Composition per tablet:

Ebastine (INN).................................................................10 mg

Excipients: microcrystalline cellulose, pregelatinised maize starch, lactose monohydrate, croscarmellose sodium, magnesium stearate, hypromellose, macrogol and titanium dioxide.

 

Pharmaceutical form and content of package

Round, white film-coated tablets with one side marked E10.

Packages of 10 (1x10), 20 (2x10) and 30 (3x10) tablets.

Not all the presentations are available in all markets.

 

Pharmacological properties

Ebastine, the active ingredient of Ebastel, induces a potent and prolonged selective blockade of the H1 histamine receptors. It is free of anticholinergic and sedative effects, since ebastine and its metabolites do not cross the blood-brain barrier. Ebastel

does not increase the sedative effects of alcohol. Its duration of action means Ebastel can be administered once daily.

 

Pharmacokinetic properties

Ebastine is rapidly absorbed after oral administration, undergoing a notable first pass hepatic metabolism effect which gives rise to its acid metabolite, carebastine. After a single oral dose of 10 mg, maximum plasma levels of the metabolite are obtained between 2.6 and 4 hours and reach values of 80 to 100 ng/ml. The half-life of the acid metabolite is between 15 and 19 hours, with 66% of the drug excreted in urine, mainly as conjugated metabolites. After repeated administration of 10 mg once daily, steady state is reached in 3 to 5 days with maximum plasma levels between 130 and 160 ng/ml.

Ebastine is metabolised to carebastine via enzyme CYP3A4. Concomitant administration of ebastine with CYP3A4 inhibitors

to healthy volunteers is associated with significantly raised plasma concentrations of ebastine and carebastine, especially with ketoconazole. Both Ebastine and carebastine present high protein binding: > 97%.

No statistically significant differences are observed in the pharmacokinetic profile of elderly patients when compared with

young adults. Ebastine and carebastine plasma concentrations in patients with mild, moderate or severe renal impairment (daily doses of 20 mg/day) and in those with mild, moderate (both with doses of 20 mg/day) or severe (dose of 10 mg/day) hepatic

impairment were similar to those reached in healthy volunteers, indicating that the pharmacokinetic profile of Ebastine and its

metabolite does not change significantly in patients with various degrees of hepatic or renal impairment.

 

Pharmacodynamic properties

The studies carried out have demonstrated a clinically and statistically significant effect, initiating after 1 hour and lasting more than 48 hours. After suspending administration in a 5-day treatment with Ebastine, the antihistamine effect was apparent for more than 72 hours. This activity ran parallel to plasma levels of the main active acid metabolite, carebastine. The inhibition of peripheral receptors remained constant after repeated administration. There was no tachyphylaxis. These results suggest that a dose of at least 10 mg of Ebastine causes rapid, intense and lasting inhibition of the peripheral histamine H1 receptors, consistent with a single daily administration. No significant increase in sedation was observed at the recommended dose. These results are in line with those

obtained in double-blind clinical trials: the incidence of sedation is comparable between placebo and Ebastine. The cardiac effects of Ebastine have been examined in clinical trials. No significant cardiac effects were observed in detailed analyses at daily doses of up to 100 mg (ten times the recommended daily dose).

 

Indications

Ebastel is indicated in the symptomatic treatment of allergic processes such as seasonal or perennial allergic rhinitis

associated or not with allergic conjunctivitis (such as runny nose, itchy nose, itchy eyes, tears, sneezing), chronic urticaria and allergic dermatitis.

 

Contraindications

• Known hypersensitivity to the active ingredient or any of the excipients.

• This presentation is not indicated for children under 12 years of age. Oral solution is recommended for this group of

patients. Special warnings and precautions in use Administer Ebastine with caution in patients with known cardiac risk, such as prolonged QT interval, in patients with altered blood potassium levels, concomitant treatment with drugs increasing the QT interval or those inhibiting the CYP3A4 enzyme, such as azole antifungals and macrolide antibiotics. Ebastine should be used with caution in patients with severe hepatic impairment. Since Ebastine reaches its therapeutic effect from 1 to 3 hours after administration, it should not be used in acute emergency allergy situations.

 

Warnings

Fertility, pregnancy and lactation

 

Fertility

There are no fertility data regarding ebastine in humans.

 

Pregnancy

Given that the risk of teratogenicity cannot be entirely excluded with absolute certainty, this medication should not be used

during pregnancy, except when clearly necessary.

 

Breastfeeding

It is not known whether ebastine is excreted in mother’s milk. The high degree of protein binding (> 97%) of ebastine and its

main metabolite, carebastine, would suggest that excretion of the medication in mother’s milk does not occur. As a

precautionary measure this medication should not be used when breastfeeding.

