Kestin lyophilized instructions for use. Drug Almirall Kestin rapid dissolution lyophilized tablets
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 by 1.6-2 times, but this does not lead to a change in the time to reach it Cmax and has no effect on clinical effects Kestina. In elderly patients, pharmacokinetic parameters do not change significantly. At renal failure T1/2 increases to 23-26 hours, and when 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 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, lactation; - childhood up to 12 years. 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 release of ebastine in breast milk not 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. In case of liver dysfunction daily dose should not exceed 10 mg.
Kestin tablets- 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 maximum concentration of carabastine in plasma is achieved 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%. The half-life of carabastine ranges 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 by 1.6-2 times, but this does not lead to a change in the time to reach its maximum concentration and does not affect the clinical effects of Kestin.
In elderly patients, pharmacokinetic parameters do not change significantly. In case of renal failure, the half-life 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 for use
Pills Kestin are used to eliminate allergic rhinitis seasonal and/or year-round (caused by household, pollen, epidermal, food, medicinal and other allergens; with urticaria (caused by household, pollen, epidermal, food, insect, medicinal allergens, exposure to the sun, cold, etc.).Directions for use
Pills Kestin take orally, regardless of food intake.Children from 12 to 15 years: 10 mg (1/2 tablet) once a day.
Adults and children over 15 years of age are prescribed 10-20 mg (1/2-1 tablet) of the drug 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.
Side effects
When using tablets Kestin such side effects, How headache, dry mouth. In rare cases - dyspepsia, nausea, insomnia, drowsiness, abdominal pain, asthenic syndrome, sinusitis, rhinitis.Contraindications
:Taking pills is contraindicated Kestin at hypersensitivity to the drug, pregnancy, lactation period. 20 mg film-coated tablets are not intended for use in children under 12 years of age.
With caution: in case of renal and/or liver failure; in patients with an increased QT interval, hypokalemia.
Pregnancy
:Safety of use Kestina has not been studied in pregnant women, 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.
Interaction with other drugs
It is not recommended to prescribe Kestin simultaneously with ketoconazole and erythromycin due to an increased risk of prolongation of the QT interval on the ECG. Kestin does not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.Overdose
:A special antidote for the drug Kestin does not exist. In case of overdose, gastric lavage and monitoring of vital signs are recommended. important functions body, symptomatic treatment.
Storage conditions
List B. At a temperature not exceeding 30°C in a place protected from light, out of reach of children.Release form
Kestin- tablets, coated film-coated, 20 mg.10 tablets in a blister made of PVC film and aluminum foil.
1 or 2 blisters in a cardboard box.
Compound
1 tablet Kestin 20 mg contains:Active substance: ebastine 20 mg
Excipients: magnesium stearate 2.6 mg, microcrystalline cellulose 40 mg, pregelatinized corn starch 10.4 mg, lactose monohydrate 177 mg, croscarmellose sodium 10 mg, hypromellose 2.85 mg, titanium dioxide 0.95 mg, macrogol 6000 ( polyethylene glycol 6000) 0.95 mg.
Additionally
: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).
Basic parameters
| Name: | KESTIN TABLETS 20 MG |
Kestin ®
International nonproprietary name
Dosage form
Film-coated tablets 10 mg, 20 mg
Cleaving
One tablet contains
active substance - ebastine 10 mg or 20 mg,
excipients: microcrystalline cellulose, pregelatinized corn starch, lactose monohydrate, croscarmellose sodium, magnesium stearate,
shell composition: hydroxypropyl methylcellulose, titanium dioxide (E 171), polyethylene glycol 6000.
Description
Round, white or almost white film-coated tablets marked “E/10” on one side.
Round, white or almost white, film-coated tablets marked “E 20” on one side.
Pharmacotherapeutic group
Antihistamines systemic action other. Ebastine.
ATX code R06AX22
Pharmacological properties
Pharmacokinetics
After oral administration, it is quickly absorbed and almost completely metabolized in the liver, turning into the active metabolite carebastine.
