Kestin lyophilized. Medicinal product Almirall Kestin fast dissolving lyophilized tablets

Allergic diseases are one of the most urgent problems of modern health care. According to WHO forecasts, the prevalence of this pathology among the world's population is increasing annually by 1-2%. Antihistamines can help manage allergy symptoms. One of the effective means with prolonged action is Kestin.
Kestin is included in the pharmacological group of antihistamines - HI receptor blockers. It has an anti-allergic effect in many diseases caused by allergic reactions. Reduces the susceptibility of tissues to histamine, relieves the main manifestations of allergies: rhinitis, conjunctivitis, bronchospasm, edema, urticaria. Available in several dosage forms: tablets and syrup.

Action Kestin

The action of Kestin is determined by its belonging to the II group of HI histamine blockers. Histamine is produced by cells of the immune system in response to an allergen entering the body, and is involved in the implementation of most of the symptoms associated with allergies. The active substance of Kestin - ebastine does not allow histamine to contact the H1 receptors of blood vessels and smooth muscle cells. This leads to the relief of symptoms such as itching, spasm of the smooth muscle fibers of the respiratory tract; capillary permeability decreases, tissue swelling decreases.

Kestin's benefits include:
Rapid onset of treatment.
The long duration of the main effect is more than 24 hours.
Selective action only on HI receptors, does not block other types of receptors.
In therapeutic doses, the blood-brain barrier does not pass, so there is no sedative effect on the nervous system.
There is no dependence of the absorption of the drug in the intestine on food intake.
Does not develop addiction (tachyphylaxis) to the drug even with prolonged use,

Kestin's analogs

Kestin analogs may contain either the same active substance as it, or belong to other drug groups, but be used in the treatment of the same diseases.
An overview of drugs that act like Ketastine:
Espabastin,
diazolin,
erius,
Allegra,
claritin,
Suprastin.

How to take Kestin?

Kestin is a long-acting antihistamine. The active substance of the drug, getting into the body, retains its effect for 2 days. To achieve a therapeutic effect, it is enough to take it once a day. The duration of the course and dose is determined by the doctor depending on the clinical picture.

Is Kestin compatible with alcohol?

Information about the possibility of drinking alcoholic beverages in the treatment of Kestin is contradictory. Of course, you can not directly drink tablets with an ethanol-containing drink, however, like any other medicine. As a result of the study, it was found that ebastine (the active substance of Kestin) does not interact with ethanol. During an exacerbation of the disease, when taking the medicine, it is recommended to avoid additional stress on the body in the form of alcohol.

Does Kestin cause drowsiness?

II generation antihistamines, which include Kestin, do not penetrate the blood-brain barrier and do not have a depressing effect on brain structures. In rare cases, as a manifestation of a side effect, or with a significant increase in dose, a reaction from the nervous system to taking the drug in the form of daytime sleepiness is possible.

Does Kestin cause any side effects?

At the reception of each pharmacological drug, including Kestin, from various organs there are undesirable side effects of varying severity: from 1% to 3.7% of cases.
Digestive system, liver: nausea, dryness of the oral mucosa, abdominal pain, signs of dyspepsia, increased levels of liver enzymes in the blood.
Nervous system: headaches, irritability, insomnia or drowsiness.
With slow metabolism (excretion), cardiac arrhythmias are possible - prolongation of the QT interval on the ECG.
Respiratory system: sinusitis, rhinitis.
Asthenic syndrome (weakness, fatigue, decreased performance), allergic reactions in less than 1% of cases.

What diseases does Kestin help with?

Indications for the appointment of Kestin:
Allergic rhinitis of any origin: year-round, seasonal (during an exacerbation).
All types of urticaria, regardless of the etiological factor.

Who is Kestin tablets suitable for?

In its group of antihistamines, Kestin is the most effective drug, therefore it is used for especially severe manifestations of allergies: Quincke's edema, suffocation, rhinitis, conjunctivitis, massive skin rashes in the form of urticaria.
Indicated for use in adults and children over 15 years of age. Kestin in syrup is approved for children from 6 years of age.

