Antidiarrheal drug for adults and children loperamide. Loperamide - instructions for use Loperamide recipe in Latin

If constipation or bloating develops during treatment, Loperamide-Akrikhin should be discontinued. In patients with impaired liver function, careful monitoring for signs of toxic damage to the central nervous system is necessary. During the treatment of diarrhea, it is necessary to replace the loss of fluid and electrolytes.

Detailed instructions for use are published on this page. Loperamide. The available dosage forms of the drug (tablets and capsules 2 mg), as well as its analogues, are listed. Information is provided on the side effects that Loperamide can cause and on interactions with other medications. In addition to information about the diseases for the treatment and prevention of which the drug is prescribed (diarrhea or diarrhea), administration algorithms, possible dosages for adults and children are described in detail, and the possibility of use during pregnancy and breastfeeding is clarified. The abstract for Loperamide is supplemented with reviews from patients and doctors. Composition of the drug.

Instructions for use and dosage

Orally, without chewing, with water.

For adults with acute and chronic diarrhea, 2 capsules (0.004 g) are initially prescribed, then 1 capsule (0.002 g) after each bowel movement in case of loose stools. For acute diarrhea, children over 6 years of age are prescribed 1 capsule (0.002 g) after each bowel movement in case of loose stools.

Maximum daily dose. For acute and chronic diarrhea in adults - 8 capsules (0.016 g); for children - 3 capsules (0.006 g).

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

Compound

Loperamide hydrochloride + excipients.

Release forms

Capsules 2 mg.

Tablets 2 mg.

Loperamide- antidiarrheal agent. Reduces the tone and motility of intestinal smooth muscles, apparently due to binding to opioid receptors in the intestinal wall. Inhibits the release of acetylcholine and prostaglandins, reducing peristalsis and increasing the transit time of contents through the intestines.

Increases the tone of the anal sphincter. The action occurs quickly and lasts 4-6 hours.

Pharmacokinetics

Absorption - 40%. Does not penetrate the blood-brain barrier. Almost completely metabolized in the liver by conjugation. Excreted primarily by the intestines; a small part is excreted by the kidneys (in the form of conjugated metabolites).

Indications

• symptomatic treatment of acute and chronic diarrhea of ​​various origins (allergic, emotional, medicinal, radiation: with changes in diet and quality food composition, with metabolic and absorption disorders: as an adjuvant for diarrhea of ​​infectious origin);
• regulation of stool in patients with ileostomy.

Contraindications

• hypersensitivity to the drug;
• lactose intolerance;
• lactase deficiency or glucose-galactose malabsorption;
• diverticulosis;
• intestinal obstruction;
• ulcerative colitis in the acute stage;
• diarrhea due to acute pseudomembranous enterocolitis;
• as monotherapy - dysentery and other gastrointestinal infections;
• pregnancy (1st trimester);
• lactation period;
• Loperamide capsules are not prescribed to children under 6 years of age.

special instructions

If there is no effect after 2 days of using Loperamide, you should consult a doctor.

If constipation or bloating develops during treatment, loperamide should be discontinued. In patients with impaired liver function, careful monitoring for signs of toxic damage to the central nervous system is necessary.

During the treatment of diarrhea, it is necessary to replace the loss of fluid and electrolytes.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Side effect

• allergic reactions (skin rash);
• drowsiness or insomnia;
• dizziness;
• dryness of the oral mucosa;
• intestinal colic;
• abdominal pain or discomfort;
• nausea, vomiting;
• flatulence;
• urinary retention;
• intestinal obstruction.

Drug interactions

It is believed that when used concomitantly, cholestyramine may reduce the effectiveness of loperamide.

When used simultaneously with co-trimoxazole and ritonavir, the bioavailability of loperamide increases, which is due to inhibition of its metabolism during the “first pass” through the liver.

In case of an overdose of loperamide, naloxone is used as an antidote.

Analogues of the drug Loperamide

Structural analogues of the active substance:

• Vero Loperamide;
• Diara;
• Diarol;
• Imodium;
• Laremid;
• Lopedium;
• Loperacap;
• Loperamide Grindeks;
• Loperamide Acri;
• Loperamide hydrochloride;
• Superilop;
• Enterobene.

Use in children

The drug in capsules is contraindicated in children under 6 years of age.

Use during pregnancy and breastfeeding

Contraindicated in the 1st trimester of pregnancy.

In the 2nd and 3rd trimesters of pregnancy, Loperamide can be prescribed in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

Since small amounts of Loperamide are found in breast milk, use during breastfeeding is not recommended.

(lat. Loperamide) is an antidiarrheal drug.

Chemical compound: 4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-alpha,alpha-diphenyl-1-piperidine butanamide (as hydrochloride). The empirical formula is C 29 H 33 ClN 2 O 2. Phenylpiperdine derivative.

