Opioids Oral heroin - Is there any objective reason that this is a bad idea?

[Nicholai]

Really, no. I think if you're going to dabble with H, this is the least risky way. So many of us got into trouble messing with other ROAs, because it was cheaper, more recreational, etc. We can do better for harm reduction than some of these comments. Gather it up, guys.

 

[G_Chem]

Oral heroin is absolutely plausible, in fact, the very first form of heroin available from Bayer was usually prescribed in 5mg instant release tablets for oral usage. They were prescribed for the "usual" reasons, namely chronic cough, pain relief, morphine dependence, "female problems", etc. - and unsurprisingly people realized that exceeding the prescribed dosage made you feel great, taking large doses everyday, until the eventual onset of dependence and withdrawal. Pretty much an early version of the whole Oxy epidemic thing. History repeats itself.

As far as I can tell, oral heroin is much better absorbed by the oral route because it is rather more lipophilic and less polar due to the esterification of both the 3' and 6' position alcohol groups on morphine, thereby reducing the ability of the molecule to donate hydrogen bonds.

Apparently the actual BA of heroin taken orally depends on the size of the dose and also whether or not you're a chronic user. Larger doses, and taking the drug orally for longer, both increase bioavailibility according to this study. It does however state: The maximum plasma concentration of morphine was twofold higher after oral diacetylmorphine than after morphine administration. That means that very simply, you an take oral morphine doses, and divide by 2, to get an approximate oral heroin dose. So for a naive user, anywhere between 5 and 15mg should be good.

It's also worth mentioning that so much of the "heroin" available on the market is tainted with fentanyl, which is something like 40 times more potent than heroin is. A lethal dose for an opioid naive user is about 2 milligrams, meaning that doing 100mg (aka a "point") of heroin with 2% fentanyl would be lethal. You really need to have your stuff professionally tested, or at the very least, find or buy some fentanyl test strips. I could write an essay on why I think the whole fentanyl game is a crock of shit, but I've written enough for now.

So if lipophilicity is the key to making oral diacetylmorphine more bioavailable then would a substance like dibenzoylmorphine be even better orally?

I’m finding what I believe to be mono-benzoylmorphine to be very effective orally and trying to figure out why..

-GC

 

[dopamimetic]

I have experienced the difference between oral and intranasal morphine by myself and while I can't bring any reasonable explaination, the oral route felt like being at least x5 times as addictive and had some wird extra side effects that I would attribute to kappa agonsim - even when this shouldn't happen. Maybe it is about first pass metabolism leading to much higher levels of a certain metabolite when doing oral?

I struggled with withdrawal from oral morphine for months and found out by accident that the most distressing symptoms like diarrhea, feeling sick, depression, anxiety are barely present when switching to an equal snorted dose and build that down over just a few days. Low dose DXM is of great help too. It heavily potentiates morphine and mostly substitutes for it without inducing physical dependence by itself. If it only wasn't such a psychotic beast which severly limits its usability imho. The arylcyclohexylamine nmda antagonists are much much less psychotic, yet also less potent as opioid substitution or potentiators.

I know there are a few studies and papers around about this matter but unfortunately most only in animals as the limits for human experiments are high and nobody wants to mess with drug abuse.
So we have all the theory, animal results and anecdotal reports yet apparently nothing gets used in medicine, sadly.

But I am interested in what other people experienced, am I an exception or does it commonly go like that?

 

[emkee_reinvented]

So I think "Only 6 more days until ... (add drug of choice) " is an improvement :D

Yep I know that feeling.

 

[muie]

Besides the economical aspect, there is absolutely nothing wrong with oral heroin - its in the same boat as oral hydromorphone! If you had a 32mg hydrocontin, would you crush and eat it or crush and snort/inject it? I've always wondered what the oral heroin high is like as morphine is my favorite of all opioids! I find heroin to be a slightly more stimulating version of morphine (which is the most sedating by far).

Dopamimetic wrote that "the oral route felt like being at least x5 times as addictive"
Care to explain how? With oral there's no rush nor fiending nor anything like that...

p.s. Plugged morphine was the most intense opiate experience of my life. Purple/green in the face throwing up massivley, going in and out of consciousness while standing up/erect (not nodding - I couldn't nod as it was hitting me much too powerfully. Meanwhile extreme body high, rushing, pulsating in my purple head resulting in another vomit.

 

[Ganjcat]

Just smoke it on foil wtf or melt it on foil until it turns black, remove it and out it in a cigarette works well as long as I melt it into shatter otherwise it does nothing except smell

 

[Ganjcat]

This sounds like a great way to waste a lot of money and also become addicted to heroin. Either don't use heroin or accept that you're going to become addicted with even semi regular use. There's no point wasting money taking it in an inefficient way, you'll waste some but what does get into you will get you high and addicted just the same.

