Opioids Plugging cyclizine?

[Survival0200]

Would there be any point in administering cyclizine rectally with an oral opiate? Just wondering if the onset would be faster and bioavailability greater?

 

[Fertile]

From it's invention, rectal administration of cyclizine was studied. I have to point out that cyclizine is a dubious drug with many cases of bad outcomes. I know it's used that way because people on methadone will plug cyclizine tablets. I do not quite know what the interaction is, I just know that the UK saw a truly massive cyclizime epidemic which resulted in papers with titles like 'Cyclizine - the limitations of Harm Reduction'. I think it's because people would try to estimate the hit of Diconal by mixing Physeptone tablets and Valoid tablets.

I even discovered that it was travelling salesmen who 'smurfed' the pharmacies. They could buy 100 Valoid tablets for £25 and sell them for £50. If you can do that 5 days a week, it's quite a useful extra income. Dealers would then sell them for £1 per tablet. I've watched someone on methadone shoot a tablet every 10 minutes for hours and hours... until they collapsed and I called in emergency services (having hidden everything in a public space).

It's a bad scene.

 

[DrPetro]

@Survival0200 ,I'm just awaiting an online cyclizine order. I use plugging as my second route next to IV for most drugs excluding cannabis and I am on a significant Methadone prescription which I'm interested in boosting. As a former harm reduction drug worker/advocate I'm well aware of the risks I'm taking and would prefer to avoid the messy business of trying to prep cyclizine tablets for a hit. I am interested in how you got on?
I'd also like to know from anyone with a better understanding of chemistry whether heating a cyclizine hydrochloride soup with citric acid might convert some of the hydrochloride to the water soluble citrate
Hope to hear from you,
Keep ASAP (as safe as practical)
Dr Petro

 

[Fertile]

Well, DDN had a cover (in the 1980s) whichsimply stated 'Cyclizine - a Limit to Harm Reduction' in which they were not even able to isolate WHY people get hooked on doing a pill every 10 minutes. But when they do, they tend to die. So it causes intense compulsion and if you already struggle with drug compulsion, this is dangerous.

It's use died out because all of the users died.

 

[DrPetro]

@Fertile . Interesting, I've written an occasional article for DDN so I shall dig this one out. I have a rather dangerous compulsion to try most Opiod /cns depressant combination out there and I must admit that my decision to order cyclizine was partially driven by xanax induced recklessness.
I'm very happy to report back on my experience and readers can assume death if bluelighters get no update.
Phenazepam and GBL have both had an unfortunate impact on my life for a while and the closest I've come to waking up surrounded by paramedics/not waking up. at all was when I came across a xanax solution in PG that was injectable but no doubt I've also skated close to the edge with gbl/IV heroin/benzo combinations. So far I've never had emergency services in a 22year habit and I do have more positive impulses too which have seen me re start some cardio exercise and strength training with a pal at the gym. Im much more ambivalent than I might appear and would freely admit to a Christmas rough patch. Time will tell if 2023 ends up being the positive year I envisage and I quite understand your warnings. I just have a push the envelope side to my character when left to my own devices.
Yours, Dr Petro

 

[ChemicallyEnhanced]

Any answers for sure on this? I actually deliberately got myself prescribed Cyclizine a few years ago after reading Trainspotting lol. I definitely think it makes a difference, but I have never considered plugging it over taking it orally?

 

[ChemicallyEnhanced]

Well, DDN had a cover (in the 1980s) whichsimply stated 'Cyclizine - a Limit to Harm Reduction' in which they were not even able to isolate WHY people get hooked on doing a pill every 10 minutes. But when they do, they tend to die. So it causes intense compulsion and if you already struggle with drug compulsion, this is dangerous.

It's use died out because all of the users died.

People would abuse Cyclizine *alone*?? I take it by itself sometimes (I get severe nausea from pancreatitis) but haven't noticed any benefits other than when it potentiates opiates.
Wouldn't taking it "every 10 minutes" like that just give you horrific anticholinergic syndrome?

 

[DrPetro]

People would abuse Cyclizine *alone*?? I take it by itself sometimes (I get severe nausea from pancreatitis) but haven't noticed any benefits other than when it potentiates opiates.
Wouldn't taking it "every 10 minutes" like that just give you horrific anticholinergic syndrome?

I will happily let folk on here know my own results. Im from the UK and have decades of opiod/opiate habit and I'm also well informed about previous patterns of cyclize/methadone or diconal addiction. Leeds Addiction Unit have a couple of folk on Diconal scripts (not that I know the recipients-I heard this from the prescribing consultant psych.

 

[DrPetro]

Well, DDN had a cover (in the 1980s) whichsimply stated 'Cyclizine - a Limit to Harm Reduction' in which they were not even able to isolate WHY people get hooked on doing a pill every 10 minutes. But when they do, they tend to die. So it causes intense compulsion and if you already struggle with drug compulsion, this is dangerous.

