Indication for the appointment of loperamide. What helps Loperamide? Instructions for use. Composition, physical and chemical properties, price

Country of origin

Product group

Antidiarrheal agent.

Release form

• 10 - cellular contour packs (1) - packs of cardboard. 10 - cellular contour packs (1) - packs of cardboard. 10 capsules in a pack of 10 pcs. - cellular contour packings (1) - packs of cardboard. 10 pieces. - cellular contour packings (2) - packs of cardboard. 20 capsules in a blister pack made of PVC film and aluminum foil printed lacquered Capsules 2 mg - 20 pcs in a pack. Capsules 2 mg. 10 capsules in a blister pack. 1 or 2 blisters, together with instructions for use, are placed in a cardboard pack. pack of 20 capsules pack of 20 tablets

Description of the dosage form

• Tablets Capsules capsule number 4 yellow. The contents of the capsules are white or white with a yellowish tint powder. Yellow capsules, size No. 4; the contents of the capsules are white or white with a yellowish tint powder. Green capsules No. 3. The contents of the capsules are white or white with a yellowish tint powder. Tablets No. 3 hard gelatin capsules, gray capsule body, green capsule cap. The contents of the capsules are white or almost white powder.

pharmachologic effect

Pharmacokinetics

Special conditions

Compound

• 1 caps. loperamide hydrochloride 2 mg Excipients: lactose, corn starch, colloidal silicon dioxide (aerosil), talc, magnesium stearate. The composition of the capsule shell: titanium dioxide, quinoline yellow dye, sunset yellow dye, gelatin. Loperamide hydrochloride 2mg; Auxiliary in-va: lactose, potato starch, calcium stearate Loperamide hydrochloride 2 mg; Auxiliary substances: lactose, potato starch, calcium stearate loperamide hydrochloride 2 mg Loperamide hydrochloride 2 mg. Excipients: lactose monohydrate, corn starch, magnesium stearate, stearic acid, povidone.

Loperamide indications for use

• - symptomatic treatment of acute and chronic diarrhea of ​​various origins (allergic, emotional, medicinal, radiation); - when changing the diet and the qualitative composition of food, in violation of metabolism and absorption; - as an aid in diarrhea of ​​infectious origin; - regulation of stool in patients with ileostomy.

Loperamide contraindications

• Hypersensitivity, intestinal obstruction, acute ulcerative colitis, diverticulosis, diarrhea against the background of acute pseudomembranous enterocolitis, dysentery and other infections of the gastrointestinal tract. Pregnancy (1 trimester), lactation, children under 2 years of age (Loperamide-Akri® in capsules is not prescribed for children under 6 years of age).

Loperamide dosage

• 0.002 g 0.002 g 2 mg 2 mg

Loperamide side effects

• Allergic reactions: skin rash, itching, angioedema, in some cases - erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis. From the digestive system: dryness of the oral mucosa, pain or discomfort in the abdomen, nausea, vomiting, constipation, bloating, intestinal colic, in some cases - intestinal obstruction. From the side of the central nervous system and peripheral nervous system: fatigue, drowsiness, dizziness. Other: urinary retention.

drug interaction

Overdose

Storage conditions

• store in a dry place
• keep away from children
• store in a place protected from light

Synonyms

• Vero-Loperamide, Diarol, Imodium, Lopedium ISO, Loperamide, Loperamide-Ratiopharm, Loperamide-Acri, Loperamide-Rivo, Loperamide-Rivopharm, Loperamide hydrochloride, Loperamide hydrochloride "LH", Neo-enteroseptol, Superilop, Enterobene

1 capsule or tablet includes 2 mg loperamide hydrochloride - active ingredient.

Depending on the manufacturer, the composition of the additional ingredients indicated in the annotation to the drug may differ, but most often they are: aerosil, lactose, corn starch, magnesium stearate and talc.

Release form

Forms of release of the drug are Loperamide tablets or capsules with a different number of pieces per package (usually 10-20 units).

pharmachologic effect

Antidiarrheal .

