Opioids Loperamide (Imodium) Megathread v. 2

[Lorne???]

You most certainly are. This ^ post is useless, and the only other post you've made on this forum is unreadable. Take some time and write things using correct grammar (in English...) and dividing up multiple sentences into cohesive thoughts separated into their own paragraphs.

Damnit Lolz know how hard is that big meanie you is¡¡¡

 

[Lorne???]

Damnit, LOLZ, clear your inbox!!!

 

[ParappaTheRapper]

@noone in specific, but

I just ran into doxylamine for opiate wd. I've taken diphenydramine for a year for sleep, but, had no idea there was such a big difference between antihistamines.

Its such a powerful sedative/anti-nausea I'm almost surprised.

I could see loperamide + doxylamine going a long way for knocking out opiate w/d.

 

[southeast]

Ill try this-- I miss sleeping so much. Thanks. Loperamide is a god send I just wish the side effects weren't such shit.

 

[ksralyv2mch]

So my question with is: Is the Tagamet/Omeprazole/etc. necessary to help with opiate withdrawal? Or does it just act like a potentiator, a powerful one at all from what I've read, so like if I didn't have the -dine drug or w.e and I take 40mg would it still work or would it be wiser to take the Tagamet or w.e and a lesser dose of Lope?

sorry about the bad grammar, nodding out... I broke weak again today and picked up BTH when this week I took off from work was to detox... yippy...

 

[Lorne???]

So my question with is: Is the Tagamet/Omeprazole/etc. necessary to help with opiate withdrawal? Or does it just act like a potentiator, a powerful one at all from what I've read, so like if I didn't have the -dine drug or w.e and I take 40mg would it still work or would it be wiser to take the Tagamet or w.e and a lesser dose of Lope?

sorry about the bad grammar, nodding out... I broke weak again today and picked up BTH when this week I took off from work was to detox... yippy...

Yes, it is much better with cimetidine, you can reduce your dose significantly.

CYP3A4/PPG inhibitors(like cimetidineWGJ) dramatically increase the BA of loperamide, and if used correctly allow you to take a fraction if the dose.

Will it word without? For me personally, I've never gotten full WD relief(and the minor CNS effects that come with that) without high dose inhibitors. However I am extra sensitive to the intestinal effects of loperamide(and all other opioids).

But I think it's clear at this point it works without inhibitors, however larger doses are needed.

As for the cimetidine, start with 4-5 tablets(800-1'000mg). Take 600-800 the next day. Wait at least 30 minutes after taking the cimetidine to take the loperamide. Start slow. And remember, it literally takes 3-4 hours to feel the full effects from loperamide. I wouldn't take more than 40mg initially, wait a few hours, you can then take another 10-20mg if you need it, and another 10mg every 4 hours. Once you achieve WD relief however, do NOT take anymore; it will relieve WD, but you CANNOT catch any buzz or high(at least not safely).

Seriously though, start slow, lope has some weird side effects if you get too much into systemic circulation.

I wish you luck, and if you tell us your tolerance, we can suggest a starting dose.

(BTW, stick with cimetidine, it is much more effective. Actually, I'm not at all sure if omeprazole is a practical inhibitor).

 

[ksralyv2mch]

Yes, it is much better with cimetidine, you can reduce your dose significantly.

CYP3A4/PPG inhibitors(like cimetidineWGJ) dramatically increase the BA of loperamide, and if used correctly allow you to take a fraction if the dose.

Will it word without? For me personally, I've never gotten full WD relief(and the minor CNS effects that come with that) without high dose inhibitors. However I am extra sensitive to the intestinal effects of loperamide(and all other opioids).

But I think it's clear at this point it works without inhibitors, however larger doses are needed.

As for the cimetidine, start with 4-5 tablets(800-1'000mg). Take 600-800 the next day. Wait at least 30 minutes after taking the cimetidine to take the loperamide. Start slow. And remember, it literally takes 3-4 hours to feel the full effects from loperamide. I wouldn't take more than 40mg initially, wait a few hours, you can then take another 10-20mg if you need it, and another 10mg every 4 hours. Once you achieve WD relief however, do NOT take anymore; it will relieve WD, but you CANNOT catch any buzz or high(at least not safely).

Seriously though, start slow, lope has some weird side effects if you get too much into systemic circulation.

I wish you luck, and if you tell us your tolerance, we can suggest a starting dose.

(BTW, stick with cimetidine, it is much more effective. Actually, I'm not at all sure if omeprazole is a practical inhibitor).

THANK YOU FOR THE SPEEDY RESPONSE!

Yes, I've never done it with the cimetidine and I've only read of others using drugs in the same class (acid reduces or something I believe... too lazy to research. I have been smoking .5 grams of black tar heroin a day for the past 2 1/2 weeks, I know it's not that long of a run but prior to this run's start I used .75 grams of tar a day for 2 months and only having 2 weeks inbetween when I stopped from the 2 months and when this current 2 1/2 week run started.

