Kestin tablets p/o 10mg №10×1

NameKestin coated tablets 10mg N10. The main active ingredientEbastine Release formCoated tablets 10mg N10. Pharmacological action Mechanism of action Ebastin leads to a rapid and long-term inhibition of the effects of histamine, and has a high affinity for H1 receptors. After oral administration, neither ebastine nor its metabolites cross the blood-brain barrier. This property is consistent with the low level of sedative effect, according to the results of studies in which the effects of ebastine on the central nervous system were studied. Data from in vitro and in vivo studies have shown that ebastine is a potent long-acting selective H1 histamine receptor antagonist with no CNS side effects and an anticholinergic effect. Pharmacodynamics Studies of papules caused by histamine have shown a clinically and statistically significant antihistamine effect that develops 1 hour after ingestion and lasts more than 48 hours. After the end of the 5-day course of treatment with Kestin, the antihistamine effect persisted for another 72 hours. This action corresponded to the level of its main active metabolite, an acidic nature, carebastin, in blood plasma. With prolonged use, inhibition of peripheral receptors remained at a constant level without the development of tachyphylaxin. These results showed that ebastine at a dose of at least 10 mg once a day leads to a rapid, intense and long-term blockade of peripheral H1 histamine receptors. Sedation was studied using encephalograms, cognitive function studies, visual-motor coordination, and subjective assessments. When taking the recommended dose, there was no significant increase in sedative effect. These results are consistent with the results of a double-blind clinical study: the level of sedation of ebastine is comparable to placebo. The effects of ebastine on the heart have been studied in clinical trials. There was no significant effect on the heart when a detailed analysis of the intake of a daily dose of up to 100 mg (ten times the recommended daily dose). Pharmacokinetics After oral administration, ebastine is rapidly absorbed, being highly metabolized during the first passage through the liver, with the formation of the active metabolite of carebastin. With a single dose of 10 mg, the maximum concentration of the metabolite in the blood plasma is reached after 2.6-4 hours and is 80-100 ng / ml. The half-life of the active metabolite is 15-19 hours, and 66% of the drug is excreted in the urine, mostly in the form of conjugates. With daily administration of the drug at a dose of 10 mg, the equilibrium concentration is reached after 3-5 days, and the maximum plasma level is 130-160 ng / ml. The results of an in vitro study with human microsomal liver enzymes showed that ebastine is metabolized to carabastin by the enzyme CYP3A4. Simultaneous administration of ebastine with ketoconazole or erythromycin (both drugs are CYP3A4 inhibitors) to healthy volunteers caused a significant increase in the concentration of ebastine and carebastin in the blood plasma, especially with ketoconazole (see section “Interaction with other drugs”). Both ebastine and carebastine showed a high degree of protein binding, over 97%. There were no statistically significant differences in pharmacokinetic parameters for elderly and young patients. Plasma concentrations of ebastine and carebastin on the first and fifth days of treatment in patients with mild, moderate or severe renal insufficiency (daily dose of 20 mg) and in patients with mild to moderate hepatic insufficiency (in both groups, a dose of 20 mg / day) or severe severity (dose 10 mg/day) was at the same level as the concentration in healthy volunteers. This showed that the pharmacokinetic parameters of ebastine and its metabolite do not change significantly in patients suffering from hepatic or renal insufficiency of varying severity. Preclinical Safety Studies Data from preclinical studies, which included routine studies of safety pharmacology, repeated dose toxicity, genotoxicity, possible carcinogenicity, and reproductive toxicity, showed no specific risk factors in humans. Indications for use The drug Kestin is indicated for symptomatic treatment of: allergic rhinitis (seasonal and year-round), accompanied or not accompanied by allergic conjunctivitis; chronic idiopathic urticaria; allergic dermatitis. Dosage and administrationAdults and children over 12 years of age The recommended dose is 1 tablet once a day. If you miss a tablet, do not double the dose to make up for the missed dose. The missed dose must be taken at the usual time. The duration of treatment is determined by the attending physician. Elderly patients Dose adjustment is not required. Patients with renal insufficiency In patients with mild, moderate or severe renal insufficiency, dose adjustment is not required. Patients with hepatic insufficiency No dose adjustment is required in patients with mild to moderate hepatic insufficiency. No studies have been conducted with the appointment of a dose exceeding 10 mg in patients with severe hepatic insufficiency, therefore, such patients should not exceed the maximum recommended dose (10 mg ebastine / day). Treatment should be continued until symptoms disappear. Directions for use For oral administration Tablets can be taken with or without food. The tablet is taken with a glass of water. Use during pregnancy and lactation Pregnancy, fertility, lactation Data on the use of ebastine during pregnancy are limited. Animal studies have shown no direct or indirect harmful effects in terms of reproductive toxicity. It is preferable to avoid the use of ebastine during pregnancy. Fertility No data are available on the effect of ebastine on human fertility. Lactation It is not known whether ebastine is excreted in breast milk. The high