Kestine coated pills 20mg N10
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Active ingredients
Ebastine
Release form
Pills
Composition
Ebastine 20 mg. Auxiliary substances: magnesium stearate, microcrystalline cellulose, pregelatinized corn starch, lactose monohydrate (177 mg), croscarmellose sodium, hypromellose, titanium dioxide, macrogol 6000 (polyethylene glycol 6000).
Pharmacological effect
Kestin; - blocker of H1-histamine receptors of long-acting. Warns histamine-induced smooth muscle spasms and increased vascular permeability. After taking the drug inside the pronounced anti-allergic effect begins after 1 h and lasts for 48 hours. After a 5-day course of Kestine treatment, antihistamine activity persists for 72 hours due to the action of active metabolites. It does not have anticholinergic activity, does not penetrate the blood-brain barrier, does not cause sedation. At a dose of up to 80 mg, the QT interval does not extend on the ECG.
Pharmacokinetics
After ingestion, it is rapidly absorbed and almost completely metabolized in the liver, turning into the active metabolite carbastin. After a single dose of 10 mg of the drug Cmax carbastin in plasma is reached after 2.6-4 h and is 80-100 ng / ml. Fatty food accelerates absorption (concentration in the blood increases by 50%). It does not penetrate the blood-brain barrier. When daily intake of 10 mg of the drug, the equilibrium concentration is reached in 3-5 days and is 130-160 ng / ml. Communication with plasma proteins ebastine and carbastine is more than 95%. T1 / 2 of carbastine is from 15 to 19 hours, 66% of the drug is excreted in the form of conjugates with urine. When a drug is administered simultaneously with food intake, the concentration of carbastine in the blood increases 1.6-2 times, but this does not change the time to reach it Cmax and has no effect on the clinical effects of Kestine. In elderly patients, the pharmacokinetic parameters do not change significantly. In renal insufficiency, T1 / 2 increases to 23-26 hours, and in hepatic insufficiency, it increases to 27 hours, but the concentration of the drug when administered 10 mg / day does not exceed therapeutic values.
Indications
- seasonal and / or year-round allergic rhinitis (caused by household, pollen, epidermal, nutritional, medicinal, etc.allergens); - urticaria (caused by domestic, pollen, epidermal, food, insect, drug allergens, exposure to the sun, cold, etc.).
Contraindications
- hypersensitivity to the drug, pregnancy, lactation period; - children's age up to 12 years old. With caution: in case of renal and / or liver failure; in patients with increased QT-interval, hypokalemia.
Use during pregnancy and lactation
The safety of Kestine in pregnant women has not been studied, so taking Kestine during pregnancy is not recommended. Nursing mothers are not recommended to take Kestine, since the release of Ebastine in breast milk has not been studied.
Dosage and administration
Inside, regardless of the meal. Children from 12 to 15 years: 10 mg (1/2 tablet) 1 time per day. Adults and children over 15 years old are prescribed 10-20 mg (1 / 2-1 tablet) of the drug 1 once a day. The daily dose of 20 mg is prescribed on the recommendation of a doctor. In case of abnormal liver function, the daily dose should not exceed 10 mg.