Combinations - Loperamide activation by Doxepine

[sineP]

SWIM found this in a german drug wiki and became quite interested, but since he could not get Doxepin he could not yet try on himself. Anyway he thought it might be interesting for some of you because the only Loperamide threads he found here so far where about smoking or snorting Loperamide without a "Catalyst" or Booster.

Here is the German original, Translation is below:

Einige Tage später schnappte ich dann im Loperamid-Thread auf, dass ein User herausfand, dass man Doxepin als Booster (Kat.) benutzen konnte, um das Loperamid ins Gehirn zu bringen, und dem Opiat die Wirkung zu ermöglichen. Natürlich war ich erstmal sehr überrascht, da ich an DIESE Möglichkeit sicher nicht gedacht hatte. Wie es der Zufall wollte, hatte ich noch eine Packung Doxepin zuhause.
Mir war nicht ganz wohl dabei, da es so gut wie KEINE Versuche zuvor gab (und gibt ), und ich mitunter eine Art Premiere (nach dem User x) darstellte, sprich ich wusste nicht wirklich etwas über die Dosierung des Doxepins noch der des Loperamids. Es war sehr vage.
Doch während ich diesen gedanken dachte, musste ich unweigerlich in mich reingrinsen, da ich wusste, ich würde diesen kranken Versuch starten, komme was wolle. Mir war zu diesem Zeitpunkt absolut nicht bewusst, worauf ich mich einließ...
Ich wusste zwar, dass sich leute im Opioidforum mit Chinidin & Loperamid beinahe auf den Mond geschossen hatten, doch verdrängte ich dies zu diesem Zeitpunkt wohl.

Ein Tag später war Samstag, soweit ich mich erinnerte. Mir fiel nach dem Frühstück ein, was ich am Vortag vorhatte.
Als mein Magen wieder einigermaßen nüchtern war, nahm ich um die 50-55mg Doxepin zu mir, und wartete ungefähr 10 Minuten. Die Wirkung flaute sehr langsam an, doch war sie noch nicht klar vorhanden.
Ich setzte mich an meinen Schreibtisch, holte die Packung Loperamid hervor, und öffnete vorsichtig eine der grünen Kapseln. Das weiße Pulver, dass einen chemischen Geruch verströmte, schüttete ich vorsichtig auf meinen Daumennagel, und formte eine keine Mini-Line, da ich doch auf Nummer sicher gehen wollte.
Ich zog diese Line, wartete eine Weile, doch zeigte sich keine Wirkung, außer ein langsam zuschwellendes Nasenloch, da ich das ziehen nicht gewöhnt bin. Ein paar Minuten später zog ich dann noch eine 2. und 3. Line, insgesamt zog ich ungefähr über die halbe Kapsel. Da ich, nicht wie erwartet, breit auf meinem bett lag nahm ich aus Enttäuschung die noch ungefähr halbe Kapsel ORAL zu mir, und machte mich auf den Weg zu meiner Freundin, die ungefähr 5 Minuten zu Fuß von mir weg wohnt.


Am Anfang des Weges machte sich das Doxepin deutlich bemerkbar, und ein wenig anders als sonst. Allerdings nicht lohnenswert. Ein paar Minuten später liefen mir die Eltern meiner Freundin entgegen, die wohl meine Eltern besuchen wollten, da sie schon seit Jahren eng befreundet sind. Ich musste unweigerlich grinsen, als sie mir auf der langen geraden entgegenkamen, und ich musste mich wirklich beherrschen, die Mundwinkel unten zu lassen, was aber wirklich unmöglich war. ich grinste verstohlen in mich rein, grüßte sie freundlich, und atmete (natürlich grinsend) erstmal erleichtert auf, als sie vorbeizogen. Es war defintiv anders. Es gefiel mir, allerdings war es nicht so "berauschend", dass ich es wiederholt hätte - zu diesem Zeitpunkt.
Ich zündete mir eine Zigarette an, und setzte mich auf eine nahegelegene Treppe, und rauchte, was allerdings nicht viel brachte.
Bei meiner Freundin angekommen war ich voll auf Doxepin, und war schon sicher, dass es das gewesen war. Ich war schon ziemlich enttäuscht, und dachte schon längst nicht mehr wirklich über das Loperamid nach, da die Wirkung wiegesagt nicht spektakulär war.
Wir schauten ein paar Minuten Fernsehen, und machtes es uns gemütlich. Ein Samstag-Nachmittag wie einige im Jahr. In einem Augenblick lachte ich noch über die Sendung im TV,
und plötzlich wurde mir bewusst, " es klappt wirklich ".
Doch Zeit zum Staunen oder zum "ich stelle mich mal langsam drauf ein" blieb mir nicht....


