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

Active substance:
ebastine	10.0 mg
Excipients:
microcrystalline cellulose	20.0 mg
corn starch pregelatinized starch	5.2 mg
lactose monohydrate	88.5 mg
croscarmellose sodium	5.0 mg
magnesium stearate	1.3 mg
Shell:
hypromellose	1.725 mg
macrogol-6000	0.575 mg
titanium dioxide	0.575 mg

Description:

Tablets of round form, covered with a film shell, from white to almost white. On one side of the tablets there is a risk and an E10 engraving.

Pharmacotherapeutic group:antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

R.06.A.X.22 Ebastin

Pharmacodynamics:

Ebastin is a blocker H₁-long-acting histamine receptors.

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 Kestin®, antihistamine activity remains 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 QT-Interval of ECG in a dose of 100 mg - a dose exceeding the recommended daily dose (10 mg) by 10 times.

Pharmacokinetics:

After oral administration, it is rapidly absorbed and almost completely metabolized in the liver, becoming an active metabolite of carabastine. After a single Admission 10 mg of the drug the maximum concentration of carbastine in plasma is achieved after 2.6-4 hours and is 80-100 ng / ml.

With daily intake of 10 mg of the drug, the equilibrium concentration is reached after 3-5 days and is 130-160 ng / ml. Binding to proteins plasma 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 year-round);

- hives of various etiologies, including chronic idiopathic.

Contraindications:

Hypersensitivity to the drug components, pregnancy, lactation, children under 12 years of age, lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Carefully:

Use in patients with an increased QT interval, hypokalemia, with renal failure and severe liver function disorders (Child-Pugh class C); with simultaneous administration with ketoconazole or itraconazole and 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 solve the problem of stopping breastfeeding.

Dosing and Administration:

Inside, regardless of food intake.

Adults and children over 12 years of age the recommended standard dose of the drug is 10 mg per day in the form of tablets coated with a film coat.

In case of insufficient effectiveness of the chosen dosage, it is recommended to prescribe 2 tablets of Kestin® preparation with a dosage of 10 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: correction of the dose is not required. Patients with mild to moderate hepatic insufficiency (class A, B according to the Child-Pugh classification): dose adjustment is not required. In severe violations of liver function (class C according to the Child-Pugh classification), the daily dose should not exceed 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.

From the liver and bile ducts:

very rarely: deviations of functional liver samples.

From the skin and subcutaneous fat:

very rarely: urticaria, rash, dermatitis.

On the part of the reproductive system:

very rarely: menstrual disorders.

General 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 of ebastin (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 prolonging the QT interval on the ECG is likely to increase.

Rifampicin reduces the concentration of ebastin in the blood plasma and has an inhibitory effect on the 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 concentration and speed of psychomotor reactions

Form release / dosage:

Tablets, film-coated, 10 mg.

Packaging:

For 5 or 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:П N015154 / 01

Date of registration:10.09.2008

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®)