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, a pronounced antiallergic effect develops in 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 does not cause significant anticholinergic and sedative effects. No effect of Kestin on QT interval duration on ECG has been noted, even at a dose of 80 mg.

Pharmacokinetics

Absorption and distribution

After oral administration, ebastine is rapidly absorbed from the gastrointestinal tract and is almost completely biotransformed in the liver to form the active metabolite carabastine. Taking together with fatty food accelerates absorption (plasma concentrations increase by 50%).

After a single use of the drug in a dose of 10 mg, the Cmax of carabastine in plasma is reached after 2.6-4 hours and is 80-100 ng/ml. With a daily dose of 10 mg, Css is reached after 3-5 days and is 130-160 ng/ml.

It does not penetrate through the HEB.

The binding to plasma proteins of ebastine and carabastine is more than 95%.

If the drug is taken simultaneously with meals, the blood level of carabastine is increased by 1.6-2 times, but this does not change time to reach Cmax of metabolite and does not influence clinical effects of Kestin.

Metabolism and excretion

The T1/2 of carabastine is 15 to 19 h 66% of the active substance is excreted as conjugates in the urine.

Pharmacokinetics in special clinical cases

In elderly patients pharmacokinetic parameters do not change significantly.

In patients with renal insufficiency, the T1/2 is increased to 23-26 h and in hepatic insufficiency to 27 h, but the drug concentration when taken at a dose of 10 mg/day. does not exceed the therapeutic values.

Indications

Allergic rhinitis seasonal and/or year-round (caused by household, pollen, epidermal, food, drug allergens);

Hives (caused by including.

Hives (caused by household, pollen, epidermal, food, insect, drug allergens, exposure to the sun, cold).

Active ingredient

Composition

The active ingredient:

Ebastin 20 mg.

Auxiliary substances:

magnesium stearate,

microcrystalline cellulose,

corn starch pregelatinized,

lactose monohydrate (177 mg),

croscarmellose sodium,

Hypromellose,

Titanium dioxide,

Macrogol 6000 (polyethylene glycol 6000).

How to take, the dosage

Interaction

Kestin® should not be administered concomitantly with ketoconazole and erythromycin because of an increased risk of prolongation of the QT interval.

There have been no clinically significant drug interactions of Kestin with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.

Special Instructions

Pediatric use

In children aged 6 to 12 years, the use of the drug in the form of syrup or in the form of 10 mg tablets (5 mg/day) is preferable.

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

The drug Kestin does not affect the ability of patients to drive vehicles and operate machinery.

Contraindications

With caution: use the drug in cases of renal and/or hepatic insufficiency, with prolonged QT interval in ECG, with hypokalemia.

Side effects

CNS disorders: possibly – headache; rarely – somnolence, insomnia.

The digestive system: possibly – dry mouth; rarely – dyspepsia, nausea, abdominal pain.

Others: rare – sinusitis, rhinitis, asthenic syndrome.

Overdose

Treatment: There is no specific antidote.

Gastric lavage is recommended, medical observation; symptomatic therapy if necessary.

Pregnancy use

Kestin® is contraindicated in pregnancy and lactation because of the lack of reliable clinical data confirming the safety of the drug.

Kestin® should not be taken during breastfeeding because of lack of data about excretion of the active substance in the breast milk.

Similarities