Theirs nothing more addictive than h imo I have temporarily quit a few times but now I can limit my use as much as the desire to redose doesn't matter because I have felt wds and know what they are like it you can limit your use and gets some on loan incase you fuck up also you should have an emergency stash just don't hide it in some next place you won't remember like me

 

[MJ420]

You're lying to yourself if you think you can have a non addictive relationship with heroin by swallowing it . Still gets in your bloodstream and less of a high. So addiction for shitty buzz

 

[Gaffy]

Depends on what "parts" of the body need medicating. Your bowels are just as "sensitive" to the drug as your brain, they just result in different pharmacodynamics. Heroin oral was also prescribed to aleviate diarrhea and shitty stools, resulting in better food absorption etc..

 

[G_Chem]

From my past experience heroin oral isn’t all that great, not compared to the mono benzoyl ester which seems like Oxycodone in its oral BA.

One time me and my guy go and pick up for us and one other guy who didn’t ride along. Soon as we got our bags we were so distracted on getting high we forgot we set this dudes bundle on the center console.

We pull up to dudes house and freak out tearing the car apart trying to find it, when allthe sudden as we were it’s like we both simultaneously realized we had left it on the center console. In slow motion we both leaned in from each side of the car and looked into an empty fast food water cup with its top off.

Sure enough the heroin bundle had fallen right into the water...

Long story short we looked like a bunch of fiends that just robbed this dude when we really are complete morons in all actuality lol. We made it good, I gave guy part of mine and my buddy got more later.

I decided since I gave up my bag I’d drink the heroin down. Fairly big bag. Not too strong of effects sadly, I’m sure I had a tolerance but still it was very very weak.

-GC

 

[GetMeOutOfThisCRAP]

Heroin is the worst opiate to be addicted too. People have done seed tea, methadone, etc. but none of those have destroyed as many lives as heroin.

I know I sound like a DARE poster but I've seen it first-hand when my pill junkie friend switched to heroin and absolutely ruined his entire life. Before you wouldn't have known he was on any drug, and went to raving dope crack monster lol within less than a month. He was snorting it which doesn't have the highest BA as other routes too.

If you dabble in heroin, you're going to lose something. That's all I'm saying. It's easy to just see people on a forum telling you that heroin is a bad idea, but those are just words. To actually go through your life crippled from heroin abuse is another story. Imo the main difference is the effects. People can mask when they're on oxycodone because they're energized and in a good mood, but on heroin you're down down downnnn. Also if you swallow some fentalogue it could be game over right then and there.

Is oxy/seed tea really not good enough? I understand if you insist on trying it/end up making it a habit in time but you can't say you haven't been warned You're risking being hooked on Suboxone/subutex for your entire life.

 

[dopamimetic]

Why is oxycodone so different, I keep reading that it's energizing and antidepressant while most(?) opiates/opioids are more sedating and sometimes pro-depressive, at least the docs of the local maintenance clinic told me so and methadone for sure made me lethargic in a bad way, morphine a tad less and it's less sedating but still I would never use a words like energizing for them. Granted, morphine can actually be, but only in you have little to no tolerance and take the right, big but not too big dose, then chances are that you'll stay up all night for once but the same dose on day 2 or 3 will be sedating.

Also, how much different is heroin from (pure, not time-released and not via oral) morphine in relation of addiction? Yeah it's a bitch to get it off, but more so because I actually like/want/need some sort of "protection" for/against my emotions.. so I always began using again sooner or later. With the aid of things like DXM, Loperamid, Clonidine etc. it's not soo hard to go through acute withdrawal.

But yea, probably what I really want to ask (besides that the question above is something I had in mind for quite some time), is it really such a difference from morphine to oxycodone? Why then isn't that one used in maintenance? Just know they did codeine, then switched to methadone/l-polamidon (because, as they say, codeine was more addictive. Have a hard time to believe that. More that the ceiling effect will have been a problem for the heavier users?) and recently added time-released morphine. Bupe of course as the partial agonist/antagonist it is. There was this weird Levoacetylmethadol being used in the past in Germany, but none of the "happier" ones like oxycodone, tilidine (?).

If it is, then I want to switch to oxy. Doesn't make sense to combat side effects of morphine with (lisdex)amphetamine and similar when there is a substance with more favorable profile of effects.

