Loperamide indications for use instructions. Loperamide: instructions for use, analogues and reviews, prices in Russian pharmacies. Appointment in special cases

Loperamide is an antidiarrheal drug used for symptomatic (i.e., to eliminate the effect, not the cause) treatment of diarrhea of ​​​​various origins, including allergic, medical, emotional, and also for various digestive disorders. The mechanism of its action is based on the ability to act on the opioid receptors of the smooth muscle structures of the intestinal wall and inhibit the release of acetylcholine and prostaglandin mediators. Due to this, loperamide slows down the peristaltic contractions of the intestine, thereby prolonging the period of passage of intestinal contents through the digestive tract, increases the muscle tone of the external rectal sphincter, helps to retain stool in the rectum and reduces the frequency of the urge to defecate. In addition, loperamide prevents the release of fluid and electrolytes with feces. In high concentrations, it can suppress gastric secretion of hydrochloric acid. The drug acts quickly and remains active for 4-6 hours. It is important that addiction does not develop to loperamide; cases of drug dependence to it in medical practice were also not observed. It should be noted that loperamide is relatively poorly (only 40% of the total dose) absorbed in the gastrointestinal tract, which leaves its mark on the dosing regimen of the drug.

Loperamide is available in two dosage forms, both for oral administration: tablets and capsules. The dose and frequency of administration are determined individually depending on the indications. For adult patients in cases of acute diarrhea, the following rules are followed: to take the drug after each act of defecation in case of unformed stool. The initial dose is 4 mg (2 tablets or capsules), then 2 mg each with a daily maximum of 16 mg (for chronic diarrhea, due to long-term use, the daily dose should not exceed 4 mg). The marker for the end of drug therapy is the normalization of stool consistency or its absence for more than 12 hours. For children from 6 years of age, the drug is prescribed at a dose of 2 mg after each act of defecation with loose stools with a daily maximum of 6 mg. If within 2 days with acute diarrhea there is no improvement in the clinical picture or persistent constipation, partial intestinal obstruction, bloating develops, then loperamide should be suspended. The use of loperamide in chronic diarrhea is possible only under medical supervision. This statement is also true for young children, because they are hypersensitive to the opiate-like effect of the drug on the central nervous system.

Pharmacology

Antidiarrheal agent. Reduces the tone and motility of the smooth muscles of the intestine, apparently due to binding to opioid receptors in the intestinal wall. Inhibits the release of acetylcholine and prostaglandins, reducing peristalsis and increasing the time it takes for the contents to pass through the intestines.

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

Pharmacokinetics

After oral administration, the absorption of loperamide is about 40%, undergoes intensive metabolism during the "first pass" through the liver. A small amount of unchanged loperamide enters the systemic circulation. Does not penetrate the BBB.

Metabolized in the liver.

T 1/2 is 9-14 hours. It is excreted through bile with feces in the form of conjugated metabolites, a small part is excreted in the urine.

Release form

10 pieces. - cellular contour packings (1) - packs of cardboard.

Dosage

For adults with acute diarrhea, the first dose is 4 mg, then 2 mg after each act of defecation in case of loose stools. In chronic diarrhea, the first dose is 2 mg, the maintenance dose is selected so that the stool frequency is 1-2 times a day (2-12 mg / day).

The maximum daily dose for adults is 16 mg.

Children aged 4-8 years - 1 mg 3-4 times / day for 3 days; 9-12 years - 2 mg 4 times / day for 5 days.

Interaction

It is believed that with the simultaneous use of cholestyramine may reduce the effectiveness of loperamide.

With simultaneous use with co-trimoxazole, ritonavir, the bioavailability of loperamide increases, which is due to inhibition of its metabolism during the "first pass" through the liver.

Side effects

From the digestive system: abdominal pain, bloating, nausea, constipation, dry mouth.

From the side of the central nervous system: increased fatigue, drowsiness, dizziness.

Allergic reactions: skin rash.

Indications

Symptomatic treatment of acute and chronic diarrhea of ​​​​various genesis (including allergic, emotional, medicinal, radiation; with a change in diet and qualitative composition of food, with metabolic and absorption disorders; as an adjuvant for diarrhea of ​​​​infectious genesis). Stool regulation in patients with ileostomy.

