diPropionyl 'tar' heroin, acetylcodeine toxicity and a few Qs

[Limpet_Chicken]

Well then. Been doing a bit of reading, and getting some 'black tar' heroin, which in this particular case, is NOT the standard BTH (black tar heroin), that goes around the US, but rather, an alkaloidal extract of opium which has been acylated with propionyl chloride, rather than acetylated as usually happens. Not a commercial product, but one of those things one occasionally, if lucky, runs into when somebody gets enterprising

Lets not go into synthesis discussion at all, that isn't nescessary information anyway to me, I already understand the chem that will have gone into it, it isn't exactly advanced or complex to begin with.

What I want to know is, acetylcodeine is known to be dangerous when IV'ed. I certain't will NOT be using this intravenously, plugged or possibly nasally, although given my oxycodone tolerance (need 2 OC80s a day, min. thanks to my screwed up joints and bursitis).

HOW is this toxicity exerted? I have read two different theories-one, that it may be a convulsant, somebody here in a thread found via TFSE stated that acetylcodeine is 2-3x as potent of a convulsant when used intravenously as diacetylmorphine..that seems an acceptable risk for non-parenteral use, if treated with care.

The other theory, seems to revolve around potential for massive histamine release, which is also known to be the mode by which regular, un-acylated codeine is toxic, resulting in pulmonary oedema when taken intravenously. Which, as stated, will not be happening..ick..gross. I can't even imagine shooting black tar itself, although to the best of my knowledge, BTH is a US/mexican thing really and doesn't exist in the UK.

Lets not go into how to make such a product, such information is available if anybody wishes to put the effort into seeking it out, and I do not need to do so, nor do I want this thread shut down because someone else starts posting synth info.

Is it known if propionylcodeine shares in the toxicity of acetylcodeine? I am going to assume that it does indeed do so unless presented with reliable information to the contrary. In this product I'll be trying out, some propionylcodeine will undoubtedly be present, but given the ratio of codeine:morphine in most opium I would imagine that there probably isn't going to be a great deal, and that given the great potency of dipropionylmorphine, an active dose of the latter should be able to be dosed enterally without too much risk? of course, antihistamines would be preloaded anyway, as I do with most opioids regardless, to prevent excessive histaminergic effects.

Can anybody provide solid tox. data on propionylcodeine? also solubility data in various solvents would be most appreciated, I'd like to wash out this impurity.

 

[adams49]

Limpet_Chicken,
I did not know acetylated codine was around. AS u probably know morophine is methylated to make codine. dimorophine is what u call heroin in UK. They won't let us use it here in he US. I dont know why!!%$#&. AS to your question, you might try DMSO to get impurities out. Antihistamine loading is a good idea I nevre gave much thought. I work in a med lab and I looked at my blood cells on and off opiates. Usually I will see 0-1 eosinophils not on but on I see dosens. These r produced for histamine response. Supposed 2 stop itching but the body will not produce enough to stop itching because to many eos could b life threatning. Thanks 4 the info & I hope DMSO works 4 u. I will do a little research and see if I can find somthing if the DMSO doesn't work.

adams49

 

[Limpet_Chicken]

DMSO (along with HMPA) was just about the one solvent I wished to avoid. Its a damn pain to pull off as its so high boiling.

This needs doing relatively quickly really, otherwise I'm headed up shit creek, sans paddle. Although the product will be biassayed as is, carefully. I imagine this shouldn't pose a problem, given the potency of dipropionylmorphine, and the fact that this is not 'cut' with anything whatsoever.
Whilst this product could contain propionylcodeine, only enteral use will be attempted, I just want to clean it up to remove this, so that its suitable for shooting.


Acetylated codeine ISN'T 'around', in the sense of on the street, sold as that, or used medically. Its a poison, not something used as a drug of abuse. If its present, it is as a byproduct of heroin manufacture, remaining in the H, or as a byproduct of acetylation of opium (which is where this dipropionylmorphine gear is coming from, only it was acylated with the appropriate process to introduce the propionyl rather than acetyl moieties. More of an acylated papaveretum/pantopon than isolated morphine alone (that is, containing opium isolates as a full-spectrum extract)

In the form available to me, it will come as a somewhat cleaned up version of black tar most likely. But I wouldn't even shoot actual black tar H, not that its actually available in my country in the first place, at least, I don't think so. I shudder to think what that crap does to people's veins.