Pharmacodynamics and pharmacokinetics

The antidiarrheal efficacy of Loperamide is due to the ability of its active ingredient to bind to opioid (opiate) receptor complexes located in the walls of the intestine, as a result of which, under the influence of guanine nucleotides, stimulation occurs adrenergic and cholinergic neurons . The result of inhibition of release and acetylcholine is decreased motility and tone smooth intestinal muscles. Capsules or tablets inhibit intestinal motility and increase the time period during which its contents completely pass through it. The drug also enhances anal sphincter tone , reduces the number of urges to empty the bowels ( defecation ) and contributes to the containment of fecal masses in it. Capsules and tablets for diarrhea begin to act quickly enough and remain effective for 4-6 hours.

The absorption of the drug when taken orally is at the level of 40%. Plasma Cmax is detected after about 150 minutes. Binding to plasma proteins (mostly with) occurs at 97%. The main part of the active ingredient of the drug is amenable to metabolic transformations in the liver by conjugations , does not pass through GEB . T1 / 2, depending on the individual characteristics of the body, ranges from 9-14 hours. The primary route of excretion is with bile, the secondary (in a small amount in the form of conjugated metabolites) is with urine.

Instructions for use Loperamide

Indications for use Loperamide-Stada and Loperamide-Acri, as well as all other drugs with a similar active ingredient, are:

• states chronic and acute developed for various reasons, including its allergic , medicinal , emotional and radiation origin (for symptomatic therapy);
• development situations diarrhea due to a sharp changes food composition and diet in violation of absorption and metabolism ( traveler's diarrhea );
• infectious diarrhea (as an auxiliary remedy);
• the need to regulate stool consistency in patients with ileostomy .

Contraindications

In the clinical practice of using the drug, painful and other conditions of the human body were identified, which are significantly negatively affected by Loperamide capsules and tablets, from which they are prohibited for use when they are detected. Before taking medicines containing this active ingredient, you should ensure that the following conditions are not present, for which appropriate tests and / or tests are indicated.

Contraindications to the use of the drug include:

• intestinal obstruction ;
• personal hypersensitivity to the active and/or additional ingredients;
• in the acute phase;
• (in the first trimester);
• acute;
• subileus;
• pseudomembranous enterocolitis ;
• age up to 4 years (some manufacturers of capsules up to 6 years).

Side effects

• flatulence ;
• (including and / rash skin);
• nausea, vomiting;
• gastralgia ;
• feeling of dryness in the mouth;
• hypovolemia ;
• discomfort/abdominal pain;
• electrolyte disturbances;
• intestinal colic ;
• (rarely);
• intestinal obstruction (rarely).

Instructions for use Loperamide (Method and dosage)

Loperamide tablets, instructions for use

The drug in tablets, for example Vero-Loperamide, prescribed to adult patients in case of diarrhea acute nature at the initial dose of 4 mg. Subsequently, after each liquid defecation , 2 mg, up to the restoration of the normal consistency of the stool.

When chronic diarrhea initially prescribed 2 mg of the drug, with further individual selection of dosages, leading to the frequency of acts hard defecation twice a day. The dose range in this case may vary within 2-12 mg.

For 24 hours, you can take up to 16 mg of drugs as much as possible.

Capsules Loperamide, instructions for use

Instructions for use Loperamide-Acri, Shtada, Grindeks and other companies producing the drug in capsules, recommends that adults with acute diarrhea initial intake of 4 mg and subsequent 2 mg (after each act liquid defecation ).

At chronic diarrhea reception of Loperamide in a daily dosage of 4 mg is shown.

In both cases, the maximum allowable use is 16 mg of the drug in 24 hours.

Instructions for use for children

The drug in tablets is indicated for children 4-8 years old at a daily dosage of 3-4 mg, divided into 3-4 doses (1 mg at a time), for 3 days; children 9-12 years old - at a dose of 2 mg four times in 24 hours, for 5 days.

Given the contraindications for taking capsules, they begin to be prescribed to children from 6 years of age. At acute diarrhea shows the reception of 2 mg of drugs after each liquid defecation , with a maximum daily dose of 8 mg.

At chronic diarrhea , as a rule, appoint 2 mg in 24 hours, with a maximum daily dose of 6 mg per 20 kilograms of weight.

Overdose

In case of an overdose of any of the forms of drugs, the following signs of CNS suppression were noted: incoordination , stupor, respiratory depression , miosis , increased skeletal muscle tone, and intestinal obstruction .