Contraindications

Intestinal obstruction; constipation, bloating, subileus, acute dysentery (as monotherapy), acute ulcerative colitis, pseudomembranous colitis resulting from the use of broad-spectrum antibiotics; children under 4 years of age, I trimester of pregnancy, hypersensitivity to loperamide.

Application features

Use during pregnancy and lactation

Contraindicated in the first trimester of pregnancy. In the II and III 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 a small amount of loperamide is found in breast milk, use during breastfeeding is not recommended.

Application for violations of liver function

Use with caution in patients with impaired liver function, with liver failure.

Use in children

Contraindicated in children under 4 years of age.

special instructions

Use with caution in liver failure.

Should not be used in clinical situations where inhibition of intestinal motility is required.

If there is no effect after 2 days of using loperamide, it is necessary to clarify the diagnosis and exclude the infectious genesis of diarrhea.

Use with caution in patients with impaired liver function.

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

Everyone experiences diarrhea from time to time. It can be provoked by poisoning, taking certain medications, excessive nervous tension, a change in habitual nutrition.

Diarrhea disrupts the rhythm of a person's life, interferes with work and rest, in addition, it is expressed not only by frequent loose stools, but also by pain in the abdomen. To cope with these symptoms, in particular, Loperamide, an antidiarrheal agent, helps.

An indication for the use of loperamide is diarrhea, which appears when:

• Severe manifestation of food allergies;
• Intestinal dyskinesia;
• in acute or chronic manifestation (non-infectious);
• Treatment of cancer with radiation therapy;
• food poisoning and vomiting;
• Emotional surges;
• The use of antibiotics and other drugs that destroy the microflora;
• When regulating bowel function in people with iliostomy.

The active substance of this drug is loperamide hydrochloride, it:

• helps to reduce the tone of the intestinal muscles, thereby reducing motility and peristalsis;
• in the sphincter muscle, on the contrary, the tone increases, which helps to contain frequent stools;
• reduces the frequency of stool and slows its progress.

Loperamide is a powerful drug. In Russia, doctors do not recommend taking this drug to children before they reach 6 years of age - capsules, tablets up to 4 years of age, but abroad, doctors agree that in some cases loperamide hydrochloride can be prescribed to children after 2 years.

Before giving it to a child, a pediatrician must be consulted.

Varieties and composition

There are different medicines containing loperamide hydrochloride - Loperamide-Akri, Loperamide Akrihin, Loperamide Shtada, Loperamide Grindeks, Loperamide SVS, Stopex - they are all very similar in composition and similar to each other in medicinal properties.

Loperamide release form:

• round white tablets;
• gelatin capsules.

In both varieties, the main element is loperamide hydrochloride - 2 mg.

To improve absorption into the blood, tablets are added:

• polyvidone;
• potato starch;
• lactose;
• stearic acid.

Other elements in capsules:

• talc;
• corn starch;
• silica;
• milk sugar;
• stearic acid.

The bio-shell of the capsule consists of gelatin, titanium dioxide, dyes.

Loperamide is also produced in drops, but in Russia they are not allowed for sale, since as a result of self-medication there were often overdoses that led to serious complications and even death.

Pharmacological properties

The antidiarrheal property of the drug Loperamide is achieved by combining the active substance with opiate cells of the intestinal walls, guanine nucleotides act on adrenergic and cholinergic neurons and stimulate them.

The drug helps the release of prostaglandins and acetylcholine, resulting in reduced contraction of the intestinal muscles, peristalsis. The tone of the sphincter muscles increases, the number of urges decreases.

The drug acts quickly, the improvement of well-being begins within an hour and a half after administration, and remains effective for 5-6 hours.

After taking the drug is absorbed by 40% and reaches the highest concentration in the body after 2.5 hours.

Excretion of the drug occurs 12 hours after metabolization in the liver, mainly with the stool, the rest is excreted in the urine.

Instructions for use Loperamide

Tablets "Loperamide" are washed down with a large amount of liquid (it is necessary to drink large quantities of water, as it helps to avoid dehydration) and swallowed without chewing.

The doctor usually prescribes the following treatment regimen for adults:

Loperamide capsules are also taken with a large amount of liquid:

• Dose (acute diarrhea): the first dose is 4 mg, and after each subsequent stool, 2 mg. Dosage per day - 16 mg.
• Chronic diarrhea: capsules are drunk 2 times a day, 2 mg (up to 4 mg per day).

