Imodium Express tablets 2mg, No. 20

• symptomatic treatment of acute and chronic diarrhea (allergic, emotional, medicinal, radiation genesis, with a change in diet and quality composition of food, with metabolic and absorption disorders);

• as an adjunct drug for infectious diarrhea;

• for the purpose of stool regulation in patients with ileostomy.

The drug is administered orally. The tablet is put on the tongue, within a few seconds it dissolves, after which it is swallowed with saliva without drinking water.

Adults and children over 6 years old

For acute diarrhea, the initial dose is 2 tab. (4 mg) for adults and 1 tab. (2 mg) for children , then 1 tab. (With 2 mg) after each bowel movement in case of loose stools.

For chronic diarrhea, the initial dose is 2 tab. (4 mg) / day for adults and 1 tab. (With 2 mg) for children ; further, the initial dose should be adjusted so that the frequency of normal stool was 1-2 times / day, which is usually achieved with a maintenance dose of 1 to 6 tab. (2-12 mg) / day.

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

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

ImodiumЃ Express is not used in children under 6 years of age .

When treating elderly patients, dose adjustment is not required.

When treating patients with impaired renal function, dose adjustment is not required.

Although there are no pharmacokinetic data in patients with hepatic insufficiency , in such patients ImodiumЃ Express should be used with caution due to the slowed down presystemic metabolism.

Directions for use

Since lyophilisate tablets are quite fragile, they should not be pushed through foil to avoid damage.

In order to get the tablet out of the blister, you must do the following:

• take the foil by the edge and completely remove it from the cell in which the tablet is located;

• gently push down and remove the tablet from the package.

Lyophilisate tablets are white or almost white, round; on one side of the tablet, the presence of a bulge in the center, an uneven rough surface and uneven thinned edges is allowed; on the other side - a chamfer, surface roughness is allowed.

loperamide hydrochloride 2 mg

Excipients : gelatin - 5.863 mg, mannitol - 4.397 mg, aspartame - 0.75 mg, mint flavor - 0.3 mg, sodium bicarbonate - 0.375 mg, purified water - 136.315 mg (removed during lyophilization).

• hypersensitivity to loperamide and / or other components of the drug;

• children under 6 years of age;

• phenylketonuria;

• I trimester of pregnancy;

• lactation period (breastfeeding).

ImodiumЃ Express cannot be used as the main therapy:

• in patients with acute dysentery, which is characterized by bloody stools and high fever;

• in patients with ulcerative colitis in the acute phase;

• in patients with bacterial enterocolitis caused by pathogenic microorganisms, incl. Salmonella spp., Shigella spp. and Campylobacter spp.);

• in patients with pseudomembranous colitis associated with taking broad-spectrum antibiotics.

ImodiumЃ Express should not be used in cases where the slowdown of peristalsis is undesirable due to the possible risk of serious complications, incl. intestinal obstruction, megacolon and toxic megacolon. ImodiumЃ Express should be canceled immediately if constipation, bloating or intestinal obstruction occurs.

It should be used with caution in patients with impaired liver function due to slowed first pass metabolism.

Pharmacotherapeutic group - antidiarrheal agent

Pharmacological properties

Pharmacodynamics

Loperamide, by binding to opioid receptors in the intestinal wall, inhibits the release of acetylcholine and prostaglandins, thus slowing down peristalsis and increasing the time it takes for the contents to pass through the intestine. Increases the tone of the anal sphincter, thereby reducing fecal incontinence and the urge to defecate.

As a result of a clinical study, evidence was obtained that the antidiarrheal effect occurs within one hour after taking a single dose (4 mg).

Pharmacokinetics

Most of loperamide is absorbed in the intestine, but due to active first-pass metabolism, the 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 an inhibitor of CYP3A4 and CYP2C8 isoenzymes. Due to active presystemic metabolism, the concentration of unchanged loperamide in 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 mainly in the feces.

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.

Indications for use

Symptomatic treatment of acute and chronic diarrhea (genesis: 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. Stool regulation in patients with ileostomy.

Contraindications

ImodiumЃ Express lyophilisate tablets should not be used in children under 6 years of age.

ImodiumЃ Express is contraindicated in patients with hypersensitivity to loperamide and / or any of the components of the drug, as well as in the first trimester of pregnancy.

ImodiumЃ Express is not recommended for taking during breastfeeding.

ImodiumЃ Express lyophilisate tablets are contraindicated in patients with phenylketonuria.

ImodiumЃ Express cannot be used as the main therapy:

- in patients with acute dysentery, which is characterized by bloody stools and high fever;

- in patients with ulcerative colitis in the acute stage;

- in patients with bacterial enterocolitis caused by pathogenic microorganisms, including Salmonella, Shigella and Campylobacter;

- in patients with pseudomembranous colitis associated with broad-spectrum antibiotic therapy.

