NPR is reporting on the latest drug scare, involving an over-the-counter antidiarrheal drug that is being used for its opioid-like effects by addicts:
Some people addicted to oxycodone and other opioids are now turning to widely available diarrhea medications to manage their withdrawal symptoms or get high. The results can be dangerous to the heart — and sometimes fatal — warn toxicologists in a study [open, DOI: 10.1016/j.annemergmed.2016.03.047] recently published online in the Annals of Emergency Medicine.
The researchers describe two case studies where people who were addicted to opioids tried to ease their withdrawal symptoms by taking many times the recommended dose of loperamide, a drug commonly used treat diarrhea. Both patients died.
"Because of its low cost, ease of accessibility and legal status, it's a drug that is very, very ripe for abuse," says lead author William Eggleston, a doctor of pharmacy and fellow in clinical toxicology at the Upstate New York Poison Center, which is affiliated with SUNY Upstate Medical University.
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(Score: 4, Interesting) by Anonymous Coward on Wednesday May 04 2016, @05:43PM
First let me say that I've been a long-time member of a drug-based forum where I routinely give out advice to people concerning this very medication.
Some start information for everyone:
Loperamide, while being a potent mu-opioid agonist, doesn't cross the blood-brain-barrier in sufficient quantities to cause analgesia. However over time small amounts of loperamide can make it into the brain if large doses are taken. I've personally, when in the throws of opium withdrawal, taken up to 75mg a day of the stuff for about a week, and it actually works. It doesn't feel like you are on opioids, or really even high. It just calms down the symptoms of opioid withdrawal and makes it manageable.
As far as the health concerns go, I can honestly say that heart damage is kinda out of left field for me. I did a LOT of research on lope and heart damage was never anywhere that I read. In fact most people using Loperamide are far more worried about the possibly toxic metabolite LPP+ than they are about heart damage. So this adds a new facet to the whole debate, but I am wondering exactly how this damage occurred. Anecdotally (and I realize the plural of anecdote is NOT data) there have been many individuals (including myself) who have taken on multiple occasions, over multiple days, large doses of loperamide. What would be very useful is some data on dosages and how long the users were actually on the lope. Id be willing to bet this damage isn't instantaneous but rather cumulative in nature. Its rather unfortunate but Loperamide is still one of the best OTC medications for relieving the symptoms of opioid withdrawal, even with this danger.
The whole argument that Lope is being abused, or ripe for abuse, is complete bullshit as well. I have known maybe one or two people in my entire life that have professed themselves as abusers of loperamide. Its not common and its not really a drug of abuse since it doesn't get you high like other opioids. Its a tool that addicts use to relieve horrible withdrawal symptoms. Its not about to be the DOC for heroin addicts everywhere, and its disingenuous to say that its "very, very ripe for abuse".
(Score: 2) by devlux on Wednesday May 04 2016, @05:58PM
It's not damage per se. It's just that it messes with the heart's ability to regulate. The effect is acute, not chronic as far as they can tell.
These chumps are taking mega doses "trying" to get high.
You should go onto your drug forum and let them know this study is bullshit, you'll get more of a high by hyperventalting into a plastic bag because that's pretty much what they're describing here.
Like I said, Imodium is a counter measure for Naxolene if you're going to be interrogated. It wouldn't work that way if it was screwing with your heart permanently and at human levels of doses. Taking a box of this stuff at maximum strength is going to make you puke, not make you high.
(Score: 0) by Anonymous Coward on Wednesday May 04 2016, @06:43PM
Imodium is not a counter measure for naloxone, I don't know where you read or heard that ridiculousness. Loperamide's effects are limited to the peripheral nervous system unless extreme doses are taken, and even then the binding affinity of loperamide to the mu-receptors is lower than that of naloxone so it wouldnt matter anyway.
(Score: 2) by devlux on Wednesday May 04 2016, @07:43PM
Nice but where are you getting the information from?
To clarify my point...
Loperamide is not a counter measure once the Naloxone is in the system. It's that Naloxone increases sensitivity to pain, which is useful when performing an enhanced interrogation, but if you take Loperamide prior to being subjected to such, it will block the Naloxone from taking effect (as much) allowing you to better resist torture. I really wish I had a citation for you, but that particular info was given to me by word of mouth by someone that I used to work with who also happened to be an MD.
So feel free to ignore it.
(Score: 2) by sjames on Wednesday May 04 2016, @05:59PM
So in other words, if we don't want loperamide abused, we should treat opiate addiction as a medical problem rather than a criminal one. If we do similar with other drugs, perhaps we can start getting cold medicine that actually works again.
