How to use loperamide tablets. What are loperamide capsules for?

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

Which appeared so inopportunely before a wedding, important exams, during an urgent trip or a long-awaited vacation, it is difficult to find something more convenient to use than this inexpensive and effective drug. However, in its use there are important nuances that must be taken into account.

Loperamide is an antidiarrheal agent.

When taking, you need to be guided by the instructions for use. It is recommended to start with a double dose of 4 mg, moving from the next dose of the drug to a dose of 2 mg. However, if the diarrhea is not pronounced, do not double the dose, it is better to start with 2 mg, and continue to be guided by your well-being. For a day, you can not take more than 16 mg of the drug. Features of the use of various dosage forms of loperamide:

• capsules are taken with water in an amount of at least 250 ml;
• chewable tablets should not be swallowed without chewing them thoroughly;
• shake the suspension well before use, measuring it with a measuring spoon

Take the drug on an empty stomach or with meals, trying to drink as much liquid as possible. There is no exact scheme for its use, unless loperamide is prescribed by a doctor as part of a comprehensive treatment.

If an overdose occurs, first of all, you need to seek qualified medical advice, at least call an ambulance. This can be understood by the following symptoms: confusion, pain and swelling in the intestines, extremely rare urination.

If they are joined by swelling of the face, throat, skin itching with red spots, it is possible that this is how side effects from taking the drug manifest themselves in the form of Side effects can also be manifested by increased diarrhea, the appearance of blood in the stool. In such cases, delay is unacceptable, urgent medical consultation is needed. Such phenomena are extremely rare, the most that can threaten when taking the drug is constipation for 1-3 days, slight lethargy, rarely dizziness

Loperamide: indications for use

Loperamide: release form - tablets

Indications for the use of loperamide is diarrhea or The name of the drug itself and the name of the main active substance, its active base are identical. They are similar in their effect and contain loperamide in their composition, such drugs as Enterobene, Laremid, Lopedium. Loperamide reduces the intensity of intestinal contractions, which consistently move the food bolus along it. Thanks to this, food does not rush through the digestive tract at an unusual speed, both liquid and nutrients have time to be absorbed through the intestinal walls, and dehydration of the body does not occur.

In addition, under the action of the drug, the amount of mucous secretion produced by the intestinal walls decreases, and the density of feces approaches normal. At the same time, the drug increases the tone of the anal sphincter, which almost completely eliminates the endless urge to defecate, these unpleasant symptoms of intestinal upset.

The peculiarity of this drug is that it only relieves the unpleasant symptoms of diarrhea, but cannot cope with its cause.

Before you start using loperamide, you need to be sure that diarrhea does not appear as a result of food poisoning. It is in such cases that it is extremely undesirable to fight diarrhea, because with the help of loose stools, the body gets rid of it and does not allow the products of bacteria and toxins to be absorbed into the blood. Indications for the use of loperamide may be such conditions as:

• diarrhea caused by nervous system overload, stress (“bear disease”);
• "traveler's diarrhea", caused by a change in climate, habitual diet;
• chronic bowel disease,
• condition after chemotherapy;
• when the contents of the intestine in severe diseases are excreted through an opening in the abdominal wall.

Without consulting a doctor, loperamide can be used only in the first and second cases, and even then, if, apart from diarrhea, there are no such symptoms: fever, headaches, blood in the stool, fever, abdominal pain.

Prohibitions and restrictions in taking loperamide

If the drug is taken for a short time, only as a symptomatic agent, then as soon as the stool returns to normal, it should be stopped. Since loperamide can depress the nervous system in large doses, it is forbidden to use it in children under 6 years of age and with extreme caution in adolescents under 12 years of age. The effect of the drug on the central nervous system is due to a ban on during treatment, as well as on driving a car. It should be taken into account that the period of excretion of the drug from the body is quite long, that is, long-term consequences are possible.

As for taking loperamide during pregnancy, it is better to refrain from it, especially the first 3 months. If it is absolutely necessary to use the drug, a pregnant woman should consult a doctor and minimize the dosage. The drug taken during breastfeeding enters in the amount of 0.03%, however, even such a meager dose can cause slow breathing and drowsiness in the infant. Medical contraindications to the use of loperamide will be erosions, intestinal ulcers and diverticulosis in order to avoid perforation of the intestinal walls and occurrence. It cannot be used for bacterial intestinal infections and, as well as for reduced liver function.