Antidiarrheal therapy lasts 1-2 days. What to do if it doesn't help? It is necessary to check the diagnosis - perhaps the infectious origin of the disease that caused diarrhea.

In this case, in addition to diarrhea, other symptoms appear:

• a person becomes lethargic, pale, loses appetite;
• chills begin, the temperature rises;
• joins vomiting, pain in the intestines of a cramping type;
• blood streaks may appear in the stool.

With diarrhea provoked by an infection, Loperamide should not be used only if a doctor prescribes, since in this case the medicine not only does not help the body, but can cause serious harm.

Body reactions such as vomiting and diarrhea help to eliminate harmful substances and infection from it, and if they are stopped, then the disease from the intestines will enter the bloodstream and spread throughout the body.

When treating with loperamide, it is necessary to monitor the patient's well-being and if the above symptoms appear, stop taking the medicine. It is important to remember that it does not cure the disease, but only relieves its symptom.

Application for children

The method of treating children with Loperamide, depending on their weight and number of years:

• 0.5 tablets (1 mg) for a child from 2 to 5 years old 3 times a day. The norm per day is 1.5 mg.
• 1 tablet (2 mg) for a child from 6 to 8 years old 2 times a day. The norm per day is 4 mg.
• 1 tablet (2 mg) 3 times a day - a child aged 9 to 12 years. The norm per day is 6 mg.

In case of acute who is over 5 years old, the doctor prescribes 1 loperamide tablet after each bowel movement. The highest dosage per day is 8 mg.

In the chronic form first they give 1 tablet, and the rest of the medication is calculated by the weight of the child's body - 1 mg per 10 kg of weight. The maximum allowable rate of the drug per day is 6 mg per 20 kg.

Contraindications for use

When prescribing Loperamide, the doctor must take into account contraindications for use:

In addition to the above, the capsules are contraindicated in people with lactose intolerance, lactase deficiency, diverticulosis and glucose-galactose malabsorption.

Side effects of Loperamide

Loperamide is usually well tolerated and helps to manage the disease, but like other medicines, it can cause unwanted effects:

drug overdose

With the wrong choice of dosage, it manifests itself:

• Ataxia;
• Increased muscle tone;
• Slow reaction;
• Constriction of the pupils;
• Intestinal obstruction;
• Sleep disorder (insomnia, drowsiness);
• Respiratory failure.

If an overdose is detected, a person needs to call emergency help, rinse the stomach, give a sorbent that helps to remove toxins from the body, in case of a critical overdose, emergency doctors administer Naloxone to reduce the effect of the drug.

Interaction with other medicines

When using the substance loperamide with cholestyramine, the effectiveness of the former is reduced.

When the drug interacts with co-trimoxazole, ritonavir, the bioavailability of the substance loperamide increases.

Interaction with alcohol

The instructions for Loperamide do not say anything about the effect of alcohol on the body during treatment, but since both negatively affect the functionality of the central nervous system and liver, harm to the body increases, therefore, it is worth giving up alcohol during treatment with Loperamide.

Loperamide during pregnancy and lactation

During childbearing and breastfeeding, Loperamide is contraindicated., as it easily enters the child's body and can adversely affect his liver.

In some cases (in the 2nd and 3rd trimesters), when the perceived risk to the child is significantly lower than the benefit to the mother, the medication is still allowed. But it is worth giving up lactation during therapy and a day after taking the last pill, until the drug is completely out of the body.

Storage conditions and shelf life

Loperamide must be stored at temperatures up to 25 in a light and moisture-proof place, away from children.

Duration of storage of tablets - 3 years, and capsules - 2 years.

Pharmacy drug cost

Loperamide is available from any pharmacy without a prescription from a doctor.

Depending on the manufacturer, the cost of the drug may be different, but still quite small:

• Loperamide blister No10 (10 tablets or capsules) from 10 to 20 rubles;
• Loperamide Akri No10 - 20 rubles, No20 - 40 rubles;
• Loperamide STADA No10 - 25 rubles, No20 - 40 rubles;
• Loperamide No20 (production of the Russian Federation) - 15 rubles.