In the caution of use and in the constant monitoring of the possible CNS toxicity patients with disabilities need .

Throughout the treatment diarrhea often seen electrolyte depletion and liquids requiring constant replenishment.

Due to the potential for CNS suppression by the drug, caution should be exercised when performing hazardous work, as well as driving a vehicle.

Analogues

Analogues of the drug are represented by combined drugs , Uzara , Loflatil and Diaremix .

Synonyms

Synonyms for drugs are Loperamide-Acri , diara , Loperamide-Stada , Vero-Loperamide , Loperamide-Lekhim , superilop etc.

Loperamide or Imodium - which is better?

Give an unambiguous answer which of these two drugs is more effective and safer in symptomatic treatment of diarrhea, very difficult, and all because both of these products include the same active ingredient with an identical mass content. It is possible that , produced in Belgium, has a better purification of its active ingredient compared to domestic counterparts, and therefore its action will be more productive and less toxic.

loperamide for children

An unequivocal medical opinion whether it is possible to give children drugs with this active ingredient, for example Loperamide-Stada, from which this drug helps and what risks it can lead to for the child's body, still does not exist. Different manufacturing companies indicate different age limits for taking Loperamide, which range from 2-12 years.

Following the recommendations of domestic manufacturers (described above), the appointment of any of the dosage forms of Loperamide for children under 4 years of age is prohibited. It is also contraindicated to use the drug in the form of capsules for the treatment of children under 6 years of age, from which Loperamide-Acri, Shtada, Grindeks and some other manufacturers, as a rule, releasing the drug in capsules, are not prescribed before reaching this age.

With alcohol

Although the official instructions do not indicate the joint use of Loperamide and alcohol , this combination will definitely have a negative effect on liver and CNS , due to complementary suppressive effects on their function. For this reason, during the antidiarrheal therapy drinking alcohol is not recommended.

Loperamide during pregnancy and lactation

It is absolutely forbidden to use Loperamide during (in the first trimester) and . A relative contraindication, taking into account all the possible risks for the fetus compared to the positive effect on the body of the expectant mother, is the entire subsequent period pregnancy .

Reviews about Loperamide

In the case of the use of the drug according to indications, reviews of Loperamide in 95% of cases are positive and speak of a fairly rapid and effective action of the drug. Only a few patients, belonging to the remaining 5%, experience serious negative consequences of therapy associated with personal hypersensitivity or moderate side effects. Naturally, the ongoing treatment can be successful only if the drug is used for its intended purpose and will be ineffective, and sometimes dangerous, if diarrhea bacterial , secretory , viral and other etiologies. For this reason, prior to antidiarrheal therapy it is best to accurately determine the cause of the pathological process, and based on these data, prescribe the appropriate treatment.

Loperamide price, where to buy

The price of Loperamide in Russian pharmacies is available to any category of patients and, depending on the manufacturer of the drug and the number of tablets, varies between 15-60 rubles. For example, the price Loperamide-Acri No. 20 on average is 50 rubles, buy 20 capsules of the drug produced by Nizhpharm OJSC ( Loperamide-Stada), you can for 35 rubles, and the cost of 20 tablets from Veropharm's diarrhea ( Vero-Loperamide) fluctuates around 15-20 rubles.

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ZdravCity

Diara (loperamide) tab. zhev. 2mg n12JSC Obolenskoye pharm. company

Loperamide tab. 2mg n20 Ozone LLC

Loperamide-Acriquin caps. 2mg n10 JSC Akrikhin

Loperamide-Acriquin caps. 2mg n20 JSC Akrikhin

An antidiarrheal drug used for the symptomatic (i.e., to eliminate the effect, not the cause) treatment of diarrhea, including allergic, medical, emotional, and digestive disorders.

Instructions for use:

Loperamide was first synthesized in 1969 in Belgium. The main contribution to the creation of this drug was made by Paul Janssen, who in 1982 became the winner of the international Gairdner Prize.

Indications for the use of Loperamide - frequent bowel movements and loose stools. 7 years after the discovery, Loperamide managed to become the best-selling diarrhea drug in the United States. In 2013, the World Health Organization added this drug to the list of essential medicines.

