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Questions and Info about loperamide

As he's on probation, I guess any illegal substances are out of question. But substitution (or one of those exceptional doctors who could prescribe you hard opioids for 'pain' ... actually, what he describes sounds like fuckin' real pain to me. Just depends on the point of view.)? Or if really nothing else is possible, tianeptine (from anecdotal reports it seems to be exceptionally safe even in insane doses, and possibly has a greatly reduced potential to depress respiration) or even U-47700?
 
615 is the ratio between stomach opiate activity & central opiate activity. US 3714159 has a table on page 4. just look down the rightmost column to find 615; that's loperamide.

I strongly advise people not to use loperamide. You are using up the bodies glycoprotein which is there to remove unwanted stuff inside the BBB. By overloading it, other compounds may have increased toxicity. I've come across several 'near misses' with people awaking in hospital 3 days later. Even with the -Cl removed, the ratio is still a massive 300 (OK, x10 potency - but that's about codeine. This is far from a safe drug when taken at 'Heroic Doses' and it won't belong before a fatal.
 
clubcard said:
615 is the ratio between stomach opiate activity & central opiate activity. US 3714159 has a table on page 4. just look down the rightmost column to find 615; that's loperamide.

I strongly advise people not to use loperamide. You are using up the bodies glycoprotein which is there to remove unwanted stuff inside the BBB. By overloading it, other compounds may have increased toxicity. I've come across several 'near misses' with people awaking in hospital 3 days later. Even with the -Cl removed, the ratio is still a massive 300 (OK, x10 potency - but that's about codeine. This is far from a safe drug when taken at 'Heroic Doses' and it won't belong before a fatal.
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De-chloro-nation (that a "chemistry" word?) potentiates loperamide ten fold?
 
So, more interested in spelling than bothering to look at the patent which I gave you. 2 Kinds o people in the world - those who look for problems and those who look for answers. Pretty clear from your petty attitude which you are.
 
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clubcard said:
So, more interested in spelling than bothering to look at the patent which I gave you. 2 Kinds o people in the world - those who look for problems and those who look for answers. Pretty clear from your petty attitude which you are.
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I have limited time online and other things to do. I don't have a connection, I come to the library. I have no clue what you are talking about concerning "spelling" either.
 
Look, put simply, if your taking enough for it to have a mental effect, you are using up the bodies resources to remove it and other nasties from brain. The dose/response isn't linear (you reach a point where the Dose/response curve suddenly takes a sharp left meaning that your body can't pump it out so much smaller increases will have a much greater effect). It's quite apparent that people are getting addicted to it, but for chronic toxicity, nobody knows but the signs are BAD.

I know it causes compartment syndrome in all 4 limbs and even the head.

I bet we are a decade before the abuse comes to light and professionals study it BUT when they do, I will offer 10/1 odds on that it's damaging the brain.

It's also a slightly freaky habit - I'm sure a single vicoprofen would have more effect.
 
i'm glad you said this - i'm about 10 days of Loperamide ( 400 mg every other day for 5 months! ) and the first few days felt like a typical opiate withdrawal but around 5-6 days, i started having weird withdrawal symptoms, i was experiencing the withdrawals i had from BENZO's years before!

the extreme mood swings, panic attacks waking me up at night, weird cold and hot/tingling sensations in the face/arms

i wen't to the E.R to make sure i wasn't dying, Chest xrays,ct/mri of chest/lungs, ECG, blood work, ultrasound of my legs/arms for blood clots and everything came back good, except i had acute gastritis ( which makes sense, due to my digestion system probably had to retrain itself with months of loperamide )

anywho, this shit is bad, and it breaks my heart seeing people on a daily on this website take heroic dose after another, even with the known dangers :(
 
clubcard said:
615 is the ratio between stomach opiate activity & central opiate activity. US 3714159 has a table on page 4. just look down the rightmost column to find 615; that's loperamide.

