Kestin lyophilized instructions for use. The drug Almirall Kestin rapid dissolution lyophilized tablets. What diseases does Kestin help with?

Composition and release form

Film-coated tablets - 1 tablet:

• active ingredients: micronized ebastine - 10 mg;
• excipients: MCC - 20 mg; corn starch - 5.2 mg; lactose monohydrate - 88.5 mg; structured sodium carboxymethylcellulose - 5 mg; magnesium stearate - 1.3 mg;
• shell: hydroxypropyl methylcellulose - 1.725 mg; polyethylene glycol 6000 - 0.575 mg; titanium dioxide - 0.575 mg.

There are 5 or 10 pcs in a blister; 1 blister in a cardboard pack.

Syrup - 1 ml:

• active ingredients: ebastine - 1 mg;
• excipients: lactic acid 85% - 6.6 mg; glycerol oxystearate - 10 mg; neohesperidin dihydrochalcone - 1.06 mg; anethole - 0.25 mg; sodium propyl parahydroxybenzoate - 0.3 mg; sodium methyl parahydroxybenzoate - 1.2 mg; glycerin - 200 mg; sorbitol solution 70% - 100 mg; dimethylpolysiloxane - 0.014 mg; sodium hydroxide - up to pH 4.2; distilled water - up to 1 ml.

In dark glass bottles of 60 or 120 ml, complete with a measuring device in the form of a syringe; 1 set in a cardboard pack.

Description of the dosage form

Film-coated tablets: round, white. On one side of the tablets there is a line and an engraving “E 10”.

Syrup: a clear, colorless or slightly yellowish solution with an anise odor.

pharmachologic effect

Blocks H1 receptors and prevents histamine from binding to them.

Pharmacokinetics

It is rapidly absorbed and almost completely metabolized in the liver to the active metabolite, carabastine. After a single dose of 10 mg tablets, Cmax of carabastine (80-100 ng/ml) is achieved after 2.6-4 hours; after a single dose of syrup at a dose of 5 or 10 mg, Cmax of carabastine (108-209 ng/ml) is achieved after 2.8-3.4 hours. Fatty foods accelerate absorption (blood concentration increases by 50%). Does not penetrate the BBB. Simultaneous administration of tablets with food increases the level of carabastine in the blood by 1.6-2 times, but does not change the time to reach Cmax and clinical effects.

When taking tablets daily at a dose of 10 mg, the equilibrium concentration (130-160 ng/ml) is recorded after 3-5 days. When taking tablets, the binding of kestin and carabastine to plasma proteins is more than 95%, T1/2 of carabastine is 15-19 hours. 60-66% is excreted in the urine in the form of conjugated metabolites. Against the background of renal failure, T1/2 of carabastine increases to 23-26 hours, with liver failure - up to 27 hours, however, the concentration of the drug when taken 10 mg/day does not exceed therapeutic values. The values ​​of pharmacokinetic parameters do not depend on age.

Pharmacodynamics

After oral administration, a pronounced antiallergic effect begins within 1 hour and lasts for 48 hours. After a 5-day course of treatment, antihistamine activity persists for 72 hours due to the action of active metabolites. The drug does not have a pronounced anticholinergic and sedative effect.

Indications for use

• allergic rhinitis, seasonal and/or year-round (caused by household, pollen, epidermal, food, medicinal and other allergens);
• urticaria (caused by household, pollen, epidermal, food, insect, medicinal allergens, exposure to the sun, cold, etc.).

Contraindications for use

• hypersensitivity to the drug;
• pregnancy;
• breastfeeding period;
• children up to 12 years of age.

With caution: in case of renal and/or liver failure; in patients with an increased QT interval, hypokalemia.

Use during pregnancy and children

The safety of using Kestin® in pregnant women has not been studied, therefore its use during pregnancy is not recommended.

Side effects

Headache, dry mouth. Rarely - dyspepsia, nausea, insomnia, drowsiness, abdominal pain, asthenic syndrome, sinusitis, rhinitis.

Drug interactions

It is not recommended to prescribe Kestin simultaneously with ketoconazole and erythromycin. Kestin does not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.

Dosage

Inside, regardless of food intake.

Adults and children over 15 years of age: 10–20 mg (1/2–1 tablet) 1 time per day.

Children 12–15 years old: 10 mg (1/2 tablet) 1 time per day.