As a remedy for diarrhea, loperamide is an effective and affordable medicine. Recommended for adults, except for early pregnant women and nursing mothers. The drug is also recommended for children from 6 years old, but at a dosage reduced by 2 times.

Description of the drug Loperamide is not intended for prescribing treatment without the participation of a physician.

Release form and composition

As excipients in loperamide tablets are used:

• calcium stearate;
• granulac-70;
• potato starch.

Loperamide in yellow capsules, inside - white or yellowish-white powder. Excipients:

• corn starch;
• lactose;
• aerosil;
• magnesium stearate;
• talc.

Pharmacological properties

Loperamide, by binding to the opioid receptors of the intestinal wall (stimulation of choline and adrenergic neurons through guanine nucleotides), reduces the tone and motility of intestinal smooth muscles, slows down the passage of intestinal contents, and reduces the excretion of fluid and electrolytes with feces. Increases the tone of the anal sphincter, helps to retain feces and reduce the urge to defecate. The action comes on quickly and lasts 4-6 hours.

Pharmacokinetics

Instructions for use Loperamide

Symptomatic treatment acute and chronic diarrhea of various genesis (allergic, emotional, medicinal, radiation: when changing the diet and food composition, in violation of metabolism and absorption: as an adjuvant for diarrhea of ​​​​infectious genesis). Stool regulation in patients with ileostomy.

Method of application and dosage

Inside, without chewing, drinking water.

Capsules

Tablets

children

Side effect

• allergic reactions (skin rash);
• drowsiness or insomnia;
• dizziness;
• hypovolemia;
• electrolyte disturbances;
• dryness of the oral mucosa;
• intestinal colic;
• gastralgia;
• pain or discomfort in the abdomen;
• nausea;
• vomit;
• flatulence.

Rarely - urinary retention, extremely rarely - intestinal obstruction.

Contraindications for use

• hypersensitivity to the drug;
• lactose intolerance;
• lactase deficiency or glucose-galactose malabsorption;
• diverticulosis;
• intestinal obstruction;
• ulcerative colitis in the acute stage;
• diarrhea against the background of acute pseudomembranous enterocolitis;
• dysentery and other infections of the gastrointestinal tract;
• pregnancy (I trimester);
• lactation period;
• loperamide capsules are not prescribed for children under 6 years of age.

Application for violations of liver function

Liver failure. In patients with impaired liver function, careful monitoring for signs of CNS toxicity is necessary.

Use during pregnancy and lactation

Contraindicated in the first trimester of pregnancy.

In the II and III trimesters of pregnancy, Loperamide is prescribed in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus. Since a small amount of Loperamide is found in breast milk, not recommended during breastfeeding.

loperamide and alcohol

A side effect of loperamide is increased drowsiness and dizziness. Under the influence of ethanol, these effects are enhanced and cause significant discomfort to the patient. Recommended avoid sharing loperamide and alcohol.

special instructions

Overdose

Symptoms

• stupor;
• lack of coordination;
• drowsiness;
• miosis;
• muscle hypertension;
• respiratory depression;
• intestinal obstruction.

Treatment

The antidote is naloxone. Given that the duration of action of loperamide is longer than that of naloxone, repeated administration of the latter is possible.

Symptomatic treatment

• Activated carbon;
• gastric lavage;
• artificial lung ventilation.

Medical supervision is required within 48 hours.

Interaction with other drugs

With simultaneous use with colestyramine, the effectiveness of Loperamide is sometimes reduced. When used together with ritonavir, co-trimoxazole, the bioavailability of loperamide increases. Simultaneous use with opioid analgesics increases the risk of severe constipation.

Terms and conditions of storage

Terms of dispensing from pharmacies

The drug is approved for use without a prescription.

Loperamide's analogs

Loperamide analogs that contain the same main component in the base:

• Diara;
• Diarol;
• Imodium;
• Laremid;
• Lopedium;
• Loperacap;
• Loperamide Grindeks;
• loperamide-acry;
• loperamide hydrochloride;
• Superilop;
• Enterobene.

Prices for Loperamide

The price of Loperamide is on average.

Loperamide is a symptomatic antidiarrheal drug indicated for the treatment of acute and chronic non-infectious diarrhea.

The active substance - loperamide hydrochloride - reduces the motor activity of the gastrointestinal tract and inhibits the movement of intestinal contents.