Loperamide is the international nonproprietary name (INN) of the drug. According to the pharmacological index, loperamide belongs to the group “Antidiarrheals”. According to ATC - to the group “A07 Antidiarrheal drugs”, subgroup “Drugs that reduce gastrointestinal motility” and has code A07DA03.

"" (and " Loperamide hydrochloride», « Loperamide-Acree», « Vero-Loperamide"), in addition, is the trade name of a number of drugs produced by pharmaceutical enterprises in the republics of the former USSR and India. Loperamide is available in the form of tablets or capsules (containing 2 mg of loperamide hydrochloride). Capsules, as excipients, contain: corn starch, lactose, talc, aerosil and magnesium stearate. The price for such a drug starts (as of September 2009) at approximately 13 rubles per package.

Loperamide is used for acute diarrhea of ​​a non-infectious nature, as well as for infectious diarrhea of ​​mild and moderate severity. Loperamide is the drug of choice for the treatment of traveler's diarrhea. The effect of the drug occurs quickly and lasts 4-6 hours. Loperamide inhibits intestinal motility, increases the tone of the anal sphincter, thereby reducing the urge to defecate and retains feces in the rectum.

Loperamide stimulates opioid mu receptors in the intestinal wall, resulting in inhibition of the release of acetylcholine and prostaglandins, which, in turn, leads to a decrease in propulsive intestinal motility and an increase in the transit time of its contents. This increases the absorption time of water and electrolytes, reduces their loss and reduces the loss and increases the time of the protective action of immunoglobulins, which are released into the intestinal lumen during acute intestinal diarrhea. Loperamide increases the tone of the anal sphincter, resulting in a decrease in the frequency and severity of the urge to defecate. Loperamide reduces mucus hypersecretion in the colon, in addition, it has an antisecretory effect, which is realized through both opioid and non-opioid receptors. Loperamide, due to the inhibition of calmodulin and blockade of calcium channels and due to the suppression of intestinal peptides and neurotransmitters that increase the permeability of plasma membranes, affects intestinal secretion (Ivashkin V.T.).

Currently, loperamide is the most effective drug with antidiarrheal action, and its antidiarrheal effect is due to inhibition of both the motor component of diarrhea and intestinal secretion. Loperamide belongs to the group of synthetic opiates, but binds only to peripheral opiate receptors, does not have a systemic narcotic effect and does not penetrate the blood-brain barrier. This is explained by the peculiarities of its biotransformation during the first passage through the liver and the absence of active metabolites in the blood. Loperamide can be successfully used for motor diarrhea with increased peristalsis (irritable bowel syndrome (IBS) and functional diarrhea), but is not effective for diabetic enteropathy, scleroderma, amyloidosis. Moreover, in these situations it can worsen diarrhea. For secretory diarrhea, loperamide is also very effective due to its antisecretory opiate-like effect. For infectious diarrhea, the drug should be prescribed with caution, since the retention of the infectious agent in the body increases diarrhea and intoxication. Loperamide relieves diarrhea well in Crohn's disease, but it is not recommended for use in ulcerative colitis due to its blocking effect on the tone of the intestinal wall and the risk of developing toxic dilatation (Belousova E.A., Zlatkina A.R.).

Loperamide is the drug of choice for hypermotor variants of irritable bowel syndrome, so-called functional diarrhea, which, unlike organic (for example, infectious) diarrhea, is observed mainly in the morning, is associated with psycho-emotional factors and is not accompanied by pathological changes in stool tests. Loperamide inhibits the release of acetylcholine and prostaglandins in the colon and reduces its motor activity. The dose of loperamide is selected individually and, depending on the consistency of the stool, is from 1 to 6 capsules of 2 mg per day (Sheptulin A.A.).

Loperamide, as a drug that inhibits intestinal motility, is recommended for use in drug therapy for diabetic diarrhea (Kolesnikova E.V.). For anorectal dysfunction, which is a complication of diabetes mellitus, symptomatic therapy with loperamide will have a positive result and reduce the symptoms of urgency (Leites Yu.G., Galstyan G.R., Marchenko E.V.).

Professional medical publications addressing the effects of loperamide on the gastrointestinal tract :

• Belousova E.A., Zlatkina A.R. Diarrhea syndrome in the practice of a gastroenterologist: pathophysiology and differentiated approach to treatment. Pharmateka. 2003, No. 10, p. 65-71.


• Sheptulin A.A. Diagnosis and treatment of gastrointestinal motility disorders.


• Kolesnikova E.V. Endocrine diseases and pathology of the digestive organs // Journal “Mystery Likuvannya”. Ukraine. - 2006. - 8(34).