Compound

Active ingredients: ebastine 20 mg.
Excipients: gelatin - 13.00 mg, mannitol - 9.76 mg, aspartame - 2.00 mg, mint flavor - 2.00 mg.
Release form
Lyophilized tablets
Package
10 tablets in a blister of Aluminium/PVC and Aluminium/PET.
1 blister with instructions for use is placed in a cardboard box.

Pharmacological properties

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 anti-allergic effect begins after 1 hour and lasts for 48 hours. After a 5-day course of treatment with Kestin® tablets, lyophilized 20 mg, antihistamine activity persists for 72 hours due to the action of the active metabolite.
With prolonged use, a high level of blockade of peripheral histamine H1 receptors remains without the development of tachyphylaxin. The drug does not have a pronounced anticholinergic and sedative effect.
There was no effect of the drug Kestin® 20 mg lyophilized tablets on the QT ECG interval at a dose of 100 mg, which is 5 times the recommended daily dose (20 mg).
Pharmacokinetics
Suction
After oral administration, it is rapidly absorbed and almost completely metabolized in the liver, turning into the active metabolite carabastin. After a single dose of 20 mg of the drug, the maximum concentration of carabastin in the blood plasma is reached after 1-3 hours and averages 157 ng / ml. Fatty foods accelerate the absorption of carabastin (the concentration in the blood increases by 50%) and first pass metabolism (the formation of carabastin).
Distribution
With daily administration of the drug, the equilibrium concentration is reached after 3-5 days and is 130-160 ng / ml. Plasma protein binding of ebastine and carabastin is more than 95%.
breeding
T1 / 2 carabastin is from 15 to 19 hours. 66% of the drug is excreted in the form of conjugates by the kidneys.
Pharmacokinetics in special clinical situations
In elderly patients, pharmacokinetic parameters do not change significantly.
In renal failure, T1 / 2 increases to 23-26 hours, and in liver failure - up to 27 hours, but the concentration of the drug does not exceed therapeutic values.

Indications for use

Allergic rhinitis of various etiologies (seasonal and / or year-round).
Urticaria of various etiologies, incl. chronic idiopathic.
Use during pregnancy and lactation
The use of the drug during pregnancy and lactation (breastfeeding) is contraindicated.

Contraindications

Hypersensitivity to the components of the drug;
phenylketonuria;
pregnancy and lactation (breastfeeding):
children's age up to 15 years;
hypersensitivity to the components of the drug.
With caution: use in patients with an increased QT interval, hypokalemia, with renal and / or hepatic insufficiency.

Mode of application

The drug is intended for resorption in the oral cavity, regardless of the meal.
Adults, children and adolescents over 15 years of age: appoint 20 mg (1 lyophilized tablet) 1 time / day. The course of treatment is determined by the disappearance of the symptoms of the disease.
In elderly patients, dose adjustment is not required.
In patients with impaired renal function, dose adjustment is not required.
With minor and moderate liver failure, the drug can be used at the usual dose. In severe hepatic impairment, a daily dose of 10 mg ebastine should not be exceeded.
Special precautions for handling the drug
To avoid damage to the tablets, do not remove the tablet from the blister by pressing. Open the package by carefully lifting the free edge of the protective film.
Remove protective film.
Carefully squeeze out the drug without touching it. Carefully remove the tablet and place it on the tongue where it will quickly dissolve. There is no need to drink water or other liquid. Eating does not affect the effect of the drug.

Side effect

From the nervous system: from 1% to 3.7% - headache, drowsiness; less than 1% - insomnia.
From the digestive system: from 1% to 3.7% - dryness of the oral mucosa; less than 1% - dyspepsia, nausea, abdominal pain.
From the respiratory system: less than 1% - sinusitis, rhinitis.
Others: less than 1% - asthenic syndrome; allergic reactions are possible.

