Lopedium 2 mg 10 capsules — Made in Germany by Sandoz — Free Delivery

Pharmacological properties

Pharmacodynamics. Lopedium® is a potent long-acting antidiarrheal preparation.

Loperamide hydrochloride binds to opiate receptors in the intestinal wall. As a result, the release of acetylcholine and prostaglandins is suppressed, thus reducing the propulsive peristalsis and increasing the transit time of the contents through the digestive tract, as well as the ability of the intestinal wall to absorb fluid. Loperamide hydrochloride increases the tone of the anal sphincter, thereby reducing fecal incontinence and the urge to defecate.

Loperamide is a highly specific substance for the intestinal walls, reaches systemic circulation in a limited volume and practically does not penetrate the BBB. The central action threshold is much higher than the dose at which the maximum effect against diarrhea is manifested.

Pharmacokinetics. Absorption: Most of the oral loperamide is absorbed in the intestine, but as a result of intense first pass metabolism, the systemic bioavailability is only ≈0.3%.

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

Metabolism: Loperamide is almost completely extracted by the liver, where it is predominantly metabolized, conjugated and excreted in the bile. Oxidative N-demethylation is the main metabolic pathway of loperamide, this process is mediated mainly by the isoforms CYP 3A4 and CYP 2C8. Due to the very intense effect of the first passage through the liver, the concentration of unchanged preparation in the blood plasma remains very low.

Elimination: T½ of loperamide in humans is ≈11 hours with a range of 9-14 hours. Excretion of unchanged loperamide and its metabolites occurs mainly in the feces.

Pediatric patient population: No pharmacokinetic studies have been performed on the pediatric patient population. The pharmacokinetic parameters of loperamide and preparation interactions with loperamide are expected to be similar to those in adults.

Indications

Symptomatic treatment for acute diarrhea in adults and children over the age of 12 years.

Symptomatic treatment for acute episodes of irritable bowel syndrome (IBS) diarrhea in adults over 18 years of age after initial diagnosis by a physician.

Application

Lopedium® is not intended for initial therapy in severe diarrhea accompanied by a decrease in fluid and electrolyte levels. It is desirable to compensate for such a deficiency in children by prescribing parenteral or oral substitution therapy.

The capsules should be taken with a liquid.

Symptomatic treatment for acute diarrhea in adults and children over the age of 12: the initial dose is 2 capsules (4 mg), then 1 capsule (2 mg) after each subsequent loose stool. The usual dose is 3-4 capsules (6-8 mg) per day. The maximum daily dose for acute diarrhea should not exceed 6 capsules (12 mg).

Symptomatic treatment for acute attacks of diarrhea caused by IBS in adults over the age of 18 after the initial diagnosis by a doctor: the initial dose is 2 capsules (4 mg), then 1 capsule (2 mg) is taken after each case of loose stools or according to previous doctor's recommendations.

The maximum daily dose should not exceed 6 capsules (12 mg).

In case of acute diarrhea, if no clinical improvement is observed within 48 hours, the preparation Lopedium® should be discontinued.

Use in elderly patients. No dose adjustment is required for elderly patients.

Application for impaired renal function. No dose adjustment is required for patients with impaired renal function.

Application for violations of liver function. Pharmacokinetic data on the effect of the preparation in persons with impaired liver function are not available, however, these patients should be prescribed loperamide with caution due to a slowdown in first-pass metabolism

Contraindications

Hypersensitivity to loperamide hydrochloride or to any component of the preparation. children under the age of 12.

Contraindicated for primary therapy in patients with:

• acute dysentery, which is characterized by the presence of blood in the stool and fever;
• acute ulcerative colitis or pseudomembranous colitis associated with the use of broad-spectrum antibiotics;
• bacterial enterocolitis caused by microorganisms of the family Salmonella, Shigella, Campylobacter.

Lopedium® should not be used if necessary to avoid oppression of peristalsis due to the possible risk of significant complications, including intestinal obstruction, megacolon and toxic megacolon.

It is necessary to immediately stop using the preparation in case of constipation, bloating or intestinal obstruction.

Side effects

From the nervous system: headache, dizziness, drowsiness, stupor, depression or loss of consciousness, hypertonicity, impaired coordination, tremor.

From the digestive system: nausea, constipation, flatulence, abdominal pain, dry mouth, vomiting, dyspepsia, glossalgia, bloating, intestinal obstruction, including paralytic ileus; megacolon, including toxic megacolon, upper abdominal pain.

From the kidneys and urinary system: urinary retention.

On the part of the skin and subcutaneous tissue: rash; bullous rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema polymorphism; angioedema, urticaria, itching.

From the immune system: hypersensitivity reactions, anaphylactic reactions (including anaphylactic shock) and anaphylactoid reactions.

From the side of the organ of vision: miosis.

General disorders: fatigue.

Special instructions

Treatment for diarrhea is symptomatic. if the etiology of the disease can be determined (or it is indicated that this should be done), then, if possible, specific treatment should be carried out.

The use of the preparation does not exclude the use of antibiotic therapy according to indications.

People with diarrhea, especially children, may experience dehydration and electrolyte imbalances. In such cases, the most important measure is the use of replacement therapy to replace fluid and electrolytes.

The use of the preparation does not replace the introduction of an appropriate amount of fluid and the restoration of electrolytes.

