Кестин®

General characteristics. Structure:

Active agent: Ebastin of 20,00 mg
Excipients:  
Gelatin of 13,00 mg
Mannitolum of 9,76 mg
Aspartame of 2,00 mg
Fragrance of mint 2,00 mg

Description: White or almost white color, the round, lyophilized tablets.

Pharmacological properties:

Action mechanism
Ebastin is H1 blocker - histamine receptors of long action. Warns the spasms of smooth muscles induced by a histamine and increase in vascular permeability.

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® the tablets lyophilized 20 mg antihistaminic activity remains during 72 h due to action of an active metabolite. At long reception the high level of blockade of peripheral H1 - histamine receptors without development of a tachyphylaxis remains. Drug does not render expressed anticholinergic and sedation. Influence of the drug Kestin® of tablets of the lyophilized 20 mg on an ECG Q-T-interval in the dose of 100 mg exceeding the recommended daily dose (20 mg) by 5 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 20 mg of drug the maximum concentration of a karebastin in a blood plasma is reached in 1-3 h and averages 157 ng/ml. Greasy food accelerates absorption of a karebastin (concentration increases in blood for 50%) and presistemny metabolism (formation of a karebastin).
At daily administration of drug equilibrium concentration is reached in 3-5 days and makes 130-160 ng/ml. Linkng with proteins of a blood plasma of an ebastin and karebastin makes more than 95%. The elimination half-life of a karebastii 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® of a tablet the lyophilized 20 mg.
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); small tortoiseshell of various etiology, including chronic idiopathic.

Route of administration and doses:

For a rassasyvaniye in an oral cavity, irrespective of meal.
To adults and children 15 years are more senior appoint 1 lyophilized tablet (20 mg) once a day. The course of treatment will be defined by disappearance of symptoms of a disease.
Elderly patients: There is no need of change of a dose.
Patients with an impaired renal function: There is no need of change of a dose.
Patients with an abnormal liver function: At an insignificant and moderate liver failure the usual dose can be applied. At a heavy abnormal liver function it is not necessary to exceed a daily dose of an ebastin in 10 mg.

Special precautions at the treatment of drug:
1. In order to avoid damage of tablets, do not get drug from the blister by means of pressing. Open packaging, having carefully lifted free edge of a protective film (fig. 1).
2. Remove a protective film (fig. 2).
3. Carefully squeeze out drug, without touching it (see fig. 3).
4. Carefully extract drug (see fig. 4) and put it on language where it will quickly be dissolved. There is no need to wash down with water or other liquid, meal does not influence effect of drug.

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 from 1% to 3,7%: headache, drowsiness, dryness of a mucous membrane of an oral cavity.
With a frequency less than 1%: dyspepsia, nausea, sleeplessness, abdominal pains, asthenic syndrome, sinusitis, rhinitis. Allergic reactions are possible.

Interaction with other medicines:

It is not recommended to use the tablet drug Kestin® the lyophilized 20 mg along with ketokonazoly and erythromycin (increase in risk of lengthening of a Q-T-interval).
The tablet drug Kestin® the lyophilized 20 mg does not interact with theophylline, indirect anticoagulants, Cimetidinum, diazepam, ethanol and etanolsoderzhashchy drugs.

Contraindications:

Hypersensitivity to drug components, pregnancy, the lactation period, a fenilketonuriya, children's age up to 15 years.

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 15-25 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 25 °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 the lyophilized 20 mg.
On 10 tablets in the blister from Alyumiiiya / PVC and Aluminium/PET. On 1 blister with the application instruction place in a cardboard pack.