Loperamide: 7 things you need to know

#1 How does it work?

Loperamide is used to treat acute or chronic diarrhea.
Loperamide acts on opioid receptors in the intestinal wall, slowing down its contraction, increasing the transit time of intestinal contents through the digestive tract, and also enhancing the ability of the intestinal wall to absorb fluid. The stool becomes less watery and the number of bowel movements decreases.

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

Loperamide has no effect on the brain or central nervous system.

This drug suppresses the gastrocolic reflex and may directly inhibit (suppress) the secretion of fluids and electrolytes or stimulate the absorption (absorption) of salt and water.

Loperamide: indications for use

Loperamide: release form - tablets

Indications for the use of loperamide are diarrhea or diarrhea. The name of the drug itself and the name of the main active ingredient, its active base, are identical. They are similar in their effect and contain loperamide in their composition such drugs as Imodium, Enterobene, Laremid, Lopedium. Loperamide reduces the intensity of intestinal contractions, which consistently move the food bolus through 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 influence 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 disorder.

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 the diarrhea is not infectious in nature and has not resulted from food poisoning. It is in such cases that it is extremely undesirable to deal with diarrhea, because with the help of loose stools the body gets rid of intoxication and does not allow the products of bacterial activity and toxins to be absorbed into the blood. Indications for the use of loperamide may include conditions such as:

• diarrhea caused by overload of the nervous system, stress (“bear disease”);
• “traveler's diarrhea” caused by a change in climate and usual diet;
• chronic intestinal diseases, Crohn's disease;
• condition after chemotherapy;
• the presence of an ileostomy, when the contents of the intestine in severe diseases are removed 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, in addition to diarrhea, there are no such symptoms: fever, headaches, blood in the stool, fever, abdominal pain.

#3 Disadvantages of loperamide

People 18 to 60 years of age who are not taking any medications or have other medical conditions are likely to experience the following side effects:

1. Constipation (as a consequence of taking more loperamide).
2. Dizziness or drowsiness, which may affect your ability to drive or operate machines.
3. Bloating, loss of appetite, abdominal pain and skin rash.

The drug may not be suitable for you in the following cases:

• with intestinal obstruction, abdominal pain without diarrhea, blood or mucus with diarrhea;
• with rare hereditary forms of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption syndrome, since the capsules may contain lactose;
• during pregnancy and breastfeeding, except on the advice of a doctor.

Be careful!
In general, older adults and children, people with liver or kidney disease, heart disease, diabetes and seizures, and people taking other medications that interact with ibuprofen are at greater risk of developing a wide range of side effects.

How to take loperamide

Loperamide is an antidiarrheal agent

When taking loperamide, you must follow the instructions for use. It is recommended to start taking the drug 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, you should not double the dose; it is better to start with 2 mg, and then be guided by your well-being. You should not take more than 16 mg of the drug per day. Features of the use of various dosage forms of loperamide:

• capsules are taken with at least 250 ml of water;
• Chewable tablets should not be swallowed without chewing them thoroughly;
• The suspension should be shaken well before use, measuring it with a measuring spoon.

Take the drug on an empty stomach or during meals, trying to drink as much fluid as possible. There is no exact regimen 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, or at a minimum, call an ambulance. This can be understood by the following symptoms: confusion, pain and bloating in the intestines, extremely rare urination.

If they are accompanied by swelling of the face, throat, itching of the skin with red spots, perhaps this is how side effects from taking the drug manifest themselves in the form of an allergic reaction. Side effects may also include increased diarrhea and blood in the stool. In such cases, delay is unacceptable; urgent medical consultation is needed. Such phenomena are extremely rare, the most that can occur when taking the drug is constipation for 1-3 days, slight lethargy, and rarely dizziness

#5 Recommendations

1. Loperamide can be taken with or without food.
2. When using loperamide, strictly follow the instructions and do not exceed the dosages indicated therein. Use the drug only for its intended purpose.
3. Drink more fluids, as during diarrhea the body loses a lot of water and becomes dehydrated.
4. Avoid overheating and dehydration while taking loperamide.
5. If loperamide makes you drowsy, do not drive or operate machinery. Avoid using loperamide with alcohol.
6. If diarrhea does not go away within 48 hours or worsens, bloating or stomach tenderness occurs, consult your doctor.