After a single dose of 10 mg or 20 mg of the drug, the maximum plasma concentration of carebastine is achieved after 2.6 - 4 hours and is 80 - 100 ng/ml or 108 - 209 mg/ml, respectively. Fatty foods accelerate absorption (concentration in the blood increases to 50%). Excreted by the kidneys - 60 - 70%, in the form of conjugates. The normal half-life is 15-19 hours. In case of renal failure, the half-life increases to 23 - 26 hours, in case of liver failure - up to 27 hours. 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. Plasma protein binding of ebastine and carebastine is more than 95%. The half-life of carebastine ranges from 15 to 19 hours, 66% of the drug is excreted as conjugates in the urine.
When the drug is prescribed simultaneously with food intake, the concentration of carebastine in the blood increases by 1.6 - 2 times, but this does not lead to a change in the time to reach its maximum concentration and does not affect the clinical effects of Kestin ® .
In elderly patients, pharmacokinetic parameters do not change significantly. In case of renal failure, the half-life increases to 23 - 26 hours, and in case of liver failure - up to 27 hours, however, the concentration of the drug when taken is 10 mg / day. does not exceed therapeutic values.
Pharmacodynamics
Kestin ® - long-acting H1-histamine receptor blocker. Prevents histamine-induced spasms of smooth muscles and increased vascular permeability.
After taking the drug orally, the 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. The drug does not have a pronounced anticholinergic and sedative effect. No influence of Kestin noted ® on the QT interval of the ECG when prescribed at a dose of up to 80 mg.
Indications for use
Allergic rhinitis, seasonal and/or year-round, with allergic conjunctivitis or without it - urticaria of various etiologies, including idiopathic chronic urticaria
Allergic dermatitis
Directions for use and doses
Adults and children over 12 years of age are prescribed 10 - 20 mg (1 - 2 tablets) once a day.
Kestin ® taken regardless of food intake.
If liver function is impaired, the daily dose should not exceed 10 mg.
No dosage adjustment is required in patients with impaired renal function.
Side effects
Classification of unwanted adverse reactions by frequency of development: very common (>1/10); often (>1/100,<1/10); не часто (>1/1000, <1/100); редко (>1/10 000, <1/1 000); очень редко (1/10 000, включая отдельные сообщения); частота неизвестна (невозможно оценить на основе имеющихся данных).
Rarely
drowsiness
dry mouth
Very rarely
nervousness, insomnia, dizziness, hypoesthesia, headache
palpitations, tachycardia
dyspepsia, nausea, vomiting, abdominal pain
abnormal liver enzyme levels
menstrual irregularities
edema, asthenic syndrome
urticaria, rash, dermatitis
Contraindications
hypersensitivity to the drug
pregnancy and lactation
with caution in case of hepatic and/or renal insufficiency
Drug interactions
It is not recommended to prescribe Kestin ® concomitantly with azole antifungals (such as ketoconazole and itraconazole), macrolide antibiotics (such as erythromycin) and anti-tuberculosis drugs (such as rifampicin).
Kestin ® does not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.
Special instructions
Use with caution in patients with prolonged QT interval and hypokalemia.
In case of severe liver dysfunction, the daily dose should not exceed 10 mg.
Since the therapeutic effect of Kestin ® manifests itself 1-3 hours after prescription, the drug should not be prescribed to eliminate acute allergic conditions requiring emergency intervention.
The drug should not be taken by patients suffering from hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.
Kestin ® may distort the results of skin allergy tests. Therefore, it is recommended to carry out such tests no earlier than 5-7 days after discontinuation of the drug.
Use in pediatrics
Data on the use of Kestin ® There are no tablets for children under 12 years of age.
Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms
Kestin in therapeutic doses does not affect the ability to drive vehicles and machines.
Overdose
Symptoms: increased side effects.
Treatment: There is no special antidote for the drug. In case of overdose, gastric lavage and monitoring of vital body functions are recommended. Symptomatic treatment.
