Opioids 85 years old and plan to start heroin. Need advice.

[cdin]

w

It amazes me that the bioavailability of oxy is listed as being the same for oral as it is with rectal ROA's...

Anyone ever hear of a crazy little thing called FIRST PASS METABOLISM...? Opioids are highly susceptible to it, so any route besides oral, will ALWAYS be more effective for analgesia, guys.

C'mon...

∞€lixir£lask∞

w oxycodone a lot of that first pass metabolism is changing it to --> oxymorphone which is more potent than the parent compound. imo eating oc with a cyp2d6/2d4 liver enzyme inhibitor is by far the best pharmacokinetics for pain relief, or even being high as you get an extra couple of hours.

 

[Elixirflask]

w



w oxycodone a lot of that first pass metabolism is changing it to --> oxymorphone which is more potent than the parent compound. imo eating oc with a cyp2d6/2d4 liver enzyme inhibitor is by far the best pharmacokinetics for pain relief, or even being high as you get an extra couple of hours.
____________

€

€lixir£lask: Ty, cdin, you rock... Some thankfully awesome points that you just made, my friend... especially since you briefly elaborated on the 'enhancement role' that inhibiting CYP enzymatic metabolism can play by strengthening the properties of the original parental compound(s), in order to give it more 'legs' {i.e.: or, more bang'z for ones' buck'z}, which I am relatively certain is •much• appreciated info for those readers here that are currently seeking to learn more, being less uninitiated knowledgeably as you are & who may still be quite new to all of this.

All that being said, I will take it one step further, to expound on the vitally important data that you just took the time to have courteously touched upon by provisioning it for them:

1. Oxycodone is metabolized {in part} by cytochrome P450 2D6 to oxymorphone, which represents less than 15% of the total administered dose, •regardless• of what ROA is utilized to administer it.

Source(s): https://www.google.com/amp/s/www.practicalpainmanagement.com/amp/416

2. Most opioids undergo extensive first-pass metabolism in the liver before entering the systemically. First-pass metabolism, is a process which occurs •only• when the ROA is administered orally, and •dramatically• reduces the bioavailability of the opioid.

3. Oxycodone is •extensively• metabolized hepatically {through the liver} and 10% of the dose is excreted unchanged in urine in adults, however the •majority• of the metabolites are excreted through one's urine {and if someone knew an easy method of how to •ever• reclaim that 10% would make that same someone into a near instant millionaire}, but any such DIY process to successfully perform that extraction {with the nasty exception of chugging ones' own piss or perhaps even by evapping the liquidated urine down into a dried crystalized powder to consume *blech*}, remains as being still unknown, ~or at least it's still not •yet• known, to the very best of my existing knowledge.

Sources: l., 1996; Lalovic et al., 2006), (Lalovic et al., 2006).Jan 5, 2012
https://www.frontiersin.org › full

Summarily, I believe that this data that I've just illustrated, is evidenciary enough to prove beyond any further shadow of a doubt, by my own research {which is likewise backed by the respectably accepted listed sources of extrapolated information I have both found & above listed}, to reasonably disprove the many numerous claims made, that have indicated that the oral ROA of oxycodone is the most efficient way to best utilize its' active properties for both its' either analgesic and/or recreational purposes. Personally, I would think that sublingual is the best manner to have it home administered, since I do not advocate the use of IV or IM usage.

∞ €lixir£lask ∞

{I have been a Blue light lurker for •many• years now, and as a retired surgical first assistant & physician's assistant for well over half of my life, I possess both the experience & knowledge required to make all of the statements that I have just made, in what is my first ever Bluelight illustrative debate to disprove an otherwise accepted theory that I have found to be incorrect.} It's just good to be here...

 

[cdin]

yo! great to have such a knowledgeable poster. welcome to BL!

im slightly confused by the post -- I was saying i get the best pain relief eaten, w inhibitors - just from experience but also under the assumption that a) oxymorphone is an important part of the codone experience an b) making as much of it as possible will be best ( for pain relief, legs etc) - which is why I always recommend and practice eating w inhibitors. I find that gives me solid pain relief for 4h, 6h to end, as opposed to 2h pain relief snorted, maybe less IV. I see at the end of your post, you recommend sublingual - which i feel im not understanding something - sublingual would avoid the liver metabolism that creates the oxymorphone, which is double the potency oral, and MUCH more potent parenterally -- I wonder which of those applies more since it's occurring in the liver? -- so at 10mg and 10%, we're talking an extra mg of potency, or if it's closer to how it works IV, then an extra 10 times potency. im sure the truth is somewhere in between, but adding 2-5mg (equivalent) to 10-50% perhaps to your dose is nothing to sniff at...

so i guess my question is - why do you suppose sublingual best given the lack of first pass metabolism creating the more potent metabolite?

