Кестин

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Кестин

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Treatment option: Hives, Rhinitis

Medically reviewed

Marina Burgos

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Кестин

Property Description
Active ingredient Ebastine
Form Oral tablets, liquid/syrup, lyophilisates
Pharmacological class Second-generation H1-antihistamine
Common purpose Relief of allergic symptoms
Origin Synthetic (Piperidine derivative)

Defining the Drug's Identity and Class

Кестин is the specific trade name for the pharmaceutical product containing the active ingredient Ebastine, which is classified as a potent, long-acting, second-generation H1-antihistamine. This classification indicates its suitability for sustained relief from histamine-mediated symptoms.

This medicine is a synthetic compound derived from the piperidine chemical structure. It is characterized as a non-sedating agent. Its distinct profile is due to its high peripheral selectivity, meaning the drug primarily acts upon histamine receptors located outside the central nervous system. This targeted action establishes its description as a non-sedating antihistamine at typical clinical concentrations.

Composition, Formulation, and General Purpose

Кестин is a single-ingredient product designed exclusively for oral administration, available chiefly as film-coated tablets. A key factor for this preparation is the availability of an aqueous syrup/liquid or a rapidly dissolving orally disintegrating lyophilisate form. These variations are specifically designed to accommodate diverse patient groups, notably children and those with swallowing difficulties.

The drug's general purpose is to mitigate the symptoms of common allergic disorders by functioning as a selective H1-receptor antagonist. After ingestion, Ebastine is rapidly converted in the liver to carebastine, its major active metabolite, which is responsible for the sustained antiallergic activity. This mechanism helps manage typical allergy scenarios, such as the persistent sneezing and itching associated with perennial allergic rhinitis.

What side effects are possible with Кестин?

Possible Side Effects and Safety Information

The safety profile of Кестин (Ebastine) is documented through clinical trials and post-marketing surveillance, with adverse reactions classified by frequency and System Organ Class (SOC) in regulatory documents.

Frequency-Classified Adverse Reactions

The following are examples of adverse reactions listed according to their official frequency categories:

  • Very Common (Affects ge 1 in 10 patients): Headache.
  • Common (Affects 1 to 10 in 100 patients): Drowsiness (Somnolence), Dry mouth.
  • Rare (Affects 1 to 10 in 10,000 patients): Reactions affecting the Cardiac System (e.g., Palpitations, Tachycardia) and the Hepatobiliary System (e.g., Abnormal liver function tests, Hepatitis).
  • Not Known (Frequency cannot be estimated): Weight increased and Increased appetite have been reported in the post-marketing setting.

Serious Adverse Reactions and Safety Constraints

Serious Adverse Reactions officially documented in regulatory texts include severe Hypersensitivity reactions, such as Anaphylaxis and Angioedema (swelling of the face or throat). Additionally, signs of severe liver dysfunction, such as Hepatitis, are listed as rare adverse effects.

Population-Specific Safety Notes state that caution is warranted in certain groups. The product is restricted from use in individuals with severe hepatic impairment (severe liver problems). Furthermore, official labeling advises caution in patients with known QTc interval prolongation or hypokalemia, as well as during concomitant use with other medicinal products that may affect cardiac conduction.


Regulatory Safety Summary: The official safety profile is structured to differentiate between common, generally expected reactions like headache and rare, critical reactions affecting the Cardiac and Hepatobiliary Systems. The most significant constraints involve the explicit limitation against use in severe hepatic impairment, serving as a primary safety consideration defined in regulatory documentation.

Overdose and Emergency Response

Overdose and when to seek help

Overdose scope

Documented overdose presentations:

  • Overdose may increase the regulatory-documented risks of sedation (somnolence) and antimuscarinic effects.
  • Other listed manifestations include tachycardia, hypotension, fatigue, and dry mouth.

Physiological systems affected (as stated in label):

  • Central Nervous System (CNS) — effects may necessitate intensive care.
  • Cardiovascular system — severe risk of QT interval prolongation and subsequent cardiac arrhythmias.

Dose-related or exposure-related factors (if applicable):

  • No clinically significant signs or symptoms were observed up to 100 mg once daily in studies.

Emergency-response statements (as written in official documents):

  • No specific antidote is known for this medicinal product.
  • Gastric lavage, activated charcoal, and symptomatic and supportive treatment are the mandated interventions.

When immediate medical help is required (label-derived phrasing only):

  • Contact your doctor immediately or go to the Emergency Department if overdose is suspected.
  • ECG monitoring and monitoring of vital functions must be performed and maintained until full recovery.

Overdose classifications (high-level)

Severity classification (as defined in official documents):

  • Overdose may result in mild to moderate intoxication at high doses.