Loperamide hydrochloride binds to opiate receptors in the intestinal wall, resulting in inhibition of the release of acetylcholine and prostaglandins. It slows down propulsive intestinal motility, and also increases the time it takes for intestinal contents to pass through the digestive tract and the ability of the intestinal wall to absorb fluid.

Loperamide increases the tone of the anal sphincter, thereby reducing fecal incontinence and the urge to defecate.

The elimination half-life is approximately 11 hours with a range of 9-14 hours. Excretion of unchanged active substance and its metabolites occurs mainly with feces.

Loperamide is not intended for the initial treatment of severe diarrhea that is accompanied by a decrease in fluid and electrolyte levels. Particularly in children, it is desirable to compensate for this loss by prescribing parenteral or oral replacement therapy.

If there is no effect after 2 days of therapy, you should consult a doctor. During the treatment of diarrhea, it is necessary to replenish the loss of fluid and electrolytes.

Indications for use

What helps Loperamide? According to the instructions, the drug is prescribed in the following cases:

• conditions of chronic and acute diarrhea developed for various reasons, including its allergic, medicinal, emotional and radiation origin (for symptomatic therapy);
• situations of development of diarrhea due to a sharp change in the composition of food and diet in violation of absorption and metabolism (traveler's diarrhea);
• infectious diarrhea (as an adjuvant treatment);
• the need to regulate stool consistency in patients with ileostomy.

Instructions for use Loperamide, dosage

Inside (capsules - without chewing, drinking water; lingual tablet - on the tongue, it disintegrates within a few seconds, after which it is swallowed with saliva without drinking water).

Standard dosages of Loperamide according to the instructions for use:

• in acute diarrhea, 2 mg after each act of defecation. In this case, the first dose should be 4 mg;
• in chronic diarrhea, the dose of the drug is selected so that the frequency of stool does not exceed 1-2 times a day. In this case, the first dose should be 2 mg.

For adults, the maximum daily dose of the drug should not exceed 16 mg.

Dosages of loperamide for children:

• at the age of 2 to 5 years, it is prescribed at a dose of 100 mcg / kg 2-3 times a day;
• at the age of 6-8 years, it is prescribed 2 times a day, 2 mg;
• children 9-12 years old are prescribed 2 mg three times a day. If diarrhea continues, then the drug is prescribed 2 mg after each act of defecation. In this case, the maximum daily dose of 6 mg per 20 kg of body weight should not be exceeded.

In chronic diarrhea, children over 5 years of age are prescribed in a daily dose of 2 mg.

If there is no stool for more than 12 hours and when it normalizes, the drug is canceled.

Side effects

The instruction warns of the possibility of developing the following side effects when prescribing Loperamide:

• from the nervous system: drowsiness, dizziness, fatigue;
• from the digestive tract: dry mouth, intestinal colic, nausea, pain or discomfort in the abdomen, constipation or bloating, vomiting, intestinal obstruction;
• allergic reactions: hives or skin rash; extremely rarely - bullous rash or anaphylactic shock;
• other effects: in rare cases - urinary retention.

Contraindications

Loperamide is contraindicated in the following cases:

• hypersensitivity, intestinal obstruction, diverticulosis, acute ulcerative colitis, pseudomembranous colitis caused by broad-spectrum antibiotics;
• other conditions in which inhibition of intestinal motility is unacceptable;
• acute dysentery (especially with the presence of blood in the stool and accompanied by fever);
• children's age (up to 2 years).

Overdose

In case of an overdose, the following symptoms may appear: depression of the central nervous system (stupor, incoordination, drowsiness, miosis, muscle hypertension, respiratory depression), intestinal obstruction.

Assign a specific opiate antidote - naloxone (0.4 mg / ml IV repeatedly, at 2-3 minute intervals); clinical observation within 48 hours.

drug interaction

Colestyramine can reduce the effectiveness of loperamide capsules or tablets.

When combined with ritonavir or co-trimoxazole, the bioavailability of the drug increases. This is due to inhibition of the metabolism of the active substance of the drug when passing through the liver.