But the last two days have been a struggle and yesterday I went 24+ hours before only smoking .15 grams the whole day. then today I went 24 hours exactly before I was able to pick up and I only used about .2 so far (if that) I still have .8 grams left but I'm trying to taper down before I switch to lope (my other thread about me needing heroin tapering advice: http://www.bluelight.org/vb/threads/727181-I-need-advice-on-a-proper-heroin-taper)

I have taken lope before without the cime at high doses for what I thought my tolerance was (.5 grams of tar and I Was taking 40mg of lope) I think it helped... but I still had that craving and the psychosis of my skepticism made me still feel weird so I was starting a lope taper in the morning but ended up using by night fall... so IDK if it worked but it fucked my stomach up pretty nice lol.

TL;DR: My usual dose is .5 grams of (decent) tar, smoked a day. Past two days I have used less than usual and I have .8 grams of tar left. What would you recommend a good starting point would be? And would it be smart to like take the lope the night before you get sick so that you can kind of get a head start on it? Like I know everyone says titerate (sp?) you dose but what if you just start at like 10-20mg the night before with some cime then the next morning when you're not feeling so hot (or if you're okay and it's been 24 hours since your last use and you know you should be sick but you aren't, then mission achieved!) take some more "titerate" till you feel fine. Would that not be a less painful way?

my tl:dr is an oxymoron

 

[Lorne???]

Hmm... Your habit is from a very short term use
. Be careful with loperamide, it will extend WD, if you use it too long.

Yes, taking the night before with cimetidine is a great idea. I would take 24mg tonight, with 800mg cimetidine. Tommorow, take another 24-32mg, again with 800mg cimetidine. Wait 3-4h, and if need be, take another 16mg.

Only start it tonight if you are 100% sure you're not using dope tommorow. Actually, you could just take 16mg tonight. Be careful, loperamide has fucked my stomach up badly; I would stock up on laxatives.

So 16mg tonight, 32mg tommorow, 800mg cimetidine with each.(you can take 600mg tommorow if the H2 antagonism is to severe).

Sound good? ��

And I try to check frequently, to ensure people get fast replies, to intelligent questions, especially.

 

[ksralyv2mch]

Well I still have .8 grams of dope left and I want to use that to taper as much as possible before jumping off into a QUICK lope taper (like once I find what my dose is I plan on taking lope every other day and dropping 2mg as I do. Example: Monday 20mg of lope, Wednesday 18mg of lope etc etc, or would it be better to take daily???)

anyway if you could hit up my other thread (idk if you used heroin at all) but maybe you can help me with a proper heroin taper

also would ranitidine or famotidine work? they are in the same class of drugs as cimetidine....

 

[Lorne???]

No, only cimetidine is a PPG/CYP3A4 inhibitor. The only other one you could possibly use would be omeprazole, BUT it is so mild, I am not sure if it's possible, let alone practical.

I lurv me some heroin However, I exclusively IV it(and always have). I also use powder heroin, and mainly white, which is quite potent. I could give it a shot though.

With loperamide, I'd load it into you're system the first 48 hours, then go every 36h, and then every 48 hours, while progressively lowering you're dose. LOLZ is good at loperamide tapers, if you're lucky he'll pop in.

But once you find an effective dose of lope, post it here/PM me and I'll make up a plan.

As for the tar, I'll check you're other thread, but 800mg isn't much to taper from.

 

[ksralyv2mch]

Well I have access to 2 other grams but I'd rather not touch that if necessary. and I'd totally be doing the slam dance with ol' Mr Brownstone it's just so hard to get points out here where I live. No system of harm reduction cause we are a stupid hardcore RED state with an obnoxious loud mouth bigot sheriff.

 

[Lorne???]

What state? I also live in a red state(the south) but ultimately if it's legal in your state, someone will sell them to you.<br><br>It would be better too taper from 2g, however I know I don't have the self control to taper from H  <br><br>I think you're best bet is to just enjoy you're 800mg, save a point or 2 to do later, then switch to loperamide. You've already dropped you're dose the last 2 days, you should be able to transition to lope fairly comfortably.

(make sure you save a bit though, you don't want to do a big dose of dope one night, then immediately have to start loperamide!!!

 

[Lorne???]

And don't worry about my message, I get the idea mr brownstone

 

[Lorne???]

This demonstrates how dangerous trying to catch a buzz from loperamide can be:

http://www.ncbi.nlm.nih.gov/m/pubmed/25231/

According to this study, the ED50 for analgesia, when loperamide was given orally to rats, was 149mg/kg. However, the LD50 was only 250mg/kg. That gives it a terrible therapeutic index(TI). To out that into perspective, 100mg IV might give someone analgesia, but 200mg would kill them. The effective dose(for analgesia and thus significant CNS effects) is 50% of the lethal dose.

