Loperamide instructions for use capsule 2mg. Loperamide (Imodium). Deadly risks of uncontrolled intake. Dosage release and composition
1 capsule or tablet includes 2 mg loperamide hydrochloride - active ingredient.
Depending on the manufacturer, the composition of the additional ingredients indicated in the annotation to the drug may differ, but most often they are: aerosil, lactose, corn starch, magnesium stearate and talc.
Release form
Forms of release of the drug are Loperamide tablets or capsules with a different number of pieces per package (usually 10-20 units).
pharmachologic effect
Antidiarrheal .
Pharmacodynamics and pharmacokinetics
The antidiarrheal efficacy of loperamide is due to the ability of its active ingredient to bind to opioid (opiate) receptor complexes located in the walls of the intestine, as a result of which, under the influence of guanine nucleotides, stimulation occurs adrenergic and cholinergic neurons . The result of inhibition of release and acetylcholine is decreased motility and tone smooth intestinal muscles. Capsules or tablets inhibit intestinal motility and increase the time period during which its contents completely pass through it. The drug also enhances anal sphincter tone , reduces the number of urges to empty the bowels ( defecation ) and contributes to the containment of fecal masses in it. Capsules and tablets for diarrhea begin to act quickly enough and remain effective for 4-6 hours.
The absorption of the drug when taken orally is at the level of 40%. Plasma Cmax is detected after about 150 minutes. Binding to plasma proteins (mostly with) occurs at 97%. The main part of the active ingredient of the drug is amenable to metabolic transformations in the liver by conjugations , does not pass through GEB . T1 / 2, depending on the individual characteristics of the body, ranges from 9-14 hours. The primary route of excretion is with bile, the secondary (in a small amount in the form of conjugated metabolites) is with urine.
Instructions for use Loperamide
Indications for use Loperamide-Stada and Loperamide-Acri, as well as all other drugs with a similar active ingredient, are:
- states chronic and acute developed for various reasons, including its allergic , medicinal , emotional and radiation origin (for symptomatic therapy);
- development situations diarrhea due to a sharp changes food composition and diet in violation of absorption and metabolism ( traveler's diarrhea );
- infectious diarrhea (as an auxiliary remedy);
- the need to regulate stool consistency in patients with ileostomy .
Contraindications
In the clinical practice of using the drug, painful and other conditions of the human body were identified, which are significantly negatively affected by Loperamide capsules and tablets, from which they are prohibited for use when they are detected. Before taking medicines containing this active ingredient, you should make sure that the following conditions are not present, for which appropriate tests and / or tests are indicated.
Contraindications to the use of the drug include:
- intestinal obstruction ;
- personal hypersensitivity to the active and/or additional ingredients;
- in the acute phase;
- (in the first trimester);
- acute;
- subileus;
- pseudomembranous enterocolitis ;
- age up to 4 years (some manufacturers of capsules up to 6 years).
Side effects
- flatulence ;
- (including and / rash skin);
- nausea, vomiting;
- gastralgia ;
- feeling of dryness in the mouth;
- hypovolemia ;
- discomfort/abdominal pain;
- electrolyte disturbances;
- intestinal colic ;
- (rarely);
- intestinal obstruction (rarely).
Instructions for use Loperamide (Method and dosage)
Loperamide tablets, instructions for use
The drug in tablets, for example Vero-Loperamide, prescribed to adult patients in case of diarrhea acute nature at the initial dose of 4 mg. Subsequently, after each liquid defecation , 2 mg, up to the restoration of the normal consistency of the stool.
When chronic diarrhea initially prescribed 2 mg of the drug, with further individual selection of dosages, leading to the frequency of acts hard defecation twice a day. The dose range in this case may vary within 2-12 mg.
For 24 hours, you can take up to 16 mg of drugs as much as possible.
Capsules Loperamide, instructions for use
Instructions for use Loperamide-Acri, Shtada, Grindeks and other companies producing the drug in capsules, recommends that adults with acute diarrhea initial intake of 4 mg and subsequent 2 mg (after each act liquid defecation ).
