Кестин®

General characteristics. Structure:

Active agent:  эбастин 10,0 mg
Excipients:  cellulose of microcrystallic 20,0 mg; starch of corn prezhelatinizirovanny   5,2 mg; lactoses monohydrate of 88,5 mg;  croscarmellose sodium of 5,0 mg; magnesium stearate of 1,3 mg
cover: gipromelloza of 1,725 mg; macrogoal-6000 of 0,575 mg; titanium dioxide of 0,575 mg;

Description: tablets of a round form, film coated, from white till almost white color. On one party of tablets there is risk and an engraving E 10.

Pharmacological properties:

Pharmacodynamics. 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 the drug Kestin® antihistaminic activity remains during 72 h due to action of active metabolites. Drug does not render expressed anticholinergic and sedation. Influence of the drug Kestin® on an ECG Q-T-interval in the dose of 100 mg exceeding the recommended daily dose at 5-10 times is noted.

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. 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. Linkng 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 through kidneys.
Meal does not exert impact on clinical effects of the drug 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 does not exceed therapeutic values.

Indications to use:

• allergic rhinitis of various etiology (seasonal and/or year-round, both followed, and not followed by allergic conjunctivitis);
• small tortoiseshell of various etiology, including chronic idiopathic.

Route of administration and doses:

Inside, irrespective of meal.
To adults and children 12 years are more senior appoint 10-20 mg (1-2 tablets) of drug once a day.
At an abnormal liver function the daily dose should not exceed 10 mg.

Features of use:

Ebastin can distort results of skin allergy tests. Therefore it is recommended to carry out such tests not earlier than in 5-7 days after drug withdrawal.

Influence on ability to manage vehicles and the equipment
 In case of side effects from the central nervous system, perhaps minimum decline in the ability of patients to control of vehicles and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

With a frequency more than 1%: headache (7,9%), drowsiness (3,0%), dryness of a mucous membrane of an oral cavity (2,1%).
With a frequency less than 1%: dyspepsia, nausea, sleeplessness, abdominal pains, asthenic syndrome, sinusitis, rhinitis.

Interaction with other medicines:

It is not recommended to use the drug Kestin® along with ketokonazoly and erythromycin (increase in risk of lengthening of a Q-T-interval).
The drug Kestin® does not interact with theophylline, indirect anticoagulants, Cimetidinum, diazepam, ethanol and etanolsoderzhashchy drugs.

Contraindications:

Hypersensitivity to drug components, pregnancy, the lactation period, children's age up to 12 years, deficit of lactase, a lactose intolerance, glyukozo-galaktozny malabsorption.

With care
 To apply at patients with the increased Q-T-interval, a hypopotassemia, at a renal and/or liver failure.

Overdose:

Signs of moderate impact on the central nervous system (exhaustion) and the autonomic nervous system (dryness of a mucous membrane of an oral cavity) can arise only at high doses (300 mg - 500 mg that is 30-50 times higher, than a therapeutic dose). There is no special antidote for an ebastin. In case of overdose the gastric lavage, control of the vital functions of an organism, a symptomatic treatment is recommended.

Storage conditions:

To store at a temperature not above 30 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to apply after a period of validity.

Issue conditions:

Without recipe

Packaging:

Tablets film coated 10 mg.
On 5 or 10 tablets in the blister from PVC of a film and aluminum foil. 1 blister with the application instruction is placed in a cardboard pack.