Ebastel® (ebastine)

Ebastel® contains the active ingredient ebastine, a second-generation antihistamine. It is used to treat seasonal and perennial allergic rhinitis as well as chronic idiopathic urticaria.

Ebastine is converted in the liver into the active metabolite carebastine, which is responsible for the antihistaminic effect. Carebastine has a particularly long half-life of 15–19 hours.

Ebastel® is available as an orally disintegrating tablet and as a conventional film-coated tablet. The orally disintegrating tablet dissolves on the tongue and can be taken without water – convenient when you are on the go.

Ebastine works via its active metabolite carebastine:

Mechanism of action:

• Ebastine is converted to carebastine in the liver by CYP3A4
• Carebastine selectively blocks peripheral H1 histamine receptors
• Inhibits itching, sneezing, nasal discharge, and watery eyes
• Barely crosses the blood-brain barrier

Pharmacokinetics:

• Absorption: Rapid after oral administration
• Active metabolite: Carebastine (long half-life of 15–19 hours)
• Steady state after 3–5 days of regular use
• Food slightly increases absorption

Clinical effect:

• Onset of action: Within 1–3 hours
• Duration of action: 24 hours and longer
• Good efficacy for nasal and ocular symptoms

Ebastine is suitable for:

• Adults and adolescents aged 12 years and older
• Seasonal allergic rhinitis (hay fever)
• Perennial allergic rhinitis
• Chronic idiopathic urticaria

Particularly recommended for:

• Patients who want to take their medication discreetly (orally disintegrating tablet without water)
• When a long-acting antihistamine is desired
• Patients who need to stay active during the day

Not suitable for:

• Children under 12 years of age
• Severe liver impairment
• Hypersensitivity to ebastine

Adults and adolescents aged 12 years and older:

• Standard dose: 10 mg once daily
• If needed: 20 mg once daily (as directed by a doctor)

Available dosage forms:

• Ebastel® 10 mg film-coated tablets
• Ebastel® 20 mg film-coated tablets
• Ebastel® 10 mg orally disintegrating tablets (dissolve on the tongue)
• Ebastel® 20 mg orally disintegrating tablets

Dose adjustment:

• Mild to moderate liver impairment: No adjustment needed
• Severe liver impairment: Contraindicated
• Kidney impairment: No adjustment needed

Film-coated tablets:

• Swallow once daily with a little water
• Regardless of meals (food slightly increases absorption)

Orally disintegrating tablets:

• Place on the tongue, without water
• Disintegrates within a few seconds
• Ideal when on the go or if you have difficulty swallowing

Important notes:

• Always take at the same time of day
• Take regularly during the pollen season
• Do not take more than the recommended dose
• If you miss a dose: Take the next regular dose

Tip: The orally disintegrating tablet is particularly convenient for acute allergy symptoms on the go, as no water is needed.

Ebastine must not be taken in cases of:

• Hypersensitivity to ebastine
• Severe liver impairment
• Known QT prolongation or concomitant QT-prolonging medications

Use with caution in cases of:

• Concomitant use of ketoconazole or itraconazole (CYP3A4 inhibition)
• Mild to moderate liver impairment
• Hypokalemia (low potassium)
• Hypomagnesemia (low magnesium)
• Bradycardia (slow heartbeat)
• History of heart rhythm disorders

Pregnancy and breastfeeding: Insufficient data. During pregnancy, only after a strict benefit-risk assessment. Not recommended during breastfeeding.

Common (1–10%):

• Headache
• Dry mouth
• Drowsiness

Uncommon (0.1–1%):

• Dizziness
• Abdominal pain
• Nausea
• Sleep disturbances
• Sinusitis

Rare:

• QT prolongation (especially at high doses or with CYP3A4 inhibitors)
• Hypersensitivity reactions
• Liver function disorders
• Tachycardia

Important: At the recommended dose of 10–20 mg, ebastine has a good safety profile. At higher doses or in combination with CYP3A4 inhibitors, the risk of QT prolongation increases.

Use with caution with:

• Ketoconazole, itraconazole (strong CYP3A4 inhibitors → increased ebastine levels and QT risk)
• Erythromycin, clarithromycin (moderate CYP3A4 inhibitors → increased levels)
• Other QT-prolonging medications (e.g., certain antiarrhythmics, antipsychotics)
• Grapefruit juice (CYP3A4 inhibition → slight increase in levels)

No relevant interaction with:

• Alcohol (no clinically relevant increase in sedation)
• Food (slight improvement in absorption)
• Diazepam, cimetidine

Note: Ebastine is metabolized via CYP3A4. Caution is required with strong CYP3A4 inhibitors such as ketoconazole and itraconazole. Inform your doctor about all medications you are currently taking.