Overdose

Symptoms: moderate effects on the central nervous system (fatigue) and the autonomic nervous system (dryness of the oral mucosa) can only occur at high doses (300-500 mg, which is 15-25 times higher than the therapeutic dose).
Treatment: in case of overdose, gastric lavage, control of vital body functions, symptomatic treatment are recommended. There is no specific antidote for ebastine.

Interaction

It is not recommended to use Kestin® tablets lyophilized 20 mg simultaneously with ketoconazole and erythromycin (increased risk of prolongation of the QT interval).
Kestin® lyophilized tablets 20 mg do not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.

special instructions

Ebastine may interfere with skin allergy test results. Therefore, it is recommended to conduct such tests no earlier than 5-7 days after discontinuation of the drug.
Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention
In the event of side effects from the central nervous system, a minimal decrease in the ability of patients to drive vehicles and engage in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions is possible.

Allergic rhinitis of various etiologies (seasonal and / or year-round). Urticaria of various etiologies, including chronic idiopathic.

Contraindications Kestin tablets 20mg

Hypersensitivity to the components of the drug, pregnancy, lactation, phenylketonuria, children under 12 years of age, severe liver dysfunction (Child-Pugh class C). Use with caution in patients with an increased QT interval on the ECG, hypokalemia, with renal insufficiency, and with mild to moderate hepatic insufficiency (Child-Pugh class A. B). Kestin should be used with caution while taking it with ketoconazole or itraconazole, erythromycin, rifampicin - there may be an increase in the risk of prolongation of the QT interval on the ECG. Use during pregnancy and during breastfeeding. There are no data on the effect of ebastine on human fertility. Data on the use of ebastine during pregnancy are limited. It is preferable to avoid the use of ebastine during pregnancy. Nursing mothers are not recommended to take Kestin, since it is not known whether ebastine is excreted in breast milk. The high degree of binding of ebastine and its main metabolite, carabastin, with proteins (> 97%) does not imply excretion of the drug with breast milk. As a precautionary measure, it is preferable not to use ebastine during lactation. If it is necessary to use the drug during lactation, it is necessary to resolve the issue of stopping breastfeeding.

Method of application and dosage Kestin tablets 20mg

Inside, regardless of the meal. Adults and children over 12 years of age are recommended to start therapy with a dose of 10 mg 1 time per day, using the drug Kestin film-coated tablets, 10 mg. In case of insufficient effectiveness, it is recommended to use a double dose, i.e. drug Kestin tablets, film-coated, 20 mg, 1 tablet (20 mg) once a day. The course of treatment will be determined by the disappearance of the symptoms of the disease. Elderly patients: dose adjustment is not required. Patients with impaired renal function: dose adjustment is not required. Patients with mild to moderate hepatic insufficiency (Child-Pugh class A, B) do not require dose adjustment. In severe liver dysfunction (Child-Pugh class C), the daily dose should not exceed 10 mg, therefore it is recommended to use Kestin, film-coated tablets, 10 mg.

Various dosage forms of Kestin have the following composition:

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

Release form:

• White, round, film-coated tablets with "E20" engraved on one side. Produced in cardboard packaging (1 blister of 10 pieces).
• White, round, film-coated tablets with "E10" engraved on one side. Produced in cardboard packaging (1 blister of 10 pieces).
• White, round, film-coated tablets with "E10" engraved on one side. Produced in cardboard packaging (1 blister of 5 pieces).
• Round lyophilized (for resorption in the oral cavity) white tablets. Produced in a carton pack of 10 pieces in one blister.

pharmachologic effect

Kestin belongs to the group H1 blockers - histamine receptors . Its main action is antiallergic. The drug quickly relieves tissue swelling, reduces exudation , prevents spasms of smooth muscles of the bronchi caused by histamine. Quickly and permanently removes itching, burning of the skin and mucous membranes associated with allergies. There is practically no side effect of sedation in Kestin.

