Kestin, 20 mg 10 pcs.

Pharmacodynamics

Histamine H1 receptor blocker of long action. Prevents histamine-induced smooth muscle spasms and increased vascular permeability.

After oral administration of the drug, its pronounced antiallergic action begins within 1 hour and continues for 48 hours. After 5-day course of treatment with Kestin® tablets lyophilized 20 mg the antihistamine activity is maintained for 72 hours due to the action of the active metabolite.

A high level of blockade of peripheral histamine H1-receptors without development of tachyphylaxis is maintained with long-term use. The drug has no pronounced anticholinergic and sedative effect.

There has been no effect of Kestin® Lyophilized 20 mg tablets on the ECG QT interval at a dose of 100 mg that is 5 times greater than the recommended daily dose (20 mg).

Pharmacokinetics

Intake

After oral administration, it is rapidly absorbed and almost completely metabolized in the liver, converting to the active metabolite carabastine. After a single dose of 20 mg of the drug, the maximum plasma concentration of carabastine is reached after 1-3 hours and averages 157 ng/ml. Fatty foods accelerate absorption of carabastine (concentration in blood increases by 50%) and presystemic metabolism (formation of carabastine).

Distribution

When the drug is taken daily, the equilibrium concentration is reached after 3-5 days and is 130-160 ng/ml. Binding to plasma proteins of ebastine and carabastine is more than 95%.

The T1/2 of carabastine is from 15 to 19 hours. 66% of the drug is excreted as conjugates by the kidneys.

Pharmacokinetics in special clinical cases

The pharmacokinetic parameters do not change significantly in elderly patients.

In renal failure the T1/2 is increased to 23-26 h and in hepatic failure to 27 h, but the drug concentration does not exceed therapeutic values.

Indications

Allergic rhinitis of various etiology (seasonal and/or year-round).

The urticaria of various etiologies, including chronic idiopathic.

Active ingredient

Composition

The active ingredients:

Ebastin 20 mg.

Additional Ingredients:

gelatin – 13.00 mg,

mannitol – 9.76 mg,

aspartame – 2.00 mg,

mint flavoring – 2.00 mg.

How to take, the dosage

The drug is intended to be taken by mouth, regardless of meals.

Adults, children and adolescents over 15 years of age: 20 mg (1 lyophilized tablet) 1 time/day. The course of treatment is determined by the disappearance of symptoms.

In elderly patients no dose adjustment is required.

Dose adjustment is not required in patients with impaired renal function.

In mild to moderate hepatic impairment, the drug can be used in the usual dose. In severe hepatic impairment the daily dose of ebastin 10 mg should not be exceeded.

Special precautions for handling the drug

Interaction

It is not recommended to use Kestin® Lyophilized 20 mg tablets concomitantly with ketoconazole and erythromycin (increased risk of QT interval prolongation).

Kestin® Lyophilized 20 mg Tablets does not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.

Special Instructions

Ebastin may distort the results of skin allergy tests. Therefore, it is recommended to perform such tests not earlier than 5-7 days after discontinuation of the drug.

Impact on the ability to drive vehicles and other mechanisms requiring high concentration

In case of adverse effects on the CNS, there may be minimal decrease in the ability of patients to drive vehicles and engage in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

With caution: use in patients with prolonged QT interval, hypokalemia, renal and/or hepatic failure.

Side effects

Nervous system disorders: from 1% to 3.7% – headache, drowsiness; less than 1% – insomnia.

The digestive system: from 1% to 3.7% – dry mouth; less than 1% – dyspepsia, nausea, abdominal pain.

Respiratory system: less than 1% – sinusitis, rhinitis.

Others: less than 1% – asthenic syndrome; allergic reactions possible.

Overdose

Symptoms: moderate effect on CNS (fatigue) and autonomic nervous system (dry mouth mucosa) may occur only at high doses (300-500 mg, which is 15-25 times higher than the therapeutic dose).

Treatment: in case of overdose gastric lavage, control of vital body functions, symptomatic treatment are recommended. There is no special antidote for ebastine.

Pregnancy use

The drug is contraindicated in pregnancy and during lactation (breast-feeding).

Similarities