If liver function is impaired, the daily dose should not exceed 10 mg.

Overdose

Treatment: gastric lavage, monitoring of vital functions, symptomatic therapy. There is no special antidote.

Precautionary measures

Prescribe with caution to patients with an increased QT interval and hypokalemia.

Excipients: gelatin - 13 mg, - 9.76 mg, aspartame - 2 mg, mint flavor - 2 mg.

10 pieces. - blisters (1) - cardboard packs.

pharmachologic effect

Histamine H1 receptor blocker from the group of piperidine derivatives. Has an effect. It is characterized by a long-lasting effect (up to 48 hours), which is due to the formation of active metabolites. Unlike many histamine H1 receptor blockers, ebastine has virtually no m-anticholinergic activity, and also penetrates poorly into the central nervous system and does not have a pronounced sedative effect.

Pharmacokinetics

Absorption is 90-95%. Metabolized in the liver, turning into the active metabolite carbastine. Fatty foods accelerate absorption (blood concentration increases 1.5 times) and first-pass metabolism (carebastine formation). Cmax after a single dose of 10 mg is achieved after 2.6-4 hours and is 80-100 ng/ml. C ss is reached after 3-5 days and is 130-160 ng/ml. Protein binding of ebastine and carebastine is 95%. T1/2 of carebastine is 15-19 hours, excreted by the kidneys - 60-70% in the form of conjugates. In case of renal failure, T1/2 increases to 23-26 hours, with - up to 27 hours.

Indications

Allergic rhinitis, allergic conjunctivitis, urticaria.

Contraindications

Pregnancy, lactation, hypersensitivity to piperidine derivatives.

Dosage

When taken orally, a single dose for adults is 10 mg, dosage frequency is 1 time/day.

Side effects

Maybe:, dry mouth, drowsiness.

Rarely: abdominal pain, dyspepsia, nausea, asthenic syndrome, drowsiness, insomnia, rhinitis, sinusitis.

Drug interactions

Ebastine is compatible with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.

special instructions

Use with caution in patients with impaired liver and kidney function (in these cases, T1/2 of ebastine increases significantly).

Instructions for use

Active ingredients

Release form

Pills

Compound

Ebastine 20 mg. Excipients: magnesium stearate, microcrystalline cellulose, pregelatinized corn starch, lactose monohydrate (177 mg), croscarmellose sodium, hypromellose, titanium dioxide, macrogol 6000 (polyethylene glycol 6000).

Pharmacological effect

Kestin; - long-acting H1-histamine receptor blocker. Prevents histamine-induced spasms of smooth muscles and increased vascular permeability. After taking the drug orally, a pronounced antiallergic effect begins within 1 hour and lasts 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. It does not have anticholinergic activity, does not penetrate the blood-brain barrier, and does not cause a sedative effect. At a dose of up to 80 mg, it does not prolong the QT interval on the ECG.

Pharmacokinetics

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 10 mg of the drug, the Cmax of carabastine in plasma is reached after 2.6-4 hours and is 80-100 ng/ml. Fatty foods accelerate absorption (blood concentration increases by 50%). 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. The plasma protein binding of ebastine and carabastine is more than 95%. T1/2 of carabastine is from 15 to 19 hours, 66% of the drug is excreted in the form of conjugates in the urine. When the drug is prescribed simultaneously with food intake, the concentration 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 it Cmax and does not affect the clinical effects of Kestin. 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 when taken 10 mg/day does not exceed therapeutic values.

Indications

Allergic rhinitis is seasonal and/or year-round (caused by household, pollen, epidermal, food, medicinal and other allergens); - urticaria (caused by household, pollen, epidermal, food, insect, medicinal allergens, exposure to the sun, cold, etc.).

Contraindications

Hypersensitivity to the drug, pregnancy, lactation; - children under 12 years of age. With caution: in case of renal and/or liver failure; in patients with an increased QT interval, hypokalemia.

Use during pregnancy and breastfeeding

The safety of using Kestin in pregnant women has not been studied, so taking Kestin during pregnancy is not recommended. Nursing mothers are not recommended to take Kestin, since the excretion of ebastine into breast milk has not been studied.

