Loperamide HCL - General Information
One of the long-acting synthetic antidiarrheals; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally. [PubChem]
Pharmacology of Loperamide HCL
Loperamide HCL is a synthetic anti-diarrheal indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. Loperamide HCL is also indicated for reducing the volume of discharge from ileostomies. In man, Loperamide HCL prolongs the transit time of the intestinal contents. It reduces the daily fecal volume, increases the viscosity and bulk density, and diminishes the loss of fluid and electrolytes. Tolerance to the antidiarrheal effect has not been observed. Loperamide HCL is an opioid receptor agonist and acts on the mu opioid receptors in the myenteric plexus large intestines; it does not affect the central nervous system like other opioids. It works specifically by decreasing the activity of the myenteric plexus which decreases the motility of the circular and longitudinal smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide HCL also decreases colonic mass movements and suppresses the gastrocolic reflex.
Loperamide HCL for patients
Patients should be advised to check with their physician if their diarrhea does not improve after a couple of days or if they note blood in their stools or develop a fever.
Loperamide HCL Interactions
There was no evidence in clinical trials of drug interactions with concurrent medications.
Loperamide HCL Contraindications
Loperamide hydrochloride is contraindicated in patients with known hypersensitivity to the drug and in those in whom constipation must be avoided.
Additional information about Loperamide HCL
Loperamide HCL Indication: For the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease or gastroenteritis. Also used for reducing the volume of discharge from ileostomies.
Mechanism Of Action: In vitro and animal studies show that Loperamide HCL acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide HCL inhibits peristaltic activity by a direct effect on the circular and longitudinal muscles of the intestinal wall. It is a non-selective calcium channel blocker and binds to opioid mu-receptors. Evidence also suggests that at higher concentrations it binds to NMDA receptors and to calmodulin.
Drug Interactions: Not Available
Food Interactions: Take without regard to meals. Increase liquid intake.
Generic Name: Loperamide
Synonyms: Not Available
Drug Category: Antidiarrheals
Drug Type: Small Molecule; Approved
Absorption: Not significantly absorbed from the gut
Toxicity (Overdose): Oral, mouse: LD50 = 105 mg/kg. Symptoms of overdose include constipation, drowsiness, lethargy, and nausea.
Protein Binding: 97%
Half Life: 9.1 to 14.4 hours (average 10.8 hours)
Dosage Forms of Loperamide HCL: Tablet Oral
Chemical IUPAC Name: 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-di(phenyl)butanamide
Chemical Formula: C29H33ClN2O2
Loperamide on Wikipedia: https://en.wikipedia.org/wiki/Loperamide
Organisms Affected: Humans and other mammals