Was nun folgt ist schwer fassbar, und schriftlich sehr schwer zu formulieren, doch ich versuche es..
Meine Freundin streichelte mir zu dem Zeitpunkt über die Haare, und ich fixierte den Fernseher, bzw. die Bilder die abliefen. Auf einmal merkte ich, wie etwas ungeheures, etwas seeeeehr mächtiges in mir aufkam: Es ist ein Gefühl, dass sich anfühlt, wenn man auf einem 1000 meter- hohen, einem meter breiten Turm steht, und sich gerade fallen lässt: Es fühlt sich an, als würde man an einen gigantischen Generator angeschlossen sein, der einen pro Millisekunde mit Millionen von Kilowatt aufläd bis man aus allen Nähten platzt. Diese Steigerung, die man als linear beschreiben könnte, entlud sich dann:
Eine wirklich nicht beschreibbare mächtige Euphorie
schob sich mit einem ungeheurem Druck in die letzten Windungen meines Gehirns, - es war keine smoothe Heroin-Euphorie, die "schön" ist, nein, sie war so MÄCHTIG dass sie mir unheimlich Angst machte, und ich hatte augenblicklich Angst zu sterben

Die Intensität war so heftig, dass ich (ich saß im Schneidersitz) innerhalb dieser "Welle" nach hinten umkippte (und zwar schnell), auf dem Rücken landete und um Luft japste; Ich zog die Luft in mich ein wie ein Ertrinkender, der sich Wasser in die Lungen zieht weil er Sauerstoff benötigt, und kurz daraufhin elendig verreckt.
Innerhalb dieser Zeit, die nicht sehr lange war - velleicht eine Sekunde - sah ich, peripher neben den anderen mächtigeren Eindrücken, einen Krankenwagen der vor dem haus meiner Freundin steht; gedanklich "wusste" ich, dass ich sterben würde.
Diese Euphorie ist in ihrer Form am ehesten mit einem "aufladen..." zu vergleichen, indem sich die ganze Energie von den zehenspitzen in den Kopf zieht, und sich dort mit einem überaus mächtigen GONG entläd, einer Giga-Wasserstoffbombe die explodiert, Wie ein gigantischer Strudel im Meer, der in Kilometer-Umgebung alles mit sich reißt.

Als der Euphorie-Gong abflachte, war ich natürlich erstmal erleichtert, und wusste erstmal GAR NICHTS mehr. ich musste dieses Erlebnis erstmal verarbeiten.
Meine Freundin wusste zu diesem Zeitpunkt bereits bescheid.
Ich dachte zu diesem Zeitpunkt, dass es das nun gewesen sein musste. Dann folgten 5 Minuten Pause,in denen ich mich stark wunderte und erfreut war noch unter den lebenden zu weilen, dann begann das Zeremonial von vorne:

Es folgte eine zuerst leichte (fast (!) angenehme) Euphorie, die linear stärker wurde, immer stärker, sich steigerte und sich auf dem Peak vereint in einem Punkt in einem gigantischen Euphorie-Gong entlud, ein gefühl als wäre man von einem 10Tonnen-Vorschlaghammer direkt auf den Hinterkopf getroffen worden. Dieses mal wusste ich gottseidank, dass ich beim ersten Mal nicht gestorben war, und das brachte wenigstens ein Funken Berhuigung, oder Hoffnung, besser ausgedrückt. Es ist ein gefühl, als würde man auf einer gigantischen Monster-Welle surfen, unter einem Häuser so klein wie Sandkörner, über einem blauer Himmel, und nicht so fern wie gewohnt, unter einem ein nicht beschreibbarer Abgrund.


Ich erlebte noch ungefähr 2 dieser Gongs, dann war die Sache vorbei.
Der Afterglow gestaltete sich dagegen angenehmer, ich spürte noch die Nachwehen dieser gigantischen Euphorieflut in Form von linearen Auflad-Euphorieschüben, die allerdings sehr sanft ausfielen.


Fazit:
Defintiv die heftigste und dramatischste Drogenerfahrung
die ich je erfahren habe.

