Medicines
Update of 20/06/2024
KESTINLYO®
ebastine
Forms and presentations
Orally disintegrating lyophilisate at 10 mg: Box of 30, under unit-dose thermoformed blister.Composition
| p lyophilisate | |
| Ebastine (INN)
|
10 mg |
Excipient with known effect: aspartame (1,0 mg).
Indications
Symptomatic treatment of:- seasonal and perennial allergic rhinitis;
- urticaria.
Dosage and administration
DosageFor adults and children over 12 years.
- Seasonal and perennial allergic rhinitis: 10 to 20 mg per day in 1 daily intake, during or outside meals.
- Urticaria: 10 mg per day in 1 daily intake, during or outside meals.
- Special populations:
- It is not necessary to adjust the dose in patients with mild, moderate or severe renal impairment or mild to moderate hepatic impairment. There is no experience with doses above 10 mg in patients with severe hepatic impairment. Therefore, the dose of 10 mg must not be exceeded in patients with severe hepatic impairment. Treatment should be continued until symptoms disappear.
Method of administration:
The ebastine orally disintegrating lyophilisate is placed on the tongue, where it disperses instantly. It can be administered without taking water or another liquid to swallow it.
The lyophilisate must be used immediately after opening the blister.
The blister will be carefully opened with dry hands to remove the lyophilisate from the blister without crushing it.
Contraindications
- Child under 12 years, in the absence of efficacy and safety data.
- History of hypersensitivity to the active substance or to any of the excipients listed in section Composition.
Warnings and precautions
Warnings:
The prescription of ebastine should be cautious in patients with long QT syndrome, with hypokalemia, or receiving a medicine known to prolong the QT interval or to inhibit CYP3A4, such as azole antifungals like ketoconazole and itraconazole or macrolides like erythromycin (see Interactions).
Since there is a pharmacokinetic interaction between antituberculous drugs such as rifampicin (see Interactions), caution is required when co-prescribing ebastine with molecules from this group.
This medicine contains 1 mg of aspartame per freeze-dried tablet.
Aspartame contains a source of phenylalanine. May be harmful for people with phenylketonuria (PKU), a rare genetic disease characterised by the accumulation of phenylalanine that cannot be properly eliminated.
Precautions for useEbastine should be used with caution in patients with severe hepatic impairment (see Posology and Method of administration).
Interactions
Drug interactionsCombinations not recommended :
Pharmacokinetic interactions have been observed when ebastine was given with ketoconazole, or itraconazole and erythromycin. These interactions result in an increase in plasma concentrations of ebastine and, to a lesser extent, of carebastine, which was nevertheless not associated with any significant clinical consequence. However, as a precautionary measure, combination with ketoconazole, itraconazole, erythromycin, clarithromycin, and josamycin should be avoided: increased risk of ventricular rhythm disorders in predisposed subjects (congenital long QT syndrome).
Pharmacokinetic interactions have been observed when ebastine was given with rifampicin. These interactions may lead to lower plasma concentrations of ebastine and reduce the antihistamine effect.
No interaction has been reported between ebastine and theophylline, warfarin, cimetidine, diazepam and alcohol.
Administration of ebastine with food does not modify its clinical effect.
Fertility, pregnancy and breastfeeding
Pregnancy:There is little data on the use of ebastine in pregnant women. Animal toxicity studies do not show direct or indirect harmful effects. As a precaution, it is preferable not to use ebastine during pregnancy.
Breastfeeding:
It is not known whether ebastine is excreted in human milk or not. The high level of protein binding of ebastine (97 %) and its main metabolite, carebastine, suggests that there is no excretion into breast milk. As a precaution, it is preferable not to use ebastine during breastfeeding.
Fertility:There are no fertility data with ebastine in humans.
Driving and using machines
In humans, psychomotor function has been studied extensively and no effect has been found. Ebastine, at the recommended therapeutic doses, does not affect the ability to drive vehicles and use machines. However, in sensitive subjects who react unusually to ebastine, it is advised to know individual reactions before the patient drives or performs complex activities: drowsiness and dizziness may occur (see Undesirable effects ).Adverse effects
In a pooled analysis of controlled clinical trials versus placebo with 5708 patients on ebastine, the most frequently reported adverse effects were dry mouth and drowsiness. Treatment-related adverse effects in clinical trials in children (n = 460) were similar to those observed in adults.