Inexpensive and effective, loperamide is used as a symptomatic treatment for non-infectious diarrhea. At the same time, careful consideration of contraindications and compliance with the required dosage is necessary.

Can children be given a medicine such as loperamide, you can find out from the video:

Tell your friends! Share this article with your friends on your favorite social network using the social buttons. Thank you!

Antidiarrheal symptomatic drug

Active substance

Loperamide hydrochloride (loperamide)

Release form, composition and packaging

10 pieces. - cellular contour packings (1) - packs of cardboard.
10 pieces. - cellular contour packings (2) - packs of cardboard.

pharmachologic effect

Dosage

Inside, without chewing, drinking water.

Adults in acute and chronic diarrhea, 2 capsules (0.004 g) are initially prescribed, then 1 capsule (0.002 g) after each act of defecation in case of loose stools. For acute diarrhea children over 6 years old, appoint 1 capsule (0.002 g) after each act of defecation in case of loose stools.

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

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

Side effects

Allergic reactions (), drowsiness or insomnia, dizziness, hypovolemia, electrolyte disturbances; dryness of the oral mucosa, intestinal colic, gastralgia, pain or discomfort in the abdomen, nausea, vomiting, flatulence.

Rarely - urinary retention, extremely rarely - intestinal obstruction.

Overdose

Symptoms: depression of the central nervous system (stupor, incoordination, drowsiness, miosis, muscle hypertension, respiratory depression), intestinal obstruction.

Treatment: antidote - naloxone; given that the duration of action of loperamide is longer than that of naloxone, repeated administration of the latter is possible.

Symptomatic treatment:, gastric lavage, artificial lung ventilation.

Medical supervision is required for at least 48 hours.

special instructions

In the absence of effect after 2 days. use of loperamide, you must 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 CNS toxicity is necessary.

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

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

When diarrhea occurs, it is important to be able to quickly come to the rescue. Many families have medicines in their first aid kit that effectively relieve the symptoms of diarrhea and improve well-being. In order not to harm the body, it is important to figure out how to properly take Loperamide for diarrhea, and when it is better to refuse this remedy.

"Loperamide" is a tablet for diarrhea, which is based on the active substance - loperamide hydrochloride. Available in the form of capsules or tablets. Each tablet or capsule contains 2 mg of the active ingredient. In addition to the main ingredient, the composition includes auxiliary compounds: starch, sucrose and magnesium stearate.

Prices and storage

The cost of the drug "Loperamide" differs depending on the pricing policy of the pharmacy chain and the manufacturer. The average price for a box of ten tablets is from 13–25 rubles.

You can store the drug for two years from the date of issue. Optimum conditions - in a dark place at a temperature of no more than 25 degrees. After the expiration date, the use of the drug is prohibited.

Indications for use

After reading the instructions, it becomes clear for what purposes Loperamide can be taken. This drug has the following indications:

• allergic diarrhea;
• loosening of the stool against the background of emotional experiences;
• diarrhea against the background of the use of other medicines;
• weakness of the stool with radiation sickness;
• diarrhea due to a change in diet;
• acute functional diarrhea;
• recovery after ileostomy.

If this drug is used for diarrhea, it very quickly relieves vivid symptoms and prevents the removal of vitamins and minerals from the body. The use of "Loperamide" for intestinal disorders prevents, as the body stops the loss of a large volume of fluid.

The drug "Loperamide" is effective in the treatment of chronic diarrhea. However, this drug is not suitable for use in any form of bowel disorder.

Application procedure

How to drink the medicine correctly is written in the instructions for use. The general application rules remain in effect:

• swallow the tablet or capsule whole;
• drink enough water.

The dosage of the drug for different age groups is different. And also it is worth considering the reason why the medicine is taken. This medication is almost never used as a course, but only symptomatically.

