Posts Tagged ‘blood-brain barrier’

Over-the-counter opiates used to stop diarrhea and maybe ease withdrawal

Friday, December 18th, 2009

by Chris Strosser
Posted: 11/29/06
Last Edited: 2/24/09

Most people are not aware that opiates can be found over-the-counter at the local drugstore, and that anyone can buy them. In fact, one product in particular is widely used and isn’t restricted to those under 18 years of age. The drug I’m referring to is loperamide, meperidine’s strange distant cousin and the active ingredient in the popular anti-diarrheal, Imodium AD. Loperamide is an opioid. Another common formulation known as Lomotil has diphenoxylate as the active ingredient, which is also an opioid used to stop diarrhea. One annoyingly persistent side effect of opioid usage, which all those on pain management can attest to, is constipation, which is the desired effect with these medications.

How loperamide affects the body

All opiates cause constipation by binding to opioid receptors throughout the gastrointestinal tract. This binding causes muscles in the gastrointestinal tract to become tense. The increased muscle tension causes the normal progressive movement of food waste to stop—thus, causing the infamous, unrelenting, opiate-induced constipation. Though loperamide and diphenoxylate exert a powerful effect on the gastrointestinal tract, they have no effect on the brain. Ultimately, this means no euphoric high, which is why it is still available over-the-counter. Typical opiates are fat-soluble enough to cross the blood-brain barrier (also known as the BBB), and bind to opiate receptors in the brain.

From controlled substance to over-the-counter wonder

When loperamide was first introduced to the public, it was actually classified as a Schedule V substance, meaning it required a prescription to use. The reason officials classified this drug as a Schedule V substance was because the typical opiate withdrawal symptoms were present following abrupt cessation of long-term therapy. Loperamide’s status as a controlled substance was eventually removed and its standing was downgraded to nothing more than an over-the-counter medicine. Recent studies have, however, put forth evidence that it is possible to create an environment for the molecules to move across the BBB. “Drug-containing nanoparticles were coated with polysorbate 80 and injected intravenously into mice,” A prolonged, as well as significant analgesic effect occurred upon injection of the coated loperamide.

Loperamide as a comfort medicine in opiate withdrawal

Loperamide may also work as an aid in detoxification. Several medical journals, as well as countless unofficial accounts report significantly diminished withdrawal symptoms upon dosing with loperamide; however, there is a lot controversy on this subject. At the very least, loperamide will aid in reducing the gut-retching diarrhea that comes with most opiate detoxifications. Loperamide works for some people, and doesn’t work for others. As always, one should always seek the professional advice of a doctor before starting any sort of therapy or withdrawal treatment.

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