Loperamide capsules 2mg, No. 20

• Symptomatic treatment of acute and chronic diarrhea of ??various origins (including allergic, emotional, medicinal, radiation; with a change in diet and quality composition of food, in violation of metabolism and absorption);

• as an adjunct drug for infectious diarrhea;

• regulation of stool in patients with ileostomy.

Inside with water.

Adults: for acute and chronic diarrhea, an initial dose of 2 capsules (4 mg) per day is prescribed, then - 1 capsule (2 mg) after each act of defecation (in the case of loose stools); the maximum daily dose is 8 capsules (16 mg).

Children over 6 years of age: for acute and chronic diarrhea, an initial dose of 1 capsule (2 mg) per day is prescribed, then 1 capsule after each act of defecation (in the case of loose stools); the maximum daily dose is 3 capsules (6 mg).

When stool normalization or in the absence of stool for more than 12 hours, the drug is canceled.

Elderly patients: No dose adjustment is required when treating elderly patients.

Patients with impaired renal function: No dose adjustment is required when treating patients with impaired renal function.

Patients with impaired liver function: although there are no pharmacokinetic data in patients with hepatic impairment, in such patients the drug Loperamide should be used with caution due to slow pre-systemic metabolism (see section 'Special instructions').

Composition for one capsule

Active substance:

Loperamide hydrochloride - 2.0 mg

Excipients: lactose monohydrate - 104.5 mg corn starch - 30.0 mg talc - 1.4 mg magnesium stearate - 1.4 mg silicon colloidal dioxide (aerosil) - 0.7 mg

• Hypersensitivity to loperamide and / or any of the components of the drug;

• lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

• pregnancy (I trimester);

• breastfeeding period;

• children under 6 years of age;

• acute dysentery, characterized by bloody stools and high fever;

• ulcerative colitis in the acute stage;

• bacterial enterocolitis caused by pathogenic microorganisms, including Salmonella, Shigella and Campylobacter;

• pseudomembranous colitis associated with broad-spectrum antibiotic therapy;

• intestinal obstruction (including in cases where suppression of intestinal motility should be avoided due to the risk of developing severe consequences, such as megacolon or toxic megacolon).

  Loperamide should be discontinued immediately if constipation, bloating, or intestinal obstruction occurs.

Pharmacodynamics

By binding to opioid receptors of the intestinal wall, it inhibits the release of acetylcholine and prostaglandins, thereby reducing the tone and motility of intestinal smooth muscles. Slows down peristalsis and increases the transit time of intestinal contents. Increases the tone of the anal sphincter. Promotes the retention of feces and the reduction of the urge to defecate, reduces the frequency of bowel movements. The action occurs quickly and lasts 4-6 hours.

Pharmokinetics

Most of loperamide is absorbed in the intestine, but due to active first-pass metabolism, systemic bioavailability is approximately 0.3%.

Preclinical data indicate that loperamide is a substrate for P-glycoprotein. The binding of loperamide to blood plasma proteins (mainly albumin) is 95%.

Loperamide is predominantly metabolized in the liver, conjugated and excreted in the bile. Oxidative N-demethylation is the main pathway of loperamide metabolism and is carried out mainly with the participation of isoenzymes CYP3A4 and CYP2C8. Due to active presystemic metabolism, the concentration of unchanged loperamide in the blood plasma is negligible.

In humans, the half-life of loperamide averages 11 hours, ranging from 9 to 14 hours. Unchanged loperamide and its metabolites are excreted primarily through the intestines.

Pharmacokinetic studies in children have not been conducted. The pharmacokinetics of loperamide and its interactions with other drugs are expected to be similar to those in adults.

Overdose

Symptoms: depression of the central nervous system (stupor, impaired coordination, drowsiness, miosis, muscle hypertonia, respiratory depression), urinary retention, intestinal obstruction. Children may be more sensitive to the central nervous system effects of loperamide than adults. In patients with an overdose of loperamide hydrochloride, cardiac complications were observed, such as prolongation of the QT interval, the development of torsade de pointes, other serious ventricular arrhythmias, cardiac arrest and syncope. Fatalities have also been reported.

Treatment: antidote - naloxone; given that the duration of action of loperamide is longer than that of naloxone, re-administration of naloxone is possible.

Medical supervision is necessary for at least 48 hours.

Side effects

Immune system disorders:

Very rare: hypersensitivity reactions, anaphylactic reactions, including anaphylactic shock, anaphylactoid reactions.

Nervous system disorders:

Often: headache, dizziness.

Very rarely: impaired coordination, hypertonicity, depression of consciousness, loss of consciousness, drowsiness, stupor.

Violations of the organ of vision:

Very rare: miosis.

Gastrointestinal disorders:

Often: constipation, flatulence, nausea.

Uncommon: pain or discomfort in the abdomen, dry mouth, vomiting, indigestion, dyspepsia.

Very rare: intestinal obstruction (including paralytic intestinal obstruction), megacolon (including toxic megacolon), glossalgia, bloating.

Skin and subcutaneous tissue disorders:

Very rare: angioedema, bullous rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis and erythema multiforme, pruritus, urticaria.

Kidney and urinary tract disorders:

Very rare: urinary retention.

General disorders:

Very rare: fatigue.

It is important to report the development of adverse reactions in order to ensure continuous monitoring of the relationship between the benefits and risks of the drug. If any of the side effects indicated in the instructions are aggravated, or you notice any other side effects that are not indicated in the instructions, inform your doctor. Health care providers report adverse drug reactions through national ADR systems.

Special conditions

Loperamide is used for the symptomatic treatment of diarrhea. If the cause of the disease is established, appropriate therapy should be carried out.

In patients with diarrhea, especially in children, fluid and electrolyte loss is possible. In such cases, electrolyte replacement and rehydration are urgently needed. If there is no improvement in acute diarrhea after using the drug for 48 hours, consult a doctor.

If during the treatment of diarrhea in patients with acquired immunodeficiency syndrome (AIDS) bloating develops, the drug should be discontinued immediately. In very rare cases, patients diagnosed with AIDS with infectious colitis may experience constipation with the risk of toxic megacolon.

Loperamide should be used with caution in liver failure to avoid toxic damage to the central nervous system.

If during treatment constipation develops, bloating or intestinal obstruction, the drug should be discontinued.

Note for patients with diabetes mellitus: each tablet corresponds to 0.01 XE.

Influence on the ability to drive vehicles, mechanisms

During treatment, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Drug interactions

With the simultaneous use of loperamide and inhibitors of P-glycoprotein, CYP3A4 or CYP2C8 (quinidine, ritonavir, itraconazole, gemfibrozil, ketoconazole), an increase in the concentration of loperamide in the blood plasma is possible.

With the simultaneous administration of loperamide and desmopressin for oral administration, the concentration of desmopressin in the blood plasma increases.

Drugs with similar pharmacological properties can enhance the effect of loperamide; drugs that increase the rate of passage of food through the gastrointestinal tract weaken the effect of loperamide.