degree of binding of ebastine and its main metabolite, carebastin, with proteins (> 97%) does not imply excretion of the drug with breast milk. It is preferable to avoid the use of ebastine during breastfeeding. Precautions Use with caution in patients at risk of developing heart disease, such as patients with a prolonged QT interval, hypokalemia, in combination with drugs that prolong the QT interval or inhibit the CYP3A4 enzyme, such as azole antifungals, such as ketoconazole and itraconazole, and also macrolide antibiotics, for example, erythromycin (see section “Interaction with other drugs”). Pharmacokinetic interactions may occur when using ebastine with rifampicin (see section “Interaction with other medicinal products”). Kestin should be used with caution in patients with severe hepatic impairment (see section “Method of administration and dosage”). Since the therapeutic effect of ebastine begins 1-3 hours after ingestion, it should not be used to treat acute allergic conditions requiring emergency care. Excipient warnings This medicinal product contains lactose. Patients with hereditary galactose intolerance, the Lapp lactase deficiency (a deficiency seen in some Lapland ethnic groups) or glucose-galactose malabsorption should not take Kestin. Interaction with other drugs An interaction study was conducted with ebastine with ketoconazole and erythromycin (both compounds cause prolongation of the QT interval). With both combinations, a pharmacokinetic and pharmacodynamic interaction was observed, which led to an increase in the level of ebastine in the blood plasma, and, to a lesser extent, carebastin, without clinically significant pharmacodynamic consequences. The prolongation of the QT interval occurred approximately 10 ms more than with separate administration of ketoconazole and erythromycin. However, the appointment of the drug Kestin requires caution in patients taking concomitant azole antifungal drugs, such as ketoconazole and itraconazole, as well as macrolide antibiotics, such as erythromycin. A pharmacokinetic interaction has been observed when taking ebastine with rifampicin. Such an interaction can lead to a decrease in plasma concentration and a weakening of the antihistamine effect. There have been no cases of interaction of ebastine with theophylline, warfarin, cimetidine, diazepam and alcohol. When ebastine is taken with food, the plasma level and the area under the concentration-time curve (AUC) of the main metabolite of ebastine increase by 1.5-2 times. This increase does not affect tmax. The intake of ebastine with food does not change its clinical effect. Ebastine can interfere with the results of allergy skin tests, so it is recommended to perform them 5-7 days after the end of treatment. This medicine may increase the effect of other antihistamines. Contraindications Hypersensitivity to the components of the drug, pregnancy, lactation, children under 12 years of age, lactase deficiency, lactose intolerance, glucose-galactose malabsorption. Composition Each coated tablet contains: Active ingredients: Ebastine 10.0 mg Excipients: Microcrystalline cellulose 20.0 mg Pregelatinized corn starch 5.2 mg Lactose monohydrate 88.5 mg Croscarmellose sodium 5.0 mg Magnesium stearate 1.3 mg Coating: Hypromellose1, 725 mg Macrogol 6000 0.575 mg Titanium dioxide 0.575 mg Overdose In high dose studies, no clinically significant signs or symptoms were observed at doses up to 100 mg once daily. There is no specific antidote for ebastine poisoning. Gastric lavage, monitoring of vital body functions, including ECG, and symptomatic treatment are recommended. Side effectsAccording to a pooled analysis of placebo-controlled studies of ebastine, in which 5708 patients participated, the most common adverse events were headache, dry mouth, and drowsiness. The table below lists the adverse reactions observed in clinical studies and during post-registration use of the drug, classified according to the system organ classification and their frequency of development: very often (≥1 / 10); often (≥1/100, <1/10); rarely (≥1/10,000, <1/1,000), very rare (<1/10,000). System organ classes Very common (≥1/10) Common (≥1/100, <1/10) Rare (≥1/10,000, <1/1,000) Immune system disorders hypersensitivity reactions (anaphylaxis, angioedema ) Mental disorders nervousness, insomnia Nervous system disorders headache drowsiness dizziness, hypesthesia, dysgeusia Cardiac disorders palpitations, tachycardia Gastrointestinal disorders dryness of the oral mucosa vomiting, abdominal pain, nausea, dyspepsia Liver and biliary disorders Hepatitis, cholestasis, abnormal liver function tests (increased liver transaminases, GGT, alkaline phosphatase and/or bilirubin) Skin and subcutaneous tissue disorders Urticaria, rash, dermatitis Reproductive system and mammary gland disorders Menstrual disorders General and injection site reactions edema, asthenia Reporting adverse reactions It is important to report suspected adverse reactions reactions after registration of the medicinal product in order to ensure continuous monitoring of the “benefit-risk” ratio of the medicinal product. Healthcare professionals are encouraged to report any suspected adverse drug reactions through national adverse drug reaction and drug failure reporting systems. If the patient experiences any adverse reactions, consult a physician. This recommendation applies to any possible adverse reactions, including those not listed in the package insert. You can also report adverse reactions to the adverse drug reactions (actions) information database, including reports of drug failures. By reporting adverse reactions, you help to get more information about the safety of the drug. Storage conditionsStore at a temperature not exceeding 25 °C. Keep out of the reach of children. Buy Kestin tablets p/o 10mg No. 10x1