ImodiumЃ Express should not be used in cases where slowing down of peristalsis is undesirable due to the possible risk of developing serious complications, including intestinal obstruction, megacolon and toxic megacolon. ImodiumЃ Express should be canceled immediately if constipation, abdominal distention or intestinal obstruction occurs.

Carefully

ImodiumЃ Express should be used with caution in patients with impaired liver function due to slowed first-pass metabolism.

Application during pregnancy and during breastfeeding

ImodiumЃ Express is not recommended for use during pregnancy and during breastfeeding. In case of diarrhea during pregnancy or breastfeeding, consultation with your doctor is necessary to prescribe appropriate treatment.

Method of administration and dosage

Inside. The tablet is put on the tongue, within a few seconds it dissolves, after which it is swallowed with saliva without drinking water.

Adults and children over 6 years old:

Acute diarrhea : initial dose - 2 tablets (4 mg) for adults and 1 tablet
(2 mg) for children, then 1 tablet (2 mg) after each bowel movement in case of loose stools.

Chronic diarrhea : the initial dose is 2 tablets (4 mg) per day for adults and
1 tablet (2 mg) for children; further, the initial dose should be adjusted so that the frequency of normal stool was 1-2 times a day, which is usually achieved with a maintenance dose of 1 to 6 tablets (2-12 mg) per day.

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 of the child's body weight), but should not exceed 6 tablets (12 mg).

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

Application in children

Do not use ImodiumЃ Express in children under 6 years of age.

Use in elderly patients

No dose adjustment is required when treating elderly patients.

Use in patients with impaired renal function

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

Use in patients with impaired liver function

Although there are no pharmacokinetic data in patients with hepatic insufficiency, in such patients ImodiumЃ Express should be used with caution due to the slowed down presystemic metabolism (see the section 'Special instructions').

APPLICATION INSTRUCTIONS

Since lyophilisate tablets are quite fragile, they should not be pushed through foil to avoid damage.

In order to get the tablet out of the blister, you must do the following:

- take the foil by the edge and completely remove it from the cell in which the tablet is located;

- Press gently from below and remove the tablet from the package.

Side effect

According to clinical trials

Adverse reactions observed in 1% of patients taking ImodiumЃ Express for acute diarrhea: headache, constipation, flatulence, nausea, vomiting.

Adverse reactions observed in 1% of patients taking ImodiumЃ Express for chronic diarrhea: dizziness, flatulence, constipation, nausea.

According to postmarketing studies (spontaneous reports of adverse reactions and clinical or epidemiological studies)

The following adverse reactions were classified as follows: very often (? 10%), often (1%, but <10%), infrequently (0.1%, but <1%), rarely (0.01%, but <0, 1%) and very rarely (<0.01%, including single messages).

Immune system disorders. Rarely: hypersensitivity reactions, anaphylactic reactions, including anaphylactic shock, and anaphylactoid reactions.

Nervous system disorders. Often: headache, dizziness. Uncommon: drowsiness. Rarely: impaired coordination, depression of consciousness, hypertonicity, loss of consciousness, stupor.

Violations of the organ of vision. Rarely: miosis.

Disorders from the gastrointestinal tract. Often: constipation, nausea, flatulence. Uncommon: abdominal pain, abdominal discomfort, dry mouth, epigastric pain, vomiting, dyspepsia. Rarely: bloating, intestinal obstruction (including paralytic intestinal obstruction), megacolon (including toxic megacolon), glossalgia.

Skin and subcutaneous tissue disorders. Uncommon: skin rash. Rarely: angioedema, pruritus, urticaria, bullous rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis, and erythema multiforme.

Kidney and urinary tract disorders. Rarely: urinary retention.

General disorders. Rarely: fatigue.

Overdose

Symptoms

In case of an overdose (including with a relative overdose due to impaired liver function), urinary retention, paralytic intestinal obstruction, constipation, signs of depression of the central nervous system (CNS) (respiratory depression, airway obstruction, vomiting with impaired consciousness, stupor, impaired coordination, drowsiness, miosis, muscle hypertonicity). Children and patients with impaired liver function may be more sensitive to the effect of loperamide on the central nervous system than adults.

Prolonged QT interval and QRS complex and / or severe ventricular arrhythmias, including pirouette tachycardia, have been observed in individuals who deliberately took an excessive dose (40 mg to 240 mg / day) of loperamide hydrochloride; cardiac arrest, fainting (see section 'Special instructions') . There have also been reports of fatalities due to deliberate overdose.

Abuse, misuse and / or overdose of high doses of loperamide can lead to the clinical manifestation of Brugada syndrome.