Regulatory basis (EMA / FDA / etc.):

  • Overdose information is based on official labeling (SmPC).

Resulting overdose structure

Official overdose statements:

  • The primary risk documented in regulatory sources is QT interval prolongation and associated cardiac arrhythmias, mandating ECG monitoring.
  • Manifestations include somnolence, tachycardia, and signs of antimuscarinic effects.
  • The official instruction is to seek immediate medical attention, as no specific antidote is known, and management relies on procedural steps like gastric lavage and symptomatic and supportive treatment.

Connection to the overall overdose profile (2–4 sentences): Regulatory documents define the overdose profile primarily by the documented risk of cardiovascular complications and the central nervous system effects. This risk profile mandates the official requirement to seek immediate medical attention and underlies the non-antidotal, procedural, and intensive monitoring approach required in a hospital setting, including mandatory ECG evaluation.

Therapeutic Uses of Кестин

Кестин (Ebastine) is a medication authorized for managing symptoms associated with various allergic conditions.

Quick Facts

  • Relieves Symptoms of Seasonal Allergic Rhinitis (Hay Fever): Appropriate for addressing effects such as sneezing, runny nose (rhinorrhea), and nasal itching during specific allergy seasons.
  • Relieves Symptoms of Perennial Allergic Rhinitis: Suitable for the management of non-seasonal, year-round allergic nasal symptoms.
  • Helps Manage Chronic Idiopathic Urticaria (Hives): Utilized for the symptomatic relief of skin issues related to chronic hives, including itching and redness (erythema).
  • Assists with Allergic Conjunctivitis: Can be considered for alleviating eye-related allergy symptoms.

This agent is considered for patients seeking symptomatic relief from allergic manifestations affecting the respiratory tract and skin. The therapeutic goal is to help mitigate the discomfort that these conditions may cause, supporting an improved state of well-being.

Eligibility and Restrictions for Use

This section outlines the official eligibility and non-eligibility criteria for Кестин (Ebastine), as defined by government regulatory documents.

Contraindicated and Restricted Populations

Classification Population/Condition Restriction Basis (Official Labeling)
Contraindicated Known hypersensitivity to ebastine or any excipient. Absolute prohibition by regulatory authorities [Source 1.6].
Contraindicated Patients with rare hereditary problems of galactose intolerance (if formulation contains lactose). Prohibition due to excipient content [Source 1.3].
Restricted Use Patients with severe hepatic insufficiency (severe liver impairment). The dose must not exceed 10 mg [Source 1.5, 2.5].
Special Caution Patients with known QTc prolongation or hypokalaemia (low potassium levels). Required due to potential cardiac risk factors [Source 1.4, 2.2].

Age and Physiological Eligibility Status

Official regulatory bodies classify eligibility based on age and physiological state:

  • Approved Ages: The medicine is approved for use in adults and adolescents 12 years of age and older. Use in older adults does not require a dose adjustment [Source 1.1, 2.2].
  • Pediatric Status: Use in children under 12 years of age is officially not established and is therefore prohibited [Source 1.1, 1.4].
  • Renal Function: Patients with any degree of renal impairment (kidney disease) are eligible for standard use; no dose adjustment is required [Source 2.2].
  • Pregnancy and Lactation: Use during pregnancy and breastfeeding is not recommended; regulatory documentation advises avoidance as a precautionary measure due to limited or insufficient human safety data [Source 1.6, 2.5].

What should I know about interactions with other medicines?

Interactions with other medicines and products

The regulatory profile for Кестин (Ebastine) documents specific pharmacokinetic interaction patterns, primarily involving the hepatic CYP3A4 enzyme system.

  • Exposure Increase: Co-administration with strong CYP3A4 inhibitors, such as the macrolide antibiotics ( Erythromycin, Clarithromycin) and azole antifungals ( Ketoconazole, Itraconazole), causes a significant increase in the plasma concentrations of Ebastine and its active metabolite, Carebastine. Clarithromycin and Josamycin are specifically not recommended for co-administration.

  • Exposure Decrease: Concomitant use with the CYP3A4 inducer Rifampicin leads to the reverse effect—a reduction in plasma levels of the drug and its metabolite, which may result in a reduced antihistamine effect.

  • Pharmacodynamic Risk: Caution is formally required when Ebastine is used alongside other medicines known to prolong the QTc interval. This is particularly noted in high-risk patient populations, including those with pre-existing QTc prolongation or hypokalaemia.

  • Food and Substance Effects: Administration with food results in a pharmacokinetic interaction, increasing the plasma exposure ( AUC) of Carebastine by 1.5 - to 2.0 -fold, though this does not alter its clinical effect. No interaction has been reported in clinical studies with alcohol or diazepam.