Analogues

There are quite a few drugs containing loperamide, they are all similar in their parameters - each drug helps in the antidiarrheal fight:

• VERO Loperamide includes the active ingredient Loperamide in a volume of 2 mg and additional substances - lactose, povidone, potato, silicon dioxide, starch, stearic acid, talc, aerosil. It can help patients with acute or chronic diarrhea (non-infectious origin). This drug is contraindicated in people who are allergic to loperamide, have various types of intestinal obstruction, colitis, as well as children under 4 years of age and pregnant women in the first trimester. The tablets are taken orally with a glass of water. VERO Loperamide is sold in cardboard boxes of 1 or 2 blisters, in a blister pack of 10 round yellow tablets, as well as in jars, protected from light, 10 or 20 tablets per jar. The average cost of a package (20 tablets) is 20.5 rubles.
• - the original drug, also containing loperamide and, as additional substances, gelatin, mannitol, aspartame, mint flavor, sodium bicarbonate. Helps in the symptomatic treatment of loose stools in chronic or acute form. Patients with a reaction to loperamide or other components of the drug, pregnant (1 trimester) and lactating women, children under 6 years of age are not recommended to use this medication. Also in the instructions for Imodium, the following contraindications are indicated:
  • exacerbation of ulcerative colitis;
  • pseudomembranous colitis;
  • bacterial;
  • there is a history of intestinal obstruction;
  • in case of violation of the liver, the drug is used under the close supervision of a general practitioner.

  Imodium is quite simple to use - the tablets are kept in the mouth for 10-20 seconds until completely dissolved, then swallowed. Capsules should be swallowed with water and not chewed. Imodium is produced in the form of lozenges of 10 pcs. in a blister pack, 1 or 2 blisters, as well as in the form of biocapsules in a cardboard box, 6 or 10 capsules per 1 blister. The cost of this drug is quite high compared to analogues - capsules (6 pieces) - 240 rubles, 20 pieces - 660 rubles, tablets (6 pieces) - 215 rubles; 10 pieces - 310 rubles, 20 pieces - 550 rubles.

• loperamide hydrochloride has the main component - the substance of the same name loperamide, other components - milk sugar, corn starch and stearic acid. Just like other analogues, it helps to eliminate the symptoms of certain diseases in the form of frequent loose stools. It has the same contraindications as VERO Loperamide (allergy to the components of the drug, intestinal obstruction, infectious cause of diarrhea, pregnancy and lactation). Tablets are taken orally with water. In pharmacies, it is released in cardboard boxes containing 1 or 2 blisters with 10 capsules. The average price of this medication is 10 rubles per box.
• - a drug based on, an antimicrobial agent, helps in the treatment of intestinal diseases of an infectious type. Taking the medicine is prohibited for children under 1 month old, people with hypersensitivity to the components of the drug, as well as people suffering from fructose intolerance and sucrose deficiency. Side effects are most often manifested in the form of skin allergies of a different nature - from redness and itching to urticaria and swelling, and nausea and vomiting are also among the adverse reactions. The daily norm of the drug is 800 mg, divided into 4 doses. (200 mg capsules - 1 pc. 4 times a day, 100 mg capsules - 2 pcs. 4 times a day). Children from 1 month are given a suspension: up to six months - 2.5 ml up to 3 times a day, from 7 months to 2 years - 2.5 ml up to 4 times a day, from 3 to 7 years - 5 ml up to 3 times a day . The duration of the course is up to 7 days. In a pharmacy, Enterofuril can be bought in the form of capsules (in a blister of 8 pcs. (200 mg nifuroxazide), 10 pcs. (100 mg nifuroxazide), and suspensions - in a brown glass bottle of 90 ml. The average price for capsules 100 mg of 30 pieces - 290 rubles, capsules of 200 mg of 16 pieces - 353 rubles . Suspension costs on average - 380 rubles per bottle.

Loperamide or Imodium - which is better?

Loperamide and Imodium are similar medicines, both have the main element - loperamide hydrochloride. They have the same effect on the body in terms of treatment - Imodium also helps get rid of diarrhea, their side effects also converge.

In turn, Loperamide has an important advantage in price - it costs about 8 times cheaper than Imodium.

Thus, it can be concluded that drugs based on loperamide hydrochloride are inexpensive, but effective helpers in the fight against diarrhea. Loperamide helps a sick person quickly return to their usual rhythm of life and forget about the unpleasant manifestations of diarrhea.