Loperamide analogues, price in pharmacies

If necessary, you can replace Loperamide with an analogue in terms of therapeutic effect - these are drugs:

1. Lopedium,
2. Loperamide-Akrikhin,
3. Imodium Plus,
4. Uzara,
5. Loflatil,
6. Diaremix.

ATX code:

• diara,
• imodium,
• laremid,
• Loperacal,
• Superilol.

When choosing analogues, it is important to understand that the instructions for use of Loperamide, the price and reviews of drugs of similar action do not apply. It is important to consult a doctor and not to make an independent replacement of the drug.

Price in Russian pharmacies: Loperamide 2 mg tablets 20 pcs. - from 7 to 12 rubles, capsules 2 mg 20 pcs. - from 40 to 49 rubles, according to 792 pharmacies.

Store in a dry, dark place and out of the reach of children at a temperature not exceeding +25°C. Shelf life - 2 years.

What do the reviews say?

According to doctors' reviews, Loperamide is an inexpensive, affordable, effective and fast-acting drug.

Users note that it does not help with diarrhea of ​​​​infectious etiology. The development of side effects is rarely reported.

Name:

Loperamide (Loperamide)

Pharmacological
action:

The drug has antidiarrheal (antidiarrheal) action. Reduces intestinal tone and motility by inhibiting (suppressing) the release of acetylcholine and prostaglandins, increases the tone of the anal sphincter (a circular muscle that compresses the anus).

Indications for
application:

Symptomatic treatment acute and chronic diarrhea due to changes in the diet and qualitative composition of food, metabolic and absorption disorders, as well as allergic, emotional, medicinal, radiation genesis; with diarrhea of ​​​​infectious genesis - as an adjuvant; ileostomy (in order to reduce the frequency and volume of stools, as well as to give density to its consistency).

Mode of application:

inside.
Adults at the beginning of treatment, 4 mg, and after each shapeless stool, 2 mg (but not more than 16 mg per day). The drug can be prescribed in drops: the first dose is 60 drops, then 30 drops after each liquid stool; maximum dose- 30 drops 6 times a day. In chronic diarrhea, adults are prescribed 4 mg.
Children over 8 years old 2 mg, but not more than 8 mg per day. Children from 2 to 8 years old- at the rate of 0.004 mg/kg.
The drug can be prescribed in drops: the first dose is 30 drops, then 30 drops 3 times a day; maximum dose - 30 drops 4 times a day
For chronic diarrhea children over 5 years old prescribe the drug in a daily dose of 30 drops or 2 mg.
Children aged 2-5 years the drug can be administered as a syrup at a dose of 1 mg per 10 kg of body weight; the multiplicity of reception -2-3 times a day. If the stool normalizes or if there is no stool for more than 12 hours, the drug should be discontinued.

Do not exceed a 2-day duration of use, as severe constipation may develop. If after 2 days of taking the diarrhea does not stop, you should consult a doctor.

Side effects:

Adverse effects noted during clinical studies of loperamide hydrochloride are difficult to distinguish from symptoms associated with diarrhea syndrome; usually these effects were mild and passed on their own; in most cases they were observed in the treatment of chronic diarrhea. These side effects included the following: hypersensitivity reactions, incl. skin rash, urticaria, extremely rarely - anaphylactic shock and bullous rash, including toxic epidermal necrolysis (in most cases, patients took other drugs that could cause adverse reactions or contribute to their occurrence), abdominal pain, bloating or gastric discomfort, nausea, vomiting , constipation, fatigue, drowsiness, dizziness, dry mouth.

There have been rare reports of cases of paralytic ileus in post-marketing studies. Most of these reports were recorded in acute dysentery, overdose, in children under 2 years of age.

Contraindications:

- hypersensitivity, intestinal obstruction, diverticulosis, acute ulcerative colitis, pseudomembranous colitis caused by broad-spectrum antibiotics;
- other conditions in which inhibition of intestinal peristalsis is unacceptable;
- acute dysentery(especially with the presence of blood in the stool and accompanied by increased body temperature);
- childhood(up to 2 years).

Interaction
other medicinal
by other means:

Colestyramine it is recommended to appoint no later than 2 hours before taking loperamide. Possible pharmacological interaction of loperamide with drugs that stimulate intestinal motility ( bethanechol, cisapride, metoclopramide, erythromycin), so it is not recommended to prescribe them at the same time.