Loperamide and MPTP dangers

[paranoid android]

Paranoid android-isn't the mechanism of action of the toxic muck resulting from propoxyphene administration (not to imply however that the drug itself is not toxic muck, it is, its both toxic and an utterly, utterly garbage excuse for an opioid. Had it only once, and that was only because I happened to come across a box of the stuff whilst liberating a bunch of copper pipe and lead scrap from a skip, somebody had thrown out the box of D-propoxyphene. On trying it, because I was withdrawing at the time, I realized WHY they must have done so

Had I known from subjective experience, and had I also not being in opioid withdrawal at the time, I'd probably have returned it to the place from whence it came, for a dumpster is where indeed it is most in its rightful place

Yeah (Dextro)Propoxyphene itself and Norpropoxyphene are toxic. Both are potent local anesthetics which is what makes Darvon so cardiotoxic. Norpropoxyphene is a even stronger sodium channel blocking local anesthetic then Lidocaine so it's no wonder that when it builds up or Propoxyphene is taken in large doses that cardiotoxicity and grand mal seizures are prominent signs of toxicity. Both Propoxyphene and Norpropoxyphene have a Quinidine like effect on the heart so yeah really this toxic goop is just bad news and i was thankful when it was removed from the market. Not to mention Propoxyphene along with it's unique toxic effects and qualities not reversed by Naloxone it's known for causing severe respiratory depression compared to other Opioids despite being a really weak Opioid. Combine these effects with it's fast onset of action and that's why it was so popular as a way to off yourself. Though it would be a horrible death consisting of cardiac problems and grand mal seizures until you died of cardiac arrest or respiratory depression.

I have taken propoxyphene only once and it was in the form of those godforsaken Darvon-N capsules. Ugh i will never forget what they look like as long as i fucking live i swear . A stupid doctor who has a habit of prescribing useless and dangerous pills such as Darvon-N and Ketorolac (brand name Toradol a nasty NSAID that is only supposed to be taken when all else fails and then only for a maximum of 3 days) like candy. I would have been satisfied with some lousey Tylenol#3's as i was getting tension headaches but he said that Codeine was addictive but Darvon was not . I knew this was bullshit as i looked it up in a old medical textbook i had and it was called a Opioid that had about half the Analgesic effect of Codeine (actually 65mg's of Propoxyphene hydrochloride and 100mg's of Propoxyphene Napsylate have less Analgesic activity then 500mg's of Acetaminophen or 325mg's of Aspirin) and was habit forming. I knew he was a bullshitter but i took 2 of the pills anyway plus i read that it was chemically related to Methadone s i figured it was worth a shot. Just 2 fucking pills like it said to take on the goddamn bottle. I ended up throwing up so hard that i busted blood vessels in my face from projectile vomiting so fucking hard .

From only 2 fucking pills! I don't know of any other Opiate that would make me feel sick at only 2 pills. Even the real high dose and rare 200mg Morphine SR's and 30mg Hydromorph Contin's wouldn't make me feel sick if i only took 2 of them. Though i had little tolerance at the time compared to now as the strongest Opioid i had taken alot of was Oxycodone. Basically Codeine, Percs, Oxy IR's and Demerol was as strong as i went back then. But i have never felt as sick off another Opioid as i did off those 2 Darvon pills. I threw up things i had forgotten i ate ffs and i was going around with blood vessels busted in my face for like a fucking week. Not to mention the Darvon gave me one of the most dreadful sleeps i have ever had complete with night terrors. It also gave me RLS if i remember right and how the fuck can a Opioid cause restless leg syndrome? what a toxic pile of shit. You could not get me to take Darvon again no matter how dopesick i was. I wouldn't take it for a million bucks or a bottle of Hydromorph Contin 30's. I won't take Tramadol either as it given me Migraine like headaches. Also as i have Bipolar i seem to react badly to any SNRI so Tramadol is out. I have yet to try Tapentadol but i am not too keen on finding out if i will also get a bad reaction from that. It's basically Tramadol with stronger Mu Opioid and Norepinephrine reuptake inhibitor effects so it does not sound appealing to me.