Of course, this was a study with rats, and they didn't use CYP3A4/PPG inhibitors, but nonetheless it demonstrates an alarmingly low TI. It also demonstrates that loperamide has typical CNS effects at obscenely high doses.(150mg/kg would be over 7'000mg for me, though it clearly takes far less in humans)

 

[ksralyv2mch]

What state? I also live in a red state(the south) but ultimately if it's legal in your state, someone will sell them to you.<br><br>It would be better too taper from 2g, however I know I don't have the self control to taper from H <br><br>I think you're best bet is to just enjoy you're 800mg, save a point or 2 to do later, then switch to loperamide. You've already dropped you're dose the last 2 days, you should be able to transition to lope fairly comfortably.

(make sure you save a bit though, you don't want to do a big dose of dope one night, then immediately have to start loperamide!!!

I live in AZ. So the tar is cheap and in a huge abundance. You are right I should just switch over to the lope, I gotta go to the store and I'm still sitting here with like 2 grams of heroin... I want to taper down as much as possible before jumping off to lope. I believe I can taper cause I'm under heavy surveillance by my ex-gf and parents (who I live with) so my useage is very limited on when I can use, kind of forcing me to taper, but I digress...

So the last night before I jump off I plan on taking 1 grams of Cimetidine with 20 mgs of lope then the next morning (which will hopefully be 18hrs from my last use of heroin) I will see how I feel and if I need more I'll titerate by doses of 4 mg, sound good? How often should I take the cimetidine??

 

[Lorne???]

You can go ahead and take another 20mg the next time(to load your system) then titrate up by 4-8mg at a time, keeping in mind it can take hours for lope to reach full effect.

Load the cimetidine up initially, we're talking 2 grams the first 2 days, the half a gram a day should be fine. Good luck and feel free to ask any lope questions here.

(

 

[Lorne???]

http://www.ncbi.nlm.nih.gov/m/pubmed/7438696/?i=2&from=/7371363/related




Demonstrates that 60mg of loperamide, by itself produced no miosis, yet 120mg of codeine did.

I myself have taken over 100mg by itself, and it did not at all effect my dilated pupils(my pupils become fucking huge during WD) and had no meaningful effects whatsoever, except intestinal/stomach effects.

Yet 50-60mg with large doses of multiple CYP3A4/PPG inhibitors gives me pin-point pupils and complete WD relief.

The simple fact is that if you want CNS effects from loperamide(and therefore full WD relief) you MUST USE CYP3A4/PPG inhibitors. There are multiple reasons for this:

First off, the oral bioavailability of loperamide is simply to low to use by itself. Even in large doses, only a small portion reaches the blood stream. Yet potent inhibitors have been shown to increase bioavailability by up to 500%. Also, PPG inhibitors can help to allow more loperamide to enter the CNS. Loperamide on it's own can, and does cross the BBB, but only does so poorly. Combined with it's insanely low BA(at therapeutic doses, IE 2-4mg, it's around 1%) make it impractical to take by itself, but with a large enough dose of inhibitors, it can be used, all it is still PM'S selective, and it's atypical side-effects make it unsuitable for the opioid naive, and indeed anyone not addicted. However an opioid dependent person can destroy WD symptoms, using loperamide, with 2 OTC products, which are potent CYP3A4 and mild PPG inhibitors.

This drug is still almost "unabusable", however, do again to AE's, including prolonged QT interval at high doses.
But inhibitors transform lope into an atypical opioid with CNS effects, that can be used, cautiously in WD.

 

[ksralyv2mch]

So if cimetidine is the CYP3A4 inhibitor... what is classified as a PPG inhibitor????

EDIT: cimetidine is both, right?

 

[russiankush]

Due to loperamide's high innefficiency for crossing the blood-brain barrier, could mannitol be used in order to facilitate the crossing better? I was reading on Wikipedia that mannitol shrinks the endothelial cells in the arteries, and is used to facilitate the crossing of pharmaceuticals. After intravenous administration of mannitol, the cells shrunk to the minimum after five minutes and stayed this way for thirty minutes. As mannitol is very cheaply available, maybe it could be used to help loperamide cross the blood brain barrier better? Also, possibly it could be administered via insufflation instead of intravenously, in order to create this effect? I was thinking, possibly on an empty stomach, in conjunction with all of the other CYP3A4 and PPG inhibitors, the standard dose of loperamide could be taken after insufflation or injection of mannitol, and possibly this could greatly increase the analgesic effects.

 

[ParappaTheRapper]

Can anyone explain to me why tonic water should not help with loperamide?

I've seen this in several threads.