Loperamide hydrochloride capsules 2mg №10х2

Name:
Loperamide ghl caps. 2 mg in a cell. pack No. 10×2
Description:
Hard gelatin capsules of a cylindrical shape with hemispherical ends of white color. The contents of the capsules are white or white with a yellowish tint granulate. The main active ingredient Loperamide Release form capsules Dosage 2 mg Pharmacological properties Pharmacodynamics Loperamide is a peripheral opioid receptor agonist. Its antagonist is naloxone. Loperamide inhibits the release of acetylcholine and prostaglandins, reduces propulsive peristalsis, increases the transit time of the contents through the intestines, as well as the ability of the intestinal wall to absorb fluid. Loperamide is highly specific for the intestinal wall, reaches the systemic circulation in a limited volume and practically does not penetrate the blood-brain barrier (BBB). The threshold of central action is much higher than the dose that shows the maximum effect on diarrhea. Loperamide increases the tone of the anal sphincter, helping to reduce fecal incontinence and the urge to defecate. Preclinical safety data In the course of preclinical studies in vitro and in vivo, there was no significant electrophysiological effect of loperamide on the heart at loperamide concentrations within the therapeutic range, as well as with its significant increase (up to 47 times). However, at excessively high concentrations associated with overdose (see section “Precautions”), loperamide has an electrophysiological effect on the heart, causing blockade of potassium (hERG) and sodium channels, and arrhythmia. Pharmacokinetics Absorption Most of loperamide is absorbed in the intestine, but due to the high degree of metabolism during the first passage through the liver, systemic bioavailability is about 0.3%. Distribution Results of studies on the distribution of loperamide in rats demonstrate a high affinity for the intestinal wall with preferential binding to receptors in the longitudinal muscle layer. Preclinical data have shown that loperamide is a P-glycoprotein substrate. Plasma protein binding (mainly albumin) – 95%. Loperamide practically does not penetrate the blood-brain barrier (BBB). Metabolism Loperamide is almost completely extracted by the liver, where it is metabolized by conjugation and then excreted in the bile. The main metabolic pathway is oxidative N-demethylation mediated mainly by CYP3A4 and CYP2C8. Due to the very intense first pass effect, the plasma concentration of loperamide remains very low. Withdrawal The half-life is 9-14 hours (average 11 hours). Excretion of unchanged loperamide and its metabolites occurs mainly in the feces. Pediatric patient population: Pharmacokinetic studies in the pediatric patient population have not been conducted. The pharmacokinetic characteristics of loperamide and drug interactions with loperamide are expected to be similar to those seen in adults. Indications for use Symptomatic treatment of acute diarrhea. Symptomatic treatment of chronic diarrhea of various etiologies. Treating traveler’s diarrhea. The duration of treatment is 2 days. However, in case of fever or in the presence of blood in the stool, it is recommended to stop taking the drug until the causative agent of the disease is identified. Dosage and administration Inside, without chewing, drinking water. In acute diarrhea, adults and elderly patients are prescribed an initial dose of 4 mg (2 capsules); in the future – 2 mg (1 capsule) after each act of defecation in case of loose stools. In chronic diarrhea, adults and elderly patients are prescribed an initial dose of 4 mg / day (2 capsules). Further, the dose is adjusted so that the frequency of stools is 1-2 times / day, which is usually achieved with a maintenance dose of 2-12 mg / day (1-6 capsules). Elderly people In elderly patients, dose adjustment is not required. Impaired renal function In patients with impaired renal function, dose adjustment is not required. Impaired liver function Despite the lack of data on pharmacokinetics in patients with impaired liver function, the drug for the treatment of such patients is used with caution due to a decrease in their first-pass metabolism of loperamide hydrochloride (see section “Precautions”). If after 48 hours after the start of therapy for acute diarrhea there is no clinical improvement, the drug is stopped. In the presence of diarrhea, it should be remembered that an important component of treatment is the replacement of fluids and electrolytes, especially in children. The maximum daily dose for acute and chronic diarrhea in adults is 16 mg (8 capsules). With the appearance of a normal stool or in the absence of a stool for more than 12 hours, the drug is canceled. Children Children and adolescents from 6 to 17 years of age At the beginning of the treatment of acute diarrhea and after each occurrence of liquid stools, take 2 mg of loperamide hydrochloride, which corresponds to 1 capsule. For the treatment of chronic diarrhea, the dose is 2 mg of loperamide hydrochloride per day, which corresponds to 1 capsule. The maximum dose for the treatment of acute and chronic diarrhea in children is calculated by body weight (6 mg / 20 kg = 3 capsules / 20 kg), but it should not exceed 16 mg of loperamide hydrochloride per day, which corresponds to 8 capsules. Children under 6 years of age This medicinal product cannot be prescribed to children under 6 years of age due to the high content of the active substance and the characteristics of the dosage form. Application during pregnancy and lactation Loperamide is contraindicated in the first trimester of pregnancy. Despite the absence of indications of a teratogenic or embryotoxic effect, loperamide can be prescribed in the II and III trimesters of pregnancy only in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus. Loperamide is excreted in small amounts in breast milk, so if you need to use the drug during lactation, breastfeeding should be discontinued. Influence on the ability to drive vehicles and control