Adults

Reception of "Loperamide" by adult patients is carried out according to the following scheme:

• the first time to drink 2 capsules at once;
• after each loose stool, take another 1 capsule;
• the total duration of treatment should not be more than 5 days.

If there is no improvement during the first two days during the treatment, it is no longer worth drinking Loperamide.

In chronic diarrhea, adult patients should be taken in capsules of 1-2 pieces, but not more than 8 pieces per day. The maximum daily dose of the drug is 16 mg.

children

If, "Loperamide" perfectly helps to cope with the problem. This drug is approved for use by children over 6 years of age.

In acute diarrhea, the child takes one tablet or capsule with a dosage of 2 mg. After each visit to the toilet, give the baby 1 mg of medication, dividing the tablet or capsule in two.

When treating chronic stool disorders with Loperamide, the daily dosage can be calculated based on the fact that 3 capsules can be taken for every 20 kg of body weight.

During pregnancy

"Loperamide" is an effective drug, but it should be used with extreme caution. The period of bearing a child is quite difficult, and many drugs are contraindicated. Use "Loperamide" is possible only as a last resort, when there are no alternative methods of treating diarrhea. It is most undesirable to treat bowel disorder with this drug in the first trimester.

Breastfeeding women should also be careful. Since the drug passes into breast milk in a certain amount, it is not advisable to treat it for diarrhea during lactation.

Contraindications

A drug for diarrhea such as Loperamide should not be used in the following situations:

• if there is individual sensitivity to the components of the drug;
• with intestinal obstruction;
• when infected with infections;
• with intestinal viruses;
• with severe food poisoning;
• patients with acute ulcerative colitis;
• with intestinal diverticula;
• with a tendency to constipation;
• at .

It is important to take into account all contraindications, and do not take the drug if there is at least one of the above problems. With caution, the drug can be given to children from 2-6 years. Only the tablet form of the drug is allowed.

A relative contraindication is liver failure. It is possible to be treated with "Loperamide" under the careful control of well-being.

Side effects

Side effects are possible only with an overdose or against the background of long-term treatment with Loperamide.

The following reactions are possible:

• stomach ache;
• constipation;
• increased gas formation;
• intestinal obstruction;
• fast fatiguability;
• difficult urination;
• temporary decrease in visual acuity;
• rash;
• allergic reactions.

All these phenomena occur extremely rarely and are usually associated with a violation of the drug regimen recommended by the manufacturer.

Interaction with other drugs

Do not simultaneously take "Loperamide" with such medications:

• anticholinergics;
• erythromycin;
• metoclopramide.

When using Loperamide and colestyramine, quinidine and ritonavir at the same time, it is necessary to observe a gap of at least 2-3 hours.

Analogues

"Loperamide" has both synonyms, that is, drugs that are completely similar in composition, and analogues, that is, drugs that are similar in action.

To completely identical to "Loperamide" in composition and mechanism of action, the following agents can be attributed:

• "Lopedium";
• "Enterobene";
• "Superilop";
• "Diara".

Some products are available in tablet form, while others are in capsule form.

Let's take a look at some similar tools:

1. "Diaremix". In addition to loperamide, the drug contains bacteria and dicycloverine. The medicine stops the diarrhea, but does it more gently. The tool promotes the formation of beneficial microflora in the intestines.
2. "Loflatil". The active ingredients are loperamide and simethicone. This combination of active ingredients eliminates flatulence and bloating, reduces the likelihood of side effects.
3. "Uzara". Produced in the form of syrup. Based on natural substances. Stops diarrhea. Approved for use by children over 2 years of age.



Loperamide, which we talk about on www.site, is a drug that has an antidiarrheal effect.

Composition and dosage form of loperamide

The drug Loperamide is produced in capsules, where the active compound is represented by loperamide hydrochloride, its dosage is 2 mg. In addition, the dosage form contains some forming components.

There is another dosage form of an antidiarrheal drug, which is presented in tablet form. You can buy medication in the OTC department. The shelf life and shelf life of Loperamide is two years from the date of pharmaceutical preparation of the drug.

How does loperamide capsules and tablets work?