At chronic diarrhea reception of Loperamide in a daily dosage of 4 mg is shown.
In both cases, the maximum allowable use is 16 mg of the drug in 24 hours.
Instructions for use for children
The drug in tablets is indicated for children 4-8 years old at a daily dosage of 3-4 mg, divided into 3-4 doses (1 mg at a time), for 3 days; children 9-12 years old - at a dose of 2 mg four times in 24 hours, for 5 days.
Given the contraindications for taking capsules, they begin to be prescribed to children from 6 years of age. At acute diarrhea shows the reception of 2 mg of drugs after each liquid defecation , with a maximum daily dose of 8 mg.
At chronic diarrhea , as a rule, appoint 2 mg in 24 hours, with a maximum daily dose of 6 mg per 20 kilograms of weight.
Overdose
In case of an overdose of any of the forms of drugs, the following signs of CNS suppression were noted: incoordination , stupor, respiratory depression , miosis , increased skeletal muscle tone, and intestinal obstruction .
In the caution of use and in the constant monitoring of the possible CNS toxicity patients with disabilities need .
Throughout the treatment diarrhea often seen electrolyte depletion and liquids requiring constant replenishment.
Due to the potential for suppression of CNS function by the drug, caution should be exercised when performing hazardous work, as well as driving a vehicle.
Analogues
Coincidence in the ATX code of the 4th level:Analogues of the drug are represented by combined drugs , Uzara , Loflatil and Diaremix .
Synonyms
Synonyms for drugs are Loperamide-Acri , diara , Loperamide-Stada , Vero-Loperamide , Loperamide-Lekhim , superilop etc.
Loperamide or Imodium - which is better?
Give an unambiguous answer which of these two drugs is more effective and safer in symptomatic treatment of diarrhea, very difficult, and all because both of these products include the same active ingredient with an identical mass content. It is possible that , produced in Belgium, has a better purification of its active ingredient compared to domestic counterparts, and therefore its action will be more productive and less toxic.
loperamide for children
An unequivocal medical opinion whether it is possible to give children drugs with this active ingredient, for example Loperamide-Stada, from which this drug helps and what risks it can lead to for the child's body, still does not exist. Different manufacturing companies indicate different age limits for taking Loperamide, which range from 2-12 years.
Following the recommendations of domestic manufacturers (described above), the appointment of any of the dosage forms of Loperamide for children under 4 years of age is prohibited. It is also contraindicated to use the drug in the form of capsules for the treatment of children under 6 years of age, from which Loperamide-Acri, Shtada, Grindeks and some other manufacturers, as a rule, releasing the drug in capsules, are not prescribed before reaching this age.
With alcohol
Although the official instructions do not indicate the joint use of Loperamide and alcohol , this combination will definitely have a negative effect on liver and CNS , due to complementary suppressive effects on their function. For this reason, during the antidiarrheal therapy drinking alcohol is not recommended.
Loperamide during pregnancy and lactation
It is absolutely forbidden to use Loperamide during (in the first trimester) and . A relative contraindication, taking into account all the possible risks for the fetus compared to the positive effect on the body of the expectant mother, is the entire subsequent period pregnancy .
Reviews about Loperamide
In the case of the use of the drug according to indications, reviews of Loperamide in 95% of cases are positive and speak of a fairly rapid and effective action of the drug. Only a few patients, belonging to the remaining 5%, experience serious negative consequences of therapy associated with personal hypersensitivity or moderate side effects. Naturally, the ongoing treatment can be successful only if the drug is used for its intended purpose and will be ineffective, and sometimes dangerous, if diarrhea bacterial , secretory , viral and other etiologies. For this reason, prior to antidiarrheal therapy it is best to accurately determine the cause of the pathological process, and based on these data, prescribe the appropriate treatment.
Loperamide price, where to buy
The price of Loperamide in Russian pharmacies is available to any category of patients and, depending on the manufacturer of the drug and the number of tablets, varies between 15-60 rubles. For example, the price Loperamide-Acri No. 20 on average is 50 rubles, buy 20 capsules of the drug produced by Nizhpharm OJSC ( Loperamide-Stada), you can for 35 rubles, and the cost of 20 tablets from Veropharm's diarrhea ( Vero-Loperamide) fluctuates around 15-20 rubles.
