Loperamide is an opioid drug used against diarrhea resulting from gastroenteritis or inflammatory bowel disease. In most countries it is available generically and under brand names such as, Imodium and Pepto Diarrhea Control.
Studies on How Loperamide Works
Loperamide is an opioid-receptor agonist and acts on the opioid receptors in the large intestine; by itself it does not affect the central nervous system. It works similarly to morphine, by decreasing the activity of the this part of the large intestine by increasing the amount of time substances stay in the intestine, allowing for more water to be absorbed.
It is a misconception that loperamide does not cross the blood–brain barrier. Loperamide does cross the blood brain barrier (BBB), although it is immediately pumped back out into non–central nervous system (CNS) circulation. Therefore, it is not considered to have a high potential for abuse.
Loperamide has been shown to cause a mild physical dependence during preclinical studies, specifically in mice, rats, and rhesus monkeys. Symptoms of mild opiate withdrawal have been observed following abrupt discontinuation of long-term therapy with loperamide.
Loperamide Addiction Potential
A specific clinical study designed to assess the abuse potential of loperamide at high doses resulted in a finding of extremely low abuse potential.
Studies in morphine-dependent monkeys demonstrated that loperamide hydrochloride at doses above those recommended for humans prevented symptoms of morphine withdrawal. However, in humans, the pupil test, which when positive indicates opiate-like effects, performed after a single high dose, or after more than two years of therapeutic use of loperamide hydrochloride, was negative. Orally administered loperamide formulated is both highly insoluble and penetrates the CNS poorly.
It was concluded that in its present form, i.e., capsules containing loperamide mixed with magnesium stearate, loperamide poses little threat of potential abuse.
To take enough loperamide in order to achieve any kind of “high” effect, one would have to take well over the recommended daily amount, which would cause lots of discomfort and harm. Adverse drug reactions associated with taking high doses of loperamide include abdominal pain and bloating, nausea, vomiting and constipation. Rare side-effects associated with loperamide are bowel obstruction, dizziness and rashes.
Loperamide Addiction: Personal Testimonials
This writer has trolled some drug forum blogs to see what people are saying about loperamide addiction and if it’s possible to be addicted to Imodium and similar over-the-counter medications. Many of the contributors report that they have used Loperamide to help deal with, apparently somewhat successfully, with opiate withdrawal symptoms. Others report taking very high doses of 100 mg or more per day (not recommended) in order to achieve a euphoric affect. The experience, they report is not nearly as intense as that of narcotic painkillers but, they say, it lends a sense of overall well-being.
Loperamide Addiction: Physical Withdrawal Symptoms
The strongest indication of loperamide addiction and dependence is the withdrawal symptoms that follow once you stop taking it. There are, indeed, reports of experiences of opiate-like withdrawal symptoms from the cessation of Imodium and other loperamide-containing OTCs. Symptoms such as sweats, shakes, cramps, diarrhea, and muscle aches have been reported following abrupt discontinuation of long-term therapy with loperamide.
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