 

Warning concerning excipients

This medication contains lactose. Patients with hereditary intolerance to galactose, Lapp lactase deficiency (a deficiency

observed in some populations in Lapland) or poor glucose or galactose absorption should not take this medication. Effects on ability to drive and use machinery The psychomotor function has been widely studied in humans, with no observed effects. Ebastine does not affect the ability to drive or to use machinery at the recommended therapeutic doses.

However, in sensitive individuals who react unusually to ebastine, knowledge of their individual reactions is recommended before the patient drives or carries out complex activities: drowsiness or dizziness could occur.

 

Children

Use of the oral solution is recommended in children since the pharmaceutical form as tablets is not suitable for administration of doses below 10 mg.

 

Interactions

• The administration of Ebastine in combination with drugs inhibiting enzyme CYP3A4 (ketoconazole, itraconazole or

erythromycin) causes pharmacokinetic and pharmacodynamic interactions. Ebastine plasma levels increase as a result. Caution is recommended when administering Ebastel to those patients in concomitant treatment with ketoconazole, itraconazole or erythromycin.

• Pharmacokinetic interactions have been observed when administering ebastine with rifampicin. These interactions could lead to a decrease in plasma concentrations and to a reduction of the antihistamine effects.

• No interactions have been described between ebastine and theophylline, warfarin, cimetidine, diazepam and alcohol.

• The administration of Ebastine with food does not modify its clinical effect.

• Ebastine could interfere with the results of skin prick tests for allergies, so it is advised not to have them until 5-7 days after

suspension of treatment.

• It could increase the effects of other antihistamines.

 

Incompatibilities None described to date.

 

Posology and administration route

Adults and children above 12 years of age

The usual dose is 1 tablet (10 mg of ebastine) once daily.

 

Children under 12 years of age

The use of the oral solution is recommended in this group of patients.

 

Elderly patients: It is not necessary to adjust the dose in elderly patients.

Renal impairment: It is not necessary to adjust the dose in patients with mild, moderate or severe renal impairment.

Hepatic impairment: It is not necessary to adjust the dose in patients with mild or moderate hepatic impairment. The

maximum recommended daily dose (10 mg/day) should not be exceeded in cases of severe hepatic impairment.

 

Administration route

Oral route. It can be taken with or without food. Take the tablets with a glass of water.

 

Overdose

No clinically significant signs or symptoms were observed with doses of up to 100 mg once daily in studies carried out with high doses. There is no specific antidote for Ebastine. Gastric lavage should be considered, together with monitoring of vital constants, including ECG and symptomatic treatment.

 

Adverse reactions

The following adverse effects have been observed in clinical trials and in post-marketing experience:

Very frequent (they could affect more than 1 in every 10 persons):

- Headache

Frequent (they could affect up to 1 in every 10 persons):

- Drowsiness

- Dry mouth

Rare (they could affect up to 1 in every 1,000 persons):

- Hypersensitivity reactions (like anaphylaxis and angioedema)

- Restlessness, insomnia

- Dizziness, decreased sensation of touch or sensitivity, decreased or altered taste

- Palpitations, tachycardia

- Abdominal pain, vomiting, nausea, digestive problems

- Liver inflammation (hepatitis), cholestasis, anomalies in hepatic function analytic tests (raised transaminases, gamma-GT, alkaline phosphatase and bilirubin)

- Urticaria, rash, dermatitis

- Menstrual irregularities

- Oedema, fatigue

 

Not known (frecuency cannot be estimated from the available data):

- Weight increased

- Increased appetite

 

Consult your doctor or pharmacist if you observe any adverse reaction, even if it is not described in this patient information leaflet.

 

Shelf-life

This medication should not be used after the expiry date shown on the container.

Storage conditions

Do not store above 30°C.

THIS IS A MEDICAMENT

Medicament is a product, which affects your health and its

consumption contrary to instructions is dangerous for you.

Follow strictly the doctor’s prescription, the method of use and

the instructions of the pharmacist who sold the medicament.

- The doctor and the pharmacist are the experts in

medicines, their benefits and risks.

- Do not by yourself interrupt the period of treatment

prescribed.

- Do not repeat the same prescription without consulting

your doctor.

- Keep all medicaments out of reach of children.

Council of Arab Health Ministers,

Union of Arab Pharmacists.

Prescription medication

 

Keep out of the reach and sight of children

 

Manufacturer

Industrias Farmacéuticas Almirall, S.A.

Ctra. Nacional II, Km. 593

08740 Sant Andreu de la Barca

Barcelona (Spain)

Marketing Authorisation Holder

Almirall, S.A. 08022 Barcelona (Spain)

Date of revision of text: 05/2019

Origin: Spain

Laboratories: Almirall S.A.

Distributor: Droguerie Phenicia

Number & Year of Registration: 405464/2000