Since persistent diarrhea can indicate potentially more serious conditions, the preparation  should not be used for a long time until the cause of the diarrhea has been investigated.

In acute diarrhea, in the absence of clinical improvement within 48 hours, the use of loperamide hydrochloride should be discontinued and a doctor should be consulted.

AIDS patients taking Lopedium® for diarrhea should immediately discontinue treatment at the first sign of bloating. There are isolated reports of cases of intestinal obstruction with an increased risk of toxic megacolon in AIDS patients with infectious colitis (both viral and bacterial origin) during treatment with loperamide hydrochloride.

Pharmacokinetic data on the use of the preparation in persons with impaired liver function are absent, however, in these patients loperamide should be used with caution due to a slowdown in the first pass metabolism, and this can lead to a relative overdose, which can lead to toxic effects on the central nervous system.

The preparation should be used with caution in patients with exacerbation of ulcerative colitis. Medicines that prolong the transit time can lead to the development of toxic megacolon in these patients.

Given that loperamide is well metabolized and, together with metabolites, is excreted in the feces, dose adjustment is usually not required for patients with impaired renal function.

The preparation contains lactose, so it should not be prescribed to patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.

If the preparation is taken to control attacks of diarrhea due to IBS, which was previously diagnosed by a doctor, and clinical improvement is not observed within 48 hours, you should stop using loperamide hydrochloride and consult a doctor. You should also see your doctor if the nature of your symptoms has changed or if recurrent bouts of diarrhea persist for more than 2 weeks.

For the treatment of acute bouts of diarrhea due to IBS, Lopedium® should be taken only if a doctor has previously diagnosed the disease.

In the following cases, the preparation should not be used without first consulting a doctor, even if it is established that the patient has IBS:

• the patient is over 40 years old, and some time has passed since the last attack of IBS;
• the patient is over 40 years old, and this time the symptoms of IBS are different;
• recent bleeding from the intestines;
• severe constipation;
• nausea or vomiting;
• lack of appetite or weight loss;

Difficulty or painful urination

fever;

recent trip abroad.

If new symptoms develop, symptoms worsen, or if symptoms have not improved within 2 weeks, see a doctor.

Use during pregnancy and lactation. It is not recommended to take this medication during pregnancy.

Since a small amount of loperamide can be excreted in breast milk, the use of the preparation during breastfeeding is not recommended.

Therefore, pregnant women and women who are breastfeeding should be advised to see a doctor for appropriate treatment.

Children. The preparation is used in children over the age of 12 for symptomatic treatment of acute diarrhea.

The ability to influence the reaction rate when driving or working with other mechanisms. Fatigue, dizziness or drowsiness may occur with diarrhea syndrome when using loperamide hydrochloride. Therefore, it is recommended to take the preparation with caution when driving or operating machinery.

Interactions

Cases of interactions with preparations with similar pharmacological properties have been reported. Preparations that have a depressing effect on the central nervous system should not be used in children simultaneously with loperamide.

Preclinical data have shown that loperamide is a substrate for P-glycoprotein. The simultaneous use of loperamide (single dose - 16 mg) with P-glycoprotein inhibitors (quinidine, ritonavir) leads to an increase in the level of loperamide in blood plasma by 2–3 times. The clinical significance of the indicated pharmacokinetic interaction with the use of loperamide in the recommended therapeutic doses (from 2 to 16 mg) is unknown.

The simultaneous use of loperamide (4 mg once) and itraconazole, an inhibitor of CYP 3A4 and P-glycoprotein, led to a 3-4-fold increase in plasma concentrations of loperamide. In the same study, the CYP 2C8 inhibitor gemfibrozil increased the concentration of loperamide by a factor of 2. The combined use of itraconazole and gemfibrozil resulted in a 4-fold increase in the maximum plasma level of loperamide and a 13-fold increase in total plasma exposure. This increase is not associated with the effect on the central nervous system, which was determined using psychomotor tests (that is, subjective drowsiness and the test for substitution of digital symbols).

The simultaneous use of loperamide (16 mg once) and ketoconazole, an inhibitor of CYP 3A4 and P-glycoprotein, led to a 5-fold increase in the concentration of loperamide in blood plasma. This increase was not associated with an increase in the severity of pharmacodynamic effects, which was determined using pupillometry.

Concomitant treatment with oral desmopressin resulted in a 3-fold increase in plasma desmopressin concentration, probably due to slower gastrointestinal motility.

It is assumed that preparations with similar pharmacological properties can enhance the effect of loperamide, and preparations that accelerate the passage of contents through the gastrointestinal tract can weaken its effect.

Overdose

Symptoms in case of an overdose (including a relative overdose due to hepatic dysfunction), depression of the central nervous system (stupor, impaired coordination, drowsiness, miosis, muscle hypertonia, respiratory depression), urinary retention and a complex of symptoms similar to intestinal obstruction may occur. children are more sensitive to the effect on the central nervous system than adults.

Treatment. If symptoms of an overdose occur, naloxone can be used as an antidote. Since the duration of action of loperamide is longer than that of naloxone (1-3 hours), re-administration of naloxone may be necessary. In order to identify symptoms of possible depression of the central nervous system, the patient should be closely monitored for at least 48 hours.

Storage conditions

At a temperature not higher than 25 ° C. Keep out of the reach of children.