Library > Abstracts and Articles > Over-the-counter opiates used to ... and maybe ease withdrawal
Over-the-counter opiates used to stop diarrhea and maybe ease withdrawal
by Chris Strosser
11/29/06
Discussion: http://www.thatspoppycock.com/phpBB2/viewtopic.php?t=20
Did you know that opiates can be found over-the-counter at your local drugstore? It's true, and anyone can buy them. In fact, they aren't even restricted to those under 18. Loperamide, meperidine's weird distant cousin, and the active ingredient in Imodium AD, is an opioid. Diphenoxylate, also an opioid, is the active ingredient in Lomotil, which is also used to stop diarrhea. One annoyingly persistent side effect of all opiates is constipation.
The inner workings
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 a powerful effect is exerted on the gastrointestinal
tract, loperamide and diphenoxylate do not affect the brain. Ultimately,
this means no euphoric high. The powerful high is avoided because the
molecules cannot cross the blood-brain barrier which works sort of
like a "drug filter." Typical opiates are
fat-soluble enough to cross the BBB, and bind to opioid
receptors in the brain.
From controlled substance to over-the-counter
wonder
When loperamide was first introduced to the public, it was classified
as a Schedule V controlled substance. This was done because opiate
withdrawal symptoms were present upon abrupt cessation of long-term therapy with
lopermide. It was eventually downgraded to nothing more than an over-the-counter
medicine. Recent studies have put forth evidence that it is possible
to get the molecules 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.
As withdrawal treatment?
Loperamide may also work as an aid in detoxification. Several medical
journals, as well as a countless unofficial accounts report significantly
diminished withdrawal
symptoms upon dosing loperamide; however, there is a lot of mixed
information on this topic. It will, at the least, get rid of the gut-retching
diarrhea that comes with most opiate detoxifications. It works for
some, and doesn't work for others. As always, you should check with
your doctor before starting any sort of withdrawal
treatment.
See also: Opioid addiction, Suboxone FAQ, Over-the-counter Comfort Medicine
Sources