Interesting, about your observation of the blood. Do you recommend a thin film, or thick, whilst preparing slides?
Just because I feel like taking a look myself sometime, I have an excellent quality microscope in the lab, although there aren't really very many times at all that I am not on opioids.

 

[sekio]

the amount of acetylcodeine in tar heroin is not enough to be concerned about, the major worry is injecting it pure.

it is doubtful you will be able to wash acyl esters of codeine away from esters of morphine. any solvent that dissolves the one will dissolve the other. maybe with column chromatography.

given that people inject tar heroin made directly from acetylation of morphine without too many acute ill effects I don't see why proprionyl-heroin would be different,

 

[Limpet_Chicken]

Well if its being made directly from morphine (as opposed to papaveretum), then no acetylcodeine would be present (or, propionylcodeine)

It seems my concerns about IV use of this might be unfounded, reading turned up the interesting titbit of info, that the morphine syrettes that are issued to US troops are apparently, according at least, to wikipedia (I know, I know, but I'd think such info reliable due to the ease of obtaining and verifying this), actually a poppy isolate, not pure morphine.

At any rate, IV will only be attempted by very slow push, with preloaded antihistamines. As far as possible convulsant properties go, I already take chlormethiazole, which should provide a measure of protection from such occurences, should it all go pear-shaped.

As far as dipropionylmorphine itself goes, its known to be somewhat more potent, but a little slower acting than heroin. Anyone actually tried the stuff? I did use TFSE, but I couldn't find anything at all. How much more potent is it, mg for mg (as compared to both H and to unacylated morphine? the only reports I could find were from another forum, where someone stated they had prepared some, and 'a matchhead' knocked him flat on his arse, with a fair bit of tolerance. Sounds pretty good to me

 

[sekio]

actually a poppy isolate, not pure morphine.

it's essentially pure morphine isolated from poppies, not pantopon. seperation of morphine from codeine and thebaine by way of its ability to form a phenolic salt is one step of the process.

a couple studies suggest that DPM is likely slightly more potent and moderately longer lasting. so it's probably around 3mg DPM per 10mg morphine IV equivalent.

its probably some margin more potent then heroin when ingested orally because the propanoate esters are a little harder to hydrolise than acetyl groups

https://www.ncbi.nlm.nih.gov/pubmed/402470?dopt=Abstract

 

[Limpet_Chicken]

http://en.wikipedia.org/wiki/Omnopon Is this wrong, or outdated, then?

3mg/10mg morphine (IV), I thought diamorphine was around this potency itself?

At any rate, I should soon find out :D I'm interested to know if the increased lipophilicity of dipropionylmorphine leads to a greater rush when IV'ed (now wouldn't that be something..IV morphine has always been the opioid that has given me the most rush when shot, I've used H, but never had it IV. I'm on oxy for pain, but it really doesn't have much in the way of a rush IMO)..or does the slower onset compared to diacetylmorphine offset this I wonder..

 

[sekio]

Is this wrong, or outdated, then?

the wikipedia article is the only mention i've seen of morphine syrettes actually being pantopon, and doesn't provide a source. regardless, the impact of adding a few parts papaverine and codeine is probably of no concern.

assuming heroin is 2.2.x morphine, 10mg morph = 4.5 diamorphine.

I'm interested to know if the increased lipophilicity of dipropionylmorphine leads to a greater rush when IV'ed

if anything it would be *less* of a rush - generally more lipophilicity means the movement of the drug is slowed by fat more.

 

[Limpet_Chicken]

Hm. I was under the impression that the speed of onset, and rush provided by heroin was in part at least, due to the acyl moieties making the drug more lipophilic, and able to pass the BBB faster, thus getting into the CNS quicker. Is this not the case?