But, and somehow I hate it to say that, me too under-estimated the potency of opioids to induce dependency. They, maybe together with benzodiazepines(?), are certainly the worst psychotropics in relation to what you get and what you have to pay for, in longer term especially and for people who are not in otherwise unbearable physical pain (and for them, they should put more effort in researching the dissos as they can make excellent pain killers too).

 

[JTemperance]

Why is oxycodone so different, I keep reading that it's energizing and antidepressant while most(?) opiates/opioids are more sedating and sometimes pro-depressive, at least the docs of the local maintenance clinic told me so and methadone for sure made me lethargic in a bad way, morphine a tad less and it's less sedating but still I would never use a words like energizing for them. Granted, morphine can actually be, but only in you have little to no tolerance and take the right, big but not too big dose, then chances are that you'll stay up all night for once but the same dose on day 2 or 3 will be sedating.

Also, how much different is heroin from (pure, not time-released and not via oral) morphine in relation of addiction?

Morphine is certainly responsible for the bulk of heroin's effects in the brain, for better or worse, so they have an intrinsic similarity. I would guess injected morphine is quite close to injected heroin in terms of addiction, if you account for the potency difference (about 2.5x IIRC). Where it's used medically, heroin (aka diamorphine) is preferred over morphine because it tends to produce somewhat less nausea, and it has a slightly quicker onset and shorter duration of action.

In terms of addiction use, the major difference I see is that heroin is a bit easier to sustain a large habit with logistically speaking, since it is more water-soluble (so a 1ml insulin needle can hold as much as anybody wants, unlike morphine) and since it triggers less of a histamine release than morphine (which can cause a painful pins-and-needles sensation when using large amounts). Orally, they are exactly the same but with heroin having the worse bioavailability and being weaker.

Historically, it took quite a while for heroin to displace morphine on the black market. The initial reason heroin became popular among street users, around 1910-13 in the US to begin with, was because it can be snorted quite effectively, mirroring the use of cocaine which had already become a popular street drug used intranasally about ten years earlier. Morphine has less bioavailability than heroin intranasally (... I think) and it was already strongly associated with injection use by the time heroin came on the market.

Legal factors played a role as well, since opium smoking had been essentially banned on a federal level in 1909, prompting some opium smokers (many of whom were used to snorting drugs in the form of cocaine) to switch to a cheaper opiate. At the same time, many states had started to pass laws restricting the sale/use of morphine before the Harrison Act did so federally, but heroin was relatively unknown and was often less regulated at the time.

Outside the US and China, heroin took even longer to displace morphine as the dominant opiate of the black market. Even in the US, throughout the 20s and into the 30s, morphine remained the dominant street opiate outside of greater New York City, where heroin was most popular. In the early 1930s, League of Nations controls started to more effectively curtail the excessive exporting of narcotics from European pharmaceutical firms and illicit factories in the Balkans were closed, the quality of black market drugs started to go down, and heroin became more valued for its 2-3x superior potency over morphine for smuggling purposes, gaining ground over morphine. When Japan invaded China in 1937, the last major conduit of narcotics was thrown into chaos, and a major "panic" began that didn't really resolve until after 1945, and even then the purity of black market heroin didn't reach 1930s levels for quite a long time.

The other major historical factor is the shift to intravenous injection, which also took place on a large scale around the early 1930s, for some of the same reasons. It is somewhat surprising, but morphine and heroin injectors in the early 20th century all pretty much just injected subcutaneously. Intravenous injection by street users was first documented in 1924, but only really took off in the 1930-34 period, while purity was declining.

The difference between heroin and morphine is more noticeable when they are injected intravenously than subcutaneously, with heroin probably having somewhat more euphoria and "rush" than morphine due to higher lipophilicity, and the histamine release of morphine being stronger IV than SC/IM and thus more of an impediment. So once the vast majority of user had completed the transition from SC to IV injecting (certainly by 1940), heroin would have an additional reason to be preferred over morphine due to ROA, and would appear to be more addictive compared to the morphine that continued to be used by much smaller numbers.

 

[JTemperance]

But yea, probably what I really want to ask (besides that the question above is something I had in mind for quite some time), is it really such a difference from morphine to oxycodone? Why then isn't that one used in maintenance? Just know they did codeine, then switched to methadone/l-polamidon (because, as they say, codeine was more addictive. Have a hard time to believe that. More that the ceiling effect will have been a problem for the heavier users?) and recently added time-released morphine. Bupe of course as the partial agonist/antagonist it is. There was this weird Levoacetylmethadol being used in the past in Germany, but none of the "happier" ones like oxycodone, tilidine (?).

As for your second question, the history of maintenance drugs shows a lot more having to do with the political significance of the drugs rather than their particular pharmacological properties, and it's a long story.

