Espa-Bastin^® (Tablets) Instructions for Use

Marketing Authorization Holder

Aristo Pharma, GmbH (Germany)

Manufactured By

Laboratorios Medicamentos Internacionales, S.A. (Spain)

ATC Code

R06AX22 (Ebastine)

Active Substance

Ebastine (Rec.INN registered by WHO)

Dosage Forms

	Espa-Bastin®	Film-coated tablets, 10 mg: 10 pcs.
		Film-coated tablets, 20 mg: 10 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets from white to almost white, round, flat-cylindrical, with a score on one side.

Excipients: microcrystalline cellulose – 85 mg, sodium carboxymethyl starch (type A) – 3 mg, colloidal anhydrous silicon dioxide – 1 mg, magnesium stearate – 0.5 mg.

Composition of the film coating Opadry Y-1-7000 white: hypromellose-5cP – 4.69 mg, titanium dioxide – 2.34 mg, macrogol 400 – 0.47 mg.

10 pcs. – blisters (1) – cardboard packs.

Film-coated tablets from white to almost white, round, (slightly) biconvex, with a score on one side.

Excipients: microcrystalline cellulose – 171 mg, sodium carboxymethyl starch (type A) – 6 mg, colloidal anhydrous silicon dioxide – 2 mg, magnesium stearate – 1 mg.

Composition of the film coating Opadry Y-1-7000 white: hypromellose-5cP – 9.38 mg, titanium dioxide – 4.68 mg, macrogol 400 – 0.94 mg.

10 pcs. – blisters (1) – cardboard packs.

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

Antiallergic agent – H₁-histamine receptor blocker

Pharmacological Action

A blocker of histamine H₁-receptors from the group of piperidine derivatives. It has an antiallergic effect. It is characterized by a long-lasting action (up to 48 hours), which is due to the formation of active metabolites.

Unlike many histamine H₁-receptor blockers, ebastine has practically no m-cholinoblocking activity, penetrates the CNS poorly, and does not have a pronounced sedative effect.

Pharmacokinetics

Absorption is 90-95%. It is metabolized in the liver, turning into the active metabolite carebastine. Fatty food accelerates absorption (blood concentration increases by 1.5 times) and presystemic metabolism (formation of carebastine).

C_max 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. Plasma protein binding of ebastine and carebastine is 95%.

T_1/2 of carebastine is 15-19 hours, it is excreted by the kidneys – 60-70% in the form of conjugates.

Indications

Allergic rhinitis (seasonal and/or perennial), allergic conjunctivitis, urticaria of various etiologies (including chronic idiopathic).

ICD codes

Dosage Regimen

Administer orally, with or without food.

For adults and adolescents aged 12 years and older, the standard daily dose is 10 mg to 20 mg.

Select the appropriate strength based on symptom severity and individual response.

For mild to moderate allergic conditions, use 10 mg once daily.

For severe symptoms or inadequate response, use 20 mg once daily as the maximum dose.

Do not exceed the maximum recommended daily dose of 20 mg.

For the 20 mg tablet, the score line allows for splitting into two equal 10 mg halves if needed.

In patients with mild to moderate hepatic impairment (Child-Pugh class A or B), do not exceed 10 mg once daily.

Contraindicated in patients with severe hepatic impairment (Child-Pugh class C).

Use with caution in patients with renal impairment.

The duration of treatment depends on the indication; continue for the period of allergen exposure or as directed.

Adverse Reactions

Nervous system disorders: headache, drowsiness, dizziness, hypesthesia, dysgeusia.

Gastrointestinal disorders: dry mouth, nausea, abdominal pain, vomiting, dyspepsia.

Cardiac disorders: palpitations, tachycardia.

Hepatobiliary disorders: hepatitis, cholestasis, deviation of liver function tests (increased activity of hepatic transaminases, GGT, ALP, bilirubin).

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

Reproductive system and breast disorders: menstrual cycle disorder.

Immune system disorders: hypersensitivity reactions (anaphylaxis, angioedema);

General disorders and administration site conditions: edema, asthenia.

Contraindications

Hypersensitivity to ebastine; severe liver dysfunction (Child-Pugh class C); pregnancy, breastfeeding period; pediatric age – depending on the dosage form.

With caution

Patients with prolonged QT interval on ECG, hypokalemia, renal failure, mild and moderate degree of hepatic impairment (Child-Pugh class A, B); concomitant use with ketoconazole or itraconazole, erythromycin and rifampicin (possible increased risk of QT interval prolongation on ECG).

Use in Pregnancy and Lactation

Contraindicated during pregnancy. If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided.

Use in Hepatic Impairment

Contraindicated in severe liver dysfunction (Child-Pugh class C). Should be used with caution in patients with mild and moderate degree of hepatic impairment (Child-Pugh class A, B).

Use in Renal Impairment

Use with caution in patients with renal failure.

Pediatric Use

Can be used in children according to indications, in age-appropriate recommended doses and dosage forms. It is necessary to strictly follow the instructions in the ebastine drug leaflets regarding contraindications for the use of specific ebastine dosage forms in children of different ages.

Special Precautions

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 ebastine.

Effect on ability to drive vehicles and machinery

During the use of ebastine, patients should exercise caution when driving vehicles and machinery, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use of ebastine with ketoconazole or itraconazole and erythromycin, an increase in the QT interval on the ECG is possible.

With simultaneous use, rifampicin reduces the plasma concentration of ebastine and has an inhibitory effect on the antihistamine effect of ebastine.

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

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.