Imodium (Loperamide) Causes Torsades de Pointes in Patient Seeking High

[monkey business (OP)]

http://www.empr.com/case-studies/over-the-counter-drug-causes-torsades-de-pointes-in-patient-seeking-high/article/473323/2/

Anyone that takes high doses of lope regularly should definitely read this article:

"Loperamide, an anti-motility opioid agonist that's available over-the-counter, was associated with Torsades de Pointes (TdP) in a recently published case study. Loperamide has generally been considered safe for the treatment of diarrhea, given its µ receptor specificity and low abuse potential.

The case involved a 26-year old male who presented to the ER after a transient episode of loss of consciousness. He had a history of heroin abuse, and three days into his admission he would divulge how he had been taking loperamide for the past 2 months to help relieve diarrhea caused by heroine withdrawal. The day before his admission he significantly increased his daily dose of loperamide after he read on a blog that high doses of loperamide give a similar ‘high' as heroin.

On the day of admission his maximum ingested dose reached 192mg – or 96 tablets – the label daily limit is 16mg. Upon arrival his vital signs showed a heart rate of 50 beats/min, blood pressure at 125/60mmHg, and a respiratory rate of 14 breaths/minute; EKG showed sinus bradycardia with normal PR, QRS, and QT/QTc intervals. Soon after he developed shortness of breath, diaphoresis and sustained ventricular tachycardia with ventricular rate 220 beats/minute. He was defibrillated before sinus bradycardia was attained again, however bradycardia worsened with heart rate of 40 beats/min.

Over the course of one hour he experienced two episodes of self-limiting TdP, each episode lasting less than 10 seconds and a third ending up in pulseless ventricular tachycardia. The patient was defibrillated and with CPR he regained his pulse immediately; sinus bradycardia continued with heart rate at 40 beats/minute. The patients was then given magnesium IV 2gm and isoproterenol; this had the intended effect and he maintained a heart rate of 90 beat/minute for the next 48 hours.

On the third day of his admission, isoproterenol was stopped after no further ventricular arrhythmias were noted. The patient's heart rate subsequently remained between 50–60 beats/min. Transthoracic echocardiogram and cardiac angiography showed no abnormalities.

Loperamide has poor and variable bioavailability (roughly 10 to 20%), which makes it hard to predict drug levels related to the ingested dose. Given the amount of drug consumed and the fact that loperamide decreases peristalsis, which keeps the medication in the gastrointestinal tract for a longer period, the amount systemically absorbed would be much higher than what would be seen with a normal dose. Also, prolonged consumption could lead to fat depots of loperamide not accounted for in serum levels.

With these points in mind, the serum loperamide level of the patient on the third day of hospitalization was found to be 2ng/mL, which is the expected peak level after taking an 8mg oral dose, suggesting that the level on presentation may have been considerably higher.

Persistent sinus bradycardia likely predisposed the patient to the development of QT prolongation and TdP. Some animal studies have shown that opioid receptor stimulation has been shown to inhibit β1 and β2 adrenergic receptor activity in cardiac muscle cells, thereby restricting the inotropic and chronotropic effect of adrenergic stimulation on the heart. Cases of serious cardio toxic effects have been previously reported in patients taking large doses of loperamide to obtain euphoric effect.

The authors hope their research can increase the index of suspicion of such toxic cardiac events, while raising concerns about the safety profile of loperamide as it remains easily available over the counter."



Thoughts?

[Zoops]

My thoughts on this is that it seems that it was already known, if not commonly, among the medical community that loperamide can cause cardiac arrhythmias, so there's cause for alarm, like they are going to take it off the shelves tomorrow. More of a reason for them to do that would be that opiate-dependent people are "abusing" it, "seeking a 'high'," which is quite laughable, as we all well know.

If there's any possibility of you getting a buzz off of it, then you must withdraw it from the market entirely, or at least relegate it to prescription status. Only reason that hasn't happened yet with DXM is the OTC drug lobby. I mean if you just stand still in this country's legislative environment and don't push back against negative publicity, then your product is going to be banned. That's just how it is - it takes millions in lobbying dollars a year, depending on how badly the media is currently portraying it, to keep a product like DXM available OTC. It's been pretty quiet lately with reports of DXM abuse among teenagers ("think of the children" aren't we all tired of that trope?), so there probably haven't been a lot of calls on Capitol hill to change the laws regarding its distribution. Same for loperamide. If this issue starts making more noise, you better hope the OTC drug lobbyists are there to whisper in the congresspeople's ears about campaign funding if they vote against something like that because it would hurt jobs in their district or state, impair their image as someone who doesn't care about the struggling single mother of 10 who can't pay for her kids to see a doctor and relies upon, yes in fact the lives of her children depend on, the availability of a good tried-and-true OTC cough suppressant like DXM or OTC anti-diarrheal like loperamide.

As soon as a bunch of concerned parents get behind their keyboards or pick up a pen, though, you can be sure that the congressional representatives that they write to will be first to report to someone in the relevant committee that "something must be done about this ____ thing," though. Congressmen and senators are so eager for re-election, stuff like this that is likely to receive bipartisan support - "for the children" are more likely to receive attention rather than the real issues that plague our country, because they want to be perceived as "making a difference for America," and stuff like that, in ways that everyone can feel good about.

Shit, think of the junkies for once!

Just my $0.000000000000000002 (2 attodollars).

[theSWPK]

It makes me so angry whenever I read articles like this and they claim that the person taking it was either getting high by abusing lope or attempting to get high from loperamide. I see this all too often lately.
I think the addicts like this guy, who have been maintaining on loperamide for awhile, understand that you do not get high or even a small buzz. I bet they tell the hospital staff that they are using it simply to maintain and even go into detail as to why/how that's possible, but then hospital staff records it as getting high...

Several stores near me now have to keep the lope behind the counter because too many fuckheads keep stealing it. This is in a city of only 20,000 people too, so I can only imagine what it's like in more densely populated cities.
The guys stealing every bottle in the shelf are doing their best to make sure that future down and out theSWPK can't do the same thing if necessary (very rare occurance)! Only I can have double standards!

I really hope this doesn't lead to it being controlled tighter like Rx only.

Oh well, I prefer loperoxymorphone for my diarrhea anyway.