Espa-Bastin - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline - 85.00 mg / 171.00 mg, sodium carboxymethyl starch (type A) - 3.00 mg / 6.00 mg, silicon dioxide colloidal anhydrous - 1.00 mg / 2.00 mg, magnesium stearate - 0, 50 mg / 1.00 mg.

Film sheath Opadry Y-1-7000 white, consisting of: hypromellose-5cP - 4.69 mg / 9.38 mg, titanium dioxide - 2.34 mg / 4.68 mg, macrogol 400 - 0.47 mg / 0.94 mg.

Description:

For the dosage of 10 mg: round, flat-cylindrical tablets, film-coated, from white to almost white with a risk on one side.

For the dosage of 20 mg: round, (slightly) biconvex tablets, film-coated, from white to almost white with a risk on one side.

Pharmacotherapeutic group:antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

R.06.A.X.22 Ebastin

Pharmacodynamics:

H₁-gistamine receptor blocker long-acting.

After a single oral intake of antihistamine action begins after 1 hour and persists for 48 hours. With prolonged reception, a high level of blockade of peripheral H₁- histamine receptors 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 has no pronounced anticholinergic and sedative effect, does not penetrate the blood-brain barrier. No effect of the drug on the interval QT on an ECG at a dose of 100 mg - a dose exceeding the recommended daily dose (20 mg) by 5 times.

Pharmacokinetics:

After ingestion, the drug is rapidly absorbed and almost completely metabolized in the liver, becoming an active metabolite of carabastine. After a single dose of 20 mg of the drug, the maximum concentration of carbastine in the blood plasma is achieved after 1-3 hours and is 157 ng / ml.

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

The half-life of carbastine is from 15 to 19 hours, 66% The drug is excreted as conjugates through the kidneys.

Eating does not affect the clinical effects of the drug.

In elderly patients pharmacokinetic parameters do not change significantly.

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

Indications:

- Allergic rhinitis of different etiology (seasonal and / or year-round);

- hives of various etiologies, including chronic idiopathic.

Contraindications:

- Hypersensitivity to the active substance or other components of the drug;

- severe liver dysfunction (Child-Pugh class C);

- pregnancy;

- lactation period;

- children's age (up to 12 years).

Carefully:

Interval lengthening QT on ECG, hypokalemia, renal and / or mild and moderate degree of hepatic insufficiency (class A, B according to Child-Pugh classification).

Caution should be applied to the drug while taking with ketoconazole or itraconazole and erythromycin - possibly increasing the risk of lengthening the interval QT on the ECG.

Pregnancy and lactation:

The safety of the drug in pregnant women is not investigated, therefore, taking Espa-Bastin® during pregnancy is contraindicated.

It is not recommended to take the drug during breastfeeding.

Dosing and Administration:

Inside, regardless of food intake.

Adults and children over 12 years of age it is recommended to begin therapy with a dose of 10 mg 1 time per day, using the preparation Espa-Bastin®, film-coated tablets, 10 mg.

In case of insufficient effectiveness, it is recommended to use a double dose, i.e. preparation Espa-Bastin®, film-coated tablets, 20 mg of 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 and moderate hepatic impairment (class A, B according to the Child-Pugh classification): dose adjustment is not required.

In severe violations of liver function (class C according to Child-Pugh classification) daily dose should not exceed 10 mg, therefore it is recommended to use Espa-Bastin® preparation, film-coated tablets, 10 mg.

Side effects:

According to the World Health Organization (WHO), unwanted effects are classified according to their frequency of development as follows: very often (≥ 1/10), often (≥ 1/100, <1/10) infrequently (≥ 1/1000, < 1/100), rarely (≥ 1/10000, <1/1000) and very rarely (<1/10000); frequency is unknown (the frequency of occurrence of phenomena can not be determined on the basis of available data).

Disorders from the gastrointestinal tract: often: dryness of the oral mucosa; rarely: nausea, abdominal pain, indigestion; very rarely: vomiting.

Disturbances from the nervous system: often: drowsiness, headache; very rarely: nervousness, insomnia, dizziness, paresthesia, dysesthesia.

Disturbances from the liver and bile ducts: Very rarely: hepatitis, cholestasis, changes in laboratory parameters (increased activity of hepatic transaminases, GGT, alkaline phosphatase, bilirubin).

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

Disorders from the cardiovascular system: rarely: tachycardia, palpitation.

Disturbances from the skin and subcutaneous tissueth: rarely: urticaria, rash, dermatitis.

Disorders from the reproductive system: rarely: menstrual disorders.

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

Overdose:

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

A specific antidote has not been identified.

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

Interaction:

It is not recommended to appoint simultaneously with ketoconazole or itraconazole and erythromycin (increased risk of lengthening the interval QT).

There was no clinically significant interaction with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing medications.

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

May enhance the effect of other antihistamines.

Special instructions:

Ebastin can distort the results of skin allergic tests. Therefore, it is recommended to carry out such tests no earlier than 5-7 days after drug withdrawal.

During therapy, caution should be exercised in the presence of an elongated QT interval on the electrocardiogram, hypokalemia, as well as with the simultaneous administration of azole antimycotic agents and antibiotics of the macrolide group (see section "Interaction with other drugs").

Caution should be exercised when taking the drug in patients with severe hepatic impairment (see section "Method of administration and dose").

Effect on the ability to drive transp. cf. and fur:

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

In the event 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 requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 10 mg and 20 mg.

Packaging:

10 tablets, film-coated, in a blister of Al-PVC / PVDC.

1 blister in pack of cardboard with instructions for use

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-003460

Date of registration:16.02.2016

Expiration Date:16.02.2021

The owner of the registration certificate:Esparma GmbHEsparma GmbH Germany

Manufacturer: & nbsp

ADVANCE PHARMA, GmbH Germany

Representation: & nbspESPARMA GmbH ESPARMA GmbH Germany

Information update date: & nbsp31.07.2016

Illustrated instructions

Instructions

Espa-Bastin® (Espa-Bastin®)