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Opioids Loperamide 2020

Nicomorphinist

Bluelighter
Joined
Apr 18, 2019
Messages
1,401
I am hearing that there is another push to make loperamide harder to use back in the States, like packaging restrictions:


So something is up. Part I is a political rant. Part II is a somewhat detailed description of my research, including as a guinea pig.

It is the same pressure groups yelling about kratom, tianeptine, poppy seeds, who want more people paying five and six figures a pop for rehab or dying, and some retailers like Wal-Mart apparently rolled over even harder than that, jacking up the price, putting it behind the counter, which could have a couple of reasons. One article says "Customers buying more than one package . . . that gives pharmacists a chance to have a discussion with them."

No, particularly with what the US and most states and turned the profession into (who can name me a state where the old pharmacist prescribing ability is still in place?), and especially technicians and retail clerks, let me tell you as a longtime member of the brother and sisterhood in a number of capacities that doing such a thing is not your place, and if you do, you will only expose yourself to assault and battery and worsen the Inventory Shrinkage problem that plagues a lot of retailers in general, not to mention that some percentage of your techs and delivery people are going to get sticky fingers too. Maybe, as always the junior detectives amongst your number deserve to be hit in the face with a basket or crutch or cane for messing with customers, but why do you want to make more trouble for yourselves? The customer is always right; before I left the country because of all of this nonsense I always walked around with a cane with a big heavy silver head on it, hard-soled shoes, and at least four to six other people with me sometimes more than 10 and I am sure there are others especially old folks who could also start a nice riot for you.

Why are you people doing the work of the gangsters in the rehab business anyways? What kind of bone have they thrown you? I'm sure pharmacies get ripped off by the manufacturer on Suboxone just like patients do, and do they even let all pharmacies fill methadone for maintenance people? And how can you help them if they are dead? Don't tell me that all hydrocodone going to Schedule II and Darvon disappearing, even tramadol going to Schedule IV from uncontrolled and all of the prescription monitoring database rackets snaring codeine and dihydrocodeine syrup haven't cut into the fun that some of your unwise colleagues used to have diverting those medicines a few tablets or ml or an exempt register 120 ml bottle or four at a time. The new benzodiazepine and gabapentinoid jihad is already starting up . . . some of these bastards even whine about bupropion. What the fuck, as the kids these days say.

At least the prescription monitoring databases give some of your people new opportunities to ask for cash honouraria and handjobs, blowjobs, clit polishing and other fun when it is time to dole out the benzodiazepines, gabapentinopids, buprenorphine, codeine and the like, am I right? The Schedule II stuff too, now that I think of it. You don't want to fall behind doctors and inspectors and people from the prosecutors' offices and even the occasional journalist in getting yours, do you? Durum et durum non faciunt murum -- don't tell me they don't teach that to doctors, dentists, veterinarians, and those in the allied trades, do they? You are part of an honourable ancient iron triangle with doctors and patients, even if the regulators and politicians don't respect you. Or respect the the patients or doctors either. Stand up for yourselves and stop doing the politicians and rehab millionaires and De Sade gangster disciples' dirty work! Every time some politician and local doogooder wants some press it's going to get worse. Somebody has to break the spiral of silence . . .

If you people think all of this is going to give you new power and respect you are sadly mistaken -- just ask the doctors what is happening to them.

Do I even have to mention what the environmentally unfriendly package is doing to the elderly and others with arthritis? Then you have the people who melt the packages with a blow torch. A family or neighbours or bridge club or local political party can have a scissors party and have a bowl of 1000 tablets inside of an hour. So what good has it done?

I feel your anger. I know your dreams. What you have to do is fight back and get the latitude and respect that all of that studying for degrees and licensures should have guaranteed for you, even without decamping to Canada or Europe as at least a few have, not roll over. If I am preaching to the choir, you need to fight back within your professional organisations as well because they have not responded creditably to any of this.