 

[Nagelfar]

Anybody notice this New York Times Article from last month? They get their info from Bluelight and mention the site by name:

The New York Times: Addicts Who Can’t Find Painkillers Turn to Anti-Diarrhea Drugs. By Catherine St. Louis. May 10, 2016

 

[paranoid android]

The active ingredient, loperamide, offers a cheap high if it is consumed in extraordinary amounts. But in addition to being uncomfortably constipating, it can be toxic, even deadly, to the heart.

WTF? Do people actually take Loperamide to get high? I thought people where just taking fuckloads of it while in withdrawal because they mistakenly believe that taking huge doses of Loperamide will somehow relieve other symptoms of Opioid withdrawal besides Diarrhea. Hell i didn't even find it to help stomach cramps and high doses (for me this is over 8mg's) make me constipated (i find it far worse then even Codeine in causing this side effect), makes the stomach cramps worse and increases nausea. None of which are desirable effects especially when i am already in Opiate withdrawal. If people are trying to get high off this shit (or shit blocker in this case) it certainly wouldn't be a cheap high as the giant packets of Loperamide are not cheap and the syrup is still rather expensive. If someone where to say take 40 fucking mg's of the stuff that's 20 of those not to small pills. I couldn't imagine trying to get 20 of those fucking pills down in me and that alone would be enough to cause intense nausea.

I can't see this being a problem in Canada as you can get OTC Codeine which even though it's a relatively weak Opiate atleast produces a high and is not Cardiotoxic. It's also cheaper to get a bottle of 100 AC&C's aka Aspirin with Codeine or Acetaminophen with Codeine then it is to get a giant packet of Loperamide or a bottle of the syrup. So there's no economic incentive to buy it here either. Abusing Loperamide to try and catch a high makes no fucking sense to me. Atleast the other common anti-diarrhea drug Diphenoxylate (the Opioid in Lomotil) has CNS effects as it crosses the blood brain barrier granted not very well so abusing that atleast makes some sense.

 

[N0 W4RN1NG]

^^^ I hate to break it to you, but a lot of your above post is misinformation.

Loperamide is extremely cheap, firstly. The "dollar stores" in USA sell 24mg (12 count, 2mg pills) for $1USD.

And that's just if you buy one box, not bulk pricing. If you go to amazon, you can get around 480mg of loperamide for less than $5USD.

Also, Loperamide does cross the blood brain barrier. Not efficiently, but yes, it does.

Why does it pin your pupils, cause bradycardia and severely decreased respiration, and take away craving for other opioids, if it only works on PNS opioid receptors? I implore you to read the entire thread again.

Just as a footnote, I recently had to sell my remaining suboxone for cash. I didn't take it for two days in a row and I was sick as a dog.

I went to a grocery store on the 3rd day, bought a 2L bottle of white grapefruit juice from concentrate(potent CYP3A4 inhibitor).

Drank the entire thing and took 40mg omeprazole(pGP inhibitor). Added in 60mg Dextromethorphan(NMDA antagonist pro drug, commonly used to increase or "potentiate" suboptimal doses of opioid), and 50mg diphenhydramine(greatly reduces some common opioid side effects, such as nausea, itching, etc).

After around a half hour, I then took 48mg of Loperamide HCl.

Around 2 hours after ingesting the loperamide, I began to feel a wave of relief passing over me. My body aches and nausea had subsided. I was actually hungry. My pupils were PINNED. I had a stomach ache but it was probably from drinking all that grapefruit juice.

My heart rate was decreased by around 40BPM. Keep in mind, my resting heart rate was much more elevated than usual, before taking the loperamide, due to withdrawal. It was around 120BPM. 3 hours after loperamide, 80BPM.

For those few days of withdrawal from Suboxone, I couldn't enjoy anything. Every idea I came up with to distract myself ended up being either irritating or boring.

After the loperamide kicked in, I found myself very relaxed and sedated, and getting really into a JRPG I was playing on a SNES emulator. I love playing this game normally, but for the few days without suboxone it was actually completely uninteresting and I had no desire to play it.

I have used loperamide for withdrawals before but usually at much higher dosage, around 120mg.