- Internet pharmacies in Russia Russia
- Internet pharmacies of Ukraine Ukraine
- Internet pharmacies of Kazakhstan Kazakhstan
ZdravCity
Diara (loperamide) tab. zhev. 2mg n12JSC Obolenskoye pharm. company
Loperamide tab. 2mg n20 Ozone LLC
Loperamide-Acriquin caps. 2mg n10 JSC Akrikhin
Loperamide-Acriquin caps. 2mg n20 JSC Akrikhin
Loperamide is one of the medicines that help with diarrhea in children. Acute diarrhea in children begins suddenly and most often goes away after a few days. If diarrhea occurs, it is initially recommended to drink plenty of water to prevent dehydration. We will take a closer look at the use of loperamide in children and its analogues.
Composition, principle of action and dosage form of Loperamide
Loperamide contains the following inactive ingredients: colloidal dioxide, gelatin, iron oxides, lactose, magnesium, microcrystalline cellulose, starch and titanium dioxide. Available in the following types:
- Tablets 2 mg. Contains a small amount of lactose. Take with a glass of water, milk or juice. Chewing is not recommended.
- Capsules 2 mg. The content and use is the same as that of tablets.
- Powder 1 mg. Diluted in 5 ml of water.
Loperamide slows down bowel activity and promotes water retention, preventing dehydration. Reduces daily stool volume, increases stool viscosity and bulk density, reduces fluid and electrolyte loss.
In what cases is the drug prescribed?
Before taking this drug, it is highly recommended to consult a specialist.
Loperamide helps with acute diarrhea Why does the doctor prescribe Loperamide:
- To prevent diarrhea. Diarrhea occurs due to an infection or an allergy to the components of the food used.
- As an additional drug to the main medications after surgery.
- To cope with severe diarrhea that lasts for several hours.
At what age can a child be given this medicine for diarrhea?
Is it possible to give Loperamide to children and from what age? This drug is contraindicated in children under 2 years of age. If the pediatrician nevertheless prescribed this medicine to the child, then it is worth strictly observing the dosage indicated by the doctor in order to avoid negative consequences. If your baby is two years old, then there are no contraindications.
Children from two to seven years old should follow the dosage indicated in the instructions for use. In case of an overdose, you should immediately consult a doctor.
Application restrictions
Restrictions on the use of the drug arise in the following circumstances:
- stomach ache;
- diarrhea with high fever;
- ulcerative colitis;
- bloody, black, or tarry loose stools;
- allergic to loperamide.
When a doctor prescribes Loperamide to a child, be sure to inform the specialist about:
- fever
- mucus in the stool;
- liver diseases;
- already taken antibiotics.
Loperamide must be taken strictly according to the instructions. When taking Loperamide, you need to drink plenty of fluids. In this case, it may take about 48 hours of taking Loperamide before the patient's condition improves. Continue to use this medicine as directed and tell your doctor if there is no improvement after 4 days of treatment.
Dosages of capsules and tablets for children
The drug is dispensed in a pharmacy without a prescription. For children aged 2 to 5 years, the medicinal powder is diluted in water (5 ml) and given orally. For ages 6 and older, tablets or capsules are recommended.
- from two to five years: 1 mg 3 times a day (body weight 13-20 kg);
- older than six years: 2 mg 2 times a day (body weight 20-30 kg).
Follow-up recommended dosage: After the first day of treatment, it is recommended that previous doses (1 mg per 10 kg of body weight) be administered only after loose stools. The daily dose does not exceed the recommended figures of the first day.
Side effects and overdose
Strictly follow the instructions for use. Exceeding the dose can lead to constipation, heart disease, liver and kidney disease, etc.
Rarely, some children experience side effects when using this medication, which can lead to negative consequences and even death if the cause is not identified in time. Tell your doctor or get medical help right away if your child has any of the following symptoms after using this medicine:
- signs of an allergic reaction such as hives, itching, blistering or scaly skin with or without fever;
- wheezing;
- chest pain or palpitations;
- constipation;
- bloating;
- black, tarry or bloody stools.
