Imodium - instructions for use, doses, side effects, contraindications

Composition of cap capsule: titanium dioxide (E 171) 1.6%, iron oxide black (E 172) 0.4%, iron oxide red (E 172) 1.0%, iron oxide yellow (E 172) 0.8%, gelatin to 100 %.

Capsule body composition: indigo carmine (E 132) 0.03%, titanium dioxide (E 171) 1.0%, iron oxide black (E 172) 0.0075%, iron oxide yellow (E 172) 0.085%, gelatin up to 100%.

Description:

Hard gelatin capsules (size 4), consisting of a body of light green color and a cap of brown color. The contents of the capsules are white powder.

Pharmacotherapeutic group:Antidiarrhoeic remedy

ATX: & nbsp

A.07.D.A Drugs that reduce the peristalsis of the digestive tract

A.07.D.A.03 Loperamide

Pharmacodynamics:

Loperamide, by binding to opioid receptors in the intestinal wall, suppresses the release of acetylcholine and prostaglandins, thus slowing down the peristalsis and increasing the transit time of the contents through the intestine. Increases the tone of the anal sphincter, thereby reducing the incontinence of stool and the urge to defecate.

Pharmacokinetics:

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

Pre-clinical studies indicate that loperamide is a substrate of P-glycoprotein. Binding of loperamide with blood plasma proteins (mainly with albumin) is 95%.

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

In humans, the half-life of loperamide is an average of 11 hours, varying from 9 to 14 hours. Unchanged loperamide and its metabolites are excreted mainly with feces.

Pharmacokinetic studies in children have not been conducted. It is expected that the pharmacokinetics of loperamide and its interaction with other drugs will be similar to those in adults.

Indications:

Symptomatic treatment of acute and chronic diarrhea (genesis: allergic, emotional, drug, radiation, with a change in diet and qualitative composition of food,with metabolic and absorption disorders). As an auxiliary medicine for diarrhea of infectious genesis. Regulation of stool in patients with ileostomy.

Contraindications:

Imodium ® capsules should not be used in children younger than 6 years of age.

Imodium® is contraindicated in patients with hypersensitivity to loperamide and / or any of the components of the drug.

Imodium ® capsules are contraindicated in case of deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

Imodium® is contraindicated in the first trimester of pregnancy.

Imodium® is not recommended for breastfeeding.

Imodium® can not be used as a primary therapy:

- in patients with acute dysentery, which is characterized by a stool with an admixture of blood 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.

Imodium® should not be used in cases,when the slowing of peristalsis is undesirable because of the possible risk of serious complications, including intestinal obstruction, megacolon and toxic megacolon. Imodium ® should be immediately discontinued if there is constipation, bloating, or intestinal obstruction.

Carefully:

Imodium® should be used with caution in patients with impaired hepatic function due to delayed presystemic metabolism.

Pregnancy and lactation:

Application during pregnancy

The data that loperamide has teratogenic or embryotoxic effects, are absent. Imodium® is contraindicated in the first trimester of pregnancy. In the period of pregnancy Imodium ® is not recommended to be used without consultation with the attending physician. The drug can be prescribed only if the intended benefit of therapy for the mother exceeds the potential risk to the fetus.

Application during lactation

A small amount of loperamide can penetrate into breast milk, so Imodium® is not recommended for breastfeeding.

Dosing and Administration:

Inside, washing down with water.

Adults and children over 6 years of age:

Acute diarrhea: the initial dose is 2 capsules (4 mg) for adults and 1 capsule (2 mg) for children, then 1 capsule (2 mg) after each act of defecation in the case of a loose stool.

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

The maximum daily dose for acute and chronic diarrhea in adults is 8 capsules (16 mg); the maximum daily dose in children is calculated based on body weight (3 capsules per 20 kg body weight of the baby), but should not exceed 8 capsules (16 mg).

When the chair is normalized or if there is no stool for more than 12 hours, the drug is canceled.

Use in children

Do not use Imodium in children under 6 years of age.

Application in elderly patients

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

Use in patients with impaired renal function

In the treatment of patients with impaired renal function, dose adjustment is not required.

Use in patients with impaired hepatic function

Although pharmacokinetic data are not available in patients with hepatic impairment,In such patients, Imodium® should be used with caution because of delayed presystemic metabolism (see section "Special instructions").

Side effects:

Undesirable reactions are undesirable phenomena, for which a causal relationship with loperamide is to be proven on the basis of a comprehensive assessment of the available information on the undesirable phenomenon. In some cases, it is rather difficult to establish reliably the causal relationship between the administration of loperamide and the occurrence of the listed symptoms. In addition, because clinical trials are conducted under different conditions, the incidence of adverse reactions in clinical trials of one drug can not be directly compared with the incidence of adverse reactions in clinical studies of another drug and may not reflect the incidence of unwanted reactions in clinical practice.

