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Loperamide is a μ-opioid receptor agonist that works in the intestines. [1] Although it is an opioid , it has no effects on the central nervous system . It reduces diarrhea by slowing the transit time of contents through the intestinal tract thereby allowing more water to be reabsorbed from the intestinal lumen .
Loperamide, sold under the brand name Imodium, among others, [1] is a medication of the opioid receptor agonist class used to decrease the frequency of diarrhea. [5] [4] It is often used for this purpose in irritable bowel syndrome, inflammatory bowel disease, short bowel syndrome, [4] Crohn's disease, and ulcerative colitis. [5]
By binding to μ-opioid receptors, loperamide inhibits acetylcholine release and decreases excitation of neurons in the myenteric plexus, which leads to a decrease in peristalsis. [4] Decreasing intestinal motility prolongs the transit time of food content through the digestive tract, which allows for more fluid absorption; thereby alleviating ...
A notable opioid for the purpose of relief of diarrhoea is loperamide which is only an agonist of the μ opioid receptors in the large intestine and does not have opioid affects in the central nervous system as it doesn't cross the blood–brain barrier in significant amounts. This enables loperamide to be used to the same benefit as other ...
By being excluded from the CNS, drugs may act on the rest of the body without producing side-effects related to their effects on the brain or spinal cord. For example, most opioids cause sedation when given at a sufficiently high dose, but peripherally selective opioids can act on the rest of the body without entering the brain and are less ...
The phase III trial for approval was published in 2000 as an industry-funded randomized, placebo-controlled trial (PCT). Its authors found 1 mg alosetron, taken orally twice daily for 12 weeks, was associated with a 12% (CI 4.7-19.2) improvement in relief from abdominal pain and discomfort associated with diarrhea-predominant patients. [4]