Instruction for use: Kestine

Dosage form: Syrup; Lyophilized tablets; Coated tablets; Film-coated tablets

Active substance: Ebastine*

ATX

R06AX22 Ebastine

Pharmacological group

Antiallergic agent - blocker of H1-histamine receptors [H1-antihistamines]

The nosological classification (ICD-10)

J30.1 Allergic rhinitis caused by pollen of plants: Hay fever; Hay fungus; hay fever; Hypersensitivity to pollen of plants; Polyposis allergic rhinosinusitis; Seasonal pollinosis; Seasonal rhinitis

J30.2 Other seasonal allergic rhinitis: Allergic rhinitis seasonal; Seasonal rhinitis of an allergic nature

J30.3 Other allergic rhinitis: Allergic rhinitis year-round; Allergic rhinoconjunctivitis

L50 Urticaria: Idiopathic chronic urticarial; Injury Urticaria; Chronic urticarial; Hives of the newborn

L50.1 Idiopathic urticaria: Idiopathic urticarial; Chronic idiopathic urticarial

T78.4 Unspecified Allergy: Allergic reactions to insulin; Allergic reactions to insect stings; Allergic reactions similar to systemic lupus erythematosus; Allergic diseases; Allergic diseases of mucous membranes; Allergic diseases and conditions resulting from increased release of histamine; Allergic diseases of mucous membranes; Allergic symptoms; Allergic symptoms in the mucous membranes; Allergic reactions; Allergic reactions caused by insect bites; Allergic reactions; Allergic conditions; Allergic laryngeal edema; allergopathy; allergic conditions; Allergy; House dust allergy; Anaphylaxis; Cutaneous reactions to medications; Skin reaction to insect stings; Cosmetic allergy; Drug allergy; Acute allergic reaction; Laryngeal edema allergic genesis and background radiation; Food and drug allergy

Composition and release form

Tablets, coated with a coating.

Ebastin 20 mg

Auxiliary substances: magnesium stearate - 2,6 mg; MCC - 40 mg; Corn starch, pregelatinized - 10.4 mg; Lactose monohydrate - 177 mg; Croscarmellose sodium - 10 mg; Hypromellose - 2.85 mg; Titanium dioxide - 0,95 mg; Macrogol 6000 (polyethylene glycol 6000) - 0.95 mg

In the blister 10 pcs .; In a pack of cardboard 1 or 2 blisters.

Description of dosage form

Round tablets coated with a film coat, white or almost white. On one side of the tablets is the engraving "E20".

Pharmacology

Mode of action - antiallergic.

Pharmacodynamics

Kestine is a blocker of long-acting histamine H1 receptors. Prevents histamine-induced spasms of smooth muscles and increased vascular permeability. After taking the drug inside, the expressed antiallergic effect begins after 1 hour and lasts for 48 hours. After a 5-day course of treatment with Kestine, antihistamine activity persists for 72 hours due to the action of active metabolites. Does not possess anticholinergic activity, does not penetrate the BBB, does not cause sedation. In a dose up to 80 mg does not extend the QT interval on the ECG.

Pharmacokinetics

After oral administration, it is rapidly absorbed and almost completely metabolized in the liver, becoming an active metabolite of carabastine. After a single administration of 10 mg of Cmax carbastine in plasma is achieved after 2.6-4 hours and is 80-100 ng / ml. Fatty food accelerates absorption (concentration in the blood increases by 50%). Does not penetrate the BBB.

With daily intake of 10 mg of the drug, the equilibrium concentration is achieved after 3-5 days and is 130-160 ng / ml. Binding to plasma proteins ebastin and carbastine - more than 95%. T1 / 2 carbastine - from 15 to 19 hours, 66% of the drug is excreted as conjugates with urine.

When the drug is administered concomitantly with food intake, the concentration of carbastine in the blood increases 1.6-2 times, but this does not change the time to reach its Cmax and does not affect the clinical effects of the Kestine preparation.

In elderly patients, pharmacokinetic parameters do not change significantly. With renal insufficiency T1 / 2 increases to 23-26 hours, and with liver failure - up to 27 hours, but the concentration of the drug when taking 10 mg / day does not exceed therapeutic values.

Indication of the Kestine

Allergic rhinitis seasonal and / or all-the-year-round (caused by domestic, pollen, epidermal, food, medicinal and other allergens);

Urticaria (caused by domestic, pollen, epidermal, food, insect, drug allergens, exposure to the sun, cold, etc.).

Contraindications

Hypersensitivity to the drug;

pregnancy;

The period of breastfeeding;

Children under 12 years.

Carefully:

With kidney and / or liver failure;

In patients with an increased QT-interval, hypokalemia.

Application in pregnancy and breastfeeding

The safety of Kestine in pregnant women has not been studied, so its use during pregnancy is not recommended.

Nursing mothers are not recommended to take Kestine, since the release of ebastin into breast milk has not been studied.

Side effects

Headache, dry mouth. Rarely - dyspepsia, nausea, insomnia, drowsiness, abdominal pain, asthenic syndrome, sinusitis, rhinitis.

Interaction

It is not recommended to prescribe Kestine simultaneously with ketoconazole and erythromycin because of the increased risk of prolonging the QT interval on the ECG.

Does not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.

Dosing and Administration

Inside, regardless of food intake.

Adults and children over 15 years of age: 10-20 mg (1 / 2-1 table) once a day.

Children 12-15 years: 10 mg (1/2 table) once a day.

The daily dose (20 mg) is prescribed on the recommendation of a doctor.

If the liver function is impaired, the daily dose should not exceed 10 mg.

Overdose

Treatment: there is no special antidote for the drug. In case of an overdose, it is recommended to wash the stomach, monitor vital body functions, and symptomatic treatment.

Special instructions

Kestine in therapeutic doses does not affect the ability to drive vehicles and mechanisms.

In children aged 6 to 12 years, it is preferable to use Kestine syrup at a dose of 5 mg / day or tablets of 10 mg (1/2 tablets per day).

Storage conditions of Kestine

In the dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life of the drug Kestine

3 years.

Do not use after the expiry date printed on the package.