With the potentiation combo I just mentioned, I felt very pronounced effects from only 48mg.

This is coming from someone who used to take 320mg oxycodone a day. (Albeit, many years ago) and has been on 4mg suboxone (lower doses, 2-4mg of buprenorphine, work much better for me than doses of 8mg+) for many, many years.

Studies in humans have proved that loperamide, when coadministered with a pGP inhibitor, causes respiratory depression.

No offense, seriously, but please read through the thread before you post - you are asking for a "QED"

EDIT: The pills are usually not big, at all. They are usually quite tiny, light green oval shaped tablets, each smaller than a baby aspirin. I took the 48mg (24 pills) in one gulp with milk.

Also, diphenoxylate is not OTC, and loperamide is. In USA codeine is not available OTC. (Technically it is, in some states, in some pharmacies, available without a prescription as a "behind the counter" medication, KIND OF similar to how pseudoephedrine products are stored. But the codeine available this way is never sold in large amounts, is always distributed as a combination product in syrup form, and is very expensive. Which makes extraction a lengthy process, and the whole thing is completely impractical for anything except a novelty experiment)

Even in Canada, codeine OTC products are more expensive than loperamide off Amazon. Also, codeine has a rather low ceiling. I was affected much more from the 48mg Loperamide(with said potentiation combo) than I would have been from 300mg codeine.

All medicines used in the afore mentioned combination were easily acquired for a combined total of about $8 USD. That is cheaper than suboxone IME. The grapefruit juice and omeprazole were purchased from a grocery store, everything else was from a dollar store.

EDIT2: I also had been taking diphenhydramine every day during the suboxone withdrawal to attempt to alleviate withdrawal nausea and lack of appetite. It helped to an extent by itself, but there is simply no way that all the relief I experienced after trying this combination could be attributed to just the diphenhydramine.

In addition, I was having SEVERE insomnia issues during the buprenorphine withdrawal. I slept like a baby after the loperamide, for a solid 10 hours. Woke up feeling really well rested! I also was much less sweaty and had no shivers.

 

[paranoid android]

^ Loperamide did not pin my pupils when in withdrawal or take away any of the withdrawal effects besides the shits. Not even the stomach cramps where helped by it granted my Dicycloverine script covers that. Also Loperamide does not cross the BBB in medical or above medical doses like diphenoxylate does. And yes i know it's not OTC but i used it as a example. Loperamide only seems to cross the BBB in doses strong enough to have any CNS effect when taken in huge amounts that are fucking insane from a health point of view. Also here in Canada at most drug store OTC Codeine is cheaper then generic Loperamide. A bottle of APAP with Codeine costs $6 for 100 pills at my local pharmacy while a pack of about 25 generic Loperamide runs roughly the same cost. So i think in this case Codeine wins out economically.

Taking 40 something mg's of fucking Loperamide just seems insane to me. Also unless you are getting another type of tablet like say sublingual ones they are only slightly smaller then a 325mg Tylenol caplet which is not small at all. As someone who suffers from IBS i would say i have had most generic brands of Loperamide out there. 4mg's with my Morphine dose does help my IBS when it get's really bad hence why i always have Loperamide around the house.

 

[N0 W4RN1NG]

^^^I said, if you remember, that the price of loperamide *specifically* on AMAZON was cheaper than OTC codeine. Also, do not forget, the acetaminophen/codeine pills contain, what, 8mg codeine each? So for $6 you get 800mg codeine. This is, for an opioid dependant person, TWO doses, at best. And even if you are doing CWEs a bit of APAP always comes through. Taking codeine (via the method one would be forced to use if OTC products were the source of codeine) every day for opioid dependence management would certainly eventually have a deleterious effect on the hepatic systems. (And, ignoring the health risks of continued exposure to potentially high levels of APAP, From a purely economical perspective: compare $6/800mg codeine to [≤$1]/24mg loperamide...)

I do not suggest that loperamide maintenance is without fault - but it is still my firm opinion that it is cheaper, easier, and less dangerous (especially when taken with a CYP3A4 inhibitor {like the grapefruit} to prevent LPP+ production in vivo) than a CWE OTC codeine long term "treatment".

