Кестин®

General characteristics. Structure:

Active agent: эбастин 20,0 mg
Excipients:  
magnesium stearate of 2,6 mg
cellulose of microcrystallic 40 mg
starch of corn previously gelated   10,4 mg
lactoses monohydrate of 177 mg
croscarmellose sodium of 10 mg
gipromelloza of 2,85 mg
titanium dioxide of 0,95 mg
macrogoal 6000 (polyethyleneglycol 6000) of 0,95 mg

Description: Tablets of a round form, film coated, white or almost white color. On one party of tablets there is an engraving "Е 20".

Pharmacological properties:

Pharmacodynamics. Kestin - a blocker of H1-histamine receptors of long action. Warns the spasms of smooth muscles induced by a histamine and increase in vascular permeability. After administration of drug inside the expressed antiallergic action begins in 1 h and lasts for 48 h. After a 5-day course of treatment Kestin antihistaminic activity remains during 72 h due to action of active metabolites. Has no anticholinergic activity, does not get through a blood-brain barrier, does not cause sedation. In a dose to 80 mg does not extend QT interval on an ECG.

Pharmacokinetics. After intake it is quickly soaked up and it is almost completely metabolized in a liver, turning into an active metabolite карэбастин. After a single dose of 10 mg of drug the maximum concentration of a karebastin in plasma is reached in 2,6-4 h and makes 80-100 ng/ml. Greasy food accelerates absorption (concentration increases in blood for 50%). Does not get through a blood-brain barrier.
At daily reception of 10 mg of drug equilibrium concentration is reached in 3-5 days and makes 130-160 ng/ml. Communication with proteins of plasma of an ebastin and karebastin makes more than 95%. The elimination half-life of a karebastin makes from 15 to 19 h, 66% of drug are removed in the form of conjugates with urine.
At purpose of drug along with meal concentration of a karebastin increases in blood by 1,6-2 times, however it does not lead to change of time of achievement of its maximum concentration and does not exert impact on clinical effects of Kestin.
At patients of advanced age pharmacokinetic indicators significantly do not change. At a renal failure the elimination half-life increases up to 23-26 h, and at a liver failure - up to 27 h, however concentration of drug at reception of 10 mg/days does not exceed therapeutic values.

Indications to use:

• allergic rhinitis seasonal and/or year-round (caused household, pollen, epidermal, food, medicinal, etc. by allergens);
• the small tortoiseshell (called by household, pollen, epidermal, food-borne, insektny, medicinal allergens, influence of the sun, cold, etc.).

Route of administration and doses:

Inside, irrespective of meal.
Children from 12 to 15 years: 10 mg (½ tablets) once a day.
To adults and children 15 years are more senior appoint 10-20 mg (½-1 a tablet) drug once a day.
The daily dose of 20 mg is appointed according to the recommendation of the doctor.
At an abnormal liver function the daily dose should not exceed 10 mg.

Features of use:

Kestin in therapeutic doses does not influence ability to manage vehicles and mechanisms.
At children aged from 6 Kestin in a dose of 5 mg/days or tablets on 10 mg is up to 12 years more preferable to use syrup (on ½ tablets a day).

Side effects:

Headache, dryness in a mouth. In rare instances - dyspepsia, nausea, sleeplessness, drowsiness, abdominal pains, an asthenic syndrome, sinusitis, rhinitis.

Interaction with other medicines:

Kestin along with ketokonazoly and erythromycin because of increase in risk of lengthening of an interval of QT at an ECG is not recommended to appoint.
Kestin does not interact with theophylline, indirect anticoagulants, Cimetidinum, diazepam, ethanol and etanolsoderzhashchy drugs.

Contraindications:

• hypersensitivity to drug, pregnancy, the lactation period.
Tablets, coated 20 mg are not intended for reception at children up to 12 years.
With care
 At a renal and/or liver failure.
At patients, with the increased QT interval, a hypopotassemia.

Use at pregnancy and a lactation
Safety of use of Kestin for pregnant women is not investigated therefore it is not recommended to accept Kestin during pregnancy.
To nursing mothers Kestin as allocation of an ebastin in breast milk is not studied is not recommended to accept.

Overdose:

The special antidote for drug does not exist. In case of overdose the gastric lavage, observation of the vital functions of an organism, a symptomatic treatment is recommended.

Storage conditions:

List B. At a temperature not above 30 °C in the place unavailable to children protected from light. Period of validity 3 years. Not to use after expiry date.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in the blister from PVC of a film and aluminum foil. 1 or 2 blisters with the application instruction place in a cardboard pack.