EbastineDosage form
film-coated tabletsCompound
1 film-coated tablet contains:
Description
Round, film-coated tablets, white or almost white. On one side of the tablets there is an engraving "E 20".
Pharmacotherapeutic group
antiallergic agent - H1-histamine receptor blocker ATX:R.06.A.X.22 Ebastine
Pharmacodynamics
Ebastine is a long-acting H1-histamine receptor blocker.
After taking the drug orally, a pronounced antiallergic effect begins within 1 hour and lasts more than 48 hours. After a 5-day course of treatment with Kestin®, antihistamine activity persists for 72 hours due to the action of active metabolites. With long-term use, a high level of blockade of peripheral H1-histamine receptors is maintained without the development of tachyphylaxis. The drug does not have a pronounced anticholinergic or sedative effect and does not penetrate the blood-brain barrier. There was no effect of the drug Kestin® on the QT interval on the ECG at a dose of 100 mg - a dose exceeding the recommended daily dose (20 mg) by 5 times.
Pharmacokinetics
After oral administration, the drug is rapidly absorbed and almost completely metabolized in the liver, turning into the active metabolite carabastine. After a single dose of 20 mg of the drug, the maximum concentration of carabastine in the blood plasma is reached after 1-3 hours and is 157 ng/ml.
When taking the drug daily from 10 mg to 40 mg, the equilibrium concentration is achieved after 3-5 days, does not depend on the administered dose and is 130-160 ng/ml. The binding of ebastine and carabastine to plasma proteins is more than 95%. The half-life of carabastine ranges from 15 to 19 hours, 66% of the drug is excreted in the form of conjugates through the kidneys.
Food intake does not affect the clinical effects of Kestin®.
In elderly patients, pharmacokinetic parameters do not change significantly. In case of renal failure, the half-life increases to 23-26 hours, and in case of liver failure - up to 27 hours, but the concentration of the drug does not exceed therapeutic values.
Indications for use
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 components of the drug, pregnancy, lactation, children under 12 years of age, lactase deficiency, lactose intolerance, glucose-galactose malabsorption, severe liver dysfunction (class C according to the Child-Pugh classification).
With caution
Use in patients with an increased QT interval on the ECG, hypokalemia, renal failure and mild to moderate liver failure (class A, B according to the Child-Pugh classification).
Kestin® should be used with caution when taken concomitantly with ketoconazole or itraconazole and erythromycin - there may be an increased risk of prolongation of the QT interval on the ECG.
Pregnancy and lactation
The safety of using Kestin® in pregnant women has not been studied, so taking the drug during pregnancy is not recommended. Nursing mothers are not recommended to take Kestin®, since it is unknown whether
ebastine with breast milk.
If it is necessary to use the drug during lactation, you must stop breastfeeding.
Directions for use and doses
Inside, regardless of food intake.
Adults and children over 12 years old It is recommended to start therapy with a dose of 10 mg 1 time per day using the drug Kestin®, film-coated tablets, 10 mg. If effectiveness is insufficient, it is recommended to use a double dose, i.e. drug Kestin® film-coated tablets, 20 mg, 1 tablet (20 mg) once a day.
The course of treatment will be determined by the disappearance of symptoms of the disease.
Elderly patients: No dose adjustment required.
Patients with impaired renal function: no dose adjustment is required. Patients with mild to moderate liver failure(class A, B according to the Child-Pugh classification): no dose adjustment is required.
For severe liver dysfunction(class C according to the Child-Pugh classification) the daily dose should not exceed 10 mg, therefore it is recommended to use the drug Kestin®, film-coated tablets, 10 mg.
Side effect
Listed below are the adverse reactions observed in clinical trials and during post-registration use of the drug, taking into account the following criteria: very often (? 1/10); often (from 1/100 to<1/10); нечасто (от 1/1000 до <1/100); редко (от 1/10000 до < 1/1000); очень редко (<1/10000).