Ich bin fest überzeugt, dass diese Erfahrung einmalig ist / war, und man soetwas mit nichts vergleichen kann.
-by grasmoral for dF

Translation by sineP
-----------translation start-----------
Some day later i read in the Loperamide thread that you could use Doxepine as a Booster (Catalyst) to bring the Loperamide into the brain and allow it to work as an Opiate.
Of course i was suprised first because i sourely had not thought of THAT possibility. How coincidence wanted it, i had a box of Doxepine at home.
I did not feel completly well with it, since there had been (and are) as good as NO trials before, an I was something like a premiere (right behind User X). say i did not really know anything about the dosage of neither Doxepine nor Loperamide. I was very vague.But while in these thoughts i had to smile, knewing i would start this sick experiment, come what may.
At that time i had no idea what i was getting myself into...
I knew that people from the Opioideforum had shot thereselfs almost to the moon with Chinidine & Loperamide, but i was pushing these thoughts away at that time.

The next day was satuarday as far as i remember. After breakfast i remembered what i wanted to do the day before.

When my stomach was empty again i took about 50-55mg Doxepine and waited about 10 minutes.
The effects started but where not clearly there yet.
I sat down at my desk, grabbed the pack of Loperamide, and carefully opene one of the green capsules*.
I carefully poured the white powder with a chemical smell on the nail of my thumb and formed a small Mini-Line, since i wanted to be on the safe side.
I snorted the first line and waited a while, but no effects showed besides a slowly closing nostril, since i am not used to snorting.

A few minutes later i snorted a second and a third line, overall i had snorted more than helf of the capsule.
Since i did not lay on my bed stoned as i expected to, i took the rest of the Capsule ORALLY beeing full of disappointment and got on my way to my girlfreind who lives about 5minutes away.

At the beginning of the way the Doxepine kicked in heavily, and a bit different from other times. Anyhow not worthwhile. A few minutes later my gf's parents crossed my way, who appearingly wanted to visit my parents since the have been close friends for years. I had to smile, and it was really impossible not to. I smiled into myself an greeted friendly and breathed trough with relief after i had passed them(of course smiling). It was defitely different. I liked it, anyway at that time it was not that "exhilarating" that i would have repeated it.
I lighted a Cigarette and sat down on some neartby stairs to smoke, which did not bring alot.
Arriving at my gf i was fully on Doxepine, and was sure that it had been all. I was quite disappointed, and was long not tinking about the Loperamide anymore, since the effect was as said not spectacular.
We watched TV for some minutes and got comfortable, a satuarday afternoon as many in a year. One moment i was laughing about the program on TV

and suddenly i realised: "it is really working!".

But i was not left time to marvel or for "i tune into it slowly"....

The following is highly elusive and hard to couch in terms but i will try...
My girlfriend was palming my hair at that time and i was focussing the TV, respectevely the pictures on it. Suddenly i noticed something decuman, something veeeeery mighty was coming up in me. It is a sensation, feeling
like standing on a 1000meters high and one meter wide tower and just letting yourself fall: It feels like getting connected to a gigantic generator that charges you with Millions of Kilowatts per milisecond until you burst at the seams. This augmentation, which could be described as linear, finally discharged:

A really undescribable mighty Euphoria

beeing pushed into the last meanders of my brain with prodigious pressure.
it was no smooth Heroine-Euphoria, which is "beautiful", no, it was so MIGHTY that it frightened me eerily, and instantly i was afraid to die.

The intensity was so extreme, that during this "wave" i (i sat cross-legged) fell on my back (and that fast) and gasped for air; I hauled air into my lungs like someone drowning hauls water into his because he needs oxygen, and than pegs out woefully.

During this time, which was not very long - maybe a second- i saw,
circumferential to the other more mighty impressions, an ambulance standing in front of my gs's house. notional i knew i would die.

This Euphoria is in its form best compared with some kind of "charging...",
in which all the energy from the point of the toes goes into the head,
and there discharges in a overwhelmingly large GONG, a giga-Hydrogenbomb exploding, like a gigantic vortex in the ocean sweeping along everything within kilometers.

As the Euphoria-Gong flattened, i was firstly reliefed of course, und for some moments i did KNOW NITHING. i had to work up this Experience first.

My girlfriend knew what was going on at that time.
I thought back then, that this was supposed to have been it.
Following where 5 minutes break, durings which i was quite amazed and glad to be still under the living, then the ceremonial started over:


It followed a mild (almost(!) pleasant) Euphoria, getting stonger lienarly, stonger and stronger, rising and then united in one spot at the peak discharged in a gigantic Euphoria-gong. A feeling as if beeing hit with a 10ton Hammer right in the back of your head. Thanks god this time i knew i had survived the first time so there was a spark of relaxation or better hope. It is a feeling like surfing a giant Monsterwave, below one houses as small as sandcorns, above one the blue sky, and not as far away as usual, below one there is an undescribable abyss.