Formula: C29H33ClN2O2, chemical name: 4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-alpha,alpha-diphenyl-1-piperidine butanamide (as hydrochloride).
Pharmacological group: organotropic agents / gastrointestinal agents / antidiarrheal agents.
Pharmachologic effect: antidiarrheal.

Pharmacological properties

Loperamide interacts with opiate receptors located in the circular and longitudinal muscles of the intestinal wall and inhibits the release of prostaglandins and acetylcholine. Loperamide inhibits intestinal motility and increases the transit time of intestinal contents. Loperamide increases the tone of the anal sphincter, helps to reduce the urge to defecate and retain stool. Loperamide inhibits the release of electrolytes and fluid into the intestinal lumen and/or stimulates their absorption from the intestine. In high doses, loperamide can reduce the formation of hydrochloric acid in the stomach. The action of loperamide develops rapidly and lasts 4-6 hours.
After taking loperamide, there were no cases of development of drug dependence or tolerance. But in monkeys, a morphine-like dependence was observed when using high doses of loperamide.
It is poorly absorbed in the gastrointestinal tract (approximately 40% of the dose). Due to the high degree of biotransformation during the "first pass" through the liver and the high affinity of the drug for intestinal wall receptors, the content of unchanged loperamide after using 2 mg of the drug is less than 2 ng / ml. The maximum concentration in the blood is reached 2.5 hours after taking the solution and 5 hours after taking the capsules. Loperamide binds to proteins by 97%. The half-life is 9.1-14.4 hours (mean approximately 10.8 hours). Loperamide is metabolized in the liver, mainly excreted as metabolites in the bile and faeces, and partially excreted in the urine. In a study in rats (duration 1.5 years), no carcinogenic effects of loperamide were found at doses up to 133 times the MRDH. No mutagenicity studies have been performed with loperamide. Reproduction studies in rats have shown that loperamide can cause reduced fertility in males and infertility in females at high doses (150 to 200 times the MRHD). Reproduction studies in rabbits and rats have shown no harm to offspring and no teratogenic effects at doses up to 30 times the MRHD of loperamide. It is not known whether loperamide passes into breast milk. In a study of post- and prenatal development of offspring of rats, a decrease in offspring survival was noted when using 40 mg / kg of loperamide in lactating females.

Indications

Symptomatic therapy of chronic and acute diarrhea, which is caused by a change in the qualitative composition of food and diet, malabsorption and metabolism, as well as emotional, allergic, radiation, medicinal origin; with diarrhea of ​​​​infectious origin, as an adjuvant; ileostomy (to reduce the volume and frequency of stools, to give density to its consistency).

Method of application of loperamide and doses

Loperamide is taken orally (regardless of food intake; a lingual tablet is placed on the tongue, after a few seconds it disintegrates, after which, without drinking water, it is swallowed with saliva; capsules are taken with water, without chewing). The dosage regimen depends on the indications. Acute diarrhea, adults: 4 mg - initial dose, then after each shapeless stool 2 mg, 16 mg - maximum daily dose; chronic diarrhea, adults 4 mg / day. If there is no stool for more than 12 hours or if the stool consistency returns to normal, therapy should be discontinued. Children aged 2-12 years are prescribed under the supervision of a doctor, depending on age and body weight.
If constipation, partial intestinal obstruction, bloating develops within 2 days during acute diarrhea, or there is no clinical improvement, then loperamide should be discontinued. In chronic diarrhea, the use of loperamide is possible only according to the doctor's prescription and his control. Caution must be exercised in the use of loperamide in young children due to the high sensitivity to the opiate-like properties of loperamide - effects on the central nervous system. In the treatment of diarrhea (especially in children), it is necessary to replenish the loss of electrolytes and fluids. Dehydration of the body can cause a change in the reaction to loperamide. Caution should be exercised in the use of loperamide in elderly patients (as there may be variability in the response to loperamide and masking symptoms of dehydration). In patients with impaired liver function, it is necessary to carefully monitor for signs of toxic damage to the central nervous system (due to slowing down the metabolism of loperamide). In patients with traveler's diarrhea, the decrease in intestinal motility caused by loperamide can cause a prolonged increase in temperature due to inhibition of the excretion of microorganisms (Salmonella, Shigella, some strains of Escherichia coli and others) and their penetration into the intestinal mucosa. During therapy with loperamide, extreme caution must be exercised when driving or operating machinery.

