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 etiologies (seasonal and/or year-round).

Urticaria of various etiologies, incl. chronic idiopathic.

Pharmacological effect

Pharmacodynamics

Long-acting histamine H1 receptor blocker. Prevents histamine-induced spasms of smooth muscles and increased vascular permeability.

After taking the drug orally, a pronounced antiallergic effect begins after 1 hour and continues for 48 hours. After a 5-day course of treatment with Kestin® with 20 mg lyophilized tablets, the antihistamine activity persists for 72 hours due to the action of the active metabolite.

With long-term use, a high level of blockade of peripheral histamine H1 receptors is maintained without the development of tachyphylaxis. The drug does not have a pronounced anticholinergic and sedative effect.

There was no effect of the drug Kestin® lyophilized tablets 20 mg on the QT interval of the ECG at a dose of 100 mg, which exceeds the recommended daily dose (20 mg) by 5 times.

Pharmacokinetics

Suction

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

Distribution

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

Removal

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

Pharmacokinetics in special clinical situations

In elderly patients, pharmacokinetic parameters do not change significantly.

In case of renal failure, T1/2 increases to 23-26 hours, and in case of liver failure – up to 27 hours, however, the concentration of the drug does not exceed therapeutic values.

Special instructions

Ebastine may interfere with allergy skin test results. Therefore, it is recommended to carry out such tests no earlier than 5-7 days after discontinuation of the drug.

Impact on the ability to drive vehicles and other mechanisms that require increased concentration of attention

In the event of side effects from the central nervous system, a minimal decrease in the ability of patients to drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions is possible.

Active ingredient

Ebastine

Composition

Active ingredients:

ebastine 20 mg.

Excipients:

gelatin – 13.00 mg,

mannitol – 9.76 mg,

aspartame – 2.00 mg,

mint flavor – 2.00 mg.

Pregnancy

The use of the drug is contraindicated during pregnancy and lactation (breastfeeding).

Contraindications

Hypersensitivity to the components of the drug, pregnancy, lactation, phenylketonuria, children under 12 years of age, severe liver dysfunction (class C according to the Child-Pugh classification).

Side Effects

From the nervous system: from 1% to 3.7% – headache, drowsiness; less than 1% – insomnia.

From the digestive system: from 1% to 3.7% – dryness of the oral mucosa; less than 1% – dyspepsia, nausea, abdominal pain.

From the respiratory system: less than 1% – sinusitis, rhinitis.

Other: less than 1% – asthenic syndrome; Allergic reactions are possible.

Interaction

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

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

Overdose

Symptoms: moderate effects on the central nervous system (fatigue) and autonomic nervous system (dry oral mucosa) can only occur with high doses (300-500 mg, which is 15-25 times higher than the therapeutic dose).

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

Storage conditions

Store out of the reach of children at a temperature not exceeding 25°C.

Shelf life

3 years.

Manufacturer

Industrias Pharmaceuticas Almiralle S.A., Spain