Directions for use and doses

Orally, regardless of food intake. Children from 12 to 15 years old: 10 mg (1/2 tablet) 1 time per day. Adults and children over 15 years old are prescribed 10-20 mg (1/2-1 tablet) of the drug 1 once a day. A daily dose of 20 mg is prescribed on the recommendation of a doctor. If liver function is impaired, the daily dose should not exceed 10 mg.

Country of origin

Product group

antiallergic agent - H1 - histamine receptor blocker

Release forms

• 10 - blisters (1) - cardboard packs. 10 - blisters (1) - cardboard packs. 10 - blisters (2) - cardboard packs. pack 10 tablets pack 5 tablets

Description of the dosage form

• lyophilized tablets Film-coated tablets Film-coated tablets, white or almost white, round, with “E20” engraved on one side

pharmachologic effect

Pharmacokinetics

Special conditions

Compound

• ebastine 10 mg Excipients: magnesium stearate, microcrystalline cellulose, pregelatinized corn starch, lactose monohydrate (177 mg), croscarmellose sodium, hypromellose, titanium dioxide, macrogol 6000 (polyethylene glycol 6000). ebastine 10 mg Excipients: Microcrystalline cellulose - 20.00 mg Gel-like maize starch - 5.20 mg Lactose monohydrate - 88.50 mg Structured sodium carboxymethylcellulose - 5.00 mg Magnesium stearate - 1.30 mg ebastine 20 mg Excipients: magnesium stearate, microcrystalline cellulose, pregelatinized corn starch, lactose monohydrate (177 mg), croscarmellose sodium, hypromellose, titanium dioxide, macrogol 6000 (polyethylene glycol 6000) ebastine 20.00 mg Excipients: Gelatin 13.00 mg Mannitol 9.76 mg Aspartame 2 .00 mg Mint flavor 2.00 mg

Kestin indications for use

• allergic rhinitis, seasonal and/or year-round (caused by household, pollen, epidermal, food, medicinal and other allergens); urticaria (can be caused by household, pollen, epidermal, food, insect, drug allergens, exposure to the sun, cold, etc.); allergic diseases and conditions caused by increased release of histamine.

Kestin contraindications

• - pregnancy; - lactation (breastfeeding); - childhood and adolescence up to 12 years; - increased sensitivity to the drug. The drug is prescribed with caution in case of renal and/or liver failure, with an increase in the QT interval on the ECG, or with hypokalemia.

Kestin dosage

• 1 mg/ml 10 mg 20 mg

Kestin side effects

• With a frequency of 1% to 3.7%: headache, drowsiness, dry mouth. With a frequency of less than 1%: dyspepsia, nausea, insomnia, abdominal pain, asthenic syndrome, sinusitis, rhinitis. Allergic reactions are possible.

Drug interactions

Overdose

Storage conditions

• keep away from children
• store in a place protected from light

Various dosage forms of Kestin have the following composition:

• Kestin tablets in a film shell - 1 tablet contains 20 mg of active substance ( ebastine ) and excipients: Magnesium stearate , microcrystalline cellulose , pregelatinized corn starch , lactose monohydrate , croscarmellose sodium , hypromellose, titanium dioxide , macrogol 6000 ; the shell composition includes: hydroxypropyl methylcellulose, polyethylene glycol 6000, titanium dioxide;
• Kestin tablets in a film shell - 1 tablet contains 10 mg of active substance ( ebastine ) and excipients and shell composition are the same as in 20 mg tablets;
• Kestin tablets lyophilized (for resorption in the oral cavity) – 1 tablet contains 20 mg of active substance ( ebastine ) and excipients: gelatin , , mint flavor ;

Release form:

• Round, white, film-coated tablets with “E20” engraved on one side. Available in cardboard packaging (1 blister of 10 pieces).
• Round, white, film-coated tablets with “E10” engraved on one side. Available in cardboard packaging (1 blister of 10 pieces).
• Round, white, film-coated tablets with “E10” engraved on one side. Available in cardboard packaging (1 blister of 5 pieces).
• Round lyophilized (for resorption in the oral cavity) white tablets. Available in cardboard packaging of 10 pieces in one blister.

pharmachologic effect

Kestin belongs to the group H1-histamine receptor blockers . Its main effect is antiallergic. The drug quickly relieves tissue swelling, reduces exudation , prevents histamine-induced spasms of bronchial smooth muscles. Quickly and permanently relieves itching, burning of the skin and mucous membranes associated with allergies. Kestin has virtually no side effects of sedation.

