Kestine tabs 20mg #10

Kestine instruction for use

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Clinical and pharmacological group

The blocker of histamine H1 receptors. Anti-allergic drug

Form of release, composition and packaging

Tablets are lyophilized white or almost white in color, round.
1 tab.
Ebastin 20 mg
Excipients: gelatin - 13.00 mg, mannitol - 9.76 mg, aspartame - 2.00 mg, mint flavor - 2.00 mg.
10 pieces. - blisters (1) - packs of cardboard.

pharmachologic effect

The blocker of histamine H1 receptors is long-acting. It 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 Kestin's drug, 20 mg of lyophilized tablets the antihistamine activity persists for 72 hours due to the action of the active metabolite.
With prolonged admission, a high level of blockade of peripheral histamine H1 receptors remains without the development of tachyphylaxin. The drug has no pronounced anticholinergic and sedative effect.
There was no effect of the Kestin drug tablets lyophilized 20 mg on the QT interval of the ECG at a dose of 100 mg exceeding the recommended daily dose (20 mg) 5-fold.

Pharmacokinetics

Suction
After oral administration, it 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 carabastine in the blood plasma is achieved after 1-3 hours and averages 157 ng / ml. Fatty food accelerates the absorption of carbastine (blood concentration increases by 50%) and presystemic metabolism (formation of carabastine).
Distribution
With daily intake of the drug, the equilibrium concentration is achieved after 3-5 days and is 130-160 ng / ml. Binding to plasma proteins of ebastin and carbastine is more than 95%.
Excretion
T1 / 2 cariesten is between 15 and 19 hours. 66% of the drug is excreted as conjugates by the kidneys.

Pharmacokinetics in special clinical cases

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 does not exceed therapeutic values.

Indications

- allergic rhinitis of different etiology (seasonal and / or year-round);
- hives of various etiology, incl. chronic idiopathic.

Contraindications

- phenylketonuria;
- Pregnancy;
- lactation period (breastfeeding):
- children's age till 15 years;
- Hypersensitivity to the components of the drug.
Use with caution in patients with an increased interval of QT, hypokalemia, with renal and / or liver failure.

Dosage

The drug is designed for resorption in the oral cavity, regardless of food intake.
Adults, children and adolescents over 15 years of age are prescribed 20 mg (1 lyophilized tablet) 1 time / day. The course of treatment is determined by the disappearance of the symptoms of the disease.
In elderly patients, dose adjustment is not required.
In patients with impaired renal function, dose adjustment is not required.
With minor and moderate hepatic insufficiency, the drug can be used in a usual dose. In severe liver dysfunction do not exceed the daily dose of Ebastin 10 mg.

Special precautions for handling the drug

1. To avoid damage to the tablets, do not remove the tablet from the blister by pressing. Open the package by gently lifting the free edge of the protective film.
2. Remove the protective film.
3. Gently squeeze the drug without touching it.
Carefully remove the tablet and put it on the tongue, where it will quickly dissolve. No need to drink with water or other liquid. Eating does not affect the effect of the drug.

Side effects

From the nervous system: from 1% to 3.7% - headache, drowsiness; less than 1% - insomnia.
On the part of the digestive system: from 1% to 3.7% - dryness of the oral mucosa; less than 1% - dyspepsia, nausea, abdominal pain.
On the part of the respiratory system: less than 1% - sinusitis, rhinitis.
Other: less than 1% - asthenic syndrome; allergic reactions are possible.

Overdose

Symptoms of moderate effects on the central nervous system (fatigue) and the autonomic nervous system (dryness of the oral mucosa) can occur only at high doses (300-500 mg, which is 15-25 times higher than the therapeutic dose).
Treatment: in case of an overdose, gastric lavage, monitoring of vital body functions, symptomatic treatment is recommended. There is no special antidote for ebastin.

Drug Interactions

It is not recommended to use Kestin tablets lyophilized 20 mg concomitantly with ketoconazole and erythromycin (increased risk of lengthening the QT interval interval).
Kestine tablets lyophilized 20 mg 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.
Impact on the ability to drive vehicles and manage mechanisms
In the event of side effects from the central nervous system, it is possible to minimize the ability of patients to drive vehicles and engage in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Pregnancy and lactemia

Contraindicated use of the drug during pregnancy and lactation (breastfeeding).

Application in childhood

Contraindicated in children under the age of 15 years.
In case of violations of kidney function
Use with caution in patients with renal failure.
With violations of liver function
Use with caution in patients with hepatic insufficiency.

Application in old age

In elderly patients, dose adjustment is not required.

Terms and conditions of storage

The drug should be stored out of reach of children at a temperature of no higher than 25 ° C. Shelf life - 3 years.