Loperamide side effects and contraindications. Loperamide (Imodium). Deadly risks of uncontrolled use. Prices for Loperamide

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 the composition of food 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:

Lopedium,
Loperamide-Akrikhin,
Imodium Plus,
Uzara,
Loflatil,
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.

Akrikhin HFC (Russia)

Pharmacological action

Antidiarrheal.

Interacts with opiate receptors of the longitudinal and circular muscles of the intestinal wall and inhibits the release of acetylcholine and prostaglandin.

Slows down peristalsis and increases the transit time of intestinal contents.

Increases the tone of the anal sphincter, promotes fecal retention and reduces the urge to defecate.

Absorbed in the gastrointestinal tract, metabolized in the liver.

The time to reach maximum concentration is about 8.5 hours after taking the solution and 5 hours after taking the capsules; binds to plasma proteins by 97%.

The half-life is 9-14 hours (average 11 hours), excreted mainly in the form of conjugates with bile and feces.

Side effects of Loperamide

Drowsiness, dizziness, weakness, fatigue, dry mouth, nausea, vomiting, abdominal pain, constipation or bloating (rare).

Indications for use

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 bowel movements in patients with ileostomy.

Contraindications Loperamide

Hypersensitivity, intestinal obstruction, acute ulcerative colitis, diverticulosis, diarrhea due to acute pseudomembranous enterocolitis, dysentery and other gastrointestinal infections.

Pregnancy (1st trimester), lactation period, children under 2 years of age (The drug is not prescribed to children under 6 years of age).

With caution.

Liver failure.

Directions for use and dosage

For acute diarrhea:

adults - 4 mg, then 2 mg;
children (over 6 years old) - 2 mg, then 2 mg after each loose stool.

For chronic diarrhea:

adults - 4 mg, then in a dose that ensures stool frequency 1-2 times a day (2-12 mg per day); maximum daily dose - 16 mg;
children - 2 mg, then select the dose in the same way, but not exceeding the maximum daily dose (6 mg per 20 kg of body weight).

Overdose

Symptoms:

depression of the central nervous system (stupo,
lack of coordination
sleepy,
muscle hypertension,
respiratory depression,
intestinal obstruction.

Treatment:

Naloxone is used as an antidote.

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

Immediately after an overdose, activated charcoal is administered and the stomach is washed; if necessary, support respiratory function.

Interaction

No information available.

Special instructions

During treatment of diarrhea (especially in children), it is necessary to replace the loss of fluid and electrolytes.

If acute diarrhea does not improve clinically within 48 hours or if constipation, bloating, or partial intestinal obstruction develops, loperamide should be discontinued.

In patients with liver dysfunction, careful monitoring for signs of CNS toxicity is necessary.

If you experience weakness, fatigue, drowsiness or dizziness, it is not recommended to drive a car or operate machinery.

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.

An antidiarrheal drug used for symptomatic (i.e., to eliminate the effect, not the cause) treatment of diarrhea, including allergic, drug-induced, emotional, as well as for 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 a laureate of the International Gairdner Prize.

Indications for use of Loperamide are frequent bowel movements and loose stools. 7 years after its discovery, Loperamide managed to become the best-selling anti-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 use by adults, with the exception of early pregnant women and nursing mothers. The drug is also recommended for children over 6 years old, but in a dosage reduced by half.

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

Release form and composition

The following are used as excipients in Loperamide tablets:

calcium stearate;
granulak-70;
potato starch.

Loperamide capsules are yellow in color, inside there is a white or yellowish-white powder. Excipients:

cornstarch;
lactose;
Aerosil;
magnesium stearate;
talc.

Pharmacological properties

Loperamide, by binding to 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 in feces. Increases the tone of the anal sphincter, helps retain feces and reduce the urge to defecate. The action occurs quickly and lasts 4-6 hours.

Pharmacokinetics

Indications for use of Loperamide

Symptomatic treatment acute and chronic diarrhea of various origins (allergic, emotional, medicinal, radiation: with changes in diet and food composition, with metabolic and absorption disorders: as an adjuvant for diarrhea of infectious origin). Regulation of bowel movements in patients with ileostomy.

Directions for use and dosage

Orally, without chewing, with water.

Capsules

Pills

For children

Side effect

allergic reactions (skin rash);
drowsiness or insomnia;
dizziness;
hypovolemia;
electrolyte disturbances;
dryness of the oral mucosa;
intestinal colic;
gastralgia;
abdominal pain or discomfort;
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 due to acute pseudomembranous enterocolitis;
dysentery and other gastrointestinal infections;
pregnancy (first trimester);
lactation period;
Loperamide capsules are not prescribed to children under 6 years of age.

Use for liver dysfunction

Liver failure. In patients with impaired liver function, careful monitoring for signs of toxic damage to the central nervous system is necessary.

Use during pregnancy and breastfeeding

Contraindicated in the first trimester of pregnancy.