Loperamide also lasts significantly longer than codeine. An opioid dependant person will have to take codeine multiple times a day, in divided doses, in order to keep WDs at bay.

Also, you say in the beginning of your post, that loperamide does not cross the BBB, but then a paragraph later, admit that it DOES cross the BBB in higher than clinically recommended doses...this is exactly what I was stating...of course loperamide does not have CNS effects at the recommended doses and slightly higher. I don't think any one in this thread was suggesting that it did.

In addition, if you think 48mg of loperamide is a lot, I want to remind you that Nagelfar has posted many times here, that he has been taking 200mg loperamide/day for two years now.

I am not suggesting that this is a good idea, or that it is healthy, but clearly it is not as insane as you seem to think...again, it makes me suspect you have not read this thread in it's entirety.

Finally, I feel I should mention I experienced no constipation at all from 48mg loperamide.

EDIT: I am not from Canada, but I assure you, the generic Loperamide 2mg pills we have in USA at the dollar stores, and the ones you get 240 pills of on Amazon for dirt cheap, are TINY PILLS. They are not sublingual. I can fit 5 pills on my thumb nail.

EDIT2: You say loperamide did not pin your pupils during withdrawal, but then go on to state that 40mg is a "fucking insane" dose...the thing is, 40mg (without potentiation methods) isn't really even a threshold dose to keep WDs away.

So I'm assuming your attempts to stave off withdrawals involved significantly less than 40mg loperamide. Therefore, it is no surprise that it did not work for you - I understand that you are entitled to your opinion but it seems you are attempting to discredit something, using personal experience as proof, despite the fact that you have not really taken enough of the substance to realistically achieve the effects you attempt to discredit.

It's like if you took 1mg of morphine orally, and then commented that it wasn't an effective pain killer...

EDIT3: You say that there has been no medical evidence confirming loperamide's activity in the CNS, despite me assuring you otherwise. In response, I must direct you to this:

http://www.ncbi.nlm.nih.gov/pubmed/11014404

A very well-done experiment, cited by 382 other studies as of 6/30/16. The study confirmed loperamide's CNS activity, when coadministered with a pGP inhibitor. They also used relatively TINY doses of loperamide (just 16mg!) - imagine the effects if they used the amounts we discuss here.

Therefore:

The very thing it was required to have shown.

(Q.E.D.)

 

[Nagelfar]

WTF? Do people actually take Loperamide to get high? I thought people where just taking fuckloads of it while in withdrawal because they mistakenly believe that taking huge doses of Loperamide will somehow relieve other symptoms of Opioid withdrawal besides Diarrhea. Hell i didn't even find it to help stomach cramps and high doses (for me this is over 8mg's) make me constipated (i find it far worse then even Codeine in causing this side effect), makes the stomach cramps worse and increases nausea. None of which are desirable effects especially when i am already in Opiate withdrawal. If people are trying to get high off this shit (or shit blocker in this case) it certainly wouldn't be a cheap high as the giant packets of Loperamide are not cheap and the syrup is still rather expensive. If someone where to say take 40 fucking mg's of the stuff that's 20 of those not to small pills. I couldn't imagine trying to get 20 of those fucking pills down in me and that alone would be enough to cause intense nausea.

I can't see this being a problem in Canada as you can get OTC Codeine which even though it's a relatively weak Opiate atleast produces a high and is not Cardiotoxic. It's also cheaper to get a bottle of 100 AC&C's aka Aspirin with Codeine or Acetaminophen with Codeine then it is to get a giant packet of Loperamide or a bottle of the syrup. So there's no economic incentive to buy it here either. Abusing Loperamide to try and catch a high makes no fucking sense to me. Atleast the other common anti-diarrhea drug Diphenoxylate (the Opioid in Lomotil) has CNS effects as it crosses the blood brain barrier granted not very well so abusing that atleast makes some sense.

