Bilacina (Bilastine)
Second-generation antihistamine for allergic rhinitis and urticaria
Bilacina contains the active ingredient bilastine, a modern, non-sedating second-generation antihistamine used to relieve the symptoms of allergic rhinoconjunctivitis (hay fever) and urticaria (hives). Available as a 10 mg orodispersible tablet, it is designed for convenient use in children aged 6 to 11 years, dissolving directly on the tongue without the need for water. Bilastine is well-tolerated with a favorable safety profile and minimal risk of drowsiness.
Quick Facts
Key Takeaways
- Bilacina contains bilastine, a selective H1 antihistamine that effectively treats allergic rhinitis and urticaria with minimal sedation.
- The 10 mg orodispersible tablet is specifically designed for children aged 6 to 11 years, dissolving on the tongue for easy administration.
- Must be taken on an empty stomach (1 hour before or 2 hours after food) for optimal absorption and effectiveness.
- Clinical trials demonstrate a safety profile comparable to placebo, with headache being the most commonly reported adverse effect.
- Does not significantly cross the blood-brain barrier, resulting in no clinically meaningful impairment of cognitive or psychomotor function.
What Is Bilacina and What Is It Used For?
Bilacina belongs to the class of second-generation antihistamines, which are medications specifically designed to block the effects of histamine at H1 receptors throughout the body. Histamine is a naturally occurring chemical that plays a central role in allergic reactions. When the immune system identifies a harmless substance (such as pollen, dust mites, or animal dander) as a threat, it triggers the release of histamine from mast cells and basophils. This histamine then binds to H1 receptors on various cells, causing the characteristic symptoms of allergic reactions including sneezing, nasal congestion, itching, watery eyes, and skin rashes.
The active ingredient in Bilacina, bilastine, was developed as a highly selective H1 receptor antagonist with several advantages over older antihistamines. Unlike first-generation antihistamines such as diphenhydramine or chlorpheniramine, bilastine does not significantly cross the blood-brain barrier, which means it produces minimal sedation and cognitive impairment. This is a critical advantage for patients who need to maintain alertness during daily activities, including driving and operating machinery.
Bilacina is indicated for the symptomatic treatment of two primary conditions. The first is allergic rhinoconjunctivitis, commonly known as hay fever, which can be seasonal (triggered by pollen) or perennial (triggered by year-round allergens such as dust mites or pet dander). Symptoms include sneezing, nasal congestion, runny nose (rhinorrhea), itchy nose, and itchy or watery eyes. The second indication is urticaria (hives), a condition characterized by itchy, raised, red welts on the skin that can appear anywhere on the body and vary in size from small spots to large areas.
The Bilacina 10 mg orodispersible tablet formulation is specifically designed for pediatric use in children aged 6 to 11 years who weigh at least 20 kg. The orodispersible tablet dissolves rapidly on the tongue without requiring water, making it particularly convenient for children who may have difficulty swallowing conventional tablets. The tablet can be placed directly on the tongue where it disintegrates within seconds, allowing the active ingredient to be swallowed with saliva.
Clinical studies have demonstrated that bilastine provides rapid onset of action, with symptom relief typically beginning within one hour of administration. The duration of effect extends to a full 24 hours, allowing for convenient once-daily dosing. The European Medicines Agency (EMA) has approved bilastine for use in multiple European countries, and it has been included in treatment guidelines by organizations such as the Allergic Rhinitis and its Impact on Asthma (ARIA) working group.
What Should You Know Before Taking Bilacina?
Before starting treatment with Bilacina, it is essential to discuss your complete medical history with your healthcare provider. While bilastine is generally well-tolerated, there are several important considerations that may affect whether this medication is appropriate for you or your child. Understanding these precautions helps ensure safe and effective use of the medicine.
Contraindications
Bilacina should not be used in the following circumstances:
- Known hypersensitivity: Do not take Bilacina if you have previously experienced an allergic reaction to bilastine or any of the other ingredients in the tablet (excipients). Symptoms of hypersensitivity may include rash, swelling of the face or throat, breathing difficulties, or severe skin reactions.
