Imodium Express, 2 mg 10 pcs

Acute and chronic diarrhea (diarrhea); stool regulation in patients with ileostomies

Active ingredient

Loperamide

Composition

1 tablet contains:

The active ingredient:

loperamide hydrochloride 2 mg;

Excipients:

gelatin – 5.863 mg,

mannitol – 4.397 mg,

aspartame – 0.75 mg,

mint flavoring – 0.3 mg,

sodium bicarbonate – 0.375 mg,

purified water 136.315 mg (removed during lyophilization).

How to take, the dosage

Orally.

The tablet is placed on the tongue, within a few seconds it dissolves, and then it is swallowed with saliva without water.

Adults and children over 6 years:

• Acute diarrhea: initial dose -2 tablets (4 mg) for adults and 1 tablet (2 mg) for children, then 1 tablet (2 mg) after each act of defecation in case of liquid stool.
• Cronic diarrhea: initial dose is 2 tablets (4 mg) daily for adults and 1 tablet (2 mg) for children; further, the initial dose should be adjusted so that the frequency of normal stools is 1-2 times daily, which is usually achieved with a maintenance dose of 1 to 6 tablets (2-12 mg) daily.

The maximum daily dose should not exceed 6 tablets (12 mg); the maximum daily dose in children is calculated based on body weight (3 tablets per 20 kg body weight of the child), but should not exceed 6 tablets (12 mg).

In case of normalization of stool or in case of absence of stool for more than 12 hours the drug is discontinued.

Administration in children:

Do not use Imodium® in children under 6 years old.

Application in elderly patients:

In the treatment of elderly patients dose adjustment is not required.

Application in patients with renal dysfunction:

In the treatment of patients with renal dysfunction dose adjustment is not required.

Application in patients with hepatic impairment:

Although there are no pharmacokinetic data in patients with hepatic impairment, Imodium® should be used with caution in these patients due to delayed presystemic metabolism (see section “Special Precautions.

NOUtions for use

Since lyophilized tablets are quite fragile, they should not be pressed through the foil to avoid damage. In order to remove the tablet from the blister the following steps should be taken: take the foil by the edge and completely remove it from the cell, in which the tablet is located; gently press from the bottom and remove the tablet from the package.

Interaction

According to preclinical studies, loperamide is a substrate of P-glycoprotein.

When loperamide (single dose of 16 mg) and quinidine or ritonavir, which are P-glycoprotein inhibitors, are administered simultaneously, the concentration of loperamide in blood plasma increased by 2-3 times.

The clinical significance of the described pharmacokinetic interaction with P-glycoprotein inhibitors when using loperamide at the recommended doses is unknown.

Concomitant use of loperamide (single dose of 4 mg) and itraconazole, an inhibitor of CYP3A4 isoenzyme and P-glycoprotein, led to an increase of loperamide concentration in plasma by 3-4 times.

In the same study, use of the CYP2C8 isoenzyme inhibitor, gemfibrozil, resulted in an approximately 2-fold increase in plasma concentrations of loperamide.

When the combination of itraconazole and gemfibrozil was used, the peak plasma concentration of loperamide increased 4-fold and total concentration increased 13-fold. This increase was not associated with CNS effects, as assessed by psychomotor tests (i.e., subjective assessment of drowsiness and the digital character replacement test).

Simultaneous use of loperamide (single dose of 16 mg) and ketoconazole, a CYP3A4 and P-glycoprotein inhibitor, resulted in a five-fold increase in plasma loperamide concentration. This increase was not associated with an increase in pharmacodynamic action as assessed by pupil size.

Concurrent oral administration of desmopressin resulted in a 3-fold increase in plasma desmopressin concentration, probably due to slowing gastrointestinal motility.

It is expected that drugs with similar pharmacological properties may enhance the effect of loperamide, and drugs that increase the rate of passage through the gastrointestinal tract may reduce the effect of loperamide.