• Leites Yu.G., Galstyan G.R., Marchenko E.V. Gastroenterological complications of diabetes mellitus. Consilium-Medicum. 2007. No. 2.


• The FDA warns of serious cardiac problems with high doses of the antidiarrheal drug loperamide (Imodium), including abuse and misuse. June 7, 2016


• FDA limits packaging size for antidiarrheal drug loperamide (Imodium) to increase safety of its use FDA limits packaging size for antidiarrheal drug loperamide (Imodium) to increase safety of its use. January 30, 2018

• non-infectious diarrhea of ​​various forms and different origins: acute and chronic, allergic, emotional, medicinal, radiation, due to changes in diet and type of food, due to metabolic and absorption disorders
• infectious diarrhea (as an adjuvant)
• regulation of stool in patients with ileostomy

Directions for use and dosage:

For acute diarrhea, the use of the lingual form of loperamide is preferable. The lingual tablet dissolves on the tongue within 2-3 seconds, the required concentration in the body is achieved within one hour, which is faster than when using other dosage forms. The lingual tablet does not require drinking water and can be used in patients with difficulty swallowing and an increased gag reflex.

For chronic diarrhea and IBS, the usual dosage form of loperamide is prescribed. A promising drug is with the complex active substance loperamide + simethicone, which effectively absorbs gases in the intestines.

WHO position on the use of loperamide in the treatment of diarrhea in children :

The following drugs containing loperamide are registered in the USA: Diamode, Imodium A-D, Imodium A-D EZ Chews, Imodium A-D New Formula, Kao-Paverin, Kaopectate 1-D, Imodium, Maalox Anti-Diarrheal, Pepto Diarrhea Control, Imotil, Diar-Aid. In the United States, medications, depending on the content of loperamide, can be either over-the-counter or prescription.

Instructions from different loperamide manufacturers

• for Russia: “Instructions for use of the drug Loperamide-Akri”, JSC “Akrikhin”
• for Ukraine (in Russian): “Instructions for medical use of the drug Loperamide”, OJSC “Kievmedpreparat”

Loperamide has contraindications, side effects and application features; consultation with a specialist is necessary.

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 the suppression of the release of acetylcholine and prostaglandins. Slows down propulsive intestinal motility, and also increases the time of passage of intestinal contents 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 half-life is approximately 11 hours with a range of 9-14 hours. Excretion of the unchanged active substance and its metabolites occurs mainly in the feces.

Loperamide is not intended for the initial treatment of severe diarrhea that is accompanied by decreased fluid and electrolyte levels. In particular, in children, it is advisable to compensate for this loss by prescribing replacement therapy parenterally or orally.

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

Indications for use

What does Loperamide help with? According to the instructions, the drug is prescribed in the following cases:

• conditions of chronic and acute diarrhea that have developed for various reasons, including its allergic, drug, emotional and radiation origin (for symptomatic therapy);
• situations of development of diarrhea due to a sharp change in food composition and diet with impaired 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 of Loperamide, dosage

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

Standard dosages of Loperamide according to the instructions for use:

• for acute diarrhea, 2 mg after each act of defecation. In this case, the first dose should be 4 mg;
• for 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.

Loperamide dosages 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, 2 mg is prescribed 2 times a day;
• Children 9-12 years old are prescribed 2 mg three times a day. If diarrhea continues, the drug is prescribed 2 mg after each bowel movement. In this case, the maximum daily dose of 6 mg per 20 kg of body weight should not be exceeded.

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

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

Side effects

The instructions warn about the possibility of developing the following side effects when prescribing Loperamide:

• from the nervous system: drowsiness, dizziness, increased fatigue;
• from the gastrointestinal 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 taking broad-spectrum antibiotics;
• other conditions in which inhibition of intestinal motility is unacceptable;
• acute dysentery (especially with blood in the stool and accompanied by elevated body temperature);
• children's age (up to 2 years).

Overdose

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

A specific opiate antidote is prescribed - naloxone (0.4 mg/ml IV repeatedly, at 2-3 minute intervals); clinical observation for 48 hours.

Drug interactions

Cholestyramine may reduce the effectiveness of Loperamide capsules or tablets.

When used together 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.

Analogues of Loperamide, price in pharmacies

If necessary, you can replace Loperamide with an analogue for therapeutic action - these are the following drugs:

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

By ATX code:

• Diara,
• Imodium,
• Laremid,
• Loperacal,
• Superilol.

When choosing analogues, it is important to understand that the instructions for use of Loperamide, price and reviews do not apply to drugs with similar effects. It is important to consult a doctor and not change the drug yourself.

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

Store in a dry place, protected from light and out of reach of children, at a temperature not exceeding +25°C. Shelf life – 2 years.

What do the reviews say?

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

Users note that it does not help with diarrhea of ​​infectious etiology. Side effects are rarely reported.