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);

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

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 develops after 1 hour and continues for 48 hours. After a 5-day course of treatment with Kestin, antihistamine activity persists for 72 hours due to the action of active metabolites.

The drug does not cause significant anticholinergic and sedative effects. There was no effect of Kestin on the duration of the QT interval on the ECG, even at a dose of 80 mg.

Pharmacokinetics

Suction and distribution

After taking the drug orally, ebastine is quickly absorbed from the gastrointestinal tract and is almost completely biotransformed in the liver with the formation of the active metabolite carabastine. Taking with fatty foods accelerates absorption (plasma concentration increases by 50%).

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

Does not penetrate the BBB.

Plasma protein binding of ebastine and carabastine is more than 95%.

When taking the drug simultaneously with food, the level of carabastine in the blood increases 1.6-2 times, but this does not lead to a change in the time it takes to reach Cmax of the metabolite and does not affect the clinical effects of Kestin.

Metabolism and excretion

T1/2 of carabastine ranges from 15 to 19 hours, 66% of the active substance is excreted in the form of conjugates in the urine.

Pharmacokinetics in special clinical situations

In elderly patients, pharmacokinetic parameters do not change significantly.

In patients with 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 when taken at a dose of 10 mg/day. does not exceed therapeutic values.

Special instructions

Use in pediatrics

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

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

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

Active ingredient

Ebastine

Composition

Active ingredients:

ebastine 20 mg.

Excipients:

magnesium stearate,

microcrystalline cellulose,

pregelatinized corn starch,

lactose monohydrate (177 mg),

sodium croscarmellose,

hypromellose,

titanium dioxide,

macrogol 6000 (polyethylene glycol 6000).

Pregnancy

Use of the drug KESTIN® during pregnancy and breastfeeding Kestin® is contraindicated for use during pregnancy due to the lack of reliable clinical data confirming the safety of the drug.

Kestin® should not be taken during breastfeeding due to the lack of data on the excretion of the active substance in breast milk.

Contraindications

Hypersensitivity to the drug Kestin;
lactation (breastfeeding);
children and adolescents up to 12 years of age.

With caution: the drug is prescribed for renal and/or liver failure, with an increase in the QT interval on the ECG, with hypokalemia.

Side Effects

From the side of the central nervous system: possible – headache; rarely – drowsiness, insomnia.

From the digestive system: possible – dry mouth; rarely – dyspepsia, nausea, abdominal pain.

Other: rarely – sinusitis, rhinitis, asthenic syndrome.

Interaction

It is not recommended to prescribe Kestin® concomitantly with ketoconazole and erythromycin due to an increased risk of prolongation of the QT interval.

There were no clinically significant drug interactions between Kestin and theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.

Overdose

Treatment: There is no specific antidote.

Gastric lavage and medical supervision are recommended; If necessary, carry out symptomatic therapy.

Storage conditions

In a place protected from light, at a temperature not exceeding 30 °C

Shelf life

3 years

Manufacturer

Almiral S.A., Spain