I underwent about two more of these Gongs, then the whole thing was over. The afterglow however shaped more pleasant, i still felt the afterpains of this gigantic euphoria-flood in form of lienar charging-euphoria waves, which sampled out very soft.




Conclusion:



Definitely the most severe an dramatic Drugexperience i have ever made.


I am totally confident thet this Experience is unique, and one can not compare it to anything.

-----------translation end-----------

*Swim supposes it was a 2mg Loperamide Capsule, beeing not sure he would personaly start as low as .5mg insufflated Loperamid and 50mg Doxepine.


Hope this could help or at least entertain a few of you.

Reputation Comments on this post:

	great post, thanks!
	great contribution.. thanks for info & translation

[deekyleeky]

I thought I would just add this, Im not really sure what this means exactly... but here goes

Crossing the blood-brain barrier

When loperamide is taken by itself, it cannot readily cross the blood-brain barrier; however, when loperamide-containing nanoparticles are coated with polysorbate 80 and injected, the results were the same as typical opiates and opioids -- long, effective analgesia. A solution prepared using loperamide coated with polysorbate 80 resulted in a very short duration of action and less effective analgesic effect. The same study concluded that loperamide does not cause any analgesic effects when taken by itself.[3]
Concurrent administration of P-glycoprotein inhibitors such as quinidine with loperamide has been found to produce respiratory depression, indicative of central opioid action

[sineP]

Since Polysorbate 80 costs only 3,95€ per 100ml (maybe even cheaper, it was the first searchresult) swim was wondering if one could just jumble a pack of loperamide capsule powder into it to activate its "analgesic" effects.
Or would it be more demanding to coat "loperamide-containing nanoparticles" with this stuff?

[Tortoise]

Originally Posted by sineP

Since Polysorbate 80 costs only 3,95€ per 100ml (maybe even cheaper, it was the first searchresult) swim was wondering if one could just jumble a pack of loperamide capsule powder into it to activate its "analgesic" effects.
Or would it be more demanding to coat "loperamide-containing nanoparticles" with this stuff?

Much more demanding than simply mixing them.

What the hell is doxepim anyway?

[sineP]

Originally Posted by Tortoise

Much more demanding than simply mixing them.

What the hell is doxepim anyway?

Well HOW demanding would it be? Or better: which steps would be neccesary?

If you allow me to qoute http://en.wikipedia.org/wiki/Doxepin to answer your question: "Doxepin is a psychotropic agent with tricyclic antidepressant and anxiolytic properties, known under many brand-names such as Aponal®, the original preparation by Boehringer-Ingelheim, now part of the Roche group; Adapine®, Sinquan® and Sinequan® (Pfizer Inc.)."

[Paracelsus]

Well HOW demanding would it be?

Read up on nanotechnology. You'll get the general idea.

[sineP]

Well, i have read quite a bit about moving atoms with a little, few-atom wide needle, and gears only build from a few molecules and alike stuff, but I found nothing about "coating nanoparticles" at all. I'd like it alot if some one could post a link to a description of this procedure.

[Paracelsus]

http://www.occup-med.com/content/pdf/1745-6673-2-16.pdf

But I tend to believe that anyone with the capabilities to make use of nanotechnology wouldn't need to ask for advice on Drugs-Forum.

The nanoparticle delivery of loperamide is interesting but far from becoming relevant to the recreational drug scene.

[sineP]

I have just found the following on another forum, it seems to me that the procedure might not be that difficult after all.

Chemethist on bluelight 24-10-2007, 00:00,
[...]
1. The nanoparticles needed are those of Poly-butyl-cyanoacrylate.[...]
Butyl-cyanoacrylate is used extensively in bonding and for liquid sealing wounds.Once you get this you can make your own Poly-butyl-cyanoacrylate.Add the Butyl-cyanoacrylate to acidified water, and then add insulin to the reaction. This will yield nanoparticles of PBCA.
NEXT:
You mix your loperamide with the nanoparticles to create a nanoparticle solution of loperamide. Add a little of the polysorbate 80 to the loperamide nanoparticles, mix well.
Set up for injection and get ready for a ride!!![...]
Do not be afraid of this, start small of course, maybe 2-4mg of loperamide. (note: I DISAGREE STRONGLY! a "safe" start would be maybe half or third of a miligram, i'd never ever advice to go higher on a first try)
The poly-butyl cyanoacrylate and polysorbate 80 are both safe for the body and should not be feared.

