Pubdate: Wed, 11 May 2016
Source: New York Times (NY)
Copyright: 2016 The New York Times Company
Author: Catherine Saint Louis


They call it the poor man's methadone.

The epidemic of opioid addiction sweeping the country has led to 
another form of drug abuse that few experts saw coming: Addicts who 
cannot lay hands on painkillers are instead turning to Imodium and 
other anti-diarrhea medications.

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.

A report published online in the Annals of Emergency Medicine 
recently described two deaths in New York after loperamide abuse. And 
overdoses have been linked to deaths or life-threatening irregular 
heartbeats in at least a dozen other cases in five states in the last 
18 months.

Most physicians just recently realized loperamide could be abused, 
and few look for it. There is little if any national data on the 
problem, but many toxicologists and emergency department doctors 
suspect that it is more widespread than scattered reports suggest.

As efforts to limit prescription opioids intensify, a handful of 
experts are concerned that more addicts might turn to loperamide - 
much as an alcoholic might resort to mouthwash when the Jim Beam runs dry.

"We've seen patients who have been on loperamide for months at a 
time," said William Eggleston, the lead author of the recent report 
and a clinical toxicologist at SUNY Upstate Medical Center.

He added, "A subset of patients take it to get high, and other 
patients use it as a bridge" - meaning that if they cannot obtain 
heroin or morphine, they take loperamide to ease withdrawal symptoms 
like muscle pains, vomiting, diarrhea and nausea.

Sarah Peddicord, a spokeswoman for the Food and Drug Administration, 
said, "The F.D.A. is aware of recent reports of adverse events 
related to the intentional misuse and/or abuse of the anti-diarrhea 
product loperamide to treat symptoms of opioid withdrawal or produce 
euphoric effects."

After a review, she said, the agency "will take appropriate steps as 
soon as possible."

The recommended dose of loperamide is safe. The standard daily dose 
of Imodium A-D is no more than four caplets, or eight milligrams. But 
lobe abusers - as they sometimes call themselves - have reported 
ingesting 100 two-milligram tablets daily for weeks.

In a case reported by Dr. Eggleston and his colleagues, a 24-year-old 
man experiencing opiate withdrawal took so much loperamide that he 
died. Toxicology analysis found more than 25 times the regular dose 
in his blood.

In another case, a 39-year-old man collapsed at home and was 
pronounced dead at a hospital. His family said he had once managed 
his opioid addiction with prescription buprenorphine, but had taken 
to medicating with anti-diarrhea drugs.

Anti-diarrhea medications are cheap, legal and can be bought easily 
in large quantities without raising suspicion. Costco sells 400 
loperamide caplets for just $7.59.

Yet loperamide used to be a prescription drug and a controlled 
substance, in the same class as cocaine or methadone. The F.D.A. 
approved it in 1976, and it became an over-the-counter drug in 1988.

Typically, loperamide acts on opioid receptors in the 
gastrointestinal tract and does not enter the central nervous system. 
At recommended doses, there is no high, and low potential for abuse. 
But large doses can produce a high, doctors say.

Some toxicologists argue that the sales of loperamide should be 
limited, much as the nonprescription drug pseudoephedrine was 
restricted a decade ago to help prevent the manufacturing of crystal meth.

More Reporting on Opioids

"It's time for someone to step in and regulate the purchasing of 
massive quantities," said Dr. Chuck O'Connell, an emergency medicine 
physician and toxicologist at the University of California, San 
Diego, who said he had seen two loperamide overdoses.

"The average person doesn't need 400 tablets of loperamide weekly," 
he said. "I've used a handful in my whole life."

In the journal HeartRhythm Case Reports, he described a 28-year-old 
woman who said she had taken 400 to 600 milligrams of loperamide 
daily for months. An electrocardiogram showed dangerously irregular 
heartbeats and abnormal electrical conduction through her heart.

After repeated blackouts, she sought medical attention at a hospital. 
While there, unknown to doctors, she was still taking 100 tablets of 
loperamide a day from a private stockpile.

After she transferred to U.C.S.D. and confessed her habit, Dr. 
O'Connell asked her to stop. In a few days, an electrocardiogram 
showed her heart normalizing, and the fainting subsided.

"If you take enough, it rushes the gate, and some penetrates the 
blood-brain barrier," Dr. O'Connell said. "Once it crosses the 
barrier, it can act on the central nervous system and you get 
euphoric effects."

Some users complain the high does not compare to that produced by 
opioids. "You can definitely get high from it, and even kill yourself 
with it," a commenter wrote in 2013 on Bluelight, a website where 
people discuss drug use.

The high was "not worth the health risks, whatever they are," the 
commenter wrote.

Another commenter cataloged loperamide's downsides - the need to 
continually take stool softeners, for one - but wrote that the 
medication took away the misery of opioid withdrawal: "Don't wish to 
be dead ... so that's a plus."

Loperamide abuse may go undetected in emergency departments, experts 
warn, because routine drug screens cannot detect it.

"The urine toxicology we do in our hospital doesn't look for 
loperamide, so it's possible we missed cases," said Amitava Dasgupta, 
a toxicologist at the University of Texas Health Science Center at Houston.

Some loperamide abusers arrive at hospitals lethargic or not 
breathing, as if they had overdosed on heroin. Naloxone, an 
anti-opioid drug, may be given.

"When a drug screen comes back negative, emergency room staff may 
assume the test was faulty, or by that time, if the patient is 
responsive, they may write it off as nothing," said Dr. Jennifer 
Dierksen, a pathologist at the University of Texas Health Science 
Center at Houston.

In one case at the hospital, opioid abuse was suspected after a 
19-year-old Texan was found dead at home with a distended bladder 
full of urine. But a drug screen was clean. So Dr. Dasgupta used a 
test known as liquid chromatography-mass spectrometry to pinpoint 
loperamide as the culprit.

All cases of cardiac problems associated with the misuse or abuse of 
loperamide should be reported to the F.D.A.'s Medwatch online 
registry. But not all physicians do so.

"The more people sounding the alarm, the more likely the F.D.A. will 
take the problem seriously and take action," Dr. Eggleston said. "A 
first step would be legislation or regulation that places the items 
behind the counter."

Johnson & Johnson, Imodium's manufacturer, did not respond to 
requests for comment.
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MAP posted-by: Jay Bergstrom