Description
Loperamide Pharmacodynamics
Loperamide binds to opioid receptors in the intestinal wall and inhibits release of acetylcholine and prostaglandins, thus slowing down peristalsis and increasing time for passage of contents through the intestine. Increases anal sphincter tone, thus reducing fecal incontinence and urges to defecation.
Indications
Symptomatic treatment of acute and chronic diarrhea (genesis: allergic, emotional, medicinal, radiation, when changing diet and quality composition of food, in violation of metabolism and absorption). As an aid in diarrhea of infectious genesis Stool regulation in patients with ileostoma.
Contraindications
Loperamide capsules should not be used in children under 6 years of age.
Loperamide is contraindicated in patients with hypersensitivity to the active substance and/or any of the drug components.
Loperamide capsules are contraindicated in lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
Loperamide is contraindicated in the first trimester of pregnancy
Loperamide is not recommended to be taken during breastfeeding;
Loperamide should not be used as the main therapy:
– in patients with acute dysentery, which is characterized by stools with a mixture of blood and high fever;
– in patients with acute ulcerative colitis;
– patients with bacterial enterocolitis caused by pathogens, including Salmonella, Shigella and Campylobacter;
– in patients with pseudomembranous colitis associated with therapy with broad-spectrum antibiotics.
Loperamide should not be used in cases when slowing down peristalsis is undesirable because of the possible risk of serious complications, including intestinal obstruction, megacolon and toxic megacolon.
Loperamide should be stopped immediately in case of constipation, abdominal bloating or intestinal obstruction.
Dosage and administration
- Orally, with water.
- Adults and children over 6 years:
Acute diarrhea: initial dose is 2 capsules (4 mg) for adults and 1 capsule (2 mg) for children, then 1 capsule (2 mg) after each act of defecation in case of liquid stools. - Chronic diarrhea: the initial dose is 2 capsules (4 mg) daily for adults and 1 capsule (2 mg) for children; further the initial dose should be adjusted so that the frequency of normal stools is 1-2 times per day, which is usually achieved with a maintenance dose of 1 to 6 capsules (2-12 mg) daily.
- Maximum daily dose in acute and chronic diarrhea in adults is 8 capsules (16 mg); maximum daily dose in children is calculated based on body weight (3 capsules per 20 kg body weight of the child), but should not exceed 8 capsules (16 mg).
- If stools are normalized or if there are no stools for more than 12 hours, the drug should be discontinued.
- Administration in children
Do not use Loperamide in children under 6 years of age. - Use in elderly patients
No dosage adjustment is required when treating elderly patients - Use in patients with impaired renal function
No dosage adjustment is required when treating patients with impaired renal function. - Administration in patients with hepatic impairment
Although there are no pharmacokinetic data in patients with hepatic impairment, Loperamide should be used with caution in such patients due to delayed presystemic metabolism (see section “Cautionary Note”). - If after treatment there is no improvement or the symptoms worsen, or new symptoms appear, it is necessary to consult a physician. Use the drug only according to the method of administration and in such doses as specified in the instructions.