Can Loperamide be treated concomitantly with other drugs?
Be sure to tell your doctor what other medicines you are taking in parallel with Loperamide. Especially if you start or stop using:
- gemfibrozil;
- stomach acids - cimeditin, raniditin;
- ritonavir.
Loperamide can cause serious heart problems if the following drugs are used in addition to it: fluconazole, methadone, an antibiotic, an antifungal or antimalarial, heart medications, and sedatives. Be careful with this.
Means analogues
Linex for children (more in the article:) In addition to loperamide, other drugs can be given. It could be:
- Linex - contains lyophilized probiotic bacteria that regulate the intestinal microflora. These bacteria are resistant to antibiotics and other antimicrobials. They normalize the digestive tract and strengthen the immune system.
- Imodium - like Loperamide, can stop diarrhea, but only in the absence of an intestinal infection (more in the article:). Despite the fact that in the pharmacy this medicine is dispensed without a prescription, it must still be prescribed by a doctor.
- Lopedium - can be used with other drugs. Stops diarrhea by slowing down bowel activity.
- Enterol - suitable for additional treatment of acute infectious diarrhea, treatment and prevention of colitis accompanied by diarrhea, prevention of antibiotic treatment (we recommend reading:). Can be used by adults, teenagers and children from 2 to 7 years old. Children under 2 years of age are prescribed only the contents of the capsules.
Loperamide is a symptomatic antidiarrheal agent.
Release form and composition of Loperamide
Loperamide is available in the form of tablets, oral solution, capsules.
The main active ingredient of the drug is loperamide hydrochloride.
Loperamide tablets are white with a flat surface.
Each loperamide tablet contains 2 mg loperamide hydrochloride.
As excipients in loperamide tablets are used: calcium stearate, granulac-70, potato starch.
Loperamide capsules are available under the name Loperamide-acry.
Loperamide-acry capsules are yellow in color, inside is a white or yellowish-white powder.
Auxiliary substances of loperamide-acry are: corn starch, lactose, aerosil, magnesium stearate, talc.
Pharmacological action of loperamide
Loperamide is a substance that inhibits intestinal motility. It eliminates the diarrhea phenomenon, and, interacting with the opiate receptors of the intestinal walls, promotes the release of acetylcholine and prostaglandin, which ensures the suppression of the symptoms of diarrhea. During the period of action of the drug, intestinal motility slows down and the period necessary to move the contents of the intestine increases. Loperamide significantly increases the tone of the sphincter, providing a decrease in the frequency of the urge to defecate, as well as the retention of feces.
Loperamide inhibits the secretion of electrolytes and fluid into the intestinal lumen and stimulates the absorption of water and salts from the intestine. The action of Loperamide is fast and lasts 4-6 hours.
Instructions for use Loperamide
Loperamide and Loperamide-acry are prescribed for the treatment of chronic and acute diarrhea of various origins (emotional, allergic, radiation, medicinal), as well as due to changes in the qualitative composition of food and diet, malabsorption and metabolism; as an aid in diarrhea of infectious origin; for the regulation of stool in patients suffering from ileostomy.
Contraindications
According to the instructions Loperamide should not be used:
- With intestinal obstruction;
- With constipation, bloating, subileus, acute dysentery, acute ulcerative colitis, pseudomembranous colitis that occurred after treatment with broad-spectrum antibiotics;
- In childhood up to 4 years;
- In the first trimester of pregnancy;
- With hypersensitivity to loperamide.
Method of application and dosage
According to instructions. Loperamide for adult patients is administered orally:
- in acute diarrhea, 2 mg after each act of defecation. In this case, the first dose of Loperamide should be 4 mg;
- in 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.
In acute diarrhea loperamide 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, it is prescribed 2 times a day, 2 mg;
- children 9-12 years old are prescribed 2 mg three times a day. If diarrhea continues, then the drug is prescribed 2 mg after each act of defecation. In this case, the maximum daily dose of 6 mg per 20 kg of body weight should not be exceeded.
