Kestin, 10 mg 5 pcs.

Pharmacodynamics

Anti-allergic drug. After oral administration a pronounced antiallergic effect starts after 1 hour and lasts for 48 hours. After 5-day course of treatment with Kestin® antihistamine activity is maintained for 72 hours due to the action of active metabolites. The drug has no pronounced anticholinergic and sedative effect. No effect of Kestin® on ECG QT-interval was observed at a dose of 100 mg that was 5-10 times higher than the recommended daily dose.

Pharmacokinetics

After oral administration, the drug is rapidly absorbed and almost completely metabolized in the liver, converting to the active metabolite carabastine. After a single dose of 10 mg of the drug, the Cmax of carabastine in plasma is reached after 2.6-4 hours and is 80-100 ng/ml. It does not penetrate the blood-brain barrier.

When taking 10 mg of the drug 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%. T1/2 of carabastine is from 15 to 19 hours, 66% of the drug is excreted as conjugates through the kidneys.

Eating has no effect on the clinical effects of the drug Kestin®.

In elderly patients the pharmacokinetic parameters do not change significantly. In renal insufficiency the T1/2 is increased up to 23-26 h and in hepatic insufficiency – up to 27 h, but the drug concentration does not exceed therapeutic values.

Indications

Allergic rhinitis of different etiology (seasonal and/or year-round, both accompanied and not accompanied by allergic conjunctivitis).

The urticaria of various etiologies, including chronic idiopathic.

Active ingredient

Composition

Active ingredient:

Ebastin microionized 10 mg.

Auxiliary substances:

cellulose microcrystalline,

corn starch,

p> lactose monohydrate,

sodium carboxymethylcellulose structured,

magnesium stearate,

hydroxypropyl methylcellulose,

polyethylene glycol 6000,

titanium dioxide.

How to take, the dosage

Ingestion, regardless of meals.

In case of liver dysfunction the daily dose should not exceed 10 mg.

Interaction

Cestin® should not be used concomitantly with ketoconazole and erythromycin (increased risk of QT interval prolongation).

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

Special Instructions

Impact on ability to operate vehicles and other mechanisms requiring high concentration

In case of adverse effects on the central nervous system, there may be minimal impairment of patients’ ability to operate vehicles and engage in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

Side effects

With an incidence greater than 1%: headache (7.9%), drowsiness (3.0%), dry mouth (2.1%).

Frequently less than 1%: dyspepsia, nausea, insomnia, abdominal pain, asthenic syndrome, sinusitis, rhinitis.

Overdose

Symptoms: signs of moderate effect on CNS (fatigue) and autonomic nervous system (dry mouth) may occur only at high doses (300 mg-500 mg, which is 30-50 times higher than the therapeutic dose).

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

Pregnancy use

It is contraindicated during pregnancy and lactation.

Similarities