Semi-funny note: I have seen bathtub instructions on the net for turning meth into decongestant. It sorta makes sense, it is easier to get meth after business hours.
(Score: 2) by VLM on Wednesday May 04 2016, @06:26PM
I know from forum discussion elsewhere I'm not the only guy out there who "abuses" energy drinks when I have a cold and can't legally get the good stuff for my nose.
Yeah yeah I know its bad, but that's mostly chronic issues. As long as my heart isn't palpitating too much or too often and its only one difficult night till I can get to the pharmacy to get real decongestants, its "OK". The lack of sleep due to clogged nose and/or massive energy drink consumption is probably more dangerous. Actually dehydration from all the caffeine pee is a big issue.
By massive I mean like maybe 4 or 5 per day, not like 10 or 20, that would probably cause a heart attack.
Hey at least I can breath thru my nose again, and even with that much caffeine I can sleep after 20 or so hours awake, or at least I can.
When I was much younger and into experimenting with drinking I would get drunk when I had a cold... alcohol kills germs right? Mostly it made me feel better about being sick rather than actually curing anything... I think, anyway.
(Score: 2) by devlux on Wednesday May 04 2016, @06:29PM
Yeah but be careful with those "internet instructions". Side effects tend to include inflammatory reactions on par with getting your skin melted off.
http://www.liveleak.com/view?i=367_1384564447 [liveleak.com]
http://boingboing.net/2012/02/27/scientific-paper-of-the-day-h.html [boingboing.net] (link to paper is obvious troll look at the authors, you follow that and you'll be putting large quantities of HCL up your nose. )
If you need a proper decongestant and antihistamine eat a fresh clove of garlic raw. Just unwrap it and chew until your mouth goes numb.
After about 5 minutes you'll clear up and the garlic has some natural antibiotic properties that can help with secondary sinus infections. When I feel a cold coming on I'll eat a clove every 4hrs or so and it'll knock it completely out in a day or two.
(Score: 2) by sjames on Wednesday May 04 2016, @07:20PM
Naturally, it's a parody highlighting the utter failure of the DEA to do anything but inconvenience people with colds and allergies.
And yes, one must make sure to properly neutralize the HCL from the purification step. More problematic is making sure not to cause an explosion in a makeshift lab from heating the ether or not properly venting the chloroform :-)
(Score: 0) by Anonymous Coward on Wednesday May 04 2016, @07:18PM
So in other words, if we don't want loperamide abused, we should treat opiate addiction as a medical problem rather than a criminal one
No no no, NO... we cannot do that. We've contracted out the building and running of prisons to private corporations and in those contracts, there are clauses that say "the government *shall* pay at a minimum to $PRIVATE_CORP the rate of an 80% occupation of the facility even if the facility is occupied at a lower rate, it shall pay the exact rate of occupation if the facility is occupied more than 80%". Thus, we need to fill those beds. If we don't it's just throwing away money and someone might bring it up in the next election cycle that $OFFICIAL approved this stupid plan...
Can't have any of that happening now, can we?
(Score: 2) by EvilSS on Wednesday May 04 2016, @06:22PM
Like someone else said, it's not damage so much as acute dysfunction resulting from overdose. Turns out it's not only causing the expected opioid response of central nervous system depression but also causing heart arrhythmias. The study in the paper in the summary is pretty comprehensive, but this is the meat of it:
In addition to clinical manifestations consistent with opioid toxicity (miosis, central nervous system depression, and respiratory depression), significant cardiac dysrhythmias have been reported after overdose. Ventricular dysrhythmias, including polymorphic ventricular tachycardia, as well as prolongation of the QRS complex and QTc duration, have occurred in patients after supratherapeutic loperamide ingestions. Loperamide has been shown to inhibit human cardiac sodium channels in vitro, and QRS prolongation in the overdose setting suggests that this interaction also occurs in vivo. Loperamide inhibits delayed-rectifier potassium currents in vitro. Xenobiotics that inhibit delayed-rectifier potassium currents can prolong the QTc duration and increase the risk for polymorphic ventricular tachycardia, both of which have been reported after oral loperamide overdose. Additionally, loperamide is known to inhibit calcium channels, which may contribute to cardiac toxicity in overdose.1 Fatality associated with loperamide abuse has been reported; however, confirmed death caused by loperamide has not been reported outside of the forensic toxicology literature.
(Score: 0) by Anonymous Coward on Wednesday May 04 2016, @08:54PM
How does it compare to methadone?