Loperamide Grindeks capsules 2mg №10×1

Name:
Loperamide Grindeks caps. 2 mg in blister pack No. 10×1
Description:
Hard gelatin capsules. The body is pink, the lid is dark green. The main active ingredient Loperamide hydrochloride Release form 10 capsules in a blister of PVC film and aluminum foil. 1 blister with instructions for medical use in a cardboard box. Dosage 2 mg in a blister in pack No. 10×1 Special instructions The capsules contain a crimson dye 4R (E 124), which can cause allergic reactions. The capsules also contain lactose, so the drug should not be used in patients with lactose intolerance, galactosemia and glucose / galactose malabsorption. Pharmacodynamics Loperamide binds to opiate receptors in the intestinal wall. As a result, it inhibits the release of acetylcholine and prostaglandins, reducing propulsive peristalsis and prolonging the transit time of intestinal contents. Loperamide increases the tone of the anal sphincter, reducing incontinence and the need to defecate. Due to its high affinity for the intestinal wall and rapid metabolism, loperamide enters the bloodstream in very small amounts. Pharmacokinetics Absorption After oral administration, loperamide is absorbed from the intestine, however, as a result of a pronounced first-pass metabolism, systemic bioavailability is about 0.3%. Distribution Loperamide has a high affinity for receptors in the longitudinal muscles of the intestinal wall. 95% of the active substance binds to plasma proteins, mainly albumin. Loperamide is a P-glycoprotein substrate. Biotransformation Loperamide is almost completely excreted from the body through the liver, where it is metabolized, conjugated and excreted in the bile. Oxidative N-demethylation is the main route of metabolism of loperamide and is mediated by CYP3A4 and CYP2C8. Elimination The elimination half-life of loperamide is 11 hours (range 9 to 14 hours). Unchanged loperamide and its metabolites are excreted mainly in the faeces. Indications for use Symptomatic treatment of acute diarrhea in adults and children over 12 years of age. Dosage and administration Capsules are taken orally, without chewing, with a small amount of liquid. Adults and children over 12 years old The initial dose is 2 capsules (4 mg), then 1 capsule (2 mg) is used after each liquid emptying of the abdomen. The maximum daily dose should not exceed 6 capsules (12 mg). Children under 12 years of age: the drug should not be used. Elderly patients and patients with impaired renal function do not need dose adjustment. Patients with impaired liver function. Although there are no pharmacokinetic data on the effect of the drug in patients with impaired liver function, it is necessary to prescribe the drug with caution in such patients due to a slowdown in their first-pass metabolism. The duration of use should not exceed 48 hours. If symptoms do not improve within two days, stop taking the drug and consult a doctor. If the emptying of the abdomen normalizes earlier, the use of the drug should be discontinued. If you miss another dose of the drug, take it immediately. Do not use a double dose to replace a missed one. Continue taking as directed by your doctor. Application during pregnancy and lactationDespite the lack of data on the teratogenic and embryotoxic properties of the drug, prescribe loperami Loperamide in small amounts passes into breast milk, so if necessary, the use of the drug should stop breastfeeding. Precautions The possible risk from misuse of loperamide can be significantly reduced by limiting the duration of use to 48 hours, avoiding use in children under 12 years of age, as well as in case of fever or in the presence of blood in the stool. In the course of treatment with loperamide, it is necessary to follow an appropriate diet and choose the optimal regimen for fluid intake. Patients suffering from inflammatory bowel disease, with bloating, the use of the drug should be immediately discontinued, since this is one of the signs of toxic megacolon. The decrease in intestinal motility under the influence of loperamide can enhance the penetration of certain strains of microorganisms into the intestinal mucosa and, as a result, prolong diarrhea while maintaining elevated temperature. Loperamide should be used with caution in patients prone to prolongation of the QT interval, torsades de pointes and other serious arrhythmias, or who are taking inhibitors of cytochrome CYP3A4, CYP2C8, P-glycoprotein, as this may increase the side effects. Patients with impaired liver function should be warned about the possible inhibitory effect of the drug on the central nervous system due to the accumulation of loperamide in the body. In patients with impaired renal function, dose adjustment of loperamide is usually not required, since it and its metabolites are excreted mainly in the faeces. Elderly patients and children over 12 years of age may mask the symptoms of dehydration and change the response to loperamide. Therefore, during the treatment of diarrhea (especially in children), it is necessary to replenish the loss of fluid and electrolytes. Loperamide can cause urinary retention in children. Do not exceed the recommended dose of the drug. An overdose of loperamide can cause serious side effects. If there is no effect within two days of taking the drug, the diagnosis should be clarified and the infectious genesis of diarrhea should be excluded. The capsules contain dye crimson 4R (E 124), which can cause allergic reactions. The capsules also contain lactose, so the drug should not be used in patients with lactose intolerance, galactosemia and glucose / galactose malabsorption. Interactions with other medicinal products Concomitant medicinal products may