Now, loperamide, which is a 4-phenylpiperidine opioid, a substituted prodine to be specific, with a relationship also to normethadone, a precursor along with norpethidine in the more common syntheses, also has potentially neurotoxic metabolites just like pethidine, and its potential cardiotoxicity at high doses, make for two reasons it is not used clinically for analgesia or stopping withdrawal. Which it does. Since I had an appointment with my cardiologist last week, I decided to try out loperamide for a couple of weeks and I can tell people the following:

It can be made to work in doses that are much lower than the media reports are talking about. After all, when it was first introduced in many markets it was regulated like pethidine (US CSA Schedule II), then codeine (to Schedule V in July 1977) then decontrolled in April 1982. Something is in that arse glue, which is why the rehab gangsters are whining about it.

There really is no need for gobbling 100 and 200 tablets at once which is very dangerous, even if you are going into this from a high dose of another narcotic. The relationship is not linear either, which is why no equianalgesia or equi-counterwithdrawal ratio can be determined. But the "poor persons' methadone" title is apt in that it is possible to build up a serum level which allows for lower doses and/or less frequent dosing later.

The very high doses from gobbling entire economy sized bottles do also increase the chances of paralytic ileus, intestinal blockage, and at a minimum gastric stasis vomiting after a day or more of increasing discomfort, especially with larger tablets like those with carminatives and/or attapulgite in them. They tend to have chalk in them in many cases.

With my fairly high hydromorphone dose supplemented with nicomorphine and Scophedal for breakthrough pain 0 to 2 times a day, I found that 24 tablets or 48 mg every 12 to 18 hours during the first 48 hours, which is the double loading dose that loperamide, difenoxin, and diphenoxylate need when used for diarrhoea, build up a bolus that allowed me to take 32-48 mg once a day for the next five days or so, then even skip days after that, or at least take doses q36h.

Omeprazole did seem to help some, I eat oodles of black pepper anyways on my food and I am sure that helped too, and hydroxyzine worked very well potentiating it, making it possible to use less. Given all the above, it behooves people to start out at just over the anti-diarrhoeal dose and can go up every four hours at the very beginning I suppose, or phase in the loperamide by increasing the dose 10 per cent each time and seeing how much of the other medicine you need to stop the withdrawal; I would start at 25 per cent of the old dose.

If you are going to use loperamide for a shorter period, like three or four days at most, it still does not require a huge dose. A one-off for analgesia or withdrawal-related diarrhoea the same thing. There are some people who when not on other narcotics notice some anxiolysis and analgesia from a single 2 mg tablet.

I must say, I was aware of all the literature going back to the beginning right when Janssen Pharmaceutica invented it as well as diphenoxylate and difenoxin and it went into many markets and knew about the morphine addicted monkeys and other experiments, and I did try it that one time at a high dose and it felt like piritramide but I also had a case of the Fear in the hours afterwards, psychosomatic no doubt . . . So when after I got into Stage II withdrawal and I gobbled the first loperamide, hydroxyzine, and omeprazole dose with ćevapčići covered with pepper and carbonated water and took a shot of orphenadrine and tripelennamine in the arse cheek and I felt the pressure on the back of my neck and the first curls of euphoria stealing over me 35 minutes later I thought "O my goodness! It actually works!" Which shouldn't be interpreted as carpe diem if you have a 300-count bottle of 2 mg liquigels in front of you. Look at the above and start much lower because who amongst you has five decades of tolerance in you?

So my experiment with loperamide worked, but I will tell you that I did feel healthier, and quickly, after my first doses back on hydromorphone and nicomorphine. And if you are going to plan a loperamide (or even better difenoxin or diphenoxylate) bridge you probably should start to taper it during the last 30 per cent of it because it does still add to your tolerance, just like anything else. I can also say from earlier experiments with mixing it with other narcotics, like DTO (laudanum) and paregoric with belladonna tincture and morphine mixed with tripelennamine IV confirmed that it may potentiate narcotic analgesics, or just replace the part of a prior dose that was removed. The possibility of it driving up tolerance even more than it might suggest is something that some Bluelighters have reported over the years.

Would I recommend doing any of the above if you have any other choice? Probably not. But they are not giving a lot of people other choices, which is why I decided to kvetch about loperamide. Hopefully you are in a situation when considering this that you can use potentiators to stretch out what you have left of the narcotic you are taking, but problems have a way of sneaking up on everybody when it comes to planning with narcotics sometimes, it seems.
 