Methadone (as Dolophine) had started to be used for off-label and semi-clandestine maintenance by some brave US doctors in the early-mid 60s, mostly for its long duration and good oral bioavailability as compared with morphine or other opiates (at a time when controlled-release technology was relatively new and still not really abuse-deterrent).

Morphine maintenance clinics had been introduced in quite a few US cities in 1919-24, the biggest one existing in NYC for about a year in 1919-20 and the last one to close remaining in Shreveport, Louisiana. Somewhat disorganized implementation, but especially later demonization by the FBI/Treasury Dept., meant that they were held in disrepute as a failed experiment with extensive diversion and scamming, and petty crime from addicts congregating near the clinic.

The short duration of morphine (which was given as an injection on-site or at home) meant that they couldn't feasibly have once-daily dosing at the clinic. The different attributes of methadone, and the fact that it was a relatively novel drug without as much stigma, opened up a space for the doctors of the 60s to differentiate it from the seemingly discredited use of morphine for maintenance.

Some of the 1960s doctors hoped that, if arrested, they could have a test case to challenge the constitutionality of the Treasury Department's anti-maintenance interpretation of the Harrison Act in the more favorable political climate of the Warren Court, which had ruled laws against addiction-per-se and habitual drunkenness unconstitutional. Had this happened and succeeded, it could have opened up legal maintenance with morphine and other drugs as well, but federal law enforcement was also afraid of losing so they held off on prosecution for the most part.

The Dole/Nyswander studies of 1964-66 really brought major attention to methadone maintenance as a succesful addiction treatment, introducing the idea of the "blockade" that it produces, which again differentiated it from older opiates. More doctors began prescribing methadone to heroin addicts in the late 60s, and cities with big heroin problems began to run municipal clinics, especially in NYC.

However, this was still taking place in a legal grey area until the Harrison Act was repealed by Congress under the Nixon Administration and replaced with the Controlled Substances Act, with provision made to permit methadone maintenance, but regulated it federally and more strictly, restricting methadone prescribing to clinics rather than private doctors, and it remains the law. By contrast, the DATA 2000 act that permitted buprenorphine maintenance made no such requirement, just retained buprenorphine as a Schedule III drug under the CSA, which is why Suboxone and Subutex can not only be prescribed for maintenance by private doctors but with up to 5 refills, while methadone is limited to clinics and take-homes are restricted.

Nixon famously declared the "War on Drugs" and was no fan of maintenance in principal, but he made the canny political decision that if it actually did reduce heroin-related crime it would be to his benefit, which ironically placed the US ahead of some more progressive European countries in allowing formal maintenance (Britain being the big exception).

Codeine (and/or dihydrocodeine) were in fact used for off-label and semi-clandestine maintenance by (West) German doctors in the 1980s after their "heroin epidemic" took hold, before methadone maintenance was introduced nationwide in (united) Germany in the early 1990s, and DHC remains at least an option in some Central European countries.

In France, methadone treatment was extremely restricted and reached only a very small number of people during the early 1990s, but around 1995 buprenorphine was approved for maintenance treatment on a much wider basis; even though methadone treatment was later expanded, that historical progression explains the higher level of popularity that Subutex has in France versus other European countries.

 

[G_Chem]

For me and quite a few people I knew, heroin could be energizing and certainly not depressing. Morphine never quite did it for me, I’ve tried it many forms and many ROA’s except the one that probably counts... IV.

Also good info Temperance except your wrong on some of the bioavailability info. Heroin indeed is a bit better bioavailability than morphine orally.

Oral diacetylmorphine (heroin) yields greater morphine bioavailability than oral morphine: bioavailability related to dosage and prior opioid exposure - PubMed

Oral absorption of opioids is substance-, dose- and patient collective-dependent, suggesting that there may be a saturation of first-pass processes, the exact mechanism of which is not yet understood.

www.ncbi.nlm.nih.gov

Not great mind you but better.

Idk morphine just isn’t nearly as euphoric, very sedating, needs larger doses, I was never a huge fan.

Oxycodone was a great ride until I tried heroin cuz while I did enjoy Oxy, it completely killed my tolerance and when a 80mg OC doesn’t even touch you anymore it’s unfortunately time to hang up the towel. After this thread wish I had a few laying around for old times sake, it’s been soo long.


A little bit more.. Growing up in the area I did, it seemed the doctors musta just been handing Oxy out like candy cuz most kids had tried it at an early age 13-15 sometimes before their first use of cannabis or alcohol.

My first use of Oxywas really bad so I stayed off til senior year of HS I finally tried it again one day outta boredom and found it wasn’t so bad after all lol.