@Elixirflask you a WoW player? :D

 

[Nas47]

Can only say-'I like this

 

[LucidSDreamr]

I thing your decision is yours. Freedom
And. Nobody else's to tell you that you can't do. 85 should be free heroin script.

You should score pharma dilauded it's better

 

[Elixirflask]

3.18.22

Great inquisitive reply, cdin, and it's the primary reason that I chose to write my first Bluelight post on this very misunderstood topic. It was time.

After a drug is consumed orally & swallowed, it is FIRST PASS absorbed by the digestive tract, which removes much of many drugs through its' gastric enzymes BEFORE it then enters the hepatic portal {ie. the liver}. Only then is it carried through the portal veinous system and into the liver before it is systemically absorbed by the body. This is the FIRST PASS metabolism effect, which greatly reduces the bioavailability of the drug because of the gastric enzymes FIRST removing much of the drug, in this specific case, oxycodone.

However, significant hepatic extraction still occurs when the other ROA's are instead used, because of SECOND PASS metabolism, which involves the hepatic portal vein and hepatocytes, but BYPASSES first pass gastric metabolism, which is why swallowing oxycodone isn't anywhere as effective as other ROA's. See, the liver still metabolizes oxycodone, but when it hasn't first gone through the gut, there's quite simply a lot more of the medication in ones' system, that hasn't been destroyed by the gastric enzymes. So, in essence, you are not removing the metabolites at all, but you are increasing the amount of the active drug, which then additionally INCREASES the amount of metabolites, such as the oxymorphone that provisions much of the analgesic effects, just as you stated.

Four primary systems affect the first pass metabolism of a drug... the gastrointestinal lumen enzymes, gut wall enzymes, bacterial enzymes, and hepatic enzymes.

Thus, by utilizing alternative ROA's , such as nasal insufflation, IV, IM, aerosol inhalation, suppositories or sublingual, you are only avoiding the destructive first-pass metabolism effect of the gut, and instead only subjecting the oxycodone to SECOND PASS metabolism by the livers' hepatic enzymes, leaving you with a much higher bioavailability.

That's why I wrote all of that, to illustrate the erroneous thinking promoted by most people who don't understand that •second pass metabolism•, well, it beats the hell outta using •first pass metabolism•.

I hope that clears the waters a little more, and I apologize for not including all of that in my first penning.

You rock;

∞€lixir£lask

 

[Elixirflask]

yo! great to have such a knowledgeable poster. welcome to BL!

im slightly confused by the post -- I was saying i get the best pain relief eaten, w inhibitors - just from experience but also under the assumption that a) oxymorphone is an important part of the codone experience an b) making as much of it as possible will be best ( for pain relief, legs etc) - which is why I always recommend and practice eating w inhibitors. I find that gives me solid pain relief for 4h, 6h to end, as opposed to 2h pain relief snorted, maybe less IV. I see at the end of your post, you recommend sublingual - which i feel im not understanding something - sublingual would avoid the liver metabolism that creates the oxymorphone, which is double the potency oral, and MUCH more potent parenterally -- I wonder which of those applies more since it's occurring in the liver? -- so at 10mg and 10%, we're talking an extra mg of potency, or if it's closer to how it works IV, then an extra 10 times potency. im sure the truth is somewhere in between, but adding 2-5mg (equivalent) to 10-50% perhaps to your dose is nothing to sniff at...

so i guess my question is - why do you suppose sublingual best given the lack of first pass metabolism creating the more potent metabolite?

@Elixirflask you a WoW player? :D

Not a WoW player, I'm in too much pain most of the time.

I got shot in the chest one night by a random stranger {likely a gang initiation} after scrubbing out of surgery and stopping for gas on my way home one night, shattering my clavicle & leaving the bullet still painfully lodged only 1mm over my left aorta. It rendered me with CRPS, also colloquially referred to by us in the medical field as 'the suicide disease', the most painful disease known to mankind, which ranks as a 41 or 42 on the McGill pain scale, one step above having a limb amputated with no anaesthesia {"yes", I prefer the British spelling}. Except, unlike an unsedated surgical procedure, the pain for us afflicted with chronic regional pain syndrome {or, RSD, 'reflex sympathetic dystrophy'} •never• goes away, it only gets worse with time. Most patients end their own lives within the first 3 to 5 years after diagnosis, to stop the constant intense pain, but I just keep going after over 25 years of having this, though I'm not sure how.