At any rate, I shouldn't imagine this will prove to be THAT much slower acting, that is, not to the extent that I'll have too many complaints.

 

[sekio]

Hm. I was under the impression that the speed of onset, and rush provided by heroin was in part at least, due to the acyl moieties making the drug more lipophilic, and able to pass the BBB faster, thus getting into the CNS quicker. Is this not the case?

Far as I can tell - no. Curiously, it's the opposite, with less fat soluble drugs tending to have a more rapid onset (faster "rush"). The fat solubility of opioids only really matters in determining pharmacokinetics - structural interactions with the receptor in general are larger factors in determining potency.

 

[Limpet_Chicken]

That makes sense, about potency. Obviously its largely going to be dependent upon agonist strength, receptor conformation, selectivity for Mu-OR subtypes and splice variants (which seem to play a very, very significant part in the biochemistry of the morphine-like phenanthrenes especially, such as the difference between H/6-MAM, M6G and morphine for instance, and also in the development, or not, of tolerance and addiction)

But I find it puzzling that more hydrophilic opioids seem to pass the BBB quicker. Why is this?

 

[sekio]

I'm guessing because by and large, transport through the body and brain is through aqueous blood and CSF - the compounds only need to have enough fat solubility (and be small enough) to make it through the cell walls of the BBB.

 

[Limpet_Chicken]

Just to report back-a small amount of the methanolic pod mush soup, which had been soaking a fairly long time (few days) was worked up (I shall say no more), and a 3/6-monoacetyl derivative prepared (with most likely some H present), this was prepped for IV in the form of a black tar-like product, and of course, promptly IV'ed.

Needless to say, nice rush, nice high, etc. etc., all the things one expects from shooting up skag. No surprise there.

But it DID cause an instant prickling sensation and subjectively felt rise in temperature. Some strange 'catching' of the breath, as if I had to work harder to pull in a breath of air. This only lasted a minute or so, and at no point was I in any danger. I had consumed 2x4mg chlorphenamine tablets, and 2x120mg fexofenadine tablets as a preload. All the same when that effect manifested itself, which it did so very rapidly upon the injection being complete, I did grab an inhaler from..err...well I grabbed one anyway. Did not use it though, I'd have to have been in BIG trouble before I used anything like an adrenergic agonist, anything adrenergic other than clonidine and other similar drugs make me feel like total shite.

Will proceed, but with great caution. Still, that faded fast, and I'm feeling pretty damn good

 

[Tryptamite]

Not to get into synthesis discussion but did you extract the alkaloids from the poppy material or did you acetylate a kind of "refined opium", I.e. was there vegetable matter/plant material in the substance being acetylated?

 

[Limpet_Chicken]

Without synth discussion, vegetable matter was removed w/anhydrous acetone wash. Or at least some. Further nonpolar washes would be advised, but in any case, I hadn't the time to do so, solvents yes, time to evaporate them, no. Was already getting shaky and not feeling good.

Doubtless you know how it is, if you use. Its an itch that needs scratching NOW, not when one's naptha has all evaporated off :/

It was acylated with the plant garbage still in there, and then washed, so technically yes, practically, no.
And whilst some was acetylated, more of it was propionylated, in this particular case, due to both the known greater potency, and a dipropionylmorphine-omnopon based skag being the desired product.

Only had a small quantity of tar to work with, as withdrawal was starting to bite, so some of the solvent was evaporated, enough to provide enough to keep me well until I could safely brew up some pod tea out of sight of the folks after they went to bed

Lovely rush, nice high, although a heck of a histamine release. Still, all in all, it gets the thumbs up.

DO make sure you get rid of the plant muck if you attempt to do this though people, it can cause anaphylaxis if this is not done. And filter, filter, filter. As tar, its a fucking fucker to handle, literally, as it comes out from a methanolic extraction of pods (IPA apparently is better, but didn't have enough left) it is gooey, sticky, tarry intractable resinous stuff. Sticks to anything it touches, and it stains fingers, clothes, anything it touches it stains like crazy.