When I finally got into using heavily daily I had a guy who I’d bring a small amount of cash and he’d literally just give me an undetermined handful. The OC 20’s that I loved so so much.

80’s were ok but I absolutely loved the 20’s. A quarter of an 80 would get me nowhere near how I felt off a full 20mg.

OC was more social for sure looking back. I had a lot more fun and good times on it than heroin that has a more serious vibe to it.

I’ll never forget those first few times with heroin I had this feeling like I was essentially selling my soul. I knew the consequences but at the time I didn’t care enough about my life to give a shit.

One experience in particular was very eye opening. I’m 18yr old sitting in this nasty heroin den of some dudes apartment. I had just been kicked out of my house again and I remember thinking very clearly, “if I do this line, I will get addicted.”

I spent the next 48 hours in a very heavy heroin nod. The heaviest I’ve ever had before or since. I literally laid on a couch and was drifted off into the most pleasant place. Every 3-5 hours I’d get up and my buddy would feed me another line.

I walked out of that apartment knowing I was addicted. From then on I needed opiates, to this very day in fact.

Yea I would never suggest anybody try the shit. I’m also one to believe there is energy associated with how drugs are produced and distributed, heroin just feels like it steals your soul in exchange for what you think is eternal peace.


Regarding the pro depressive nature of opiates. Having recently just having a full month of full mu agonist use...

In the beginning of using them again after nearly 10yrs of nothing but Suboxone, I did indeed notice increased depression. But once I “got into it” again they became enjoyable.

I’ve realized full agonist opiates aren’t enjoyable to me unless I’m full on addicted. Like the beginning stages where you can use here and there with little consequence, the stage is no fun and little euphoria to me. Nothing better than being in nasty withdrawals, and you get that taste of opiate in your system. It’s like Christmas, Heaven, sex, and well anything good in the world all wrapped up into one moment. The sigh of relief is satisfying yet a little sickening.

-GC

 

[cosmic charlie]

Towards the end of my IV Heroin use when my veins became an issue I'd started experimenting with Oral and Rectal use of #4 Heroin. I'd been living in NJ at the time it was '12-'13 and back when it was actually Dope at least from my connect. I deal with some issues with my sinuses and get infections very easily so I tend to try and avoid sniffing things. Well plugging the Dope worked and it worked well even has a rush to it for me unlike sniffing. But not the ideal ROA if you are at work out with family etc...

So I'd dumped out bags a few times onto a plate the most I ever used at once was a whole bundle and it was a sizable amount of powder. And back as I was coming up Jersey was infamous for having highly pure Heroin. At this point it wasn't as good as in the early 2000's but it was way better then these Fentalouge mixtures. Well anyways I'd stuffed all the Dope into 000 gelcaps can't remember if it was a one or two but whatever it was I took the whole bundle at once orally.

Within 30mins or so I was coming out of Withdrawal and my pupils began to constrict. Possibly some slight warmth but not high at all really. Kept me from being sick for the rest of the day tho. But in the future never tried it again because as I said if I was to have plugged a few bags of that Dope I would have gotten high as a Kite. What I'm getting at is if you have a habit or a strong natural tolerance you may not get much out of this. If it's your first time experimenting with Heroin I'm sure you would though. But it would become a very expensive ROA as tolerance develops.

Sometimes I really miss the old days when the streets were flooded with clean Dope...but then I think about the aftermath of what it did to my life and I'm thankful for where I'm at now. Messing with Heroin is like playing with fire and whennid started I told myself I'd just sniff a bag on paydays, then that turned to only on Weekends. Before I knew it I was using around the clock and jabbing needles in my arm everyday. Is it a great high? The best, it's just a hard lifestyle on you and the ones that care about you. Regardless of what ROA you start with, eventually things will escalate. Either that or you have an iron will not seen in many that played around with this substance before you.

 

[dopamimetic]

Thanks for these detailed reports and insights but still no real answer why opioids can be and are so different, energetic vs. sedating etc.. and as you are talking about being socially active, I guess it's not just an initial difference that could be explained by differencies in onset, potency and stuff alike but a differing effect for hours on.. probably thankfully for me it's more technical, maybe due to my extended previous and parallel use of dissociatives, I continue to say that dissociatives are giving me more than opioids ever did, yet do I struggle with the opioids as you all do to get off them, and their side effects.


I remember some experiences when morphine was a stimulating cuddly blanket, but these were rare and even initially I thought of methadone being better suited for me, maybe due to its additional effects unrelated to opioid receptors, but it was too heavy and too sedating which I now think about morphine too, when I read about you writing of oxycodone and heroin. Is it a definitive difference, or something that only happens initially and fades away with tolerance?