Contraindications for use

Hypersensitivity, diverticulosis, intestinal obstruction, pseudomembranous colitis, which is caused by taking broad-spectrum antibacterial agents; acute ulcerative colitis, other conditions in which intestinal motility cannot be inhibited; acute dysentery (especially if there is blood in the stool and accompanied by hyperthermia) and other infectious diseases of the gastrointestinal tract (which are caused, among other things, by Shigella spp., Salmonella spp. and Campylobacter spp.); age up to 6 years.

Application restrictions

Severe violations of the liver, age from 2 to 12 years (only with the supervision of a physician).

Use during pregnancy and lactation

You should not use loperamide during pregnancy (especially in the 1st trimester) and breastfeeding, since there are no strictly controlled and adequate studies in lactating and pregnant women.

side effects of loperamide

Digestive system: bloating, constipation, intestinal colic, discomfort or pain in the abdomen, nausea, dry mouth, vomiting, intestinal obstruction, additionally for lozenges: tingling or burning sensation of the tongue, which occurs immediately after taking the tablets;
nervous system: drowsiness, fatigue, dizziness;
allergic reactions: urticaria, skin rash, very rarely - bullous rash, including toxic epidermal necrolysis; anaphylactic shock;
others: urinary retention.

Interaction of loperamide with other substances

The concomitant use of loperamide with opioid analgesics may increase the possibility of developing severe constipation. When loperamide and cholestyramine are used together, the effectiveness of loperamide may decrease. With the combined use of loperamide with ritonavir, co-trimoxazole, the bioavailability of loperamide increases.

Overdose

In case of an overdose of loperamide, there are: intestinal obstruction, depression of the central nervous system (drowsiness, miosis, stupor, muscle hypertonicity, respiratory depression, impaired coordination of movements).
Therapy: if necessary, the use of an antidote - naloxone. Given that the duration of exposure to loperamide is longer than that of naloxone, repeated use of naloxone is possible. Careful and prolonged (at least 1 day) monitoring of the patient and symptomatic treatment, gastric lavage, activated charcoal, artificial ventilation of the lungs (if necessary) are also necessary.

Update: October 2018

Loperamide is a fast-acting antidiarrheal drug that is taken orally immediately after the onset of loose stools. It does not affect the etiological cause of diarrhea, it is a symptomatic remedy that slows down intestinal motility, therefore it cannot be considered as the main treatment (see).

Pharmacological group: Symptomatic remedy for diarrhea.

Composition, physical and chemical properties, price

The drug is available in 2 dosage forms for oral administration: Loperamide capsules and tablets.

	Tablets	Capsules
Base substance		Loperamide hydrochloride - 2 mg
Excipients	Potato starch, granulac-70, calcium stearate	Pregelatinized starch, pressed sucrose, magnesium stearate
Physiochemical properties	Tablets, flat, beveled, white	White capsules with white-cream powder inside
Package	Tablets of 10 units in a contour pack. In a carton box - 1 or 2 packs	Gelatin capsules of 10 pieces in cell packs, 1 or 2 packs in a carton box
Price	From 20 rubles for 10 tablets	From 30 rubles for 10 tablets

pharmachologic effect

Loperamide hydrochloride after oral administration quickly enters into contact with receptors in the intestinal wall, reduces motility and tone of smooth muscle fibers and slows down the movement of feces by inhibiting the production of prostaglandins and acetylcholine. At the same time, the loss of fluid and electrolytes with feces decreases. Increasing the tone of the sphincter of the anus contributes to a more effective retention of feces and a decrease in the number of urges to empty the intestines. The duration of the drug is 4-6 hours.

Pharmacokinetics

It is absorbed by 40% of the initial amount, combining with blood plasma proteins by 97%. It takes 2.5 hours to reach the maximum concentration in the blood. The half-life of the metabolites of the drug from the body is 9-14 hours.

Almost completely metabolized by the liver (conjugation method). It is excreted mainly through the intestines, and only a small part is excreted by the kidneys in the form of conjugates.

Instructions for use Loperamide

The instructions for use of Loperamide indicate that the drug is not an etiological drug, i.e. unable to suppress the growth of pathogenic intestinal flora.