- Children under 6 years: The 10 mg orodispersible tablet formulation is not recommended for children younger than 6 years of age due to insufficient safety and efficacy data in this age group.
- Children weighing less than 20 kg: Even if the child is 6 years or older, this formulation should not be used if the child weighs less than 20 kg, as appropriate dosing cannot be assured.
Warnings and Precautions
Special care should be taken in the following situations:
- Renal impairment: Bilastine is primarily excreted unchanged through the kidneys. In patients with moderate to severe renal impairment (creatinine clearance less than 60 mL/min), plasma concentrations of bilastine may be elevated, potentially increasing the risk of side effects. Your doctor may need to adjust the dose or recommend an alternative treatment.
- Concomitant use with P-glycoprotein inhibitors: Bilastine is a substrate of P-glycoprotein (P-gp), a transporter protein that affects drug absorption. Medications that inhibit P-gp, such as ketoconazole, erythromycin, ciclosporin, ritonavir, and diltiazem, can increase bilastine plasma levels. If you are taking any of these medications, your doctor should be informed.
- Food and fruit juice interactions: Taking Bilacina with food or fruit juice (particularly grapefruit juice) significantly reduces its oral bioavailability. The medication should always be taken on an empty stomach, at least one hour before or two hours after eating food or drinking fruit juice.
- Elderly patients: While no specific dose adjustment is generally required for elderly patients, individual assessment is recommended as this population may have reduced renal function and may be taking multiple medications that could interact with bilastine.
Pregnancy and Breastfeeding
The use of Bilacina during pregnancy should be approached with caution. There are limited clinical data on the use of bilastine in pregnant women. Animal reproduction studies have not shown direct or indirect harmful effects with respect to pregnancy, embryonic or fetal development, parturition, or postnatal development. However, as a precautionary measure, it is preferable to avoid the use of Bilacina during pregnancy unless clearly necessary and prescribed by a healthcare provider.
It is not known whether bilastine or its metabolites are excreted in human breast milk. Studies in animals have shown excretion of bilastine in milk. Therefore, a decision must be made whether to discontinue breastfeeding or to discontinue Bilacina therapy, taking into account the benefit of breastfeeding for the child and the benefit of therapy for the mother. If the medication is deemed essential, the healthcare provider may recommend temporary cessation of breastfeeding during treatment.
Always take Bilacina on an empty stomach. Food and fruit juice can reduce absorption by up to 30%, significantly decreasing the medication's effectiveness. Wait at least 1 hour before eating or 2 hours after meals before taking your dose.
How Does Bilacina Interact with Other Drugs?
Drug interactions can alter how medications work and may increase the risk of side effects. While bilastine has a relatively favorable interaction profile compared to some other antihistamines, there are several important drug interactions that should be considered. Understanding these interactions helps healthcare providers and patients manage medications safely and effectively.
Bilastine is a substrate of the P-glycoprotein (P-gp) efflux transporter but is not significantly metabolized by cytochrome P450 enzymes. This pharmacokinetic profile means that bilastine is less likely to interact with drugs that are metabolized through the CYP450 system. However, drugs that inhibit the P-gp transporter can increase bilastine plasma concentrations by reducing its efflux from intestinal cells back into the gut lumen and by decreasing its renal clearance.