Anyhow I think this goes a bit to far into the chemistry direction for this particular forum. I suggest we concentrate on Medications as Loperamide Catalysts here.

[Tortoise]

Or you could just buy some smack.

[sineP]

Originally Posted by Tortoise

Or you could just buy some smack.

geeez, there ARE of course "alternatives" to loperamide activation, but this is what we talk about in here.

[0utrider]

swim still doesnt unterstand why the doxepine makes the loperamide so much more powerful, and also why no one tried that, what are the dangers (except for the obvious, like unforseeable effects and OD) ??

[poozjurry]

yes swim doesn't understand this, too, but he is interessting.
Run this with Amitriptylin, too? its almost the self chemical structure.

Hmm SWIM is very curious but also somewhat scared to try this out. He has a full script of Doxepine, either in 25 MG or 50 MG capsules. He wants to try this out but really does not see how a low dose of Doxepine could just magically cause Loperamide to cross the blood-brain barrier. When SWIM gets home he may try low doses of both (as was done in the post), IE or or two Doxepine and 2 MG of Loperamide to start maybe increasing it to 4 MG, SWIM plans to take this all orally on a mostly empty stomach and just see what happens.

Have any other Swimmer's tried this yet? Will this SWIM be the first? SWIM is pretty sure that Doxepine is a pretty rare drug and it is not given out very much these days, but SWIM's doc has tried everything (that is non-addictive) to help SWIM sleep, but the only thing that works for SWIM is Ativan.

Anyway SWIM will be sure to post his results on this in a timeline style if he decides to do it. It will be interesting because SWIM has never tried Doxepine alone, so he is not sure how that will effect him, he suspects at most it may make him tired. SWIM has taken Loperamide plenty of times alone (up to 6 MG or so) for their intended function (what Opiate user hasnt?) and knows they do not cause any issues for him. And SWIM has a very high tolerance to Opiates, it takes anywhere from 80 to 200 MG of OXY to get him high, depending on the last time SWIM did the drug. So SWIM thinks this will be fun, but he does not expect to have results like the ones listed at all, but I guess we shall see.

Stay tuned!

[Paracelsus]

I doubt that your friend is the only person on the planet who is prescribed doxepin and takes loperamide (some people use it for diarrhea, you know...).

[0utrider]

AFASWIMKs if taken with doxepine one should start low with the loperamide, but SWIM read somewhere that it takes a few more mg's to feel something..

Well SWIM tried it last night with 50 MG of Doxepine and 4 MG of Loperamide and about all he can say from it is that Doxepine is an odd drug...

SWIM consumed the stuff at around 9:00 PM, an hour later he was feeling a little different, kinda heavy headed and off, but not really tired and did not want to go to sleep. Then all the sudden at around 11:00 PM SWIM got super tired and could not really stay up any longer so he went to bed and had a bitch of a time waking up this morning.

So from this SWIM thinks that the Loperamide added nothing and it was just the Doxepine that made SWIM tired and fall asleep, which is why he was given it in the first place, tying to get up today though made it almost not worth taking at all. SWIM may try this again at some point with a higher MG of Lopermide but he does not think anything will happen besides falling alseep.

It should also be added that SWIMs pupils stayed normal size during this, they did not get smaller at all...

[Politicalchalk]

Pupil size: Excellent observation! While one supposes that loperamide may be unique relative to it's occular effects, but small pupil size would be an immediate indicator of opiate-type action (to say, an EMT or ER doc) on the CNS.

Also, being an opiate, loperamide might be expected to add CNS depression in a synergistic way with any depressants -- and tricyclics are notorious for side-effects in some people.

The poor spelling and overall quality of the translation (German no less -- where 'idea' and 'representation' are the same word!) makes SWIM suspicious of it's accuracy. The above differential experiment seems to confirm this. Loperamide AND Doxepin are both fairly older drugs, and our critical thinking skills tell us that it would have become...open knowledge about such an interaction. ESP. among chronic opiate users! But ESP. in post-marketing data/clinical observation!

If Swim recalls correctly, loperamide was actually CV for a while before being demoted to OTC. Significant studies are required to go from being Rx vs. OTC ~ the scheduling only adds another layer.