Special Instructions

Treatment of diarrhea with Imodium® is only symptomatic. In those cases where it is possible to identify the cause of diarrhea, appropriate therapy should be carried out.

In patients with diarrhea, especially in children, there may be loss of fluid and electrolytes. In such cases it is necessary to provide appropriate replacement therapy (replenishment of fluids and electrolytes).

Modium® lyophilized tablets contain a source of phenylalanine. It is contraindicated for patients with phenylketonuria.

In case of no effect after 2 days of treatment it is necessary to stop the drug, specify the diagnosis and exclude infectious genesis of

diarrhea. There have been single reports of constipation with increased risk of toxic megacolon in patients with AIDS and infectious colitis of viral and bacterial etiology who were treated with loperamide.

Although data on the pharmacokinetics of loperamide in patients with hepatic impairment are not available, Imodium® should be used with caution in such patients due to delayed presystemic metabolism, as this may lead to relative overdose and toxic CNS damage.

If the drug is out of date or expired – do not throw it in the sewage and on the street! Place the medication in a bag and put it in a trash container. These measures will help protect the environment!

Contraindications

– Acute dysentery and other gastrointestinal infections (caused by Salmonella spp, Campylobacter spp.);

– intestinal obstruction (incl. If necessary to avoid peristalsis inhibition;

– Diverticulosis;

– Acute ulcerative colitis;

– pseudomembranous enterocolitis (diarrhea caused by antibiotics);
<
– 1st trimester of pregnancy;

– lactation period (breastfeeding);

– children under 6 years of age;

– hypersensitivity to loperamide and/or other components of the drug.

Side effects

Adverse reactions are adverse events for which a causal relationship to the use of loperamide should be considered proven based on a comprehensive evaluation of the available information about the adverse event.

In some cases, it is quite difficult to reliably establish a causal relationship between loperamide administration and the occurrence of the listed symptoms.

In addition, since clinical trials are conducted under different conditions, the incidence of adverse reactions in clinical trials of one drug cannot be directly compared with the incidence of adverse reactions in clinical trials of another drug and may not reflect the incidence of adverse reactions in clinical practice.

According to the data of clinical trials adverse reactions observed in ≥1% of patients taking Imodium® in acute diarrhea are: headache, constipation, flatulence, nausea, vomiting.

Unwanted reactions observed in <1% of patients who took Imodium® in acute diarrhea: drowsiness, dizziness, headache, dry mouth, abdominal pain, nausea, vomiting, constipation, abdominal discomfort and bloating, pain in upper parts of abdomen, rash.

Unwanted reactions observed in ≥1 % of patients taking Imodium® in chronic diarrhea: dizziness, flatulence, constipation, nausea.

Unwanted reactions observed in < 1 % of patients who took Imodium® for chronic diarrhea: headache, abdominal pain, dry mouth, abdominal discomfort, dyspepsia.

Overdose

In overdose (including relative overdose due to liver dysfunction) there may appear urinary retention, paralytic ileus, signs of central nervous system (CNS) depression: stupor, coordination disorders, drowsiness, miosis, muscle hypertonus, respiratory depression.

Children may be more sensitive to the effects of loperamide on the CNS than adults.

Therapy.

If symptoms of 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), reapplication of naloxone may be required. Therefore, the patient should be closely monitored for at least 48 hours in order to detect signs of possible CNS depression in time.

Pregnancy use

Application during pregnancy

There is no data that loperamide has teratogenic or embryotoxic effects.

During the first trimester of pregnancy Imodium® Express is contraindicated.

During the II-III trimesters of pregnancy Imodium® Express may be used only after consultation with the attending physician. The drug can be

Use during breast-feeding

A small amount of loperamide may penetrate into the breast milk, therefore Imodium® Express is not recommended for use during breast-feeding.

Similarities

Lopedium, Loperamide-Acri, Imodium, Diara, Loperamide