Major Interactions
| Interacting Drug | Effect | Clinical Significance | Recommendation |
|---|---|---|---|
| Ketoconazole | Increases bilastine plasma levels by approximately 2-fold via P-gp inhibition | High | Use with caution; monitor for increased side effects |
| Erythromycin | Increases bilastine AUC by approximately 2-fold via P-gp inhibition | High | Use with caution; consider alternative antibiotic if possible |
| Ciclosporin | Significant increase in bilastine plasma concentrations via P-gp inhibition | High | Avoid concurrent use or use under close medical supervision |
| Ritonavir | Potent P-gp inhibitor; may substantially increase bilastine levels | High | Avoid concurrent use if possible; consult specialist |
Minor Interactions
| Interacting Drug | Effect | Clinical Significance | Recommendation |
|---|---|---|---|
| Diltiazem | Moderate P-gp inhibitor; modest increase in bilastine levels | Moderate | Monitor for side effects; generally safe at standard doses |
| Grapefruit juice | Reduces bilastine bioavailability by approximately 30% via OATP1A2 inhibition | Moderate | Avoid grapefruit juice when taking Bilacina |
| Alcohol | No significant pharmacokinetic interaction at 20 mg dose; no additive sedation demonstrated | Low | Moderate alcohol consumption generally acceptable; exercise caution |
| Lorazepam | No significant additive CNS depression at standard bilastine doses | Low | Standard precautions; monitor for drowsiness |
P-glycoprotein is a protein found in the gut wall, kidneys, and blood-brain barrier that acts as a pump, pushing drugs out of cells. Since bilastine relies on P-gp for its elimination, drugs that block this pump cause bilastine levels to rise. This is why it is important to inform your doctor about all medications, including over-the-counter drugs and herbal supplements.
What Is the Correct Dosage of Bilacina?
Correct dosing is essential for optimal therapeutic benefit and safety. The dose of Bilacina varies depending on the patient's age, weight, and the condition being treated. The orodispersible tablet should be placed on the tongue where it will rapidly disintegrate and can be swallowed with or without water. It is crucial that the medication is taken on an empty stomach to ensure proper absorption.
Adults and Adolescents (12 Years and Older)
Standard Adult Dose
For adults and adolescents aged 12 years and older, the standard recommended dose of bilastine is 20 mg once daily. This dose is typically prescribed as a conventional tablet formulation rather than the 10 mg orodispersible tablet. The dose should be taken at the same time each day, on an empty stomach (at least 1 hour before or 2 hours after food or fruit juice). The 20 mg dose has been extensively studied in clinical trials and provides effective 24-hour symptom control for both allergic rhinoconjunctivitis and urticaria.
Children (6 to 11 Years)
Pediatric Dose (Orodispersible Tablet)
For children aged 6 to 11 years who weigh at least 20 kg, the recommended dose is one 10 mg orodispersible tablet once daily. The tablet should be placed on the tongue immediately after removal from the blister pack. It will disintegrate within seconds and can be swallowed with saliva. No water is needed, although water may be given if preferred. The medication should always be administered on an empty stomach. The duration of treatment should be determined by the prescribing physician based on the type and duration of symptoms.
Elderly Patients
Elderly Dose Considerations
In elderly patients (65 years and older), no specific dose adjustment is generally required based on age alone. However, since renal function naturally declines with age, elderly patients may have higher plasma levels of bilastine due to reduced renal clearance. Healthcare providers should assess renal function before prescribing and may consider monitoring for increased side effects. In patients with moderate to severe renal impairment (estimated glomerular filtration rate less than 60 mL/min), dose reduction or alternative treatment should be considered.
Missed Dose
If you or your child forgets to take a dose of Bilacina, take it as soon as you remember, provided that the next dose is not due within a few hours. If it is almost time for the next scheduled dose, skip the missed dose and continue with the regular dosing schedule. Do not take a double dose to make up for a missed one. Taking two doses close together will not improve symptom control and may increase the risk of side effects.
To help remember to take Bilacina at the same time each day, consider setting an alarm or associating the dose with a daily routine (such as first thing in the morning, at least one hour before breakfast). Consistent timing helps maintain steady drug levels in the body for optimal symptom control.