In chronic diarrhea, Loperamide for children over 5 years of age is prescribed in a daily dose of 2 mg.
If there is no stool for more than 12 hours and when it normalizes, the drug is canceled.
Side effects of loperamide
In the instructions for Loperamide, side effects are noted, which, as a rule, occur with prolonged use of the drug:
- Gastrointestinal tract: bloating, constipation, intestinal colic, abdominal discomfort and pain, vomiting, nausea, dry mouth, rarely intestinal obstruction;
- Nervous system: drowsiness, fatigue, dizziness;
- Allergic reactions: urticaria, skin rash, rarely - anaphylactic shock.
- Others: rarely - urinary retention.
Use during pregnancy and lactation
Loperamide should not be taken in the first trimester of pregnancy and during breastfeeding, as adequate studies have not been conducted in pregnant women and nursing mothers.
Overdose
In case of overdose, there may be observed: intestinal obstruction, constipation, muscular hypertension, miosis, drowsiness, stupor, coordination disorders, respiratory depression.
In case of an overdose of the drug, it is necessary to administer activated charcoal and gastric lavage; if necessary - maintaining the function of breathing. If intoxication is suspected, then naloxone is used as an antidote. Since the action of loperamide is longer than that of naloxone, the patient should be observed by a doctor for at least 48 hours.
Interaction with other drugs
With the simultaneous use of Loperamide or Loperamide-acry and cholestyramine, the effectiveness of Loperamide may decrease.
With the combined use of Loperamide with ritonavir, co-trimoxazole, the bioavailability of Loperamide increases.
The simultaneous use of loperamide with opioid analgesics increases the risk of severe constipation.
special instructions
If within two days from the start of taking the drug with acute diarrhea, no clinical improvement is observed, or bloating, constipation appears, partial intestinal obstruction develops, then it is necessary to stop taking Loperamide and clarify the diagnosis in order to exclude the infectious nature of diarrhea.
If the cause of the disease is known, then the use of etiotropic agents is required.
The use of loperamide may be repeated if specific treatment and diet do not resolve the diarrhea.
Reception of Loperamide in chronic diarrhea is possible only on prescription.
Loperamide should be used with caution in children, as they are more sensitive to the opiate-like effects of the drug.
In the treatment of diarrhea, replacement of the loss of electrolytes and fluids is required. Dehydration may lead to a change in the response to the drug.
Loperamide should be used with caution in elderly patients.
Patients with liver dysfunction require careful monitoring of symptoms of toxic damage to the central nervous system.
Children under the age of 6 years, Loperamide in tablets and Loperamide-acry in capsules are not prescribed.
Since loperamide can cause drowsiness, weakness, dizziness, then when taking the drug, care should be taken when working with machinery and driving a car.
Storage conditions
The drug should be stored in a dark, dry place out of the reach of children at a temperature of 15-30º C.
(lat. Loperamide) is an antidiarrheal drug.
Chemical compound: 4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-alpha,alpha-diphenyl-1-piperidine butanamide (as hydrochloride). Empirical formula C 29 H 33 ClN 2 O 2 . A derivative of phenylpiperdine.
Loperamide is an international non-proprietary name (INN) of a medicinal product. According to the pharmacological index, loperamide belongs to the group "Antidiarrheal agents". According to ATC - to the group "A07 Antidiarrheal drugs", subgroup "Drugs that reduce gastrointestinal motility" and has the code A07DA03.
"" (as well as " loperamide hydrochloride», « Loperamide-Acri», « Vero-Loperamide”), in addition, is the trade name of a number of drugs manufactured by pharmaceutical enterprises of 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 about 13 rubles per pack.
