Imodium 2 mg 6 capsules — Made in France — Free Delivery

Pharmacological properties

Pharmacodynamics. Loperamide hydrochloride binds to opiate receptors in the intestinal wall. as a result, the release of acetylcholine and prostaglandins is suppressed and thus the propulsive peristalsis decreases and the transit time of the contents through the digestive tract increases, 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.

Pharmacokinetics. Absorption: Most of the loperamide taken orally is absorbed in the intestine, but as a result of intensive first pass metabolism, the systemic bioavailability is about 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 with 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 about 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 behavior of loperamide and preparation interactions with loperamide are expected to be similar to those seen in adults.

Indications

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

Application

Imodium is not intended for the initial treatment of severe diarrhea associated with dehydration and decreased fluid and electrolyte levels. in particular, in children, it is desirable to compensate for this loss 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 years. 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).

In acute diarrhea, if no clinical improvement is observed within 48 hours, the use of Imodium should be discontinued.

Symptomatic treatment for acute episodes of diarrhea due to IBS in adults over the age of 18 years after the initial diagnosis by a doctor. The initial dose is 2 capsules (4 mg), then 1 capsule (2 mg) is taken after each subsequent loose stool or according to the preliminary recommendations of the doctor. The maximum daily dose should not exceed 6 capsules (12 mg).

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

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

Application for impaired liver function. Although there are no pharmacokinetic data on the action of the preparation in patients with impaired liver function, Imodium should be prescribed with caution in such patients due to a slowdown in the first pass metabolism.

Contraindications

Imodium is contraindicated in patients with known hypersensitivity to loperamide hydrochloride or any of the components of the preparation; children under the age of 12; patients with acute dysentery, which is characterized by the presence of blood in the stool and an increase in body temperature; 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 salmonella, shigella and campylobacter families.

Imodium should not be used at all if it is 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 stop taking the preparation immediately if constipation, bloating, or partial intestinal obstruction develop.

Side effects

Adults and children over the age of 12

Side effects in patients with acute diarrhea. The safety of loperamide hydrochloride was evaluated in 2755 patients aged 12 years and older who participated in 26 controlled and uncontrolled clinical studies of the use of loperamide hydrochloride for the treatment of acute diarrhea.

Side effects with a frequency of 1% or more reported in these clinical trials are presented below.

Nervous system disorders: headache.

Digestive tract disorders: constipation, bloating, nausea.

Side effects that occurred with a frequency of less than 1% in the above clinical studies:

Nervous system disorders: dizziness.

Digestive tract disorders: dry mouth, flatulence, abdominal pain and discomfort, vomiting, pain in the upper abdomen.

Skin and subcutaneous tissue disorders: rash.

Post-marketing experience. The following side effects have been reported spontaneously (ranked by frequency of occurrence): very common (≥1 / 10); often (≥1 / 100, 1/10); infrequently (≥1 / 1000, 1/100); rarely (≥1 / 10,000, 1/1000); very rarely (1/10 000), including single messages.

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

From the nervous system: very rarely - impaired coordination, loss of consciousness, depression of consciousness, hypertonicity, drowsiness, stupor.

From the side of the organ of vision: very rarely - miosis.

From the digestive tract: very rarely - intestinal obstruction (including paralytic intestinal obstruction), megacolon (including toxic megacolon).

On the part of the skin and its appendages: very rarely - angioedema, bullous rash, including Stevens-Johnson syndrome, polymorphic erythema and toxic epidermal necrolysis, urticaria and itching.

From the side of the kidneys and urinary system: very rarely - urinary retention.

General disorders: very rarely - increased fatigue.

Special instructions

Treatment for diarrhea is symptomatic. if it is possible to determine the etiology of the disease (or it is indicated that this should be done), then, if possible, it is necessary to carry out specific treatment.

In patients with diarrhea, especially in children, debilitated patients and the elderly, dehydration and electrolyte imbalances may occur. In such cases, the most important intervention is replacement therapy to replenish fluid and electrolyte stores.

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

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

In acute diarrhea, when no clinical improvement is noted within 48 hours, the use of loperamide hydrochloride should be discontinued and a doctor should be consulted.

Patients with acquired immunodeficiency syndrome who take Imodium for diarrhea should immediately stop treatment at the first signs of bloating. There are isolated reports of cases of intestinal obstruction with an increased risk of toxic megocolon in the treatment of loperamide hydrochloride in patients with AIDS, infectious colitis of both viral and bacterial origin.

Although there are no pharmacokinetic data for patients with impaired liver function, in such patients Imodium should be used with caution due to a slowdown in first-pass metabolism. Loperamide hydrochloride should be used with caution in patients with impaired liver function, since it can lead to a relative overdose, which can cause toxic damage to the central nervous system.

Medicines that lengthen the transit time can put them at risk of developing toxic megacolon in this group of patients.

Given that loperamide is well metabolized, and that it and its metabolites are excreted in the feces, there is usually no need to adjust the dose of loperamide in patients with impaired renal function.

Since the preparation contains lactose, it should not be used in patients with rare hereditary forms of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption syndrome.

If the preparation is taken to control episodes 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 your symptoms have changed or if recurrent episodes of diarrhea persist for more than 2 weeks.

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

In the following cases, the preparation is not recommended to be used without first consulting a doctor, even if it is known 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; loss of appetite or weight loss; Difficulty or painful urination fever; recent trip abroad.

In case of new symptoms, worsening of symptoms, or if symptoms have not improved within 2 weeks, see a doctor.

During pregnancy and breastfeeding. It is not recommended to take this medication during pregnancy. 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 years for symptomatic treatment of acute diarrhea.

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

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 simultaneously with the preparation imodium in children.

Preclinical evidence suggests that loperamide is a substrate for P-glycoprotein. Simultaneous administration of loperamide (at a dose of 16 mg) together with P-glycoprotein inhibitors (quinidine, ritonavir) led to an increase in the level of loperamide in blood plasma by 2–3 times. The clinical significance of this pharmacokinetic interaction with the use of loperamide at the recommended doses 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 the concentration of loperamide in blood plasma. In the same study, the CYP 2C8 inhibitor gemfibrozil increased the content of loperamide by about 2-fold. The combined use of itraconazole and gemfibrozil resulted in a 4-fold increase in maximum plasma loperamide content and a 13-fold increase in total plasma exposure. This increase is not associated with the effect on the central nervous system, determined using psychomotor tests (that is, subjective drowsiness and the test for the replacement 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 is 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 expected that preparations with similar pharmacological properties can enhance the effect of loperamide, and preparations that accelerate the transit of food through the gastrointestinal tract can reduce the severity of its effect.

Overdose

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

Treatment. In case of overdose, the patient should immediately consult a doctor. If symptoms of an overdose occur, naloxone can be used as an antidote. Since the duration of action of Imodium is longer than that of naloxone (1-3 hours), reapplication of naloxone may be necessary. To identify possible depression of the central nervous system, the patient should be closely monitored for at least 48 hours.

Storage conditions

At a temperature not exceeding 25 ° C, out of the reach of children.