Symptomatic treatment of diarrhea (chronic and acute) of various origins:

• infectious (as an adjuvant)
• allergic
• emotional
• radiation (after radiation therapy)
• medicinal (against the background of taking medical treatment, for example, antibiotic therapy)
• functional, associated with a change in diet, type and composition of food
• against the background of metabolic and absorption disorders.

It is also prescribed for the correction of stool in patients with ileostomy (surgical intervention, when a loop of the ileum is brought to the abdominal wall to form a fistula) - to reduce the frequency and amount of stool, as well as a denser consistency of stool.

Can Loperamide be given to children?

It is possible, starting from 4 years (tablets) and 6 years (capsules), but as directed by a doctor who must determine the cause of diarrhea. In the case of poisoning and intestinal infections, the retention of feces leads to greater intoxication and a deterioration in the general condition.

Contraindications and restrictions

• Hypersensitivity to any components of the drug;
• Lactase deficiency or glucose-galactose malabsorption;
• Intestinal obstruction;
• Acute ulcerative colitis;
• Diarrhea associated with acute pseudomembranous enterocolitis;
• First trimester of pregnancy;
• lactation period;
• Constipation;
• Children's age up to 6 years (capsules) and up to 4 years (tablets);
• Use as monotherapy for dysentery and other gastrointestinal infections;
• Conditions in which the development of inhibition of intestinal peristalsis is unacceptable.

Carefully

• In the 2nd and 3rd trimesters of pregnancy, it is possible to prescribe only in cases where the benefit of therapy for a pregnant woman outweighs the risk to the fetus.
• Use with caution in liver failure - if necessary, this treatment is carefully monitored for possible signs of toxic liver damage.
• If there is no clinical improvement within 2 days of using Loperamide, you should immediately consult a doctor.
• If constipation and bloating are noted during treatment, the drug is canceled.
• Care should be taken if it is necessary to control mechanisms and a car - it is possible to slow down the speed of psychomotor reactions.
• During the treatment period, the loss of water and electrolytes is necessarily replenished.

Dosage and administration

Loperamide capsules and tablets are prescribed for oral administration. Accept without chewing, washing down with water.

• Adult patients: two capsules / tablets at the first dose (4 mg), and then one capsule / tablet (2 mg) after each act of defecation until diarrhea stops, observing the maximum daily dose.
• Children : one capsule/tablet after each bowel movement until diarrhea stops, observing the maximum daily dose.
• Maximum daily dose: adults - 8 capsules (16 mg), children - 3 capsules (6 mg).

After normalization of the stool or with more than 12 hours of absence of stool, Loperamide is canceled.

Side effects

More often can be observed with prolonged or uncontrolled use.

• Skin allergic reactions like urticaria, less often - bullous rash;
• Lethargy or insomnia;
• Hypovolemia and electrolyte disturbances;
• intestinal colic;
• gastralgia (stomach pain);
• Pain or discomfort in the abdomen;
• Nausea, flatulence, vomiting;
• Rarely - urinary retention, extremely rarely - intestinal obstruction.

Overdose

CNS depression develops in the form of stupor, muscle hypotension, impaired coordination, miosis, respiratory depression, drowsiness, and intestinal obstruction. There is a specific antidote - naloxone, in addition to which symptomatic treatment is also carried out.

Gross formula

C 29 H 33 ClN 2 O 2

Pharmacological group of the substance Loperamide

Nosological classification (ICD-10)

CAS code

53179-11-6

Characteristics of the substance Loperamide

Loperamide hydrochloride is a white to yellowish powder. Let's well dissolve in methanol, isopropyl alcohol, chloroform, we will slightly dissolve in water. Molecular weight 513.51.

Pharmacology

pharmachologic effect- antidiarrheal.

Interacts with opiate receptors in the longitudinal and circular muscles of the intestinal wall and inhibits the release of acetylcholine and PG. Slows down intestinal motility and increases the time of passage of intestinal contents. Increases the tone of the anal sphincter, helps to retain feces and reduce the urge to defecate. Inhibits the secretion of fluid and electrolytes into the intestinal lumen and / or stimulates the absorption of salts and water from the intestine. In high doses, it can inhibit the secretion of hydrochloric acid in the stomach. The action develops quickly and lasts 4-6 hours.