The antidiarrheal agent Loperamide reduces intestinal tone and motility, in addition, the passage of intestinal contents slows down, the tone of the anal sphincter increases. The effect of the drug comes on pretty quickly. How long does Loperamide last? Its duration is 4 or 6 hours.

The absorption of the drug is 40%. How long does it take for Loperamide to work? The maximum concentration of the antidiarrheal agent is reached after 2.5 hours. The half-life varies from nine hours to fourteen. Communication with blood proteins is 97 percent. The drug does not penetrate the blood-brain barrier.

The drug is almost completely metabolized in hepatocytes due to the conjugation process. The drug is excreted mainly by the intestines, only a small part is excreted in the urine.

What does Loperamide treat, what helps?

Indications for the use of loperamide are as follows. It is intended for the treatment of diarrhea of ​​various origins (allergic, emotional, in addition, medicinal and radiation). A medication is prescribed when changing the diet, as well as the composition of the food, in case of malabsorption.

In addition, the agent is prescribed for the regulation of defecation in persons with an ileostomy. An antidiarrheal drug is used as an auxiliary medication in the treatment of loose stools in infectious diseases.

Is loperamide harmful? Contraindications for use

There are some conditions in which the antidiarrheal agent Loperamide is contraindicated for use: hypersensitivity to the drug, lactose intolerance, lactation period, lactase deficiency, intestinal obstruction, glucose-galactose malabsorption, pseudomembranous enterocolitis, diverticulosis, ulcerative colitis, pregnancy, age up to six years. With caution, the drug is prescribed for severe liver pathology.

The use of the drug Loperamide and dosage

Capsules and tablets for diarrhea Loperamide is used orally, while the dosage form is swallowed whole, tablets or capsules should be washed down with boiled water in the required volume. Usually, the patient is first prescribed 4 milligrams of the drug, after which they switch to a dosage of 2 mg.

Treatment of diarrhea at home in an adult and a child differs in dosage. The maximum daily dose of the antidiarrheal agent Loperamide for diagnosed diarrhea in adults is 0.016 grams, and children are not recommended to use more than 0.006 grams per day. In the absence of loose stools for more than 12 hours, further use of the medication is recommended to be canceled.

Overdose of Loperamide

The instruction to Loperamide also warns about the symptoms of an overdose: the patient may experience stupor, intestinal obstruction, impaired coordination, drowsiness may be noted, miosis is characteristic, in addition, muscle hypertonicity may develop, and respiratory depression is not excluded.

Overdose treatment: an antidote is prescribed, the patient's stomach should be washed first. Assign symptomatic therapy if necessary. In this case, the patient must be under medical supervision for 48 hours.

Side effects of loperamide

The medicine for diarrhea Loperamide can provoke the development of allergic reactions, the patient will develop a skin rash, in addition, drowsiness or insomnia may occur, the patient complains of dizziness, hypovolemia and electrolyte disturbances are characteristic.

Other negative manifestations can be expressed as dryness of the oral mucosa, intestinal colic joins, gastralgia is not excluded, intestinal obstruction is sometimes noted, in addition, pain or discomfort in the abdomen, as well as nausea, vomiting, urinary retention, there may be flatulence.

With the development of any side effects, the patient must promptly consult a doctor who will correct the treatment process.

special instructions

In the absence of an antidiarrheal effect after two days of using the medication, it is recommended to consult a doctor. With the development of bloating, as well as in the presence of constipation, the patient should refuse further use of the drug.

During the period of diarrhea, it is important for the patient to replenish the loss of fluid and necessary electrolytes, while, if necessary, drug solutions can be administered parenterally.

How to replace or what analogue of Loperamide to ask a pharmacist?

Other antidiarrheal drugs for adults and children: Imodium, Superilop, Loperamide-Akri, Loperamide hydrochloride-Pharmaplant, Loperamide Grindeks, in addition, Lopedium, Loperamide, Vero-Loperamide, Loperamide-Akrikhin, Loperakap, Enterobene, Laremid, Loperamide hydrochloride, Diarol and also Diara.

Conclusion

It is necessary to use the drug Loperamide on the recommendation of a specialist. If an allergic reaction develops to the use of the medication, then the patient should consult a doctor in a timely manner.