Pharmacodynamics and pharmacokinetics

Active ingredient of the drug ebastine blocks H1-histamine receptors located in tissues, which suppresses the reaction of organs and tissues to histamine .H1-histamine receptors located in the smooth muscles of internal organs and the walls of blood vessels. By interacting with these receptors, histamine causes contraction of the smooth muscles of these organs, increases vascular permeability, stimulates the formation and secretion of mucus by the glands of the nasal cavity, as well as biologically active substances involved in the development of allergic reactions.

Ebastine prevents and weakens all effects caused by histamine, prevents the development of allergic edema, reduces redness, burning and itching, that is, it prevents the development and facilitates the course of allergic reactions. The mechanism of action of ebastine is competition with histamine for interaction with H1-histamine receptors organs and tissues. And since ebastine’s affinity for them is less pronounced than that of histamine, it does not displace the latter, but interacts only with free or released receptors. Therefore, ebastine works better as a prophylactic agent, and when an allergic reaction has already begun, it is not so effective.

Like all blockers H1-histamine receptors This drug has a fairly high degree of affinity for H1-histamine receptors , which provides a quick therapeutic effect: after oral administration, the effect of the drug occurs within an hour and lasts 48 hours. After the course of treatment, the aftereffect of the drug lasts for another three days due to the fact that the active metabolic products (metabolites), into which ebastine decomposes in the liver, are gradually eliminated from the body. Excretion of ebastine metabolites occurs through the kidneys.

Indications for use of Kestin

Treatment is carried out for the following diseases and conditions:

• at seasonal or year-round runny nose or conjunctivitis caused by any allergens;
• when and caused by any allergens, as well as physical factors (solar radiation, overheating, cold, etc.);
• for any other diseases and conditions caused by high histamine levels.

Contraindications for the use of Kestin

The drug is not prescribed:

• with increased sensitivity of the body to substances included in the composition of Kestin;
• during and breasts;
• children: film-coated tablets - up to 12 years, lyophilized tablets - up to 15 years;
• at – lyophilized tablets.

The drug is prescribed with caution in case of impaired renal and liver function, as well as in patients with coronary heart disease And hypokalemia . Since it can cause drowsiness and difficulty concentrating in some patients, they should not drive a car during the course of treatment.

Side effects of Kestin

The drug is well tolerated by patients and rarely produces side effects. However, they may be:

• from the central nervous system it is - , drowsiness or , lethargy , weakness , decreased performance ;
• from the gastrointestinal tract - various digestive disorders , nausea ,stomach ache, dry mouth;
• from the ENT organs - runny nose,
• – most often in the form of urticaria .

Kestin - instructions for use

Film-coated tablets are taken orally once a day (the intake may not be associated with food). For adults and adolescents over 15 years of age, the drug is prescribed no more than 20 mg (1-2 tablets of 10 mg or ½ - 1 tablet of 20 mg). Adolescents 12-15 years old are prescribed 10 mg (1 tablet of 10 mg or ½ tablet of 20 mg) once a day.

Instructions for use of Kestin recommend using lyophilized tablets for resorption in the oral cavity (placed on the tongue, where the tablet quickly dissolves). Taking lozenges is also not associated with food; these tablets should not be washed down. Lyophilized tablets are prescribed to adults and adolescents over 15 years of age in the same dosage as film-coated tablets. The tablets are fragile, so they should be removed from the blister with care to avoid damage.

Kestin overdose

An overdose of Kestin intensifies all of its side effects. In this case, you should immediately rinse your stomach and drink several tablets of activated carbon. If the condition does not improve, you need to call an ambulance.

Interaction of Kestin with other drugs

Kestin film-coated tablets are incompatible:

• with antifungal drugs ( , and etc.) , antibiotics from the macrolide group (, etc.) and alcohol-containing preparations - due to increased concentrations of Kestin in the blood and the risk of developing heart complications;
• With antiasthmatic drug theophylline ;
• indirect anticoagulants ;
• antiulcer means Cimethidine ;
• tranquilizer;
• any alcohol-containing drugs.

Lyophilized tablets are incompatible with And , but can be used simultaneously with Theophylline, indirect anticoagulants, Cimetidine, Diazepam and alcohol-containing drugs.