I strongly advise people not to use loperamide. You are using up the bodies glycoprotein which is there to remove unwanted stuff inside the BBB. By overloading it, other compounds may have increased toxicity. I've come across several 'near misses' with people awaking in hospital 3 days later. Even with the -Cl removed, the ratio is still a massive 300 (OK, x10 potency - but that's about codeine. This is far from a safe drug when taken at 'Heroic Doses' and it won't belong before a fatal.
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This is the chart you mean, right cc?

don't know why my number dyslexic (dysnumeric?) brain puts in 200 (mg, my daily habit; one hundred two milligram tablets) divide by 615% and get 32.5203252033 and double it by affinity to morphine and guess roughly 65mg a day pure morphine habit is what my lope habit approximates? or am I doing something way off kilter in my estimation and mathematical bumbling?
 
I can attest to the lope eye thing like standing in a rocking boat. It happened when I'd redose before it had cleared my system. I kept it in the 48-240mg range but built tolerance quickly and got minimal to no effects at doses less than 120mg in just a matter of weeks. Wd super sucked and the panic really dose reach "I gotta call an ambulance" levels. And bicycle pedaling all night. That and the sleeplessness and crying spells go on for what feels like an eternity. I ate maybe one meal every two days but couldn't finish my plate. That was after tapering off at slow, reasonable pace. It works when you need it to but it's a hard, hard price to pay. Worst dopesickness I ever had was from lope. Oh and difficulty swallowing was another side effect at high doses that hasn't been mentioned yet. Freaky feeling. I'm curious to know if anyone got that. Any opioid/opiate can constipate. For me it wasn't as bad as fentanyl.
 
Off topic, but Raysu so you get that fear, mental pain, panic and crying too from withdrawing or specially to loperamide?

Because usually and all over things like being sick, vomiting, diarrhea, hot and cold are mentioned but few at all talk about the pain of mind. The physical symptoms can be alleviated with medication, yet remains the emotional side.

So I'm wondering if many people really don't get that intense panic, pain and regret or just don't talk about?
 
Coming off lope was like my usual wd times ten. As nauseated as I could be coming off other opiates/opioids/benzos I didn't puke till this last one and the lope was the last thing I did for a few days but I'd take it on and off for months and this was my first gap with nada. Panic I've had before but it would be here and there not most of my waking hours like this time. Didn't cry before either just depressed but this level of depression was borderline unsafe. That went on for about a week and a half before starting to lift. I was so tempted to say screw it and start back up but this round had me worried that it would be worse if I did. The general feeling of being uncomfortable in my own skin still persists and the inability to sleep despite feeling tired and the restless legs. It's slow going but if I compare how I am to the weeks prior it's a little better overall. Most days drag on forever and feel the same so I just have to remind myself of each little things that's improved to have hope till I'm back to normal. As far as when I was using the panic set in when I'd go days back to back or boost the same day. But it would come and go and seemed to be worse in the mornings. So it is a different kinda drug for me but I can say the one effect it had that no other drug provided is it really diminished the obsession to use when I first started it. Like I could take a moderate dose and go about the rest of my day and night and morning before realizing I didn't have a craving. Kinda like after a good meal your brain stops thinking about food. I just stopped thinking about using for extended periods of time. Every other drug I did uppers and downers both left me wanting more and what I had was never enough to satisfy me beyond the rush. I could be too high to function and fantasize about doing more.
 
Nagelfar said:
This is the chart you mean, right cc?

don't know why my number dyslexic (dysnumeric?) brain puts in 200 (mg, my daily habit; one hundred two milligram tablets) divide by 615% and get 32.5203252033 and double it by affinity to morphine and guess roughly 65mg a day pure morphine habit is what my lope habit approximates? or am I doing something way off kilter in my estimation and mathematical bumbling?
Click to expand...

Right page. Delta receptors are also involved in morphine. I don't know where that calculation comes from but plasma levels ar no guide. The -OH is ripe for gluconation but it's high cLogP means it hides out in fat cells. Since only the brain has the appropriate removal tools - hence compartment syndrome. People think 200 to 250 might be OK, but that's the levels of the near-misses. Depending on gender, BMI & overall mass will dictate distribution, but vicoprofen is simple. Ibuprofen is totally insoluble in water - so you make hydrocodone solution. I suspect the phenol of paracetamol may be amiable to calcium oxide to crash it out, so DHC or codeine solution is possible. If you have a pepsi habit like hydrocodone - rattle. You only get out what you put in. Note - sleeping is the thing that cracks people rattling but even quite a small dose of the opiate will allow sleep. Then comes the depressions. Tricyclics are best (promote sleep, alxiolytic and cheap). You really need to talk to a doctor. I can design a damned molecule, but I lack 99% of the skills & 100% of the experience of a general practitioner.