^ Loperamide did not pin my pupils when in withdrawal or take away any of the withdrawal effects besides the shits. Not even the stomach cramps where helped by it granted my Dicycloverine script covers that. Also Loperamide does not cross the BBB in medical or above medical doses like diphenoxylate does. And yes i know it's not OTC but i used it as a example. Loperamide only seems to cross the BBB in doses strong enough to have any CNS effect when taken in huge amounts that are fucking insane from a health point of view. Also here in Canada at most drug store OTC Codeine is cheaper then generic Loperamide. A bottle of APAP with Codeine costs $6 for 100 pills at my local pharmacy while a pack of about 25 generic Loperamide runs roughly the same cost. So i think in this case Codeine wins out economically.

Taking 40 something mg's of fucking Loperamide just seems insane to me. Also unless you are getting another type of tablet like say sublingual ones they are only slightly smaller then a 325mg Tylenol caplet which is not small at all. As someone who suffers from IBS i would say i have had most generic brands of Loperamide out there. 4mg's with my Morphine dose does help my IBS when it get's really bad hence why i always have Loperamide around the house.

It takes about 200mg to "rush the gate" of the BBB to achieve the high. This is my own experience and not meant to be taken as a safe threshold by any means, HR would be therefore considering the label, at/in the very least. However, in the last few months many doctors have been quoted in many articles of various informational periodicals that people do get high on loperamide, and in the amount my own experience colloquially just attested to.

400ct 2mg pills at my local CostCo is $5.95, that is a four day supply (as I have been doing for two years now; met a woman at outpatient that said her mother was doing similar for twelve years and didn't know why until I explained it).

I have bowel movements daily, even multiple a day roughly once or twice a week, never had nausea or other ill effects outside of overdose range for my tolerance.

Again, I understand the vitriol and am not defending; just listing my own honest experience in the name of statistical information

 

[Limpet_Chicken]

The 200mg XR MS capsules? those were pretty nice. Only ever had them once though, bought a few off a hobo who had some to sell and for some strange reason seemed desperate to get rid of them. Even offered me some diaz tens with the things if I'd take them off him, which I did, although told him to keep his valium for himself, as I don't really care for the stuff much, MOST benzos don't really hit the spot very much for me. Only ones I REALLY like are nitrazepam, flubromazepam, flubromazolam, and nifoxipam. Diazepam just makes me really shaky and I don't think its coincidence that the other day when I couldn't sleep and took 4mg diaz with a bit less than a gram of chlormethiazole, I had what I am sure is a seizure during the hypnogogic phase of waking.

As far as diphenoxylate goes, its pretty shite, even if the atropine is removed first.

 

[Nagelfar]

EDIT3: You say that there has been no medical evidence confirming loperamide's activity in the CNS, despite me assuring you otherwise. In response, I must direct you to this:

http://www.ncbi.nlm.nih.gov/pubmed/11014404

A very well-done experiment, cited by 382 other studies as of 6/30/16. The study confirmed loperamide's CNS activity, when coadministered with a pGP inhibitor. They also used relatively TINY doses of loperamide (just 16mg!) - imagine the effects if they used the amounts we discuss here.

Your efforts to rebuff the naysayers are valiant, intrepid and refreshing; I however, knowing first hand the extreme addiction and full-agonistic opioid effects at the dosage I take daily, can't help but perhaps naively wish the sentiment of those who say it is completely innocuous "non-narcotic (as my once Probation Officer matter-of-factly stated, dismissing it out of hand as a non-issue)" were kept as the universal view of it even so deep into the most contingently related scene of armchair intellectual experimenters online in an educated substance use pharmacology sub-forum.

It really is a maintenance fall-back for those on endless methadone waiting lists who don't see that forthcoming (as I was for a great long while); I can't feel upwards of two bags of H on my 200mg 100ct tablet a day habit that I have been on as much for two years, it is, quite literally, a 'blocking' dose at that amount, and I am sick every morning. It has legs, those not used to it, it seems to keep them well from two to three days (!). I was not so lucky from the onset. Long term lack of opioid naiveté is what I tally that up as.

At my out-patient group, I brought it up and a newcomer to the group jumped at her epiphany that her ex-opiate addict mother took hand-fulls of "Imodium", daily for twelve years, and she never knew why.

 

[BretdaBoxer]

Will a moderator plz message me. It says im a greenlighter and it wont let me post. Iv3 read everything it asks me to!