Be careful! Stop taking loperamide and get medical help right away if you develop rash, itching, facial swelling, difficulty breathing, bloating, blood in your stool, or severe dizziness.

How to take Loperamide

Loperamide should be taken exactly as directed in the package insert or as prescribed by your doctor. If you have any doubts, you should consult your doctor or pharmacist.

Follow the dosage below

• You should take the required number of capsules of the drug, without opening them, with water. The drug is intended for oral administration only.
• Do not take more than what is indicated in the package insert.
• The drug is not intended for long-term treatment of diarrhea.

Acute short-term diarrhea

Adults and teenagers aged 12 years and older

The initial dose is 2 capsules (4 mg), then 1 capsule (2 mg) is used after each liquid bowel movement.

The duration of treatment should not exceed 48 hours. The maximum daily dose should not exceed 6 capsules.

You can replace fluid lost during diarrhea by drinking more fluid than usual.

Loperamide should not be used in children under 12 years of age.

Duration of treatment for short-term diarrhea

The duration of treatment should not exceed 48 hours. If clinical improvement is not observed within 48 hours of starting treatment for acute diarrhea, you should stop taking the drug and contact your doctor.

Diarrhea due to irritable bowel disease

Adults and teenagers over 18 years of age

The initial dose is 2 capsules (4 mg), then 1 capsule (2 mg) is used after each diarrheal bowel movement (or as prescribed by the doctor).

• You can use the drug to treat recurring attacks for 2 weeks. But should not be used in cases of diarrhea lasting more than 48 hours.
• The maximum daily dose should not exceed 6 capsules (12 mg).
• You can replace fluid lost during diarrhea by drinking more fluid than usual.
• Not for use by children and adolescents under 18 years of age.

You should stop taking the drug and consult a doctor:

• If you have used this medicine continuously for 48 hours.
• If you develop new irritable bowel symptoms.
• If symptoms of irritable bowel syndrome worsen.
• If irritable bowel symptoms do not go away within 2 weeks.

Dosage for irritable bowel syndrome

You can use the medicine to treat recurring attacks for 2 weeks.

But should not be used if attacks last more than 48 hours.

If someone has taken more Loperamide than recommended

If you take more Loperamide than prescribed by your doctor, you should contact your doctor or the nearest hospital.

Symptoms include fast heartbeat, irregular heartbeat, changes in heartbeat (these symptoms can have potentially serious, life-threatening consequences), muscle stiffness, uncoordinated movements, drowsiness, difficulty urinating, or difficulty breathing. Children are more sensitive to high doses than the elderly. If a child has taken a large amount of the drug or experiences some of the above symptoms, consult a doctor immediately.

If you forget to take Loperamide

Loperamide should be taken only as needed, exactly following the dosage stated above.

If you forget to take Loperamide, take it after your next bowel movement.

Do not take a double dose of this medication.

#7 Interaction

Medicines that interact with loperamide can reduce its effectiveness, change its duration of action, and increase side effects. An interaction between two medications does not always mean that you should stop taking one of the medications, but sometimes it is necessary to do so. Talk to your doctor about which medications can and cannot be combined with loperamide.

Medicines that may have a moderate interaction with loperamide:

• lumacaftor and other P-glycoprotein substrates;
• sincalide;
• haloperidol;
• quinidine;
• ilamiodarone;
• ondansetron;
• opioids;
• Ramosetron.

Please note that this list is not comprehensive and only includes common medications that may interact with loperamide. For more detailed advice about the interaction of loperamide with other drugs that you take, contact your doctor and carefully read the instructions for the drug.