The table below lists the adverse effects reported in clinical trials and since marketing, according to the following convention: very common (≥ 1/10), common (≥ 1/100 and < 1/10), uncommon (≥ 1/1000 and < 1/100), rare (≥ 1/10 000 and < 1/1000), very rare (< 1/10 000), and frequency not known (frequency cannot be estimated from the available data).
| SOC MedDRA | |
| Frequency | Adverse effects |
| Immune system disorders | |
| Rare | Hypersensitivity reactions (such as anaphylaxis and Quincke's oedema) |
| Very rare | Severe allergic reactions |
| Psychiatric disorders | |
| Rare | Nervousness, insomnia |
| Nervous system disorders | |
| Very common | Headache |
| Common | Somnolence |
| Rare | Dizziness, hypoesthesia, dysgeusia |
| Metabolism and nutrition disorders | |
| Frequency not known | Increased appetite |
| Cardiac disorders | |
| Rare | Palpitations, tachycardia |
| Investigations | |
| Frequency not known | Weight gain |
| Gastrointestinal disorders | |
| Common | Dry mouth |
| Rare | Abdominal pain, vomiting, nausea, dyspepsia |
| Hepatobiliary disorders | |
| Rare | Hepatitis, cholestasis, abnormal liver function tests (transaminases, gamma GT, alkaline phosphatase and bilirubin increased) |
| Skin disorders | |
| Rare | Urticaria, skin rash, dermatitis |
| Disorders of the reproductive organs | |
| Rare | Menstrual disorders |
| General disorders and administration site conditions | |
| Rare | Edema, asthenia |
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continuous monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals should report any suspected adverse reaction via the national reporting system: National Agency for the Safety of Medicines and Health Products (ANSM) and the network of Regional Pharmacovigilance Centres. Website: https://signalement.social-sante.gouv.fr.
Overdose
In studies conducted with high doses, no significant clinical signs or symptoms were observed up to 100 mg per day.
Management in case of massive overdose:- No antidote is known to date.
- Gastric evacuation.
- Symptomatic treatment.
- Monitoring of vital functions including ECG monitoring.
Pharmacodynamics
Pharmacotherapeutic class: Systemic H1 antihistamine (ATC code: R06AX22; R: respiratory system, D: dermatology).
Ebastine and its active metabolite, carebastine, are selective antihistamines acting on peripheral H1 receptors, which appear to be devoid of sedative and anticholinergic side effects at the recommended doses.
Pharmacokinetics
Ebastine is rapidly absorbed after oral administration and undergoes a very extensive intestinal and hepatic first-pass effect. It is almost entirely converted into its pharmacologically active acid metabolite, carebastine.
After administration of a single oral dose of 10 mg, peak plasma concentration is reached after 2 to 4 hours, with levels ranging between 80 and 100 ng/ml.
Studies in vitro on human hepatic microsomes shows that ebastine is metabolised mainly to carebastine via the cytochrome CYP3A4.
The half-life of the acid metabolite is between 15 and 19 hours, with urinary excretion of 66%, mainly as the conjugated metabolite. After repeated administration of ebastine at a dose of 10 mg per day as a single intake, steady state is reached in 3 to 5 days, with peak plasma concentrations ranging from 130 to 160 ng/ml.
It has been shown that the pharmacokinetics of ebastine and those of its active metabolite, carebastine, are linear at the recommended therapeutic doses of 10 to 20 mg.
Ebastine and carebastine are strongly bound to plasma proteins, with a binding rate greater than 97 %.
The passage of ebastine and its active metabolite, carebastine, across the blood-brain barrier is very low.
Passage into breast milk has not been studied.
- Elderly subjects:
- The pharmacokinetic parameters do not differ in a statistically significant way from the values recorded in young adults.
- Renal and hepatic insufficiency:
- In patients with mild, moderate or severe renal impairment treated with a daily dose of ebastine of 20 mg, as well as in patients with mild to moderate hepatic impairment treated with a daily dose of ebastine of 20 mg, or in patients with severe hepatic impairment treated with a daily dose of ebastine of 10 mg, the concentrations of ebastine and carebastine reached between day 1er and day 5e of treatment were similar to those reached in healthy volunteers. Consequently, the pharmacokinetic profile of ebastine and its metabolite does not change significantly in patients with varying degrees of renal or hepatic impairment.
- In a single-dose crossover study of ebastine orally disintegrating tablet versus ebastine film-coated tablet, the formulations were shown to be bioequivalent. Water intake after administration of ebastine orally disintegrating tablet had no effect on the fate of ebastine.
Storage conditions
- Shelf life
- 3 years.
No special precautions for storage.
HANDLING/DISPOSAL INSTRUCTIONS
No special requirements.
Prescription, supply and reimbursement
LIST II| Marketing authorisation (AMM) | 3400936759169 (2004, SmPC rev 03.06.2019). |
| Price: | 4,01 euros (30 orally disintegrating tablets). |
| Social Security reimbursement at 30%. Collect. | |
ALMIRALL SAS
3-5, bd Galliéni. 92130 Issy-les-Moulineaux
Tel: 01 46 46 19 20. Fax: 01 46 46 19 66
E-mail: pharmacovigilance.fr@almirall.com
Source: VIDAL · Updated on 10/11/2026. This information does not replace advice from a healthcare professional.