the local methadone clinics; gotta be able to find it at one, if not at least a new lead to find it.

Any help with how about to legitimately obtain naloxone would be great; and suggestions about what to say, what to act like, etc would be great; legitimate medical reasons for obtaining this.

Swim figures just going in asking about what to do in case of OD, feigning ignorance, or asking directly for an antagonist or how to get one.

Swim has to keep this entire thing under $100 bucks too.

[Cakes]

Swim did NOT "abuse", only use, proper use like everyone here preaches, and the Swim got tolerant anyway.

nope. SWIM used twice a week. and that rate will have SWIM with a drug in his system all the time. Yes, he could take a three day break and get a rush but three days is not long enough for a full clean.