Imodium Express
Imodium Express: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Imodium Express
ATX code: A07DA03
Active ingredient: loperamide (Loperamide)
Manufacturer: Catalent Yu. K. Swindon Zidis, Ltd. (Catalent UK Swindon Zydis, Ltd.) (UK)
Description and photo update: 2020-23-07
Imodium Express is an antidiarrheal agent.
Release form and composition
Dosage form - lyophilisate tablets: round, almost white or white, on one side there is a chamfer, on the other side there may be a bulge in the center, uneven surface roughness, uneven thinned edges (in a cardboard box 1-2 blisters of 10 tablets, or 1 or 3 blisters of 6 tablets and instructions for the use of Imodium Express).
Composition of 1 tablet-lyophilisate:
- active substance: loperamide hydrochloride - 2 mg;
- auxiliary components: sodium bicarbonate, aspartame, mannitol, gelatin, purified water (evaporated during lyophilization), mint flavor.
Pharmacological properties
Pharmacodynamics
Loperamide in the intestinal wall binds to opioid receptors, thereby inhibiting the release of prostaglandins and acetylcholine. This slows down the process of peristalsis and increases the time it takes for the contents to pass through the intestines. Also, the drug increases the tone of the anal sphincter, thereby reducing the urge to defecate.
According to clinical studies, the antidiarrheal effect develops within 1 hour after taking the recommended single dose of 4 mg.
Pharmacokinetics
After oral administration, most of the loperamide is absorbed in the intestine. However, the systemic bioavailability is only 0.3%, since the drug undergoes active first-pass metabolism. For the same reason, the plasma concentration of unchanged loperamide is very low.
About 95% of the dose taken is associated with plasma proteins (especially albumin).
Loperamide is metabolized mainly in the liver. After conjugation, the drug is excreted in the bile. The main metabolic pathway is oxidative N-demethylation, carried out to a greater extent with the participation of an inhibitor of isoenzymes CYP2C8 and CYP3A4.
In preclinical studies, it was possible to establish that loperamide is a substrate of P-glycoprotein.
The period of elimination of the drug from the body is 9-14 hours (average 11 hours). The unchanged substance and its metabolites are excreted mainly in the feces.
Pharmacokinetic studies of loperamide in children have not been conducted. Presumably, these indicators, as well as drug interactions with other drugs, will be the same as in adult patients.
Indications for use
- symptomatic monotherapy of acute and chronic diarrhea, regardless of origin: allergic, drug, radiation, emotional, due to impaired absorption and metabolism, changes in diet or composition of the diet;
- adjunctive treatment of infectious diarrhea;
- therapy of stool disorders with ileostomy.
Contraindications
Absolute:
- phenylketonuria;
- children under 6 years old;
- I trimester of pregnancy;
- lactation period;
- hypersensitivity to any component of the lyophilisate tablets.
As a monopreparation Imodium Express cannot be used in the following cases:
- ulcerative colitis in the acute stage;
- acute dysentery, accompanied by high fever and bloody stools;
- bacterial enterocolitis caused by pathogens (eg Campylobacter spp., Salmonella spp., Shigella spp.);
- pseudomembranous colitis caused by taking antibiotics.
The drug should also not be used in conditions when it is dangerous to slow down peristalsis due to the high risk of developing serious complications, such as intestinal obstruction, megacolon (including toxic). If Imodium Express was nevertheless accepted, then if bloating or constipation develops, it should be immediately canceled.
Imodium Express should be used with caution in case of liver dysfunction.
Imodium Express, instructions for use: method and dosage
Imodium Express is indicated for oral administration. The lyophilisate tablet should be put on the tongue and kept until completely dissolved, after which it should be swallowed with saliva without drinking water.
The tablets are quite fragile in structure. In order not to damage them, do not get out by pushing the foil. It is recommended to carefully remove the foil by grasping the edge of the foil with your hand, then lightly press down on the cell from below and carefully remove the tablet.
Recommended dosage regimen of Imodium Express:
- acute diarrhea: initial dose for adults - 4 mg (2 tablets), for children from 6 years old - 2 mg (1 tablet), then patients of any age should take 1 tablet after each visit to the toilet in case of loose stools;
- chronic diarrhea: at the beginning of treatment, adults are prescribed 4 mg per day, children from 6 years old - 2 mg. Then the dose is adjusted so that the normal stool is 1-2 times a day. The maintenance daily dose may be 2–12 mg (1–6 tablets).
The maximum permissible daily dose for adults is 12 mg, for children - 6 mg for every 20 kg of body weight, but not more than 12 mg per day.
Imodium Express should be canceled if there is no stool for more than 12 hours in a row or if it normalizes.
Side effects
The following adverse reactions of Imodium Express have been observed in clinical studies:
- with a frequency of ≥ 1% in patients with acute diarrhea: flatulence, constipation, vomiting, nausea, headache;
- with a frequency of ≥ 1% in patients with chronic diarrhea: nausea, constipation, flatulence, dizziness.
In post-marketing studies, the following side effects have been identified:
- from the gastrointestinal tract: often (from ≥ 1% to <10%) - flatulence, constipation, nausea; infrequently (from ≥ 0.1% to <1%) - dry mouth, abdominal discomfort / pain, epigastric pain, dyspepsia, vomiting; rarely (from ≥ 0.01% to <0.1%) - bloating, glossalgia, megacolon (including toxic), intestinal obstruction (including paralytic);
- from the kidneys and urinary tract: rarely - urinary retention;
- from the nervous system: often - dizziness, headache; infrequently - drowsiness; rarely - increased fatigue, hypertonicity, depression of consciousness, impaired coordination, stupor, loss of consciousness;
- on the part of the organ of vision: rarely - miosis;
- on the part of the skin and subcutaneous tissues: infrequently - skin rashes; rarely - urticaria, pruritus, angioedema, bullous rash (including toxic epidermal necrolysis, erythema multiforme, Stevens-Johnson syndrome);
- from the immune system: rarely - anaphylactoid reactions, anaphylactic shock, hypersensitivity reactions.