Loperamide is used for acute non-infectious diarrhea, as well as for mild to moderate infectious diarrhea. Loperamide is the drug of choice for the treatment of traveler's diarrhea. The action 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 keeps 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. Thus, the absorption time of water and electrolytes increases, their loss decreases and the loss decreases and the time of the protective action of immunoglobulins, which are released into the intestinal lumen during acute intestinal diarrhea, increases. Loperamide increases the tone of the anus sphincter, resulting in a decrease in the frequency and severity of the urge to defecate. Loperamide reduces mucus hypersecretion in the colon, in addition, it has an antisecretory effect, which is realized through both opioid and non-opioid receptors. Loperamide, due to 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 antidiarrheal drug, 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 due to 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 in motor diarrhea with increased peristalsis (irritable bowel syndrome (IBS) and functional diarrhea), but is not effective in diabetic enteropathy, scleroderma, amyloidosis. Moreover, in these situations, it can exacerbate diarrhea. With secretory diarrhea, loperamide is also very effective due to its antisecretory opiate-like action. With infectious diarrhea, the drug should be prescribed with caution, since the delay of the infectious agent in the body increases diarrhea and intoxication. Loperamide well relieves diarrhea in Crohn's disease, but in ulcerative colitis it is not recommended to prescribe it because of the 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, the so-called functional diarrhea, which, unlike organic (for example, infectious) diarrhea, occurs 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 is, depending on the consistency of the stool, 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 the drug therapy of diabetic diarrhea (Kolesnikova E.V.). In case of anorectal dysfunction, which is a complication of diabetes mellitus, symptomatic therapy with loperamide will have a positive result and reduce the symptoms of imperative urges (Leites Yu.G., Galstyan G.R., Marchenko E.V.).
Professional medical publications concerning the effects of loperamide on the gastrointestinal tract :
- Belousova E.A., Zlatkina A.R. Diarrhea syndrome in the practice of a gastroenterologist: pathophysiology and a 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 system // Journal "Mistetstvo 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 when taking large doses of the antidiarrheal drug loperamide (Imodium), including abuse and misuse. June 7, 2016
- The FDA is limiting the package size of the antidiarrheal drug loperamide (Imodium) to increase its safety. January 30, 2018
- non-infectious diarrhea of various forms and different genesis: 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)
- stool regulation in patients with ileostomy
Dosage and administration:
inside (capsules - without chewing, drinking water; lingual tablet - on the tongue, it disintegrates within a few seconds, after which it is swallowed with saliva without drinking water). In acute diarrhea, adults are prescribed an initial dose of 4 mg; then 2 mg after each act of defecation (in the case of liquid feces); the highest daily dose is 16 mg. When administered in drops: initial dose - 60 drops of a 0.002% solution; then 30 drops after each act of defecation; the maximum dose is 180 drops per day (for 6 times). In chronic diarrhea, adults are prescribed 4 mg per day. The maximum daily dose is 16 mg. In 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 of 30 drops of a 0.002% solution; then 30 drops 3 times a day; the maximum dose is 120 drops per day (for 4 doses). In chronic diarrhea for children over 5 years old, loperamide is prescribed in a daily dose of 30 drops or 2 mg. Children aged 2-5 years are prescribed in a solution for oral administration, 5 ml (1 measuring cap) per 10 kg; frequency of appointment - 2-3 times a day. The maximum daily dose is 6 mg per 20 kg. If a normal stool appears or if there is no stool for more than 12 hours, the drug is canceled (Instructions for use). In 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 reached within one hour, which is faster than when using other dosage forms. Lingual tablet does not require drinking water, can be used in patients with difficulty swallowing and increased gag reflex.
In chronic diarrhea, with IBS, the usual dosage form of loperamide is prescribed. Promising is the drug with a complex active substance loperamide + simethicone, which effectively absorbs gases in the intestine.
WHO position on the use of loperamide in the treatment of diarrhea in children :
The following loperamide-containing medicines are registered in the US: Diamode, Imodium A-D, Imodium A-D EZ Chews, Imodium A-D New Formula, Kao-Paverin, Kaopectate 1-D, Imodium, Maalox Anti-Diarrheal, Pepto Diarrhea Control, Imotil, Diar-Aid. In the United States, drugs can be either OTC or prescription, depending on the loperamide content.
