Kestin - instructions for use, dose, side effects, contraindications

Active substance:
ebastine	20.00 mg
Excipients:
microcrystalline cellulose	40.00 mg
corn starch pregelatinized	10.40 mg
lactose monohydrate	77.00 mg
croscarmellose sodium	10.00 mg
magnesium stearate	2.60 mg
shell:
hypromellose	2.85 mg
macrogol-6000	0.95 mg
titanium dioxide	0.95 mg

Description:

Round tablets coated with a film coat, white or almost white. On one side of the tablets there is an engraving "E 20".

Pharmacotherapeutic group:antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

R.06.A.X.22 Ebastin

Pharmacodynamics:

Ebastin is a blocker of H₁long-acting histamine receptors.

After taking the drug inside, the expressed antiallergic effect begins after 1 hour and lasts more than 48 hours. After a 5-day course of treatment with Kestin®, antihistamine activity persists for 72 hours due to the action of active metabolites.With prolonged admission, a high level of blockade of peripheral H₁histamine receptors without the development of tachyphylaxis. The drug has no pronounced anticholinergic and sedative effect, does not penetrate the blood-brain barrier. No effect of Kestin® on the interval QT on an ECG at a dose of 100 mg - a dose exceeding the recommended daily dose (20 mg) in 5 times.

Pharmacokinetics:

After ingestion, the drug is rapidly absorbed and almost completely metabolized in the liver, becoming an active metabolite of carabastine. After a single dose of 20 mg of the drug, the maximum concentration of carbastine in the blood plasma is achieved after 1-3 hours and is 157 ng / ml.

With daily intake of the drug from 10 mg to 40 mg, the equilibrium concentration is achieved in 3-5 days, does not depend on the administered dose and is 130-160 ng / ml. Binding to plasma proteins of ebastin and carbastine is more than 95%. The half-life of carbastin ranges from 15 to 19 hours, 66% of the drug is excreted as conjugates through the kidneys.

Eating does not affect the clinical effects of Kestin®.

In elderly patients, pharmacokinetic parameters do not change significantly. In renal failure, the half-life increases to 23-26 hours, and in liver failure - up to 27 hours, but the concentration of the drug does not exceed therapeutic values.

Indications:

- 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 components, pregnancy, lactation, children under 12 years of age, lactase deficiency, lactose intolerance, glucose-galactose malabsorption, severe liver function disorders (Child-Pugh class C).

Carefully:

Use in patients with increased QT interval on ECG, hypokalemia, with renal failure and with mild and moderate hepatic insufficiency (class A, B according to the Child-Pugh classification).

Caution should be applied to the preparation Kestin® while taking with ketoconazole or itraconazoleand erythromycin - there may be an increased risk of prolonging the QT interval on the ECG.

Pregnancy and lactation:

The safety of the use of Kestin® in pregnant women has not been studied, therefore, it is not recommended to take the drug during pregnancy. Nursing mothers are not recommended to take Kestin®, because it is not known whether ebastine with breast milk.

If it is necessary to use the drug during lactation it is necessary to stop breastfeeding.

Dosing and Administration:

Inside, regardless of food intake.

Adults and children over 12 years of age it is recommended to start therapy with a dose of 10 mg 1 time per day, using the preparation Kestin®, film-coated tablets, 10 mg. In case of insufficient effectiveness, it is recommended to use a double dose, i.e. preparation Kestin® tablets, film-coated, 20 mg of 1 tablet (20 mg) once a day.

The course of treatment will be determined by the disappearance of the symptoms of the disease.

Elderly patients: dose adjustment is not required.

Patients with impaired renal function: dose adjustment is not required. Patients with mild and moderate hepatic impairment (class A, B according to the Child-Pugh classification): dose adjustment is not required.

In severe violations of liver function (class C according to Child-Pugh classification) daily dose should not exceed 10 mg, therefore it is recommended to use Kestin® preparation, film-coated tablets, 10 mg.

Side effects:

The undesirable reactions observed in clinical trials and during the post-marketing use of the drug are listed below, taking into account the following criteria: very often (≥1/10); often (from 1/100 to <1/10); infrequently (from 1/1000 to <1/100); rarely (from 1/10000 to <1/1000); very rarely (<1/10000).

From the central and peripheral nervous system:

rarely: drowsiness;

very rarely: dizziness, hypoesthesia, headache, nervousness, insomnia.

From the gastrointestinal tract:

rarely: dryness of the oral mucosa;

very rarely: vomiting, abdominal pain, nausea, dyspepsia.

From the cardiovascular system:

very rarely: palpitation, tachycardia.

FROMabout the liver and bile ducts:

very rarely: deviations of functional liver samples.

FROMabout the skin and subcutaneous fat:

very rarely: urticaria, rash, dermatitis.

FROMabout the reproductive system:

very rarely: menstrual disorders.

ABOUTGreat and local reactions:

very rarely: edema, asthenic syndrome.

Unwanted reactions observed in clinical trials in children over 12 years of age (a group of 460 children) did not differ from the reactions noted in adults.

Overdose:

In studies using high doses (more than 100 mg per day), there were no clinically significant signs and symptoms.

There is no special antidote for ebastin. In case of an overdose, it is recommended to wash the stomach, monitor vital body functions, symptomatic treatment.

Interaction:

With the simultaneous use of Kestin® with ketoconazole or itraconazole and erythromycin, the risk of lengthening of the interval QT on the ECG.

Rifampicin reduces the concentration of ebastin in the blood plasma and has an inhibitory effect on antihistamine effect of ebastin.

Kestin® does not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol, and ethanol-containing drugs.

Special instructions:

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

Effect on the ability to drive transp. cf. and fur:

In the event of side effects from the central nervous system, such as drowsiness, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 20 mg.

Packaging:

For 10 tablets in a blister of PVC film and aluminum foil.

1 blister with instruction for use is placed in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LS-001046

Date of registration:28.06.2010

The owner of the registration certificate:Almiral S.A.Almiral S.A. Spain

Manufacturer: & nbsp

INDUSTRIAS FARMACEUTICAS ALMIRALL, S.L. Spain

Representation: & nbspTakeda Pharmaceuticals Ltd.Takeda Pharmaceuticals Ltd.

Information update date: & nbsp29.09.2015

Illustrated instructions

Instructions

Kestin® (Kestine®)