Overdose
An overdose of Imodium Express, including relative due to impaired hepatic function, may be accompanied by the following symptoms: urinary disorders, constipation, paralytic intestinal obstruction, depression of the central nervous system (vomiting with impaired consciousness, muscle hypertonicity, miosis, coordination disorder, airway obstruction, drowsiness, stupor, respiratory depression). The effect of loperamide on the central nervous system is more pronounced in children and patients with impaired liver function.
With deliberate intake of an excessive dose (40–240 mg per day), there are cases of prolongation of the QRS complex and the QT interval, serious ventricular arrhythmias (including tachycardia of the "pirouette" type), fainting, cardiac arrest, and even death.
In case of accidental intake of a high dose of Imodium Express, it is recommended to consult a doctor for timely ECG monitoring for prolongation of the QT interval and the development of other side effects from the cardiovascular system. As an antidote, if necessary, use naloxone (used twice, since the duration of its action is much shorter than that of loperamide). The patient is closely monitored for 48 hours to identify possible signs of central nervous system depression.
special instructions
Imodium Express tablets are used only for the symptomatic treatment of diarrhea (that is, for its relief). If the cause of diarrhea is unknown, it is necessary to reconsider the tactics of therapy.
Diarrhea in most cases is accompanied by a loss of fluid and electrolytes, therefore replacement therapy is recommended, especially in children.
If there is no effect within 2 days of taking the tablets, you should consult a doctor as soon as possible to clarify the diagnosis and exclude the infectious origin of the problem.
There have been cases of abuse and use of loperamide as an opioid substitute in opioid dependent individuals.
It has been reported about the development of ventricular arrhythmias and prolongation of the QT interval, up to death, with an overdose of Imodium Express. Therefore, the drug should not be taken for a long time without medical supervision. It is also forbidden to independently increase the recommended dose and / or duration of therapy.
Patients with AIDS and infectious viral or bacterial colitis receiving loperamide may experience constipation, and the risk of developing toxic megacolon increases. Therefore, in the event of the appearance of the first ghosts of bloating or intestinal obstruction, you should immediately stop taking Imodium Express tablets.
Influence on the ability to drive vehicles and complex mechanisms
Imodium Express in rare cases causes dizziness, increased fatigue, drowsiness and other undesirable effects that affect the speed of reactions and the ability to concentrate. For this reason, during the period of treatment with an antidiarrheal agent, it is recommended to refrain from driving a car and performing potentially dangerous types of work.
Application during pregnancy and lactation
Taking Imodium Express is not recommended during pregnancy and lactation.
Pediatric use
Imodium Express is contraindicated in children under the age of 6 years.
With impaired renal function
No dose adjustment is required for impaired renal function.
For violations of liver function
With violations of hepatic function, the presystemic metabolism of loperamide slows down, which is fraught with the development of the toxic effect of the drug in case of a relative overdose. In this regard, Imodium Express should be used with caution.
Use in the elderly
No dose adjustment of Imodium Express is required for elderly patients.
Drug interactions
Taking 16 mg of loperamide, which is a substrate of P-glycoprotein, simultaneously with quinidine or ritonavir, which are inhibitors of P-glycoprotein, was accompanied by an increase in the plasma concentration of loperamide by 2–3 times. However, when using the antidiarrheal drug in recommended doses, the significance of this interaction has not been established.
Taking 4 mg of loperamide simultaneously with itraconazole, which is an inhibitor of P-glycoprotein and the isoenzyme CYP3A4, led to an increase in the plasma concentration of loperamide by 3-4 times. In the same study, gemfibrozil (an inhibitor of the isoenzyme CYP2C8) caused an approximately 2-fold increase in plasma loperamide concentration.
Taking 16 mg of loperamide with ketoconazole, which is an inhibitor of P-glycoprotein and the isoenzyme CYP3A4, led to a 5-fold increase in the concentration of loperamide in plasma.
The simultaneous use of a combination of itraconazole and gemfibrozil with loperamide led to an increase in the maximum plasma concentration of the latter by 4 times, and the total concentration by 13 times. At the same time, no effect on the central nervous system was noted.
Loperamide, when taken together, increases the plasma concentration of desmopressin by 3 times. This is probably due to a slowdown in gastrointestinal motility.
It is expected that drugs with pharmacological properties similar to loperamide will be able to enhance its effect.
Medicines that increase the rate of passage through the gastrointestinal tract can reduce the effectiveness of loperamide.
Analogs
Analogs of Imodium Express are Diara, Diosmectite, Lopedium, Neosmectin, Smectin, Superilop, Usara, Hilak Forte, Enterol, Endosorb, etc.
Terms and conditions of storage
Store in its original packaging at a temperature of 15-30 ° C out of reach of children.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Available without a prescription.
Reviews about Imodium Express
According to most reviews, Imodium Express is an effective remedy that, due to its soluble dosage form, very quickly eliminates the symptoms of diarrhea.
Side effects include dry mouth, drowsiness and nausea. The taste of the tablets is often described as moderately mint, but some found it unpleasantly bitter.
As a disadvantage, almost all patients attribute the high cost of the drug in comparison with many other drugs with a similar effect.
Price for Imodium Express in pharmacies
The price of Imodium Express in the form of 2 mg lyophilisate tablets is from 190 rubles. per pack of 10
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