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I have been reading about Loperamide for quite a while. I was tempted to use it for heroin withdrawals years ago when I was addicted but didn't happen. I got cocky after 10 years clean of heroin and started using opium and poppy pods regularly about 6 months ago and got myself dependent on it. In comparison to my IV H& C addiction days, my current dependency is miniscule and it hasn't effected my life much, yet.
Hearing that Loperamide works efficiently in much lower doses than what people claim for a person who is on quite serious pain medication and who has decades of opiate dependency experience like you is pretty reassuring. I have to stop my current dependency (about 500mg of opium per day) before I mess my life up seriously. After hearing your experience, I think that I will start by tapering down my consumption then probably will start dosing at 24mg Loperamide in combination with Omeprazole & Hydroxyzine.
The usual addict problem is driving me crazy though, that is when to start. I know the answer which is "today" but I have to push myself to do it before I mess a variety of things up in my life.
Genuine thanks for posting this Nico. I had my doubts prior to this but hearing it from a knowledgable, decades long experienced person who posts only smart and informative threads on BL erased my doubts.
 
I have been reading about Loperamide for quite a while. I was tempted to use it for heroin withdrawals years ago when I was addicted but didn't happen. I got cocky after 10 years clean of heroin and started using opium and poppy pods regularly about 6 months ago and got myself dependent on it. In comparison to my IV H& C addiction days, my current dependency is miniscule and it hasn't effected my life much, yet.
Hearing that Loperamide works efficiently in much lower doses than what people claim for a person who is on quite serious pain medication and who has decades of opiate dependency experience like you is pretty reassuring. I have to stop my current dependency (about 500mg of opium per day) before I mess my life up seriously. After hearing your experience, I think that I will start by tapering down my consumption then probably will start dosing at 24mg Loperamide in combination with Omeprazole & Hydroxyzine.
The usual addict problem is driving me crazy though, that is when to start. I know the answer which is "today" but I have to push myself to do it before I mess a variety of things up in my life.
Genuine thanks for posting this Nico. I had my doubts prior to this but hearing it from a knowledgable, decades long experienced person who posts only smart and informative threads on BL erased my doubts.

24mgs works surprisingly well for me but my habit was more sporadic this time around. It works even better the second day because of the building affect. I find it is fairly easy to slowly start lowering down my dose over the days following and have it be relatively painless. The key is not to take it for to long and to start lowering down after a few days because it will be built up in your body, which will allow a long slow easy landing. You might have to take it a bit longer than a heroin addict because of opium's long withdrawal but I wouldn't extend it to long and there is still going to be some discomfort.
 
I have been reading about Loperamide for quite a while. I was tempted to use it for heroin withdrawals years ago when I was addicted but didn't happen. I got cocky after 10 years clean of heroin and started using opium and poppy pods regularly about 6 months ago and got myself dependent on it. In comparison to my IV H& C addiction days, my current dependency is miniscule and it hasn't effected my life much, yet.
Hearing that Loperamide works efficiently in much lower doses than what people claim for a person who is on quite serious pain medication and who has decades of opiate dependency experience like you is pretty reassuring. I have to stop my current dependency (about 500mg of opium per day) before I mess my life up seriously. After hearing your experience, I think that I will start by tapering down my consumption then probably will start dosing at 24mg Loperamide in combination with Omeprazole & Hydroxyzine.
The usual addict problem is driving me crazy though, that is when to start. I know the answer which is "today" but I have to push myself to do it before I mess a variety of things up in my life.
Genuine thanks for posting this Nico. I had my doubts prior to this but hearing it from a knowledgable, decades long experienced person who posts only smart and informative threads on BL erased my doubts.

Where is the half-gramme of opium coming from -- is it medicinal so can be assumed to be 50 mg of morphine and I think 15 mg of codeine? From other sources can be higher or lower, as is the case with all derivatives of opium.

There is also the possibility, caeteris paribus, that halving the opium dose and inducting the loperamide with half the dose for the given day, though there is also something to be said about letter early withdrawal start to the extent that one can handle it; anything beyond a few hours into Stage II withdrawal symptoms* and some tolerance is going to be start to wash out too . . .