Loperamide

Loperamide

(lat.
Loperamide
) - antidiarrheal drug.
Chemical Compound:
4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-alpha,alpha-diphenyl-1-piperidine butanamide (as hydrochloride). The empirical formula is C29H33ClN2O2. Phenylpiperdine derivative.

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

«Loperamide

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

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

Loperamide stimulates opioid mu receptors in the intestinal wall, resulting in inhibition of the release of acetylcholine and prostaglandins, which, in turn, leads to a decrease in propulsive intestinal motility and an increase in the transit time of its contents. This increases the absorption time of water and electrolytes, reduces their loss and reduces the loss and increases the time of the protective action of immunoglobulins, which are released into the intestinal lumen during acute intestinal diarrhea. Loperamide increases the tone of the anal sphincter, resulting in a decrease in the frequency and severity of the urge to defecate. Loperamide reduces mucus hypersecretion in the colon, and also has an antisecretory effect, which is realized through both opioid and non-opioid receptors. Loperamide, due to the inhibition of calmodulin and blockade of calcium channels and due to the suppression of intestinal peptides and neurotransmitters that increase the permeability of plasma membranes, affects intestinal secretion (Ivashkin V.T.). Currently, loperamide is the most effective drug with antidiarrheal action, and its antidiarrheal effect is due to inhibition of both the motor component of diarrhea and intestinal secretion. Loperamide belongs to the group of synthetic opiates, but binds only to peripheral opiate receptors, does not have a systemic narcotic effect and does not penetrate the blood-brain barrier. This is explained by the peculiarities of its biotransformation during the first passage through the liver and the absence of active metabolites in the blood. Loperamide can be successfully used for motor diarrhea with increased peristalsis (irritable bowel syndrome (IBS) and functional diarrhea), but is not effective for diabetic enteropathy, scleroderma, amyloidosis. Moreover, in these situations it can worsen diarrhea. For secretory diarrhea, loperamide is also very effective due to its antisecretory opiate-like effect. For infectious diarrhea, the drug should be prescribed with caution, since the retention of the infectious agent in the body increases diarrhea and intoxication. Loperamide relieves diarrhea well in Crohn's disease, but it is not recommended for use in ulcerative colitis due to its blocking effect on the tone of the intestinal wall and the risk of developing toxic dilatation (Belousova E.A., Zlatkina A.R.).

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

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

Publications for healthcare professionals addressing the effects of loperamide on the gastrointestinal tract

:

• Belousova E.A., Zlatkina A.R. Diarrhea syndrome in the practice of a gastroenterologist: pathophysiology and differentiated approach to treatment. Pharmateka. 2003, No. 10, p. 65-71.
• Sheptulin A.A. Diagnosis and treatment of gastrointestinal motility disorders.
• Kolesnikova E.V. Endocrine diseases and pathology of the digestive organs // Journal “Mystery Likuvannya”. Ukraine. - 2006. - 8(34).
• Leites Yu.G., Galstyan G.R., Marchenko E.V. Gastroenterological complications of diabetes mellitus. Consilium-Medicum. 2007. No. 2.
• The FDA warns of serious cardiac problems with high doses of the antidiarrheal drug loperamide (Imodium), including abuse and misuse. June 7, 2016
• The FDA is limiting packaging sizes for the antidiarrheal drug loperamide (Imodium) to increase safety for its use. January 30, 2022

On the website GastroScan.ru in the “Literature” section there are subsections “Laxatives” and “Constipation and Diarrhea”, containing articles for healthcare professionals on this topic.
Indications for use:

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

Method of administration and dosage:
orally (capsules - without chewing, with water; lingual tablet - on the tongue, it disintegrates within a few seconds, 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. When prescribed in drops: initial dose - 60 drops of a 0.002% solution; then 30 drops after each bowel movement; maximum dose - 180 drops per day (6 times). For chronic diarrhea, adults are prescribed 4 mg per 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. Drops: initial dose 30 drops of 0.002% solution; then 30 drops 3 times a day; the maximum dose is 120 drops per day (in 4 doses). For chronic diarrhea, children over 5 years of age are prescribed loperamide in a daily dose of 30 drops or 2 mg. Children aged 2–5 years are prescribed in an oral solution of 5 ml (1 measuring cap) per 10 kg; frequency of administration - 2-3 times a day. The maximum daily dose is 6 mg per 20 kg. If normal stool appears or if there is no stool for more than 12 hours, the drug is discontinued (Instructions for use).

