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

Excipients: lactose monohydrate - 88.15 mg; calcium hydrophosphate dihydrate 46.0 mg; corn starch - 8.0 mg; sodium starch glycolate - 3.5 mg; silicon dioxide colloidal - 0.6 mg; magnesium stearate - 1.75 mg.

Description:White or almost white round tablets, convex on one side, on the other side of the risk, the surface of the tablet is chamfered to the risk.

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:

Linking to the opioid receptors of the intestinal wall, inhibits the release of acetylcholine and prostaglandins, thereby reducing the tone and motility of the smooth muscles of the intestine. Slows down the peristalsis and increases the transit time of intestinal contents. Increases the tone of the anal sphincter. Promotes retention of fecal masses and reduced urge to defecate, reduces the frequency of acts of defecation.

The action comes quickly and lasts 4-6 hours.

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 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 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 of various genesis (including allergic, emotional, radiation, with a change in diet and quality of food, in violation of metabolism and absorption, drug, except for antibiotic-associated diarrhea);
regulation of stool in patients with ileostomy.

Contraindications:

Hypersensitivity to loperamide and / or any of the components of the drug;
children's age till 6 years;
pregnancy (I trimester);
lactation period;
deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;
acute dysentery;
bacterial enterocolitis mediated Salmonella, Shigella and Campylobacter;
acute pseudomembranous enterocolitis (diarrhea against the background of antibiotics);
ulcerative colitis in the acute stage;
intestinal obstruction (including in cases where intestinal motility should be avoided due to the risk of severe consequences such as megacolon or toxic megacolon).

Carefully:

Carefully the drug should be used for liver failure.

Pregnancy and lactation:

The use of the drug in the first trimester of pregnancy is contraindicated.

Before using the drug during pregnancy (II and III trimesters) and lactation it is necessary to consult a doctor.

Although there is no indication of a teratogenic or embryotoxic effect, the drug can be administered during pregnancy only if the intended benefit of therapy for the mother exceeds the potential risk to the fetus.

The drug in small amounts is excreted in breast milk, so the use of the drug during lactation is contraindicated.

Dosing and Administration:

Inside, take the tablets without chewing, drinking 100 ml of water.

Acute diarrhea

adults: Initially, 2 tablets (4 mg) per day are prescribed, followed by 1 tablet (2 mg) after each act of defecation in the case of a loose stool; children from 6 to 18 years old: Initially, 1 tablet (2 mg) per day is prescribed, followed by 1 tablet (2 mg) after each act of defecation in the case of a loose stool.

Chronic diarrhea

This dose is further individually adjusted so that the stool frequency is 1 to 2 times a day, which is usually achieved with a maintenance dose of 1 to 6 tablets per day.

The maximum daily dose in acute and chronic diarrhea for adults is 16 mg (8 tablets). In children, the maximum daily dose is calculated based on body weight (3 tablets per 20 kg body weight) to 8 tablets per day.

To patients of advanced age and with renal failure correction of the dose is not required.

After normalization of the stool or in the absence of stool for more than 12 hours, treatment should be discontinued.

Duration of treatment is 2 days. If symptoms persist for more than 24 hours, consult a doctor immediately.

Prolonged use of the drug is possible only under the supervision of a doctor.

Side effects:

According to the World Health Organization (WHO), adverse reactions are classified according to their developmental frequency as follows: very often (≥ 1/10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, < 1/100), rarely (≥1 / 10000, <1/1000) and very rarely (<1/10000); frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.

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

From the nervous system: often: headache, dizziness; infrequently: drowsiness; rarely: loss of consciousness, stupor, depressed level of consciousness, hypertension, impaired coordination.

From the sense organs: rarely: miosis.

From the digestive system: often: constipation, flatulence, nausea; infrequently: pain or discomfort in the abdomen, dry mouth, vomiting, indigestion, indigestion; rarely: intestinal obstruction, megacolon, glossalgia, bloating.

From the urinary system: rarely: retention of urination.

From the skin and subcutaneous tissues: infrequently: rashes on the skin; rarely: Bullous rash (including polymorphic erythema, toxic epidermal necrolysis and Stevens-Johnson syndrome), angioedema, hives, itching.

Other: rarely: fatigue.

Overdose:

Symptoms: depression of the central nervous system (stupor, impaired coordination, drowsiness, miosis, muscle hypertonia, respiratory depression), urinary retention, intestinal obstruction. Children may be more sensitive to the influence of loperamide on the central nervous system than adults.

In patients with an overdose of loperamide hydrochloride, cardiac complications were observed, such as prolongation of the QT interval, development of torsade de pointes, other serious ventricular arrhythmias, cardiac arrest and fainting. Lethal cases have also been reported.

Treatment: antidote - naloxone; Considering that the duration of action of loperamide is greater than that of naloxone, it is possible to re-administer naloxone.

Medical observation is necessary for at least 48 hours.

Interaction:

With simultaneous application of loperamide and P-glycoprotein inhibitors, CYP3A4 or CYP2C8 (quinidine, ritonavir, itraconazole, gemfibrozil, ketoconazole) it is possible to increase the plasma level of loperamide.

With the simultaneous use of loperamide and desmopressin for oral administration, it is possible to increase the plasma level of the latter.

Preparations having similar pharmacological properties may enhance the effect of loperamide; drugs that enhance the transit of food through the gastrointestinal tract - weaken its effect.

Special instructions:

Lopedium® Used for the symptomatic treatment of diarrhea. In case of establishing the cause of the disease, appropriate therapy should be provided.

Patients suffering from diarrhea, especially in children, may lose fluid and electrolytes. In such cases, compensation of electrolyte loss and rehydration is extremely necessary. If there is no improvement in acute diarrhea after using the drug for 48 hours, consult a doctor.

If in the treatment of diarrhea in patients with acquired immunodeficiency syndrome (AIDS) develops bloating, the drug should be immediately canceled. In very rare cases in patients diagnosed with AIDS suffering from infectious colitis, constipation with a risk of toxic megacolon is possible.

Lepedium® should be used with caution in case of liver failure in order to avoid toxic damage to the central nervous system.

If the treatment develops constipation, bloating or intestinal obstruction, the drug should be discarded.

Indication for patients with diabetes mellitus: each tablet corresponds to 0.01 XE.

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

Care should be taken during the treatment with Lodepium®. When using the drug, there may be a feeling of fatigue, dizziness, drowsiness.

Form release / dosage:Tablets 2 mg.

Packaging:

For 10 tablets in a contour mesh box made of PVC / aluminum foil or propylene / aluminum foil. For 1, 2, 3 or 5 blisters in a cardboard box together with instructions for use.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use the drug after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:П N015863 / 02

Date of registration:18.06.2009 / 10.01.2018

Expiration Date:Unlimited

The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia

Manufacturer: & nbsp

SALUTAS PHARMA, GmbH Germany

Representation: & nbspSANDOZ SANDOZ Switzerland

Information update date: & nbsp02.04.2018

Illustrated instructions

Instructions

Lopedium® (Lopedium®)