---
* Quoted at Wikipedia, more or less intact, amongst other places with blessings and encouragement of the authors and editors, this is the Inside Narcotics, 7th Edition (2015) description, even though "Wikipedia has proven itself to not be a good source or destination for our work" per the Editors' Note:

"Cessation of dosing with morphine creates the prototypical opioid withdrawal syndrome, which, unlike that of barbiturates, benzodiazepines, alcohol, or sedative-hypnotics, is not fatal by itself in otherwise healthy people.

Acute morphine withdrawal, along with that of any other opioid, proceeds through a number of stages. Other opioids differ in the intensity and length of each, and weak opioids and mixed agonist-antagonists may have acute withdrawal syndromes that do not reach the highest level. As commonly cited, they are:
  • Stage I, 6 h to 14 h after last dose: Drug craving, anxiety, irritability, perspiration, and mild to moderate dysphoria
  • Stage II, 14 h to 18 h after last dose: Yawning, heavy perspiration, mild depression, lacrimation, crying, headaches, runny nose, dysphoria, also intensification of the above symptoms, "yen sleep" (a waking trance-like state)
  • Stage III, 16 h to 24 h after last dose: Rhinorrhea (runny nose) and increase in other of the above, dilated pupils, piloerection (goose bumps – a purported origin of the phrase, 'cold turkey,' but in fact the phrase originated outside of drug treatment),[43] muscle twitches, hot flashes, cold flashes, aching bones and muscles, loss of appetite, and the beginning of intestinal cramping
  • Stage IV, 24 h to 36 h after last dose: Increase in all of the above including severe cramping and involuntary leg movements ("kicking the habit" also called restless leg syndrome), loose stool, insomnia, elevation of blood pressure, moderate elevation in body temperature, increase in frequency of breathing and tidal volume, tachycardia (elevated pulse), restlessness, nausea
  • Stage V, 36 h to 72 h after last dose: Increase in the above, fetal position, vomiting, free and frequent liquid diarrhea, which sometimes can accelerate the time of passage of food from mouth to out of system, weight loss of 2 kg to 5 kg per 24 h, increased white cell count, and other blood changes
  • Stage VI, after completion of above: Recovery of appetite and normal bowel function, beginning of transition to postacute and chronic symptoms that are mainly psychological, but may also include increased sensitivity to pain, hypertension, colitis or other gastrointestinal afflictions related to motility, and problems with weight control in either direction
In advanced stages of withdrawal, ultrasonographic evidence of pancreatitis has been demonstrated in some patients and is presumably attributed to spasm of the pancreatic sphincter of Oddi
 
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Why does the high and withdrawal form opium or Poppy pods last so much longer? Not related to lope but Ive always wanted to know.
 
Why does the high and withdrawal form opium or Poppy pods last so much longer? Not related to lope but Ive always wanted to know.

It could be properties of the liquid or solid ingested -- like when I was able to use lemon and lime juice in water on poppy pods and get an extract that lasted 21 hours when I drank it with the sludge, and the fact that morphine and codeine are in there, and codeine can actually have some cimetidine-like effects in changing the metabolism of the morphine and the codeine itself . . . those two drugs also have active metabolites, some of which have metabolites; I also have to say I would think that at least some of the thebaine could be turned into something active. Also, the inert portions of the opium and the benzylisoquinoline alkaloids probably have effects on the Liberation, Absorption, Distribution, Metabolism & Elimination profile of the others like the phenanthrene alkaloids and the small amounts from still other groups of alkaloids. I think the extended-release effect that opium products seem to have can also come from the latex, be it concentrated in balls, dissolved in alcohol or water, or washed from seeds and extracted from cell walls, because it is gummy and may not dissolve all at once. It also slows down peristalsis, meaning more time in the stomach, more time in the duodenum and everywhere else . . .
 
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Opium isn't acquired legally or prescribed so the quality isn't always the same.
You equated the amount of morphine to %10 and I thought that it was %20. I know that the percentage can vary but I'm glad that I will have to stop using ~50mg rather than ~100mg. The difference in symptoms and the length of withdrawal would be considerably different with these two amounts.