Having used every type of known drug on this planet, I am very familiar with the pharmacokinetics of pretty much everything out there.

All that said, I just posted my answer to your' multiple inquiries, and hope that helps, my friend.

Personally, I take a mouthful of Orange Crush {for •both• the acetic acid to increase the potency •&• the carbonation which enhances and speeds up the mucosal membrane absorption} and then pour a powdered 30mg oxycodone into my mouth, swish it around for ten minutes and then swallow. The analgesic effects are {quite literally} staggering. It's the only thing that reduces my agonizing pain, and I do that 3 times a day, along with Klonopin, tizanidine {zanaflex}, cyclobenzaprine {flexeril}, clonidine and metapropolol to reduce my BP, which skyrockets to over 160/120 when my pains at it's worst.

I'll go more into how to best use potentiators to supplement your' CYP 450 cytochrome inhibitors here when I have the chance to.

I also run a chronic/intractable pain patient support page to keep me busy helping others, since I can't scrub anymore.

Best regards;

∞€lixir£lask

 

[LucidSDreamr]

Not a WoW player, I'm in too much pain most of the time.

I got shot in the chest one night by a random stranger {likely a gang initiation} after scrubbing out of surgery and stopping for gas on my way home one night, shattering my clavicle & leaving the bullet still painfully lodged only 1mm over my left aorta. It rendered me with CRPS, also colloquially referred to by us in the medical field as 'the suicide disease', the most painful disease known to mankind, which ranks as a 41 or 42 on the McGill pain scale, one step above having a limb amputated with no anaesthesia {"yes", I prefer the British spelling}. Except, unlike an unsedated surgical procedure, the pain for us afflicted with chronic regional pain syndrome {or, RSD, 'reflex sympathetic dystrophy'} •never• goes away, it only gets worse with time. Most patients end their own lives within the first 3 to 5 years after diagnosis, to stop the constant intense pain, but I just keep going after over 25 years of having this, though I'm not sure how.

Having used every type of known drug on this planet, I am very familiar with the pharmacokinetics of pretty much everything out there.

All that said, I just posted my answer to your' multiple inquiries, and hope that helps, my friend.

Personally, I take a mouthful of Orange Crush {for •both• the acetic acid to increase the potency •&• the carbonation which enhances and speeds up the mucosal membrane absorption} and then pour a powdered 30mg oxycodone into my mouth, swish it around for ten minutes and then swallow. The analgesic effects are {quite literally} staggering. It's the only thing that reduces my agonizing pain, and I do that 3 times a day, along with Klonopin, tizanidine {zanaflex}, cyclobenzaprine {flexeril}, clonidine and metapropolol to reduce my BP, which skyrockets to over 160/120 when my pains at it's worst.

I'll go more into how to best use potentiators to supplement your' CYP 450 cytochrome inhibitors here when I have the chance to.

I also run a chronic/intractable pain patient support page to keep me busy helping others, since I can't scrub anymore.

Best regards;

∞€lixir£lask

What is your chronic pain page? Hopefully not on reddit since I was permabanned from the entire platform for supporting abortion in a right wing sub.

 

[LucidSDreamr]

Pharmacokinetics has quite bit more variables than what goes up ass.

What metabolite of oxy and in what percentage is handled by first pass? Does that offset like % oral BA. Are the metabolites weaker (ie. Noroxy vs oxy).

Science has a lot of variables

It's a pretty complex science In my extensive experience oxy get you a stronger peak. Orally bs nasal. It is most fun

 

[LucidSDreamr]

It amazes me that the bioavailability of oxy is listed as being the same for oral as it is with rectal ROA's...

Anyone ever hear of a crazy little thing called FIRST PASS METABOLISM...? Opioids are highly susceptible to it, so any route besides oral, will ALWAYS be more effective for analgesia, guys.

C'mon...

∞€lixir£lask∞

Might bes listing effecting BA.

Pharmacokinetics has quite bit more variables than what goes up ass.

What metabolite of oxy and in what percentage is handled by first pass? Does that offset like % oral BA. Are the metabolites weaker (ie. Noroxy vs oxy).