act synergistically by increasing the blood concentration of loperamide and blocking its excretion pathways. This leads to an increase in the pharmacological action of loperamide and its side effects. P-glycoprotein inhibitors The simultaneous use of loperamide (in a single dose of 16 mg) with P-glycoprotein inhibitors, quinidine or ritonavir, caused an increase in the concentration of loperamide in the blood plasma by 2-3 times. Itraconazole and gemfibrozil The simultaneous use of loperamide (single dose of 4 mg) with itraconazole, which is an inhibitor of CYP3A4 and P-glycoprotein, caused a 3-4 times higher plasma concentration of loperamide. The CYP2C8 inhibitor, gemfibrozil, increased the plasma concentration of loperamide approximately 2-fold. When itraconazole and gemfibrozil were combined, the maximum plasma concentration of loperamide increased by 4 times, but the total plasma effect increased by 13 times. Ketoconazole The simultaneous use of loperamide (single dose of 16 ml) with ketoconazole, which is an inhibitor of CYP3A4 and P-glycoprotein, caused a 5-fold increase in plasma concentrations of loperamide. Desmopressin Concomitant oral administration with desmopressin resulted in a 3-fold higher plasma concentration of desmopressin, possibly due to increased gastrointestinal motility. Anticholinergics Anticholinergics slow down the activity of the stomach and intestines, they can increase the effect of loperamide. Opiate analgesics Concomitant use of opiate analgesics with loperamide may lead to constipation. Co-trimoxazole Simultaneous use with co-trimoxazole increases the bioavailability of loperamide, which leads to an increase in its action. Contraindications Hypersensitivity to any component of the drug; diverticulosis; intestinal obstruction (including, if necessary, avoid suppression of peristalsis), megacolon and toxic megacolon; acute ulcerative colitis or pseudomembranous colitis associated with the use of broad-spectrum antibiotics; bacterial enterocolitis caused by microorganisms of the Salmonella, Shigella and Campylobacter families, impaired liver function necessary for drug metabolism, as this can lead to a relative overdose; acute diarrhea with concomitant fever and bloody stools; pregnancy (I trimester) and breastfeeding; children’s age up to 12 years; lactase deficiency, galactose intolerance, glucose-galactose malabsorption. Composition 1 capsule contains: active substance: loperamide hydrochloride 2 mg, excipients: lactose monohydrate, corn starch, magnesium stearate. Capsule: body: titanium dioxide (E 171), patent blue V (E 131), crimson 4R (E 124), gelatin, cap: titanium dioxide (E 171), quinoline yellow (E 104), patent blue V (E 131), iron oxide yellow (E 172), gelatin. Overdose In case of an overdose of loperamide, the following symptoms may occur: depression of the central nervous system (stupor, impaired coordination of movements, drowsiness, miosis, muscle hypertonicity, respiratory depression). Children are more sensitive to effects on the central nervous system due to the fact that their blood-brain barrier is not yet fully functional; urinary retention and a complex of symptoms similar to intestinal obstruction; Serious cardiovascular side effects including QT interval prolongation, torsades de pointes and other ventricular arrhythmias, cardiac arrest, syncope and death. Symptomatic treatment, activated charcoal, gastric lavage, artificial lung ventilation. With the development of symptoms of cardiotoxicity, it is necessary to conduct pharmacotherapy of cardiac arrhythmias with antiarrhythmic drugs or decide on electrical cardiac stimulation or cardioversion. Antidote – naloxone; given that the duration of action of loperamide is longer than that of naloxone, repeated administration of the latter is possible. In case of an overdose of the drug, medical supervision is necessary for at least 48 hours. Side effects The most commonly reported side effects with loperamide are constipation, gas accumulation, headache and nausea. The following side effects are ordered according to the MedDRA organ system classification and frequency database: very common (? 1/10), common (? 1/100 to < 1/10), infrequently (? 1/1000 to < 1/ 100), rare (? 1/10,000 to < 1/1000), very rare (<1/10,000), unknown (cannot be determined from the available data). On the part of the immune system Rarely: hypersensitivity reaction, anaphylactic reaction (including anaphylactic shock), anaphylactoid reaction. From the side of the nervous system Often: headache. Uncommon: drowsiness, dizziness. Rarely: loss of consciousness, stupor, depressed level of consciousness, hypertension, impaired coordination. From the side of the eyes Rarely: miosis. From the gastrointestinal tract Often: constipation, nausea, accumulation of gases. Uncommon: abdominal pain, abdominal discomfort, dry mouth, upper abdominal pain, vomiting, dyspepsia. Rare: ileus (including paralytic ileus), megacolon (including toxic megacolon), glossodynia, bloating. On the part of the skin and subcutaneous tissues Uncommon: rash. Rare: bullous rash (including Stevens-Johnson syndrome, toxic epidermal necrolysis and erythema multiforme), angioedema, urticaria, pruritus. From the side of the kidneys and urinary tract Rare: urinary retention. General disorders and reactions at the injection site Rare: fatigue. If the listed adverse reactions occur, as well as if an adverse reaction occurs that is not mentioned in the instructions, you should consult a doctor. Storage conditionsStore at a temperature not exceeding 25 °C. Keep out of the reach of children! Shelf life 5 years. Do not use after the expiration date indicated on the package. Buy Loperamide Grindeks capsules 2mg No. 10x1