What is loperamide used for?
The drug is aimed at getting rid of an attack of diarrhea. It works as follows: the active substance, entering the intestines, begins its effect on its muscles and ability to contract. As a result, taking Loperamide stops bowel activity while simultaneously increasing the tone of the anal sphincter, so that loose stool cannot be released uncontrollably from the rectum. An inactive state of the intestines, close to paralysis, allows food to have time to be absorbed into the bloodstream and slowly move towards the exit.
Indications and contraindications
"Loperamide" is a drug that is prescribed for various types of diarrhea:
- acute infectious and chronic form;
- irritable bowel syndrome;
- allergic form of diarrhea;
- dosage form;
- diarrhea while traveling.
That is, the drug is used to regulate stool during diarrhea. It is not recommended to combine Loperamide and alcohol, since the latter aggravates the problem, and the drug will not work at all.
Pregnant women and lactation women are not allowed to take Loperamide. It is allowed to take it in the second and third trimesters, but only after consultation with your doctor. The drug in question has other contraindications for use. So, you should not take tablets and capsules if you have intestinal obstruction, severe liver dysfunction, or individual intolerance to the drug. Since Loperamide is an opiate, it cannot be called absolutely safe. With prolonged and uncontrolled use, it can cause cardiac arrhythmias, constipation, allergic reactions, including itching and urticaria.
How to take Loperamide for diarrhea
First of all, it is important to understand the etiology of diarrhea. If diarrhea occurs due to excitement, or during a trip that provokes tourist syndrome, Loperamide will come in handy. The tablet must be taken immediately after defecation. That is, if there is a feeling that a bowel movement is about to occur, the feces should be allowed to come out, and then immediately take the drug. Loperamide will stop the bowels and strengthen the anal sphincter. If you do not allow a portion of feces to escape, intoxication may occur.
In case of poisoning, taking Loperamide is not justified, since the drug is not a sorbent and does not help stop the absorption of toxic substances into the blood. Instead, it will simply cause the intestines to freeze, and given the fact that there is low-quality food inside it, which caused diarrhea, the patient’s condition will only worsen, since the toxic substances will remain inside the gastrointestinal tract.
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, 2021
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.
A fragment of the program “About the Most Important Thing,” dedicated to bear disease. Participating: Ph.D. V.V. Vasilenko and Ph.D. S.N. Agapkin (video) |
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, 2021 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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How much does Loperamide Akrikhin cost?
There are many manufacturers producing Loperamide under different names. The addition “Akrikhin” indicates that the drug belongs to a specific company. The manufacturer Akrikhin KhFK JSC is not a representative of companies selling drugs at high prices, therefore, if the pharmacy does not have just Loperamide, and the pharmacist offers an analogue with the postscript “Akrikhin”, do not be alarmed. The price for a package of 20 tablets will cost about 59 rubles, and a box with a dozen tablets will cost only 30 rubles.
Compound
What does the medicine include? Loperamide capsules are yellow, hard gelatin, and contain a white substance (powder) with a pale yellow tint. The active component here is loperamide hydrochloride, and the auxiliary components are corn starch, lactose, magnesium stearate, talc, colloidal silicon dioxide. The capsule shell consists of gelatin, dye, titanium dioxide, and quinoline dye. The medicine belongs to the antidiarrheal symptomatic drug.
Can I take Loperamide during pregnancy?
Diarrhea that occurs during pregnancy should not become a reason to decide on self-medication. First of all, it is necessary to examine a pregnant woman for the presence of an intestinal infection. Then it is important to evaluate her diet in order to draw conclusions about the need to adjust the menu. If diarrhea is not the result of serious gastrointestinal disorders, Loperamide may be approved for use provided that the pregnancy is not in the first trimester.
Note!
The description of the drug Loperamide on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
Loperamide instructions: from what
The prescription of the drug is not always associated with the onset of diarrhea, although it is the main indication. If stool disorder occurs due to a reaction to taking medications, you should take Loperamide, which will stop the rapid movement of food through the intestines, and along with it, the medication taken.