Science has a lot of variables

It's a pretty complex science In my extensive experience oxy get you a stronger peak. Orally bs nasal. It is most fun iv till is get abbcess

 

[LucidSDreamr]

Like the title says I'm 85 years old and plan to start doing heroin. I can obtain that and much other stuff.
I'm not a previous user but don't really care. I just want to enjoy the feelings it gives. If I die from it that is fine.

This is not coming from a place of depression guys, it's we wanting to enjoy drugs. Not interested in cocaine type drugs. I used as few hydrocodone and enjoyed it. I want to go down that road. Opioids only.

I'm not going to do it by IV. Smoking it is possible and snorting it is possible. Maybe even intramuscular. Is fentadope stonger that heroin?

As a disclaimer for law enfircement: this is a fictional fantasy and none of this is real. Im making all this up and it's fake.

My man if this is a death wish of sorts i would not write-off iv. It is literally a different drug...especially with 8mg dialilided.

You your wider point there much life-changing and amazing drugs then heroin.

If the whole point is just to experiment. Psychedelics, ketamine...mdma. they outrank opioids in terms of exeprei
cne not necessarily comfort

 

[DeathIndustrial88]

For more context..

Buprenorphine is 50x stronger than morphine. But nowhere near as euphoric.

Potency doesn't always mean better. It just means you need less of the drug than you would a less potent opioid.

Another difference is receptors and receptor profile subtypes.

Heroin feels so good because it's receptor site ratio is a really good balance. It also hits the specific mu-sub types (I believe it's mu2 that causes euphoria).
Where as fentanyl may not bind to mu2 as much as heroin and might have a preference for mu1, which is more respiratory depression, but no added euphoria.

These are reasons why something that is more potent than heroin, can still be shitty and non-euphoric.


The only thing that feels as good as heroin or hydrocodone is heroin and hydrocodone.
Fentanyl is nothing compared to the semi-synthetics.

 

[Nas47]

Can only say-'I like this

For more context..

Buprenorphine is 50x stronger than morphine. But nowhere near as euphoric.

Potency doesn't always mean better. It just means you need less of the drug than you would a less potent opioid.

Another difference is receptors and receptor profile subtypes.

Heroin feels so good because it's receptor site ratio is a really good balance. It also hits the specific mu-sub types (I believe it's mu2 that causes euphoria).
Where as fentanyl may not bind to mu2 as much as heroin and might have a preference for mu1, which is more respiratory depression, but no added euphoria.

These are reasons why something that is more potent than heroin, can still be shitty and non-euphoric.


The only thing that feels as good as heroin or hydrocodone is heroin and hydrocodone.
Fentanyl is nothing compared to the semi-synthetics.

H is also strongly lipophilyc.That means,it penetrates blood-brain barrier more effectively....and yes potency have never to do with euphoric effects of a drug.

 

[Bl42]

What is your chronic pain page? Hopefully not on reddit since I was permabanned from the entire platform for supporting abortion in a right wing sub.

Not the topic. But why say you support abortion when almost nobody does one way or the other. I’m sure you don’t support abortion of a 8 month old baby. So why make a black and white statement.

 

[AbbeyLee]

OMG GET OFF MY FORUM MUM!!!

 

[LucidSDreamr]

Not the topic. But why say you support abortion when almost nobody does one way or the other. I’m sure you don’t support abortion of a 8 month old baby. So why make a black and white statement.

You must be new here.

We are all on drugs and say random things since we are on drugs.

I hope that clears everything up for you.

 

[LucidSDreamr]

OMG GET OFF MY FORUM MUM!!!

You better hide your bag.

 

[AbbeyLee]

You better hide your bag.

Mum loves her pregabalin. She also loves the smell of weed when I have it. Pregabalin has a similar effect on me as weed (and I've heard it's sold on the black market for that reason). I don't like either much, but I have to conclude mum is a stoner at heart. We have quite different brain chemistry.

 

[Nate74]

Can you overdose snorting or smoking or is it mainly an IV thing,,?

 

[Nate74]

Absolutely u can of by smoking and snorting..
I'm pretty sure u go down easier smoking fentynal.
I live in Victoria BC, at a place called the Johnson st community,which is an open use facility which is home to about 200 addicts ,with 95% addicted to down, or I should say fentynal.
The 5 years I've lived here there has been about. 40 od deaths and it's alwaya the smokers that go down.