Kestine, pills 20mg, 10pcs

Composition

Active ingredients:

Ebastine 20 mg.

Auxiliary substances:

magnesium stearate,

microcrystalline cellulose,

pregelatinized corn starch,

lactose monohydrate (177 mg),

sodium croscarmellose,

hypromellose,

titanium dioxide,

macrogol 6000 (polyethylene glycol 6000).

Pharmacological action

Pharmacodynamics

Long-acting histamine H1-receptor blocker. Prevents histamine-induced smooth muscle spasms and increased vascular permeability. After taking the drug inside, a pronounced anti-allergic effect develops in 1 hour and continues for 48 hours. After a 5-day course of treatment with Kestine, 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 Kestine on the duration of the QT interval on the ECG, even at a dose of 80 mg.

Suction and distribution

After oral use, Ebastinee is rapidly absorbed from the gastrointestinal tract and is almost completely biotransformed in the liver to form the active metabolite of carbastine. Intake together with fatty foods accelerates absorption (the concentration in blood plasma increases by 50%).

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

It does not penetrate the BBB.

The binding to plasma proteins of Ebastine and carbastin is more than 95%.

When taking the drug simultaneously with a meal, the level of carbastine in the blood increases by 1.6-2 times, but this does not change the time to reach Cmax of the metabolite and does not affect the clinical effects of Kestine.

Metabolism and elimination

of T 1/2 of carbastine is from 15 to 19 hours 66% of the Active ingredient is excreted in the form of conjugates in the urine.

Pharmacokinetics in special clinical cases

In elderly patients, the pharmacokinetic parameters do not change significantly.

In patients with renal insufficiency, T 1/2 increases to 23-26 hours, and in patients with hepatic insufficiency-up to 27 hours, but the concentration of the drug when taken at a dose of 10 mg / day. does not exceed therapeutic values.

Indications

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

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

Use during pregnancy and lactation

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

Do not take Kestine® during breastfeeding due to the lack of data on the excretion of the Active ingredient in breast milk.

Contraindications

• Hypersensitivity to Kestine;
• lactation (breastfeeding);
• children and adolescents under 12 years of age.

With caution: prescribe the drug for renal and/or hepatic insufficiency, with an increase in the QT interval on the ECG, with hypokalemia.

Side effects

From the central nervous system: possibly-headache; rarely-drowsiness, insomnia.

From the digestive system: possibly-dry mouth; rarely-dyspepsia, nausea, abdominal pain.

Other: rarely-sinusitis, rhinitis, asthenic syndrome.

Interaction

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

There was no clinically significant drug interaction of Kestine with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.

How to take, course of use and dosage

• Adults and children over 15 years of age: the drug is prescribed 10-20 mg (1/2-1 tablet) 1 time / day, regardless of food intake.
• Children aged 12 to 15 years: 10 mg (1/2 tablet) 1 time / day.
• In patients with impaired liver function: the daily dose should not exceed 10 mg.

Overdose

Treatment: There is no specific antidote.

Gastric lavage and medical supervision are recommended; if necessary, symptomatic therapy is performed.

Special instructions

Use in pediatrics

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

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

The drug Kestine does not affect the ability of patients to drive vehicles and work with mechanisms

Form of production

Film-coated tablets

Storage conditions

In a dark place, at a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Abastin

Dosage form

Tablets

Description

Children over 12 years old, For adults

Indications

Allergy, Allergic Rhinitis, Pollinosis, Allergic Conjunctivitis, Urticaria