This will allow the active substances not to be evacuated through the anus, but to remain in the intestine in order to have time to be absorbed into the blood and provide the expected therapeutic assistance. Diarrhea is often caused by taking antibiotics. If the patient takes antibacterial drugs, and they, along with frequent loose stools, immediately leave the body, no treatment will work. Therefore, diarrhea caused by taking medications is the first indication for prescribing Loperamide.
In addition, the drug is indicated for use in case of metabolic disorders. In this case, the patient, no matter how much he eats, does not gain weight, does not receive enough nutrients, as a result of which the body is rapidly depleted. Loperamide allows food to stay in the intestines, and vitamins and minerals to be absorbed through its walls.
If the patient has had surgery to remove the end of the intestine through an opening in the abdominal cavity, Loperamide may be prescribed to reduce the frequency of bowel movements and also allow food to remain in the lumen, which is especially important for those patients whose intestinal length has been significantly reduced as a result of the operation .
Contraindications and side effects
Loperamide anti-diarrhea tablets should not be prescribed for:
- hypersensitivity of the patient to the active and excipients of the drug
- patients who have been diagnosed with hereditary intolerance to galactose, because the drug contains lactose.
- exacerbation of acute dysentery, which is complicated by bleeding and fever
- diseases that are accompanied by intestinal obstruction
- ulcerative colitis, which is caused by treatment with antibiotics
- renal and liver failure.
Children under 12 years of age should not take Loperamide.
Loperamide should not be taken by pregnant women in the first trimester. In the second and third trimesters, the medicine is prescribed if the benefits of therapy do not outweigh the harmful effects on the fetus.
It is not recommended for breastfeeding women to use the drug, since loperamide can pass into mother's milk.
Loperamide in what doses should I take?
Most often, taking Loperamide is episodic in nature - during an attack of diarrhea. In case of acute stool disorder, take two tablets, which equals 4 mg of the active substance. If symptoms persist, repeat dosage is reduced to 1 tablet, but not earlier than 3 hours after taking the first two.
For chronic diarrhea, taking the drug can continue until the unpleasant symptom disappears. It is important to remember that you should not exceed the daily dose of 16 mg, which is equal to 8 tablets.
Description
This drug belongs to the opiate derivatives. The drug "Loperamide" is available in tablets and capsules. The drug does not have an analgesic effect, but affects the nerve endings that are located in the intestines, blocking the synthesis of prostaglandins. All this leads to a slowdown in intestinal motility and the movement of feces. Loperamide tones the sphincter and reduces the urge to defecate. The effect after administration lasts for four to six hours.
The medicine does not affect the cause of diarrhea (toxins, viruses, bacteria), but only eliminates the symptoms of intestinal disease and normalizes stool. If therapy for gastrointestinal infections is necessary, then Loperamide is prescribed as an additional remedy, but not the main one for fighting the infection. Is there compatibility between alcohol and Loperamide? We'll talk about this below.
Consequences
What are the consequences after taking Loperamide and alcohol? Although compatibility exists, you cannot take the pill with a strong drink. The active component of the drug does not perform its function. In addition, the consequences of Loperamide and alcohol may be as follows:
- the gastric mucosa is irritated;
- gastrointestinal diseases worsen;
- the load on the liver increases;
- the work of the cardiovascular system is enhanced;
- general health worsens.
In addition, the drug does not work 100%. It is impossible to get the desired result while taking medication and alcohol at the same time. So it is the patient who decides what is more important: to drink or undergo a therapeutic course. Doctors warn that such compatibility can negatively affect a person’s health and worsen his condition significantly.
Alcohol compatibility
Can Loperamide be taken with alcohol? This question remains to be answered. But even without delving into it, you should understand that combining medications and alcohol is still not worth it. The combined use of the drug in question and ethanol has a negative effect on a person’s well-being and health. Under the influence of ethanol, the liver begins to more actively decompose and remove alcohol from the body. Therefore, the therapeutic effect of Loperamide slows down, and diarrhea intensifies, including worsening chronic diseases. When a person drinks a Loperamide tablet and then an alcoholic drink, the result is a combination that contradicts each other and is mutually exclusive.
Loperamide and alcohol are not the best combination. Both experts and patients themselves talk about this. If you want to drink, a celebration is planned, it is better not to start treatment, but to wait for some time (if the condition is stable). Otherwise, you should avoid drinking alcohol and focus on your health.