The medicine is also formally contraindicated for use in patients with severe hepatic insufficiency due to the risk of accumulation.

Mechanism of Action

Кестин (Ebastine) functions as a prodrug which is extensively metabolized in the liver by cytochrome P450 3A4 (CYP3A4) to its principal active metabolite, carebastine. Carebastine acts as a selective inverse agonist/antagonist at the peripheral histamine H1 receptors (H1R), exhibiting minimal penetration of the blood-brain barrier. At the molecular level, carebastine competitively binds to the H1 receptors on target cells, including those in the respiratory tract, skin, and vasculature, stabilizing the receptor in an inactive conformation. This action prevents the endogenous agonist, histamine, from binding and initiating the Galpha q-mediated intracellular signaling cascade. Downstream, this H1 receptor blockade modulates the phospholipase C pathway, leading to a reduced increase in intracellular calcium ion concentration and inhibition of the subsequent activation of transcription factors like NF-kappa B. The overall systemic physiological consequence is the attenuation of H1 R-mediated processes, including capillary permeability, smooth muscle contraction, and the release of other pro-inflammatory mediators from mast cells and basophils.

Dosage and Administration Information

The use of Кестин (Ebastine) is restricted to the oral route, available as film-coated tablets, oral lyophilisates, and an oral solution for pediatric dosing. The medication is administered on a once-daily schedule, which reflects its long-acting pharmacological profile.


Standard Posology and Dosing

For adults and adolescents 12 years and older, the typical starting and maintenance dose is 10 mg taken once daily. In cases of severe symptoms, the dosage may be increased to a maximum of 20 mg once daily. Dosing for children differs by age: children 6 to 11 years are administered 5 mg once daily, while those 2 to 5 years are typically given 2.5 mg once daily via the oral solution.


Administration Guidelines

The medicine offers administration flexibility: it can be taken with or without food, as its clinical effect is not altered by meal timing. Film-coated tablets should be swallowed whole with liquid. In contrast, orodispersible tablets are designed to be placed directly on the tongue to dissolve instantly, and no water is required for consumption. If a dose is missed, the recommendation is to proceed with the next scheduled dose and not take a double dose to compensate for the forgotten one. The treatment may be continued as long as symptoms persist, with clinical experience available for up to one year of use in chronic conditions.


Dosing in Special Populations

No dose adjustment is necessary for patients with any degree of renal impairment or those with mild to moderate hepatic impairment. However, the dose must not exceed 10 mg once daily for patients diagnosed with severe hepatic impairment.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Кестин (Ebastine)

Evidence for use in Seasonal Allergic Rhinitis (SAR)

Research exploring Seasonal Allergic Rhinitis (SAR), commonly known as hay fever, was conducted using numerous short-term, randomized controlled trials (RCTs). These studies often included a placebo or other active comparators (i.e., other treatments) as a study arm. The research was evaluated in adult and adolescent populations experiencing conditions characterized by fluctuating or episodic manifestations.

Studies monitored outcomes related to physical discomfort and outcomes capturing phases of heightened symptom activity, which included the intensity of sneezing, nasal itching, and nasal discharge. The research provides insight into short-term changes, but the results apply only to the populations studied. Findings were mixed in some studies when researchers compared the standard dose against a higher dose on outcomes related to nasal congestion.


Evidence for use in Chronic Hives (Chronic Idiopathic Urticaria)

For Chronic Hives (Chronic Spontaneous Urticaria or CSU), research was studied for conditions characterized by fluctuating or episodic manifestations. Studies examined how patient-reported outcomes describing perceived discomfort (severity of itching) and the assessment of the number and size of wheals evolved over the study period. Studies monitored total scores that reflect outcomes related to daily functioning or activity level in adult populations.

Studies report how symptoms evolved in the observed populations, and research highlights changes measured during the study period. Research explored scenarios where a higher-than-standard daily amount was observed in some studies. However, this data are still emerging and predominantly based on observational studies, meaning certainty remains low compared to controlled trials.


Research Gaps and Areas of Uncertainty

The research provides context but not individual predictions. A primary research limitation is the general lack of extensive data for long-term outcomes across all indications; evidence is limited regarding continuous use for several years in controlled trial settings. As is common in clinical research, study findings describe group patterns, and research does not determine whether an individual will respond similarly, especially when symptoms may vary in intensity or presentation.

Key Studies & References

  1. KESTINE 20 mg Oral Lyophilisate - Summary of Product Characteristics (SPC) - HPRA

Frequently Asked Questions (FAQ)

Common questions about Кестин (FAQ)


Q: What is the main difference between Кестин and other allergy pills?