Instructions for different manufacturers of loperamide
Instructions for some manufacturers of medicines containing loperamide as the only active ingredient (pdf): - for Russia: "Instruction for the use of the drug Loperamide-Akri", JSC "Akrikhin"
- for Ukraine (in Russian): "Instruction for the medical use of the drug Loperamide", JSC "Kyivmedpreparat"
Loperamide has contraindications, side effects and application features, consultation with a specialist is necessary.
The abuse of over-the-counter opiate-based antidiarrheals is a growing problem that puts patients at risk of heart rhythm disturbances and death. An article on this issue, illustrated by two illustrative clinical cases, was published online on April 29, 2016. in the Annals of Emergency Medicine. The focus of this publication is loperamide (Imodium, manufactured by Johnson & Johnson), a cheap, over-the-counter antidiarrheal drug that suppresses intestinal motility through its μ-opioid receptor agonism, calcium channel blockade, calmodulin inhibition, and reduction of paracellular permeability. The potential for abuse of this drug has traditionally been thought to be very low due to its low oral bioavailability and poor central nervous system penetration.
However, two recent cases of fatal misuse of loperamide call attention to this drug. Despite the implementation of standard resuscitation measures, the death of both of these patients had to be ascertained already upon their admission to the emergency department. Taken together, these cases highlight the acute problem of opiate abuse in the United States. The scale of this problem is growing and, while the authorities of the country are doing everything to limit access to opioid drugs, addicted people are trying to find workarounds, which, as we now know, can include loperamide. At the same time, loperamide, being cardiotoxic, occupies a unique position among opiates in terms of danger.
The first of the clinical cases described in the article concerns a 24-year-old man with a history of drug addiction, for which he received buprenorphine replacement therapy. The patient was found at home with no pulse or respiration, with convulsive activity. Six empty packages of loperamide were found nearby. Standard resuscitation measures of chest compressions, naloxone, and intubation failed, and the patient was declared dead shortly after admission to the emergency department. At autopsy, there were signs that the patient was abusing loperamide to self-medicate opioid withdrawal symptoms. The concentration of loperamide in the blood taken from the cavities of the heart was 77 ng / ml (therapeutic range, 0.24 - 3.1 ng / ml). Autopsy revealed pulmonary edema, cerebral edema, urinary retention, moderate cardiomegaly, and thrombosis of the veins of the lower extremities.
The second case involved a 39-year-old man, also with a history of opiate addiction, for which he was also receiving buprenorphine. An ambulance was called to him due to fainting and difficulty breathing. Arriving ambulance officers discovered asystole and began resuscitation, which continued on the way to the hospital. Death was pronounced upon admission to the emergency department. According to the patient's relatives, after stopping buprenorphine (3 years ago), he used over-the-counter antidiarrheal drugs to self-treat his opiate addiction. Autopsy revealed cardiomegaly and severe pulmonary edema. A post-mortem toxicology study revealed a loperamide concentration in blood from the femoral artery of 140 ng/mL.
The authors of the article believe that it is not yet clear whether the OTC status of loperamide needs to be reconsidered, and also remind that the long-term effects of the drug cannot always be predicted based on animal models and preclinical studies.
However, they believe that the pharmacovigilance system itself, which monitors drugs after they are on the market, and also evaluates their impact on the population, needs to be changed. The authors point out that the US Food and Drug Administration's (FDA) voluntary program for reporting adverse events, MedWatch, is passive and rather toothless. Among the most obvious measures to optimize its work, the authors name the monitoring of patient Internet forums. With regard to loperamide, they emphasize that reports of abuse of oral loperamide appeared on bulletin boards as early as 2005. A recent analysis looking at 1,290 posts on a single website showed a 600% increase in postings between 2009 and 2011. This is also consistent with data from poison control centers that report a 7-fold increase in call rates due to misuse or abuse of lopyramide between 2011 and 2015. In another study, in the majority of these reports (70%), loperamide was discussed in forums as a self-treatment for opioid withdrawal, but about a quarter of those who posted about it on bulletin boards reported using the drug because it made them euphoric . This is a good example of how online forums can provide timely information about drug abuse.