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Loperamide, which is better known in North America by its most common brand name, Immodium, is just what the doctor ordered, so to speak, for many people who are coming off opioid pain relievers. Opioids for pain relief such as codeine, fentanyl (Actiq, Duragesic, Fentora),hydrocodone (Hysingla ER, Zohydro ER), hydrocodone/acetaminophen (Lorcet, Lortab, Norco, Vicodin), hydromorphone (Dilaudid, Exalgo), meperidine (Demerol), andmmethadone (Dolophine, Methadose), among many others, have an almost universal side effect. They cause severe constipation. However, when you stop taking these drugs, you have the opposite problem, severe diarrhea. Loperamide stops the diarrhea that can make coming off opioid pain relievers unbearable. It has a lesser effect on nausea and vomiting, but many users of the drug report that they just did not see another way to stop taking pain relievers without going on loperamide.

Loperamide is itself an opioid. The way in which it differs from opioid pain relievers is that it does not cross the blood-brain barrier. Instead, it interacts with the mu-opioid receptors in the lining of the large intestine. These receptors send out chemicals that reduce the activity of a bundle of nerves known as the myenteric plexus, which in turn reduces muscle activity in the lining of the colon. There aren't the spasms of abdominal pain that come from the contraction of abdominal muscles to force stool through the colon. In a way, it's as if the colon is still on opioids but the brain has a chance to come off them. 

Loperamide also stops the gastrocolic reflex, a nerve action that forces stool out of the colon to make room for digested food. The gastrocolic reflex usually occurs after eating, or sometimes after drinking. It's as if anything in the bowel just has to go. First, well formed, dryer, better formed rather than runny stool is released, and then even the undigested food in the small intestine is also pushed out by bowel movement. The movements are urgent, so there is little time to find a toilet once they start. They continue in most cases until the entire bowel is empty. These severe bowel movements can leave a person feeling faint and broken out in a sweat The pain can be overwhelming and nothing but defecation will relieve it. Loperamide stops this reflex and allows food to stay in the intestines so nutrients and water can be absorbed.

Immodium/loperamide is not for every kind of diarrhea. There are times that diarrhea is actually a good thing. If you have food poisoning, that is, if you have eaten food that contained a pathogen such as E. coli or Salmonella, it's actually beneficial for bowel movement to remove the germs from your digestive tract. If there is any suspicion of bacteria entercolitis, bacterial infection of any kind, or if there is bloody diarrhea, or if there is known ulcerative colitis, then Immodium/loperamide should not be used and a doctor should be consulted right away.

Not a lot can go wrong when you use loperamide. It's extremely inexpensive. The wholesale cost is about US $0.03 a dose. A bottle or gel pack of Immodium is available over the counter without a prescription in the United States for about $9 for 180 doses at Costco, or $20 for 40 doses at some of the pricier pharmacy chains. Although loperamide is an opioid, you probably can't take enough of it to get a "high," although a few people have tried. It's only when you take about 10 times too much that side effects may occur. In a very few cases people have taken irresponsibly large amounts of the medication and developed a dangerous form of constipation called megacolon.

This won't happen if you take the drug as directed. It may not be all you need to get off opioids (see your doctor), but it is extremely helpful with the main problem in getting off opioid pain relievers, severe diarrhea.

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