Pharmacodynamics and pharmacokinetics

The active ingredient of the drug ebastine blocks H1-histamine receptors located in the tissues, which suppresses the response of organs and tissues to histamine .H1-histamine receptors located in the smooth muscles of the internal organs and the walls of blood vessels. 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 the 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 the affinity of ebastine 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 acts better as a prophylactic, 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 ingestion, the effect of the drug occurs in an hour and lasts 48 hours. After the course of treatment, the aftereffect of the drug persists for another three days due to the fact that the active metabolic products (metabolites), into which ebastine decomposes in the liver, are gradually excreted from the body. The excretion of ebastine metabolites occurs through the kidneys.

Indications for the 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;
• with and caused by any allergens, as well as physical factors (solar radiation, overheating, cold, etc.);
• in any other diseases and conditions caused by an increased content of histamine.

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 breast;
• children: film-coated tablets - up to 12 years, lyophilized tablets - up to 15 years;
• with - lyophilized tablets.

With caution, the drug is prescribed for impaired renal and hepatic function, as well as for patients with ischemic heart disease And hypokalemia . Since it can cause drowsiness and impaired concentration 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 gives side effects. However, they may be:

• from the side of the central nervous system - , drowsiness or , lethargy , weakness , decrease in working capacity ;
• 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 (reception 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 10 mg or ½ tablet 20 mg) 1 time per day.

Instructions for use Kestin recommends the use of lyophilized tablets for resorption in the oral cavity (put on the tongue, where the tablet quickly dissolves). Reception of lozenges for resorption is also not associated with food, these tablets should not be washed down. Assign lyophilized tablets to adults and adolescents over 15 years of age in the same dosage as film-coated tablets. The tablets are fragile, so take them out of the blister with care so as not to damage them.

Overdose of Kestin

With an overdose of Kestin, all its side effects increase. In this case, you should immediately wash the stomach and drink a few tablets of activated charcoal. If the condition does not improve, you need to call an ambulance.

Interaction of Kestin with other drugs

Film-coated Kestin tablets are incompatible:

• with antifungal drugs ( , and etc.) , macrolide antibiotics ( , etc.) and alcohol-containing preparations - due to an increase in the concentration of Kestin in the blood and the risk of developing complications from the heart;
• With anti-asthma drug theophylline ;
• indirect anticoagulants ;
• antiulcer means Cimetidine ;
• 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.

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 inside, a pronounced antiallergic effect begins after 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, does not cause a sedative effect. At doses up to 80 mg, it does not prolong the QT interval on the ECG.

Pharmacokinetics

After oral administration, it is rapidly absorbed and almost completely metabolized in the liver, turning into the active metabolite carabastin. Fatty foods accelerate absorption (blood concentration increases by 50%). It does not penetrate the blood-brain barrier. With a daily intake of 10 mg of the drug, the equilibrium concentration is reached after 3-5 days and is 130-160 ng / ml. Communication with plasma proteins of ebastine and carabastin is more than 95%. T1 / 2 of carabastin is from 15 to 19 hours, 66% of the drug is excreted in the form of conjugates with urine. When the drug is administered simultaneously with a meal, the concentration of carabastin in the blood increases by 1.6-2 times, but this does not lead to a change in the time to reach it Cmax and does not affect the clinical effects of Kestin. In elderly patients, pharmacokinetic parameters do not change significantly. With renal failure, T1 / 2 increases to 23-26 hours, and with liver failure - up to 27 hours, however, the concentration of the drug when taking 10 mg / day does not exceed therapeutic values.

Indications

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

Contraindications

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

Use during pregnancy and lactation

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

Dosage and administration

Inside, 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. In case of impaired liver function, the daily dose should not exceed 10 mg.

3D images

Composition and form of release

in a blister 10 pcs.; in a pack of cardboard 1 or 2 blisters.

Description of the dosage form

Round, film-coated tablets, white or almost white. One side of the tablets is engraved "E20".

pharmachologic effect

pharmachologic effect– antiallergic.

