Imodium Express tablets 2 mg. №6

Description

Imodium Storage
active substance: loperamide hydrochloride;

1 tablet contains 2 mg of loperamide hydrochloride;

Excipients: gelatin, mannitol (E 421), aspartame (E 951), mint flavor (contains traces of sulfites), sodium bicarbonate.

Imodium Dosage form
Dispersible tablets in the oral cavity.

Main physical and chemical properties: rounded lyophilized tablets from white to almost white.

Imodium Pharmacotherapeutic group
Means that suppress peristalsis. ATX code A07D A03.

Pharmacological properties

Pharmacodynamics.

Loperamide binds to opiate intestinal wall receptors, reducing propulsive peristalsis, increasing the passage time of intestinal contents, and improving the absorption of water and electrolytes. Loperamide increases the tone of the anal sphincter, which helps reduce fecal incontinence and the urge to defecate.

Pharmacokinetics.

Absorption. Most loperamide is absorbed in the intestine after oral administration, but as a result of significant first-pass metabolism, systemic bioavailability is only approximately 0.3%.

Distribution. Studies of the distribution of loperamide in rats show high affinity for the intestinal wall with predominant binding to longitudinal muscle layer receptors. Plasma protein binding of loperamide is 95%, mainly with albumin. Preclinical data have shown that loperamide is a substrate of P-glycoprotein.

Metabolism. Loperamide is almost completely extracted by the liver, where it is predominantly metabolized, bound, and excreted in the bile. Oxidative N-demethylation is the major metabolic pathway of loperamide and is mediated primarily by CYP3A4 and CYP2C8. Due to this very intense first-pass effect, the concentration of unchanged drug in blood plasma remains extremely low.

Breeding. The half-life of loperamide in humans is approximately 11 hours (range 9‒14 hours). Excretion of unchanged loperamide and its metabolites occurs mainly in the feces.

Indication
Symptomatic treatment of acute diarrhea in adults and children over 12 years of age. Symptomatic treatment of acute episodes of diarrhea caused by irritable bowel syndrome in adults (over 18 years of age) after the initial diagnosis by a physician.

Contraindication
Imodium® Express is contraindicated:

patients with known hypersensitivity to loperamide hydrochloride or to any of the components of the drug to prevent severe skin manifestations, including Stevens-Johnson syndrome, toxic epidermal necrolysis and erythema multiforme;
children under 12 years old;
patients with acute dysentery, characterized by the presence of blood in the stool and fever;
patients with acute ulcerative colitis or pseudomembranous colitis associated with the use of broad-spectrum antibiotics;
patients with bacterial enterocolitis caused by microorganisms of the families Salmonella, Shigella and Campylobacter;
Imodium® Express should not be used at all if suppression of peristalsis is to be avoided due to the possible risk of significant complications, including intestinal obstruction, megacolon and toxic megacolon.

The drug should be discontinued immediately if constipation, bloating, or intestinal obstruction develops.