Кестин is classified as a second-generation H1-antihistamine. Official product information describes its minimal penetration of the blood-brain barrier, which is generally associated with a low incidence of central nervous system side effects like sedation or drowsiness at recommended therapeutic doses.


Q: How long after taking Кестин does it start to relieve symptoms?

Official information indicates that symptom relief is typically observed within 1 to 3 hours following administration. This rapid onset contributes to its use for the relief of allergic symptoms.


Q: How quickly does the effect of Кестин wear off?

Кестин is considered a long-acting medication. The active substance is converted into a metabolite that has a prolonged half-life, providing sustained antihistaminic activity. This pharmacological profile supports the standard once-daily dosing schedule.


Q: Are there any specific foods or drinks that should be avoided when using Кестин?

Regulatory documents do not specifically prohibit certain foods or non-alcoholic drinks. Official labeling states that administration with food results in increased exposure to the active metabolite in the bloodstream. However, this change is noted as not altering the clinical effectiveness of the drug.


Q: Can you use Кестин to treat a common cold, or is it only for allergies?

The drug is indicated for the relief of symptoms associated with specific allergic conditions, such as seasonal and perennial allergic rhinitis (hay fever) and chronic hives (urticaria). It is not listed in official indications for the treatment of the common cold.


Q: What are the main conditions that would make someone ineligible to use Кестин?

Regulatory documents state it is contraindicated for individuals with a known hypersensitivity (severe allergic reaction) to the drug or any of its components. It is also contraindicated for patients with rare hereditary problems of galactose intolerance if the formulation contains lactose.


Q: Why is Кестин sometimes prescribed for hives (urticaria)?

The drug is approved for chronic hives because its active metabolite acts as an H1 receptor antagonist. This action helps to attenuate the histamine-mediated effects, such as the itching and wheals associated with the condition.


Q: Are there any known issues with Кестин and driving or operating machinery?

Official documents advise that caution is warranted, as side effects such as drowsiness, dizziness, or fatigue may occur. These potential effects could impair the ability to perform skilled tasks such as driving or operating machinery.


Q: What happens if Кестин is taken with grapefruit juice?

The active ingredient is metabolized by the CYP3 A4 enzyme system. Due to the potential for inhibition of this enzyme, co-administration with such substances is associated with increased plasma concentrations of the active metabolite. Regulatory information explicitly warns against co-administration with other strong CYP3 A4 inhibitors.


Q: Is there a maximum time that Кестин is approved to be used?

Treatment duration is determined based on the persistence of symptoms. Official prescribing information notes that clinical experience has been documented for continuous use up to one year in chronic conditions. This information is intended to provide context on duration.


Q: Are there any known studies comparing Кестин to placebo?

Yes, research evidence supporting the use of this medication includes randomized controlled trials (RCTs). Official summaries confirm that the drug was compared against a placebo to assess efficacy and safety profiles for indications like allergic rhinitis and chronic hives.


Q: Why does Кестин have a specific mention about its use with certain antifungal medications?

This specific caution exists because certain antifungal medications (like ketoconazole and itraconazole) are strong inhibitors of the CYP3 A4 enzyme system. Co-administering them can slow down the metabolism of Кестин, leading to a significant increase in the plasma concentration of its active metabolite.


Q: Are headaches a common side effect of Кестин?

Headache is listed as a very common adverse reaction in official documentation. This means it is one of the most frequently reported side effects and may affect more than 1 in 10 patients.


Q: Can Кестин be taken on an empty stomach?

Yes, administration guidelines confirm that the medicine can be taken with or without food. This allows for flexibility when scheduling the once-daily dose.


Q: Does Кестин have any documented effects on weight changes?

Post-marketing surveillance has reported instances of increased appetite and weight gain. Official documents classify the frequency of these particular effects as 'not known,' as it cannot be estimated from the available data.


Q: Is the effect of Кестин immediate, or does it build up over a few days?

The onset of symptom relief is generally rapid, typically observed within 1 to 3 hours. However, the level of the active metabolite that provides relief reaches its steady-state concentration after approximately three days of once-daily use.

How should Кестин be stored and disposed of?

Storage and Disposal of Kestine (Ebastine)

Kestine must be stored according to regulatory requirements to maintain its stability and safety. The medicine must be stored at a temperature not higher than 25 C (77 F). Always keep this medicine out of the sight and reach of children.

Handling and Stability

For the orodispersible (rapidly dissolving) tablet form, the blister must be opened carefully, and the tablet should be taken immediately after removal to protect it from moisture. Packaging rules require keeping the blister in the outer carton.

Disposal

Official disposal instructions prohibit discarding the medicine via wastewater or household waste. Consult your pharmacist for advice on how to safely dispose of unused or expired Kestine, as these measures help protect the environment.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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