Pharmacodynamics

Kestin ® is a long-acting histamine H1 receptor blocker. Prevents histamine-induced spasms of smooth muscles and increased vascular permeability. After taking the drug inside, a pronounced anti-allergic effect begins after 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 BBB, does not cause a sedative effect. At doses up to 80 mg, it does not prolong the QT interval on the ECG.

Pharmacokinetics

After oral administration, it is rapidly absorbed and almost completely metabolized in the liver, turning into the active metabolite carabastin. After a single dose of 10 mg of the drug, Cmax of carabastin 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 BBB.

With a daily intake of 10 mg of the drug, the equilibrium concentration is reached after 3-5 days and is 130-160 ng / ml. Plasma protein binding of ebastine and carabastin is more than 95%. T 1/2 carabastin - from 15 to 19 hours, 66% of the drug is excreted in the form of conjugates in the urine.

When prescribing the drug simultaneously with food intake, the concentration of carabastin in the blood increases by 1.6-2 times, but this does not lead to a change in the time to reach its C max and does not affect the clinical effects of the drug Kestin ® .

In elderly patients, pharmacokinetic parameters do not change significantly. With renal failure, T 1/2 increases to 23-26 hours, and with liver failure - up to 27 hours, however, the concentration of the drug when taking 10 mg / day does not exceed therapeutic values.

Indications for Kestin ®

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, drug allergens, exposure to the sun, cold, etc.).

Contraindications

hypersensitivity to the drug;

pregnancy;

breastfeeding period;

children's age up to 12 years.

Carefully:

with renal and / or liver failure;

in patients with an extended QT interval, hypokalemia.

Use during pregnancy and lactation

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

Side effects

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

Interaction

Does not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.

Dosage and administration

inside regardless of food intake.

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

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

In case of impaired liver function, the daily dose should not exceed 10 mg.

Overdose

Treatment: There is no specific antidote for the drug. In case of an overdose, gastric lavage, monitoring of vital body functions, and symptomatic treatment are recommended.

special instructions

The drug Kestin ® in therapeutic doses does not affect the ability to drive vehicles and mechanisms.

In children aged 6 to 12 years, it is preferable to use Kestin ® syrup at a dose of 5 mg / day or 10 mg tablets (1/2 tablets per day).

Storage conditions of the drug Kestin ®

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

Keep out of the reach of children.

Shelf life of the drug Kestin ®

3 years.

Do not use after the expiry date stated on the packaging.

Synonyms of nosological groups

Category ICD-10	Synonyms of diseases according to ICD-10
J30.1 Allergic rhinitis due to plant pollen	Hypersensitivity to plant pollen
	hay fever
	Polypous allergic rhinosinusitis
	Seasonal hay fever
	seasonal rhinitis
	hay fever
	hay runny nose
J30.2 Other seasonal allergic rhinitis	allergic rhinitis seasonal
	Seasonal allergic rhinitis
J30.3 Other allergic rhinitis	Allergic rhinitis perennial
	Allergic rhinoconjunctivitis
L50 Urticaria	Idiopathic chronic urticaria
	Insect urticaria
	Urticaria of the newborn
	Chronic urticaria
L50.1 Idiopathic urticaria	Idiopathic urticaria
	Chronic idiopathic urticaria
T78.4 Allergy, unspecified	Allergic reaction to insulin
	Allergic reaction to insect stings
	Allergic reaction similar to systemic lupus erythematosus
	Allergic diseases
	Allergic diseases and conditions due to increased release of histamine
	Allergic diseases of the mucous membranes
	Allergic manifestations
	Allergic manifestations on the mucous membranes
	allergic reactions
	Allergic reactions due to insect bites
	Allergic reactions
	Allergic conditions
	Allergic edema of the larynx
	allergic disease
	allergic condition
	Allergy
	Allergy to house dust
	Anaphylaxis
	Skin reaction to medication
	Skin reaction to insect bites
	cosmetic allergy
	drug allergy
	drug allergy
	Acute allergic reaction
	Laryngeal edema of allergic origin and on the background of irradiation
	Food and drug allergies