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

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

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

:

WHO training manual “Treatment of diarrhea” (2006) Fr.

Contraindications:

• hypersensitivity to loperamide
• intestinal obstruction
• diverticular ulcerative colitis
• pregnancy (first trimester)
• lactation period
• diarrhea due to pseudomembranous enterocolitis, dysentery and other gastrointestinal infections
• children up to 2 years of age (for capsules - up to 6 years)

special instructions
:

• if there is no effect after 2 days of treatment, it is necessary to clarify the diagnosis and exclude infectious genesis of diarrhea
• Children under 5 years of age are not recommended for use in 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

Side effects.
Allergic reactions (skin rash), drowsiness, dizziness, hypovolemia, electrolyte disturbances;
dry mouth, intestinal colic, gastralgia, abdominal pain or discomfort, nausea, vomiting, constipation, flatulence. Rarely - urinary retention, extremely rarely - intestinal obstruction. When taking lozenges - a burning or tingling sensation in the tongue (Instructions for the drug). Overdose.

• Symptoms:
  central nervous system depression (stupor, impaired coordination of movements, 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, activated carbon, gastric lavage, mechanical ventilation (Instructions for the drug).

Serious cardiac problems when taking large doses of loperamide
.
In a July 6, 2016 release, the US Food and Drug Administration warns against taking larger than recommended doses of the over-the-counter (OTC) and prescription forms of the antidiarrheal drug loperamide, including through abuse or If used incorrectly, it can lead to serious cardiac problems that can cause death. The risk of these serious cardiac problems, including arrhythmias, may be increased if high doses of loperamide are taken with certain drugs that interact with loperamide (see "Examples of Drugs That May Potentially Interact with Loperamide"). Use of loperamide by pregnant and nursing mothers
. FDA fetal risk category for loperamide in pregnant women is “C” (animal studies have shown adverse effects on the fetus and there have been no adequate studies in pregnant women, but the potential benefits associated with the use of this drug in pregnant women may justify it use despite the risk).

Loperamide passes into human milk in small quantities, so breastfeeding while mothers are treated with loperamide is not recommended.

During therapy with loperamide, caution must be exercised when driving.

and other similar activities.

Trade names of drugs with a single active substance

loperamide: Vero-Loperamide, Diara, Diarol, Imodium, Laremid, Lopedium, Loperacap, Loperamide, Loperamide Grindeks, Loperamide Stada, Loperamide-Acri, Loperamide hydrochloride, Superilop, Enterobene.

Loperamide
in combinations with other active substances:
loperamide + simethicone, brand name Imodium plus.
The following drugs containing loperamide are registered in the USA: Diamode, Imodium AD, Imodium AD EZ Chews, Imodium AD New Formula, Kao-Paverin, Kaopectate 1-D, Imodium, Maalox Anti-Diarrheal, Pepto Diarrhea Control, Imotil, Diar-Aid. In the United States, medications, depending on the content of loperamide, can be either over-the-counter or prescription.

Instructions from different loperamide manufacturers

Instructions from some manufacturers of drugs containing loperamide as the only active ingredient (pdf):

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

By Order of the Government of the Russian Federation of December 30, 2009 No. 2135-r, loperamide (capsules; tablets; chewable tablets) is included in the List of vital and essential medicines.
Loperamide has contraindications, side effects and application features; consultation with a specialist is necessary.

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Additional Information

Keep loperamide, like all other medicines, out of the reach of children, never share your medicines with other people, and use medicines only as directed.

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