Espa-Bastin pills 20mg, 10pcs

Composition

Each film-coated tablet contains:

Pill Core:

Active ingredient:  

• Ebastine – 10.00 mg/20.00 mg;

excipients:

microcrystalline cellulose-85.00 mg / 171.00 mg,

sodium carboxymethyl starch (type A) – 3.00 mg/6.00 mg,

colloidal anhydrous silicon dioxide-1.00 mg/2.00 mg,

magnesium stearate-0.50 mg/1.00 mg.

Film shell

 Opadray Y-1-7000 white, consisting of:  Hypromellose-5 cP – 4.69 mg / 9.38 mg, titanium dioxide-2.34 mg/4.68 mg, macrogol 400-0.47 mg/0.94 mg

Pharmacological action

of H1-histamine receptors is a long-acting blocker.

After a single oral dose, the antihistamine effect begins in 1 hour and persists for 48 hours. With prolonged use, a high level of blockade of peripheral H1 – histamine receptors remains without the development of tachyphylaxis.

After a 5-day course of treatment, antihistamine activity persists for 72 hours due to the action of the active metabolite.

The drug does not have a pronounced anticholinergic and sedative effect, does not penetrate the blood-brain barrier. There was no effect of the drug 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 use, the drug is rapidly absorbed and almost completely metabolized in the liver, turning into the active metabolite of carbastine. After a single dose of 20 mg of the drug, the maximum concentration of carbastine in blood plasma is reached in 1-3 hours and is 157 ng / ml.

With daily use of the drug from 10 mg to 40 mg, the equilibrium concentration is reached in 3-5 days, does not depend on the administered dose and is 130-160 ng / ml. Binding to plasma proteins of Ebastine and carbastin is more than 95%.

The half-life of carbastine is 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 the drug.

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

With renal insufficiency, the half-life increases to 23-26 hours, and with hepatic insufficiency-up to 27 hours, but the concentration of the drug does not exceed therapeutic values.

Indications

Allergic rhinitis, allergic conjunctivitis, urticaria.

Use during pregnancy and lactation

The safety of the drug in pregnant women has not been studied, so taking Espa-Bastin® during pregnancy is contraindicated.

It is not recommended to take the drug during breastfeeding.

Contraindications

• Hypersensitivity to the Active ingredient or other components of the drug;

• severe liver function disorders (Child-Pugh class C);

• pregnancy;

• lactation;

• children (up to 12 years).

With caution:

Prolongation of the QT interval on the ECG, hypokalemia, renal and / or mild to moderate hepatic insufficiency (Child-Pugh class A, B).

Caution should be exercised when taking the drug concomitantly with ketoconazole or itraconazole and erythromycin – there may be an increased risk of prolongation of the QT interval on the ECG.

Side effects

According to the World Health Organization (WHO), adverse events are classified according to their frequency as follows: very common (≥ 1/10), common (≥ 1/100, <1/10), uncommon (≥ 1/1000, <1/100), rare (≥ 1/10000, <1/1000), and very rare (

Gastrointestinal disorders: common: dryness of the oral mucosa; rare: nausea, abdominal pain, dyspepsia; very rare: vomiting.

Nervous system disorders:  often:  drowsiness, headache; very rarely: nervousness, insomnia, dizziness, paresthesia, dysesthesia.

Liver and biliary tract disorders:  very rare: hepatitis, cholestasis, changes in laboratory parameters (increased activity of hepatic transaminases, GGT, alkaline phosphatase, bilirubin).

Immune system disorders:  frequency unknown: hypersensitivity reactions (e. g., anaphylaxis, angioedema).

Disorders of the cardiovascular system:  very rare:  tachycardia, palpitation.

Skin and subcutaneous tissue disorders:  very rare:  urticaria, rash, and dermatitis.

Reproductive system disorders:  very rare:  menstrual disorders.

General and local reactions:  very rare: edema, asthenic syndrome.

Interaction

It is not recommended to administer concomitantly with ketoconazole or itraconazole and erythromycin (increased risk of prolongation of the QT interval).

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

Rifampicin reduces the concentration of Ebastine in blood plasma and has an inhibitory effect on the antihistamine effect of Ebastine.

May increase the effect of other antihistamines.

How to take, course of use and dosage

Inside, regardless of food intake.

Adults and children over 12 years of age are recommended to start therapy with a dose of 10 mg once a day, using Espa-Bastin®, film-coated tablets,10 mg.

In case of insufficient effectiveness, it is recommended to use a double dose, i. e. Espa-Bastin®, 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 insufficiency (Child-Pugh class A, B): no dose adjustment is required.

For severe hepatic impairment (Child-Pugh Class C), the daily dose should not exceed 10 mg, so it is recommended to use Espa-Bastin®, film-coated tablets,10 mg.

Overdose

When taking up to 100 mg of Ebastinee per day, clinically significant symptoms of overdose are not observed.

No specific antidote was identified.

Treatment:  gastric lavage, monitoring of vital functions of the body, including ECG monitoring, symptomatic therapy.

Description

Round, (slightly) biconvex film-coated tablets, white to almost white in color with a risk on one side.

Functional features

Absorption is 90-95%. It is metabolized in the liver, turning into the active metabolite carEbastine. Fatty foods accelerate absorption (blood concentration increases 1.5 times) and presystemic metabolism (formation of carEbastine). _Cmax after a single dose of 10 mg is reached in 2.6-4 hours and is 80-100 ng / ml. C_ss is reached in 3-5 days and is 130-160 ng / ml. Binding to plasma proteins of Ebastine and carEbastine is 95%. T_1/2 of carEbastine – 15-19 hours, excreted by the kidneys-60-70% in the form of conjugates. With renal insufficiency, T_1/2 increases to 23-26 hours, with hepatic insufficiency – up to 27 hours.

Special instructions

Ebastine may distort the results of skin allergy tests. Therefore, it is recommended to conduct such tests no earlier than 5-7 days after discontinuation of the drug.

During therapy, caution should be exercised in the presence of an extended QT interval on the electrocardiogram, hypokalemia, as well as when taking azole antimycotics and macrolide antibiotics at the same time (see the section “Interaction with other drugs”).

Caution should be exercised when taking the drug in patients with severe hepatic insufficiency (see the section “Dosage and use”).

Influence on the ability to drive vehicles and fur. :

In therapeutic doses, it does not affect the ability to drive vehicles and mechanisms.

In case of side effects from the central nervous system, such as drowsiness, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

At a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf

life is 5 years.

Do not use after the expiration date.

Active ingredient

Abastin

Dosage form

Tablets

Purpose

Children over 12 years old, For adults

Indications

Allergy, Allergic Conjunctivitis, Allergic Runny Nose, Urticaria