In the second and third trimesters of pregnancy, Loperamide is prescribed in cases where the expected benefit of therapy for the mother outweighs the potential risk for the fetus. Since small amounts of loperamide are found in breast milk, Use during breastfeeding is not recommended.

Loperamide and alcohol

A side effect of Loperamide is increased drowsiness and dizziness. Under the influence of ethanol, such effects intensify and cause significant discomfort to the patient. Recommended avoid co-administration 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 ventilation.

Medical supervision is required for 48 hours.

Interaction with other drugs

When used simultaneously with cholestyramine, the effectiveness of Loperamide sometimes decreases. When used together with ritonavir, co-trimoxazole, the bioavailability of Loperamide increases. Concomitant use with opioid analgesics increases the risk of severe constipation.

Storage conditions and periods

Conditions for dispensing from pharmacies

The drug is approved for use without a prescription.

Analogues of Loperamide

Analogues of Loperamide, which contain the same main component in the base:

Diara;
Diarol;
Imodium;
Laremid;
Lopedium;
Loperacap;
Loperamide Grindeks;
Loperamide-acri;
Loperamide hydrochloride;
Superilop;
Enterobene.

Prices for Loperamide

The price of Loperamide is on average.

Symptomatic treatment of acute and chronic diarrhea caused by changes in diet and quality of food, metabolic and absorption disorders, as well as allergic, emotional, medicinal, radiation origin; for diarrhea of infectious origin - as an adjuvant; ileostomy (to reduce the frequency and volume of stool, as well as to make its consistency denser).

Release form of the drug Loperamide

Capsules 1 capsule.
loperamide hydrochloride 0.002 g
(in terms of 100% substance)
excipients: corn starch; milk sugar; talc; Aerosil; magnesium stearate

In a blister pack 10 pcs.; in a cardboard pack 1 or 2 packages.

Pharmacodynamics of the drug Loperamide

Its chemical structure is similar to phenylpiperidine derivatives and has elements of similarity to the analgesics fentanyl and pyritramide, but loperamide does not have a pronounced analgesic effect. At the same time, it actively inhibits intestinal motility, which is one of the characteristic features of opiates. Under experimental conditions, loperamide binds to opiate receptors. Increases the tone of the anal sphincter, promotes fecal retention and reduces the urge to defecate. The action develops quickly and lasts 4-6 hours.

Pharmacokinetics of the drug Loperamide

Poorly (about 40% of the dose) absorbed into the gastrointestinal tract. Due to the high affinity for the receptors of the intestinal wall 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. Tmax is about 2.5 hours after taking the solution and 5 hours after taking the capsules, while Cmax is approximately the same for both forms. Plasma protein binding - 97%. T1/2 is 9.1–14.4 hours (average 10.8 hours). Metabolized in the liver, excreted mainly in the form of conjugates with bile and feces, and partially with urine.

Use of the drug Loperamide during pregnancy

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

Teratogenic effects. Reproduction studies in rats and rabbits have shown that loperamide, when used in doses no more than 30 times the MRDC, does not cause teratogenic effects and does not cause harm to offspring.

Breastfeeding. 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 offspring survival was noted.

Other special cases when taking Loperamide

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

Contraindications to the use of the drug Loperamide

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 the presence of blood in the stool and accompanied by elevated body temperature) and other gastrointestinal infections (caused, including Salmonella spp., Shigella spp. and Campylobacter spp.); children under 6 years of age.

Side effects of the drug Loperamide

From the gastrointestinal tract: constipation and/or bloating, intestinal colic, abdominal pain or discomfort, nausea, vomiting, dry mouth, intestinal obstruction (very rare); for lozenges (optional) - a burning or tingling sensation in 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 were taking other drugs that could cause or contribute to adverse reactions).

Other: urinary retention (rare).

Method of administration and dosage of the drug Loperamide

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).

For acute diarrhea, adults are prescribed an initial dose of 4 mg; then - 2 mg after each act of defecation (in the case of liquid stool); the highest daily dose is 16 mg.

For chronic diarrhea, adults are prescribed 4 mg/day. The maximum daily dose is 16 mg. For acute diarrhea, children over 5 years of age are prescribed an initial dose of 2 mg, then 2 mg after each act of defecation; the maximum daily dose is 8 mg.

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

Overdose of Loperamide

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

Treatment: 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 observation of the patient (at least 1 day) and symptomatic therapy, gastric lavage, administration of activated charcoal, and mechanical ventilation are necessary.

Interactions of the drug Loperamide with other drugs

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

Precautions when taking Loperamide

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

For chronic diarrhea, loperamide can only be taken as prescribed by a doctor.

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

Use with caution in elderly patients (may mask symptoms of dehydration and variability in response to loperamide).

In patients with liver dysfunction, careful monitoring for signs of toxic damage to the central nervous system is necessary (loperamide metabolism slows down).

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

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

Special instructions when taking Loperamide

If there is no effect after 2 days of treatment, it is necessary to clarify the diagnosis and exclude the infectious genesis of diarrhea. Children under 5 years of age are not recommended to take capsules. 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.