According to clinical studies

Unwanted reactions observed in ≥1% of patients taking Imodium ® in acute diarrhea: headache, constipation, flatulence, nausea, vomiting.Undesirable reactions observed in <1% of patients taking Imodium ® in acute diarrhea: drowsiness, dizziness, headache, dry mouth, abdominal pain, nausea, vomiting, constipation, discomfort and bloating, upper abdominal pain, rash .

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

Undesirable reactions observed in <1% of patients taking Imodium ® in chronic diarrhea: headache, abdominal pain, dry mouth, abdominal discomfort, dyspepsia.

According to spontaneous reports of adverse reactions

The following undesirable reactions were classified as follows: very frequent (≥10 %), frequent (≥1%, but <10%), not frequent (≥0.1%, but <1%), rare (≥0.01%, but <0.1%) and very rare (<0.01%, including single messages).

Impaired immune system. Very rarely: reactions hypersensitivity, anaphylactic reactions, including anaphylactic shock, and anaphylactoid reactions.

Violations from the nervous system. Very rare: violation coordination, depression, hypertonus, loss of consciousness, drowsiness, stupor.

Disorders from the side of the organ of sight. Very rarely: miosis.

Disorders from the gastrointestinal tract. Very rarely: intestinal obstruction (including paralytic intestinal obstruction), megacolon (including toxic megacolon).

Disturbances from the skin and subcutaneous tissues. Very rarely: angioedema, bullous rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis and erythema multiforme, pruritus, urticaria.

Disorders from the kidneys and urinary tract. Very rarely: retention of urine.

General disorders. Very rarely: fatigue.

Overdose:

Symptoms

In case of overdose (including a relative overdose due to a violation of liver function), urine retention, intestinal obstruction, signs of central nervous system (CNS) depression: stupor, coordination disorder, drowsiness, miosis, hypertonic muscle, respiratory depression. Children may be more sensitive to the influence of loperamide on the central nervous system than adults.

Therapy

When symptoms of an overdose appear as an antidote, you can use naloxone. Since the duration of action of loperamide is longer than naloxone (1-3 hours), it may be necessary to re-use naloxone.Therefore, it is necessary to carefully monitor the patient's condition for at least 48 hours in order to timely detect signs of possible CNS depression.

Interaction:

According to preclinical research loperamide is a substrate of P-glycoprotein. With the simultaneous use of loperamide (once in a dose of 16 mg) and quinidine or ritonavir, which are inhibitors of P-glycoprotein, 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 in the recommended doses is unknown.

Simultaneous use of loperamide (once in a dose of 4 mg) and itraconazole, inhibitor of 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 isoenzyme inhibitor CYP2C8, gemfibrozil, led to an increase in the concentration of loperamide in blood plasma approximately 2 times. When using the combination of itraconazole and gemfibrozil, the peak concentration of loperamide in the blood plasma increased in 4 times, and the total concentration - 13 times.This increase was not related to the effect on the CNS, which was assessed by psychomotor tests (i.e., subjective assessment of drowsiness and a test for the replacement of digital symbols). Simultaneous application of loperamide (once in a dose of 16 mg) and ketoconazole, inhibitor of isoenzyme 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 the pharmacodynamic effect, estimated by the size of the pupil.

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

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

Special instructions:

The treatment of diarrhea with Imodium® is only symptomatic. In those cases where it is possible to establish the cause of diarrhea, appropriate therapy is necessary.

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

In the absence of effect after 2 days of treatment, it is necessary to stop taking the drug, clarify the diagnosis and exclude the infectious genesis of diarrhea. Patients with AIDS who take Imodium ® for the treatment of diarrhea should stop taking the drug at the first sign of bloating. There were isolated reports of constipation with an increased risk of toxic megacolon in patients with AIDS and infectious colitis of viral and bacterial etiology, which was treated with loperamide.

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

If the medicine has become unusable or the expiration date has expired, do not throw it into the waste water and into the street! Place the drug in a bag and put it in the trash. These measures will help protect the environment!

Effect on the ability to drive transp. cf.and fur:

In the period of treatment with Imodium®, you should refrain from driving vehicles and practicing other potentially dangerous activities that require increased concentration and speed of psychomotor reactions, as the drug may cause dizziness and other side effects that may affect these abilities.

Form release / dosage:

Capsules, 2 mg.

Packaging:

For 6, 8, 12 or 20 capsules in a blister of PVC and aluminum foil. 1 blister with instructions for medical use in a pack

Storage conditions:

Store at temperatures between 15 and 30 ° C.

Keep out of the reach of children.

Shelf life:

5 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:П N016070 / 01

Date of registration:23.10.2009 / 28.02.2014

Expiration Date:Unlimited

The owner of the registration certificate:Johnson & Johnson, LLC Johnson & Johnson, LLC Russia

Manufacturer: & nbsp

JANSSEN-CILAG, S.A. France

Information update date: & nbsp07.11.2017

Illustrated instructions

Instructions

Imodium® (Imodium®)