But trust me on the loperamide - too few good people in the world, we need you all.
 
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clubcard said:
But trust me on the loperamide - too few good people in the world, we need you all.
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I appreciate the worry, but as is, I've been on 200mg (100 tablets) a day since mid-'14 (two years), every day, and haven't been without it for more than three days at any time in the bulk of that period (except for a stint where two bags of heroin replaced it; didn't have the legs, but the WDs were at bay); and day three cold turkey was hell. The fact that its legal without a perscription, and doesn't show up on a U/A, and it gives me pretty much all opioid effects of a bag a day heroin habit excepting that it's a cleaner, and longer lasting, smoother-feeling form of maintenance. With tolerance none of the negative, 'blurry vision', or even constipation, effects are an issue. I've got (perhaps to their detriment) several others hooked on it. I want to try and taper, but in the meantime that doesn't look forthcoming, no primary care physician, and even the EMT that picked me up when I OD'd on 1,250mg/1.2g didn't, believe me or seem to care. When I was on dept. of corrections supervision my parole officer said "it's non-narcotic" and didn't seem to care. And I certainly don't feel a toxic "body load" or et cetera (not that one would, I'm just saying it is all subjectively positive and no negative that I'm experiencing, I'm not saying that is wise, but more valuable souls than myself have been taken down by their vices of choice with educated knowledge of the risks)
 
^ I'm curious: do you still get opioid effects from the loperamide or is your continued use purely a form of maintenance? Have you ever experienced any tremor or other motor symptoms?
 
I would be careful. Even if its a tiny %, if the tertiary -OH is dehydrated then you might end up with something carrying a charge so it can't exit the brain. Nobody is going to start monotoming rat-brains to check this out, but it could be a slower version of 'the case of the frozen addicts' or it could form irreversable bonds to the opioid receptors.... and I have no idea if that is good or bad. Generally, it's bad.
 
serotonin2A said:
^ I'm curious: do you still get opioid effects from the loperamide or is your continued use purely a form of maintenance? Have you ever experienced any tremor or other motor symptoms?
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Three people besides myself who have used 200mg (100 tablets; DON'T use liquid or gel-caps) at once have said they were amazed at how high they felt and have become hooked. Yes upon OD'ing I had walking issues; like my abdominal muscles failing after carrying a very heavy load and I bent at a right angle and couldn't stand straight like as if ones muscles just give out from over use. This was only when I OD'd from too much for my tolerance (I once had to be narcan'd over the course of 6-12 hours five separate but contingent occasions on one hospital visit with no other opioid in my system)

clubcard said:
I would be careful. Even if its a tiny %, if the tertiary -OH is dehydrated then you might end up with something carrying a charge so it can't exit the brain. Nobody is going to start monotoming rat-brains to check this out, but it could be a slower version of 'the case of the frozen addicts' or it could form irreversable bonds to the opioid receptors.... and I have no idea if that is good or bad. Generally, it's bad.
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Very interesting, do you have more on this possibility and its mechanics, cc? or how a drug could do this at all? The opposite of a BBB-type drug, do all p-glycoprotein substrates have this tendency to possibly reverse their mechanism in this way?
 
Good find - well, that's 1 relief. I know that similar drugs 'peripheral opioid agonists' were produced & tested. That Janssen made SO MANY compounds and found the minimal central activity (mostly due to the -Cl) was the follow on to diphenoxylate which WAS habit-forming in spite of lacking any analgesic effects. I think HE was amazed that it was abused and so went 1 step further. How does the cost of 100+ loperamide stack up against, say, 2 vicoprofen a day? I know the latter is illegal, but I'm purely viewing this in a safety light. I've heard of several near-misses so it's more or less certain that someone is going to get themselves hurt.... I HOPE not, but it does worry me.
 
Lope is half the price and last four times as long. It's a dirty high and kinda subtle but it's a definite and it's legal. Online is even more cost effective but it's a wicked comedown if it's taken long term.
 
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