Therapy

In case of overdose, it is necessary to start ECG monitoring to detect prolongation of the QT interval.

If symptoms of an overdose appear, naloxone can be used as an antidote. Because loperamide lasts longer than naloxone (1-3 hours), reapplication of naloxone may be necessary. Therefore, it is necessary to carefully monitor the patient's condition for at least 48 hours in order to timely detect signs of possible depression of the central nervous system.

Due to the fact that the tactics of overdose relief are constantly changing, it is recommended to contact the Poison Control Center (if available) for the most relevant recommendations for the treatment of an overdose.

Interaction with other medicinal products

According to preclinical studies, loperamide is a substrate for P-glycoprotein. With the simultaneous use of loperamide (single dose of 16 mg) and quinidine or ritonavir, which are inhibitors of P-glycoprotein,

the concentration of loperamide in blood plasma increased 2Ц3 times. The clinical significance of the described pharmacokinetic interaction with P-glycoprotein inhibitors when using loperamide at the recommended doses is unknown.

The simultaneous use of loperamide (single dose of 4 mg) and itraconazole, an inhibitor of the isoenzyme CYP3A4 and P-glycoprotein, led to an increase in the concentration of loperamide in blood plasma by 3-4 times. In the same study, the use of an inhibitor of the isoenzyme CYP2C8, gemfibrozil, led to an approximately 2-fold increase in the concentration of loperamide in blood plasma. When using a combination of itraconazole and gemfibrozil, the peak concentration of loperamide in blood plasma increased 4 times, and the total concentration increased 13 times. This increase was not associated with the effect on the central nervous system, which was assessed by psychomotor tests (i.e., subjective assessment of sleepiness and the test of substitution of digital characters).

The simultaneous use of loperamide (single dose of 16 mg) and ketoconazole, an inhibitor of CYP3A4 and P-glycoprotein, led to a fivefold increase in the concentration of loperamide in blood plasma. This increase was not associated with an increase in pharmacodynamic action as measured by pupil size.

With the simultaneous oral administration of desmopressin, the concentration of desmopressin in the blood plasma increased 3 times, probably due to a slowdown in gastrointestinal motility.

It is expected that drugs with similar pharmacological properties may potentiate the effect of loperamide, and drugs that increase the gastrointestinal tract rate may decrease the effect of loperamide.

special instructions

Treatment of diarrhea with ImodiumЃ Express is only symptomatic. In cases where it is possible to establish the cause of diarrhea, appropriate therapy should be carried out.

In patients with diarrhea (especially in children), fluid and electrolyte loss may occur. In such cases, appropriate replacement therapy (fluid and electrolyte replacement) should be carried out.

ImodiumЃ Express, lyophilisate tablets contain a source of phenylalanine. Patients with phenylketonuria are contraindicated.

If there is no effect after 2 days of treatment, it is necessary to stop taking the drug, clarify the diagnosis and exclude the infectious genesis of diarrhea.

ѕациенты со —ѕ»?ом, принимающие »модиумЃ Ёкспресс дл¤ лечени¤ диареи, должны прекратить прием препарата при первых признаках вздути¤ живота, а также признаках кишечной непроходимости. ѕоступали единичные сообщени¤ о запоре с повышенным риском развити¤ токсического мегаколона у пациентов со —ѕ»?ом и инфекционным колитом вирусной и бактериальной этиологии, которым проводилась терапи¤ лоперамидом.

»модиумЃ Ёкспресс необходимо примен¤ть с осторожностью у пациентов с печеночной недостаточностью, так как это может привести к токсическому воздействию на ?Ќ— вследствие относительной передозировки.

«лоупотребление или неправильное применение лоперамида в качестве заменител¤ опиоидов описывали у лиц с опиоидной зависимостью (см. раздел Ђѕередозировкаї).

—ообщалось об удлинении интервала QT и развитии желудочковой аритмии, включа¤ тахикардию по типу Ђпируэтї, в св¤зи с передозировкой лоперамида, в некоторых случа¤х со смертельным исходом. »модиумЃ Ёкспресс не следует использовать в течение длительного периода времени без наблюдени¤ врача, пациенты не должны превышать рекомендуемую дозу и/или рекомендуемую продолжительность лечени¤.

?сли лекарственное средство пришло в негодность или истек срок годности, не выбрасывайте его в сточные воды и на улицу. ѕоместите лекарственное средство в пакет и положите в мусорный контейнер. Ёти меры помогут защитить окружающую среду!

¬ли¤ние на способность управл¤ть транспортными средствами и механизмами

During the period of treatment with ImodiumЃ Express, one should refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions, since the drug can cause dizziness and other side effects that may affect these abilities.

Storage conditions

Store at temperatures between 15 and 30 ? C.

Keep out of the reach of children.

Store in original packaging.