I think the extended-release effect that opium products seem to have can also come from the latex, be it concentrated in balls, dissolved in alcohol or water, or washed from seeds and extracted from cell walls, because it is gummy and may not dissolve all at once.
This is definitely correct. Sometimes the opium I get is much harder so it takes longer to feel the effects; when I get softer, gum like, easy to dissolve opium, the effects take much less time to manifest.
The shape is important as well. If I want to feel it within 30 minutes, I squish the opium between my fingers so that it's like a thin membrane. On the other hand, if I want to feel it at around 1 hour, I shape it as a sphere.
 
Another potentiator which works very well with 4-phenylpiperidines is promethazine -- I have used it with loperamide, difenoxin, diphenoxylate, and ketobemidone and there is a tablet, syrup, and injectable called Mepergan commonly used which is pethidine plus promethazine. The effect can be added on top of hydroxyzine, which also is noted for the extent of the effect, so much that it is used with pethidine, alphaprodine, piminodine, and anileridine for obstetric and dental analgesia. I think those narcotics are getting plenty rare, of course, as with my last high-impact dental work and oral surgery I had to have levorphanol-nitrous oxide-oxygen anaesthesia the whole way through, which worked even better with a preload of hyoscine/scopolamine, hydroxyzine and dextromethorphan. Before it was dextromoramide straight or anileridine, hyoscine/scopolamine, hydroxyzine, and midazolam . . .
 
Opium isn't acquired legally or prescribed so the quality isn't always the same.
You equated the amount of morphine to %10 and I thought that it was %20. I know that the percentage can vary but I'm glad that I will have to stop using ~50mg rather than ~100mg. The difference in symptoms and the length of withdrawal would be considerably different with these two amounts.


This is definitely correct. Sometimes the opium I get is much harder so it takes longer to feel the effects; when I get softer, gum like, easy to dissolve opium, the effects take much less time to manifest.
The shape is important as well. If I want to feel it within 30 minutes, I squish the opium between my fingers so that it's like a thin membrane. On the other hand, if I want to feel it at around 1 hour, I shape it as a sphere.

I wonder if rolling and cutting or otherwise shaping into a cylinder then using a needle or skewer or the like to poke a hole lengthwise down the centre to get a hollow cylinder like the grain shape for some fuels, firework ingredients and so forth would make for an accelerating long-acting effect
 
I was always curious about the quinidine + loperamide combination...

Loperamide does have a dirty pethidine like high at 80mg+, at 100mg you encounter pronounced miosis and itching...

Dangerous stuff though at those doses...
 
Diphenoxylate and difenoxin have shorter metabolite chains and are less toxic and are 2 and 4 times more potent than loperamide on a milligramme basis though I have heard people say that diphenoxylate is 36 times stronger than loperamide, which are two different things, and difenoxin 50 to 72 times stronger,, in fact difenoxin is what does the work in both cases; the former is the prototype of the group that includes loperamide and the difenoxin and diphenoxylate are stronger and have a stronger piritramide resemblance than loperamide both structurally and in my experience. Manufacturers add 25 μg, ¹⁄₄₀ of the therapeutic dose, of atropine to difenoxin and diphenoxylate tablets to keep people from shooting it and more to keep the FDA off their arse during the approval process. Eating up to 40 tablets may deliver enough atropine to help kill nerve pain, for example, a known clinical use of belladonna alkaloids and anticholinergics, but much more will make one more and more uncomfortable. There used to be morphine, oxycodone, and methadone tablets with atropine in them too -- people would put these on a piece of blotter paper, put a single drop of water on them with an eyedropper or pointed object dipped into water and scrape up and use the tablet, and thereby remove a lot of it that way.

Apparently pure difenoxin is available as Lyspafen somewhere, which was specifically added to US CSA Schedule I, even higher than bulk diphenoxylate's Schedule II and the difenoxin and atropine (Motofen) is Schedule IV and the diphenoxylate equivalent (Lomotil) is Schedule V -- apparently available OTC as an exempt narcotic like codeine cough syrup in some US states like Donnagel PG, which had paregoric and belladonna tincture in it, in boxes of up to 48 tablets or possibly also dropper bottles of some size prior to 1. January 1993, when atropine, hyoscine (scopolamine) and belladonna went on ℞ only, so in the general prescription law and FDA enabling legislation &c at the federal level.
 
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