It's use died out because all of the users died.

I've found the Druglink article. https://www.drugwise.org.uk/wp-content/uploads/Limits-of-intervention.pdf

 

[ageingpartyfiend]

People would abuse Cyclizine *alone*?? I take it by itself sometimes (I get severe nausea from pancreatitis) but haven't noticed any benefits other than when it potentiates opiates.
Wouldn't taking it "every 10 minutes" like that just give you horrific anticholinergic syndrome?

I'm afraid they would unfortunately

In the 80's some idiots abused them by taking huge doses which result in 24-36 hour derealisation / full aural and visual hallucinogenic state (seeing / interracting with people who were not there etc) First hand reports were of absoluutely zero pleasant effects and just total fully-awake nightmare for the whole (very long) duration

I personally know someone who fought with customers in a shop cos he thought they were terrorists (badly injuring someone in the process) and then wildly fought the cops on arrest. Jailed for 3 years. Another guy (first guy's mate) seriously injured after jumping from a 2nd floor window attempting to escape from agang with machetes in his kitchen (who were not actually real). I also knew someone who died after jumping off a building for no discernable reason while on them...sounds like an anti-drugs propaganda advert but unfortunately 100% true, trust.

ffs keep any use to a bare minimum

 

[Fertile]

Cyclidine increases the effect of methadone. We had a rash in the 80s and a lot of people died.

 

[ChemicallyEnhanced]

I'm afraid they would unfortunately

In the 80's some idiots abused them by taking huge doses which result in 24-36 hour derealisation / full aural and visual hallucinogenic state (seeing / interracting with people who were not there etc) First hand reports were of absoluutely zero pleasant effects and just total fully-awake nightmare for the whole (very long) duration

I personally know someone who fought with customers in a shop cos he thought they were terrorists (badly injuring someone in the process) and then wildly fought the cops on arrest. Jailed for 3 years. Another guy (first guy's mate) seriously injured after jumping from a 2nd floor window attempting to escape from agang with machetes in his kitchen (who were not actually real). I also knew someone who died after jumping off a building for no discernable reason while on them...sounds like an anti-drugs propaganda advert but unfortunately 100% true, trust.

ffs keep any use to a bare minimum

Sounds like the same "high" you get from any of the first generation anti-histamines.
For some reason Cyclizine seems to potentiate opioids much more strongly than the others, though.

I think 450mg is the most Cyclizine I've taken in a day,

 

[Fertile]

The reasons are not clear but cyclizine is used for it's 'opioid sparing' properties.

 

[DrPetro]

The data about people experiencing full dissociation with the rare effect of complete hallucination of events not occuring is only matched by peoples experiences with hyoscine/scopolamine, the active principles (along with atropine) of datura. Sounds terrifying. So my highest dose in my plugging experiment was 200mg at once about 5 minutes prior to shot of opioid/opiate. It did potentiate the effect but only for a very short time and if I'm honest ended up being too much of a pain in the arse I once tried IV'ing approx 200mg too and this was no more impressive than plugging but with the unpleasantness of a shivering bad hit about an hour later. I shan't be trying either again but I was glad to finally scratch that one off my bucket list , having heard a lot about Diconal injecting some years ago.

 

[fastandbulbous]

I think it's doxylamine that's easilymore available, that potentiates opiids (as in syndol tablets) as well. Jus be bloody careful. Th best combo is by far dipipanone/cyclzine: perfect combo (well plugging 3 diconal as was blissful as I've experienced).
Of course, if you're a bit more slapdash about survival prospects, carisoprodol is fcking nice...

 

[DrPetro]

I think it's doxylamine that's easilymore available, that potentiates opiids (as in syndol tablets) as well. Jus be bloody careful. Th best combo is by far dipipanone/cyclzine: perfect combo (well plugging 3 diconal as was blissful as I've experienced).
Of course, if you're a bit more slapdash about survival prospects, carisoprodol is fcking nice...

Oooh, doxylamine is a new one on me ! Carisprodol I love too along with pregabalin, but obviously combining sedatives with opiates is a favourite if risky combination. I think the two reasons I've never had to be revived by paramedics is a) a big methadone tolerance and b) the fact that I've never been a drinker. I think that if Id had company though I might well had paramedics called if Id had company when combining alprazolam solution with opiods !

 

[Fertile]

I think it's doxylamine that's easilymore available, that potentiates opiids (as in syndol tablets) as well. Jus be bloody careful. Th best combo is by far dipipanone/cyclzine: perfect combo (well plugging 3 diconal as was blissful as I've experienced).
Of course, if you're a bit more slapdash about survival prospects, carisoprodol is fcking nice...

Have you read the GB patent on the synthesis of dipipanone? Unexpected - no enamine or so on.

Someone sold the pyrrole analogue of dipipanone and it did not sell. I suspect it would be illegal in too many nations.