When taking loperamide, there were no cases of development of tolerance or drug dependence. However, morphine-like dependence was observed in monkeys when taking high doses of loperamide.

Poorly (about 40% of the dose) is absorbed from the gastrointestinal tract. Due to the high affinity for intestinal wall receptors and the high degree of biotransformation during the “first pass” through the liver, the plasma level of unchanged substance after taking 2 mg of loperamide hydrochloride (1 capsule) is below 2 ng / ml. T max - about 2.5 hours after taking the solution and 5 hours - after taking the capsules, while C max is approximately the same for both forms. Plasma protein binding - 97%. T 1/2 is 9.1-14.4 hours (average 10.8 hours). Metabolized in the liver, excreted mainly in the form of conjugates with bile and faeces, partly in the urine.

Carcinogenicity, mutagenicity, effect on fertility

In an 18-month study in rats at doses of loperamide in excess of the MRDH (up to 133 times), no carcinogenic effects were found. Mutagenicity studies have not been performed. Reproduction studies in rats have shown that high doses of loperamide (150-200 times the MRHD) can cause infertility in females and decreased fertility in males.

Pregnancy. teratogenic effects. Reproduction studies in rats and rabbits have shown that loperamide, when used at doses up to 30 times the MRDC, does not cause teratogenic effects and does not harm offspring.

Lactation. It is not known whether loperamide passes into breast milk. In a study of pre- and postnatal development of offspring in rats, when loperamide was administered to lactating female rats at a dose of 40 mg/kg, a decrease in the survival of offspring was noted.

Application of the substance Loperamide

Symptomatic treatment of acute and chronic diarrhea caused by 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).

Contraindications

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) and other gastrointestinal infections (caused, incl. Salmonella spp., Shigella spp. and Campylobacter spp.); children's age up to 6 years.

Application restrictions

Severe liver dysfunction and children aged 2 to 12 years (possible only with medical supervision).

Use during pregnancy and lactation

It should not be used during pregnancy (especially in the first trimester) and lactation (adequate and strictly controlled studies in pregnant and lactating women have not been conducted).

Side effects of loperamide

From the digestive tract: constipation and / or bloating, intestinal colic, pain or discomfort in the abdomen, nausea, vomiting, dry mouth, intestinal obstruction (very rare); for lozenges (optional) - a burning sensation or tingling of the tongue that occurs immediately after taking the tablets.

From the nervous system and sensory organs: fatigue, drowsiness, dizziness.

Allergic reactions: 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).

Others: urinary retention (rare).

Interaction

Concomitant use of loperamide with opioid analgesics may increase the risk of severe constipation.

Overdose

Symptoms: depression of the central nervous system (stupor, impaired coordination of movements, drowsiness, miosis, muscle hypertonicity, respiratory depression), intestinal obstruction.

Treatment: the use (if necessary) of an antidote - naloxone. Given that the duration of action of loperamide is longer than that of naloxone, repeated administration of the antagonist is possible. Long-term and careful monitoring of the patient (at least for 1 day) and symptomatic therapy, gastric lavage, administration of activated charcoal, mechanical ventilation are necessary.

Routes of administration

inside.

Substance Precautions Loperamide

If within 48 hours in acute diarrhea there is no clinical improvement or constipation, bloating, partial intestinal obstruction develops, loperamide should be discontinued.

In chronic diarrhea, taking loperamide is possible only as directed by a doctor.

Loperamide should be used with caution in young children due to greater sensitivity to the opiate-like effects of loperamide - the action on the central nervous system. During the treatment of diarrhea (especially in children), it is necessary to replenish the loss of fluid and electrolytes. Dehydration may contribute to a change in the response to loperamide.

Use with caution in elderly patients (possible masking of symptoms of dehydration and variability in the reaction to loperamide).

In patients with liver dysfunction, careful monitoring for signs of CNS toxicity (lowering the metabolism of loperamide) is necessary.

In patients with traveler's diarrhea, the decrease in intestinal motility caused by loperamide can lead to a prolonged increase in temperature due to a slow elimination of microorganisms ( shigella,Salmonella some strains Escherichia coli etc.) and their penetration into the intestinal mucosa.

During the treatment period, care must be taken when driving a car or working with machinery.

Interactions with other active substances

Trade names

Name	The value of the Wyshkovsky Index ®
	0.0587
	0.0283
	0.0193