Feb 28, 2024 · Mechanism of Action. Loperamide is a lipophilic synthetic phenylpiperidine opioid and a μ-receptor agonist. At therapeutic doses, loperamide acts on the μ-opioid receptors directly on the circular and longitudinal intestinal muscles to decrease transition time, inhibit peristalsis electrolyte loss, and increase rectal tone. However, because ...

Mechanism of action. Enteric neurons synthesize and release endogenous opioid peptides and other neurotransmitters, such as acetylcholine and substance P. Endogenous opioids bind to opioid receptors expressed on these neurons to regulate gastrointestinal signalling, motility, and balance of fluids and electrolytes. 5

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]

Feb 17, 2020 · Mechanism of Action Acts directly on circular and longitudinal intestinal muscles, through the opioid receptor, to inhibit peristalsis and prolong transit time; reduces fecal volume, increases viscosity, and diminishes fluid and electrolyte loss; demonstrates antisecretory activity.

Loperamide works by a number of different mechanisms of action that decrease peristalsis and fluid secretion, resulting in longer gastrointestinal transit time and increased absorption of fluids and electrolytes from the gastrointestinal tract.

Loperamide also modifies the intestinal transport of water and electrolytes by stimulating absorption, 5 and by an antisecretory action mediated by calmodulin antagonism, a property not shared by other opioids. 6-8

The mechanism of action of loperamide on fluid and electrolyte transport is examined with reference to opiate agonism, calcium-channel blocking, calmodulin inhibition, and paracellular permeability. The colon appears to be the main site of action of …

Loperamide stimulated absorption of fluid, electrolytes, and glucose and reversed PGE2 and cholera toxin-induced secretion to absorption; this opiate analogue had no effect on cholera toxin stimulation of adenylate cyclase activity or the rise of tissue cyclic AMP (cAMP) concentrations.

Jan 23, 2025 · Mechanism of Action. In vitro and animal studies show that loperamide hydrochloride acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide binds to the opiate receptor in the gut wall.

CLINICAL PHARMACOLOGY. Mechanism of Action. In vitro and animal studies show that loperamide hydrochloride acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide binds to the opiate receptor in the gut wall. Consequently, it inhibits the release of acetylcholine and prostaglandins, thereby reducing …