Neither did the nitro homologue of metofoline (x20 codeine in mice).

But I've found something not novel... more overlooked that is x150M and is made from 3 common precursors.

Of course - their is a U-47700 homologue some x22.5 M and it's synthetically cheap and simple....

I do not know WHY things like AP-238 have shown up but NOBODY had looked at the QSAR. Azaprocin i.e.
Pharmacological Research Communications vol. 20 iss. 5 pp.383—394
Interaction of 3,8-diazabicyclo (3.2.1) octanes with mu and delta opioid receptors
DOI: 10.1016/s0031-6989(88)80014-6

p-nitrocinnamyl DBO (1d) which displayed a mu/delta selectivity and an analgesic activity respectively 25 and 17 fold those of morphine.

Conversely, the most significant changes in opioid receptors affinity and/or selectivity were induced by substitutions on the phenyl group of la. In particular, the presence of a nitro group in ortho (ib) or para position (Id) led to a 4-fold decrease in sigma affinity which in the case of id was accompanied by a 3-fold increase in mu affinity.

So maybe AP237 derivatives have significant sigma activity responsible for the negative effects. Shortening the amide by 1 carbon and adding a p-Nitro to the cinnamyl's aromatic ring seems a very obvious experiment.

By all means keep the 2 methyl groups (part of the bridge in azaprocin) to keep the piperidine in a minimum-energy state but vastly reducing sigma activity is good and tripling mu activity is also good.

Still junk in my opinion, but these days, people will pay a fortune for junk - Grisham's law. Anyone who carries out proper testing and instrumentation will make a much lower profit.... and when they see others just NOT bothering and still making a huge profit - why not them?

People COULD club together to have stuff tested, but the user base seems full of people who are just in their first steps to developing a terrible addiction.

 

[DrPetro]

Have you read the GB patent on the synthesis of dipipanone? Unexpected - no enamine or so on.

Someone sold the pyrrole analogue of dipipanone and it did not sell. I suspect it would be illegal in too many nations.

Neither did the nitro homologue of metofoline (x20 codeine in mice).

But I've found something not novel... more overlooked that is x150M and is made from 3 common precursors.

Of course - their is a U-47700 homologue some x22.5 M and it's synthetically cheap and simple....

I do not know WHY things like AP-238 have shown up but NOBODY had looked at the QSAR. Azaprocin i.e.
Pharmacological Research Communications vol. 20 iss. 5 pp.383—394
Interaction of 3,8-diazabicyclo (3.2.1) octanes with mu and delta opioid receptors
DOI: 10.1016/s0031-6989(88)80014-6

p-nitrocinnamyl DBO (1d) which displayed a mu/delta selectivity and an analgesic activity respectively 25 and 17 fold those of morphine.

Conversely, the most significant changes in opioid receptors affinity and/or selectivity were induced by substitutions on the phenyl group of la. In particular, the presence of a nitro group in ortho (ib) or para position (Id) led to a 4-fold decrease in sigma affinity which in the case of id was accompanied by a 3-fold increase in mu affinity.

So maybe AP237 derivatives have significant sigma activity responsible for the negative effects. Shortening the amide by 1 carbon and adding a p-Nitro to the cinnamyl's aromatic ring seems a very obvious experiment.

By all means keep the 2 methyl groups (part of the bridge in azaprocin) to keep the piperidine in a minimum-energy state but vastly reducing sigma activity is good and tripling mu activity is also good.

Still junk in my opinion, but these days, people will pay a fortune for junk - Grisham's law. Anyone who carries out proper testing and instrumentation will make a much lower profit.... and when they see others just NOT bothering and still making a huge profit - why not them?

People COULD club together to have stuff tested, but the user base seems full of people who are just in their first steps to developing a terrible addiction.

Genuinely fascinating, even if some of the chemistry is beyond me. As you quite rightly say, people will pay a lot for junk. In the UK we have less of a problem with street heroin being adulterated with fentanyl analogues etc and have also largely avoided things like the veterinary sedative xylazine, so it also follows that the RC opioids also appear to have not taken off in the same way as MCAT and cannabinoid analogues did. As a UK user I'd hazard the guess that this is partly to do with the much wider prevalence of opioid use across socio economic groups in the US.

 

[Fertile]

I ASSUME what an RC vendor would want (given AP 238 was/is sold) is something dirt cheap to make in the morphine class potencywise.

These exist.

 

[DrPetro]

I ASSUME what an RC vendor would want (given AP 238 was/is sold) is something dirt cheap to make in the morphine class potencywise.

These exist.

They certainly do exist but I'm suggesting that, for various reasons, RC opiods haven't taken off in a big way in the UK
Part of the reason is the fact that, once one has a dependency, the drugs are required NOW, not in a few days once the snail mail arrives.
I've never tried AP238 but have bought fent analogues from the darknet some years ago.