mechanisms During the period of treatment, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and a high speed of psychomotor reactions. Precautions Due to the content of lactose, the drug is not recommended for patients with rare congenital galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome. The drug should be stopped immediately if constipation or bloating develops. Since the treatment of diarrhea with loperamide is only symptomatic, along with this, it is necessary, if possible, to use etiotropic agents. With diarrhea, especially in children, hypovolemia and electrolyte depletion may occur. In such cases, replacement therapy to replace fluids and electrolytes is most important. In acute diarrhea, if no clinical improvement is observed within 48 hours, loperamide should be discontinued and infectious diarrhea should be ruled out. Do not use in diarrhea with blood in the stool and high fever. Patients with AIDS should stop treatment immediately at the first sign of abdominal distention. In some cases, patients with AIDS with infectious colitis, both viral and bacterial, may develop toxic expansion of the colon during treatment with loperamide. In the treatment of patients with impaired renal function, there is no need to reduce the dose of loperamide. During the treatment period, diet and fluid replenishment are recommended. Cardiac disturbances have been reported, including QT interval prolongation and torsades de pointes ventricular tachycardia, when taking loperamide at a dose higher than recommended in the instructions for medical use, as well as when misused or abused (intentionally or unintentionally). ). In some cases, death has been reported (see section “Overdose”). Patients should not exceed the recommended dose of the drug and the duration of administration. Interaction with other drugs In children, co-administration with drugs that have a depressant effect on the central nervous system should be avoided. According to preclinical data, loperamide is a substrate of P-glycoprotein. The combined use of loperamide (in a single dose of 16 mg) with quinidine or ritonavir, which are inhibitors of P-glycoprotein, causes a 2-3-fold increase in plasma concentrations of loperamide. When using loperamide at recommended doses, the clinical significance of such a pharmacokinetic interaction with P-glycoprotein inhibitors has not been established. Simultaneous administration of loperamide (in a single dose of 4 mg) with itraconazole, which is an inhibitor of the CYP3A4 enzyme and P-glycoprotein, caused a 3-4-fold increase in plasma concentrations of loperamide. In the same study, the CYP2C8 inhibitor gemfibrozil caused an approximately 2-fold increase in plasma loperamide concentrations. The use of a combination of itraconazole and gemfibrozil increased the maximum plasma levels of loperamide by 4 times, and the total exposure in blood plasma by 13 times. According to the results of psychomotor tests (ie test of subjective feeling of drowsiness and test of substitution of digital symbols) these increases in indicators had no effect on the CNS. Simultaneous administration of loperamide (in a single dose of 16 mg) with ketoconazole, which is an inhibitor of the CYP3A4 enzyme and P-glycoprotein, causes a 5-fold increase in plasma concentrations of loperamide. This increase in concentrations was not accompanied by an increase in the pharmacodynamic effects of the drug, according to pupillometry. Simultaneous oral administration of loperamide and desmopressin caused a three-fold increase in the concentration of desmopressin in the blood plasma, which is probably due to inhibition of gastrointestinal motility. It is assumed that drugs with similar pharmacological properties may enhance the effects of loperamide, and drugs that increase gastrointestinal motility may weaken its effect. Contraindications acute dysentery and other infections of the gastrointestinal tract (GIT) (caused, including Salmonella spp., Shigella spp., Campylobacter spp.); intestinal obstruction (including, if necessary, avoid suppression of peristalsis); diverticulosis; acute ulcerative colitis; pseudomembranous enterocolitis (diarrhea caused by taking antibiotics); I trimester of pregnancy; lactation period (breastfeeding); children under 6 years of age; hypersensitivity to loperamide and / or other components of the drug. Do not use in cases where necessary avoid inhibition of peristalsis, as there is a risk of serious consequences, including intestinal obstruction, megacolon or toxic megacolon. If constipation, bloating or intestinal obstruction develops, loperamide hydrochloride should be stopped immediately. With caution, the drug should be prescribed for liver failure. Composition Each capsule contains: active substance – loperamide hydrochloride – 2 mg; excipients: lactose monohydrate, corn starch, magnesium stearate. Capsule composition: gelatin, E 218 methyl parahydroxybenzoate, E 216 propyl parahydroxybenzoate, E 171 titanium dioxide. other serious ventricular arrhythmias, cardiac arrest, syncope. In some cases, death has been reported. Overdose symptoms may include: CNS depression (stupor, incoordination, drowsiness, pupillary constriction, miosis, muscular hypertension, respiratory depression), intestinal obstruction (nausea, vomiting, abdominal pain, constipation), difficulty urinating. Treatment: gastric lavage, administration of activated charcoal (no later than 3 hours after taking loperamide), if necessary, artificial lung ventilation (ALV), symptomatic therapy. The antidote is naloxone. Because the duration of action of loperamide is longer than that of naloxone (1-3 hours), it may be necessary to re-administer the latter. To identify possible CNS depression, the patient’s condition must be carefully monitored for at least 48 hours. Storage conditions In a place protected from light and moisture, at a temperature of 15 ° C to 25 ° C. Keep out of the reach of children. Buy Loperamide hydrochloride capsules 2mg №10×2 Price for Loperamide hydrochloride capsules 2mg №10×2