From the central and peripheral nervous system:
rarely: drowsiness;
very rarely: dizziness, hypoesthesia, headache, nervousness, insomnia.
From the gastrointestinal tract:
rarely: dryness of the oral mucosa;
very rarely: vomiting, abdominal pain, nausea, dyspepsia.
From the cardiovascular system:
very rare: palpitations, tachycardia.
From the liver and biliary tract:
very rarely: abnormal liver function tests.
For the skin and subcutaneous fat:
very rare: urticaria, rash, dermatitis.
From the reproductive system:
very rare: menstrual disorders.
General and local reactions :
very rarely: edema, asthenic syndrome.
Adverse reactions observed in clinical studies in children over 12 years old(a group of children of 460 people) did not differ from the reactions noted in adults.
Overdose
In studies using high doses (more than 100 mg per day), no clinically significant signs and symptoms were observed.
There is no special antidote for ebastine. In case of overdose, gastric lavage, monitoring of vital body functions, and symptomatic treatment are recommended.
Interaction
With simultaneous use of the drug Kestin® with ketoconazole or itraconazole and erythromycin, the risk of prolongation of the QT interval on the ECG may increase.
Rifampicin reduces the concentration of ebastine in the blood plasma and has an inhibitory effect on the antihistamine effect of ebastine.
The drug Kestin® does not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.
Special instructions
Ebastine may interfere with allergy skin test results. Therefore, it is recommended to carry out such tests no earlier than 5-7 days after discontinuation of the drug.
Effect on ability to drive a vehicle
In case of side effects from the central nervous system, such as drowsiness, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Release form
Film-coated tablets, 20 mg.
Package
10 tablets in a blister made of PVC film and aluminum foil.
1 blister with instructions for use is placed in a cardboard box.
Storage conditions
Store at a temperature not exceeding 25 °C.
Keep out of the reach of children.
Best before date
Do not use after expiration date.
Conditions for dispensing from pharmacies
Over the counterRegistration number
LS-001046Registration Certificate Holder
Owner of the Registration Certificate: Almirall S.A.Manufacturer
INDUSTRIAS FARMACEUTICAS ALMIRALL, S.L. SpainTakeda Pharmaceuticals LLC
Allergic rhinitis of various etiologies (seasonal and/or year-round). Urticaria of various etiologies, including chronic idiopathic.
Contraindications Kestin tablets 20 mg
Hypersensitivity to the components of the drug, pregnancy, lactation, phenylketonuria, children under 12 years of age, severe liver dysfunction (class C according to the Child-Pugh classification). Use with caution in patients with an increased QT interval on the ECG, hypokalemia, renal failure, and mild to moderate liver failure (class A. B according to the Child-Pugh classification). Kestin should be used with caution when taken simultaneously with ketoconazole or itraconazole, erythromycin, rifampicin - there may be an increased risk of prolongation of the QT interval on the ECG. Use during pregnancy and breastfeeding. There is 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 unknown whether ebastine is excreted in breast milk. The high degree of protein binding of ebastine and its main metabolite, carabastine (> 97%), does not imply excretion of the drug in breast milk. As a precaution, it is preferable not to use ebastine during lactation. If it is necessary to use the drug during lactation, it is necessary to decide on stopping breastfeeding.
Method of application and dosage Kestin tablets 20 mg
Inside, regardless of food intake. 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. If effectiveness is insufficient, it is recommended to use a double dose, i.e. drug Kestin film-coated tablets, 20 mg, 1 tablet (20 mg) once a day. The course of treatment will be determined by the disappearance of symptoms of the disease. Elderly patients: no dose adjustment is required. Patients with impaired renal function: no dose adjustment is required. Patients with mild to moderate hepatic impairment (Class A, B according to the Child-Pugh classification) do not require dose adjustment. In case of severe liver dysfunction (class C according to the Child-Pugh classification), the daily dose should not exceed 10 mg, therefore it is recommended to use the drug Kestin, film-coated tablets, 10 mg.