Overdose
In clinical studies, bilastine doses up to 220 mg (11 times the standard adult dose of 20 mg) were administered to healthy volunteers without serious adverse effects. However, if an overdose is suspected, standard supportive and symptomatic treatment should be provided. There is no specific antidote for bilastine. Contact your local poison control center or emergency medical services if a significant overdose is suspected. Due to the high protein binding of bilastine, hemodialysis is unlikely to be effective in removing the drug.
| Patient Group | Age Range | Dose | Frequency | Notes |
|---|---|---|---|---|
| Children | 6-11 years (≥20 kg) | 10 mg ODT | Once daily | On empty stomach; dissolve on tongue |
| Adolescents | 12-17 years | 20 mg | Once daily | On empty stomach; standard tablet |
| Adults | 18-64 years | 20 mg | Once daily | On empty stomach |
| Elderly | ≥65 years | 20 mg | Once daily | Assess renal function; adjust if impaired |
| Renal impairment | Any age | Individualized | As directed | Consult physician; dose reduction may be needed |
What Are the Side Effects of Bilacina?
Like all medicines, Bilacina can cause side effects, although not everybody experiences them. In clinical trials involving thousands of patients, bilastine demonstrated an excellent safety profile with adverse event rates comparable to placebo. The majority of reported side effects were mild to moderate in intensity and resolved spontaneously without requiring discontinuation of treatment.
Understanding the frequency of side effects can help you identify what to watch for and when to seek medical attention. Side effects are categorized according to internationally standardized frequency conventions used by the European Medicines Agency (EMA) and the World Health Organization (WHO). These categories range from "very common" (affecting more than 1 in 10 patients) to "very rare" (affecting fewer than 1 in 10,000 patients).
It is important to note that bilastine has been specifically designed to minimize central nervous system (CNS) effects. Unlike first-generation antihistamines (such as diphenhydramine), bilastine does not readily cross the blood-brain barrier, which is why sedation and cognitive impairment are significantly less frequent. Multiple studies, including driving performance studies, have confirmed that bilastine at the recommended dose does not impair driving ability to a clinically significant degree.
Uncommon
May affect up to 1 in 100 patients
- Headache
- Somnolence (drowsiness)
- Dizziness
- Abdominal pain (upper)
- Nausea
- Fatigue
Rare
May affect up to 1 in 1,000 patients
- Tachycardia (rapid heartbeat)
- Vertigo
- Dyspnea (shortness of breath)
- Dry mouth
- Dyspepsia (indigestion)
- Pruritus (itching - not allergy-related)
- Herpes labialis (cold sores)
- Increased appetite
- Anxiety
- Insomnia
Very Rare / Post-Marketing Reports
May affect fewer than 1 in 10,000 patients
- Hypersensitivity reactions (anaphylaxis, angioedema, skin rash)
- ECG abnormalities (no clinically significant QTc prolongation observed in studies up to 100 mg)
- Weight increase
- Abnormal liver function tests
Seek emergency medical help if you experience signs of a severe allergic reaction: swelling of the face, lips, tongue, or throat; difficulty breathing or swallowing; severe skin rash or hives; rapid heartbeat with lightheadedness. These reactions are extremely rare but require immediate medical intervention.
In pediatric studies specifically evaluating the 10 mg dose in children aged 2 to 11 years, the adverse event profile was consistent with that observed in adults. Headache and abdominal pain were the most frequently reported events, and the overall incidence was comparable to placebo groups. No new or unexpected safety signals were identified in the pediatric population.
If you experience any side effects, including those not listed above, you should inform your healthcare provider or pharmacist. Reporting side effects helps regulatory agencies continue to monitor the safety of medications. In the European Union, you can report side effects through the national reporting system of your country.
How Should You Store Bilacina?
Proper storage of Bilacina is important to maintain the quality and effectiveness of the medication. Orodispersible tablets are particularly sensitive to moisture, as they are designed to disintegrate rapidly when exposed to moisture on the tongue. Incorrect storage can compromise the structural integrity of the tablets and potentially reduce their effectiveness.
Follow these storage guidelines for Bilacina orodispersible tablets:
- Temperature: Store below 30°C (86°F). Do not freeze. Avoid exposing the medication to extreme temperatures or direct sunlight.
- Moisture protection: Keep the tablets in the original blister packaging until immediately before use. The blister pack provides essential moisture protection for the orodispersible formulation. Do not remove tablets from the blister and store them in pill organizers or other containers.
- Light protection: Store in the original carton to protect from light when not in use.
- Handling: Handle the orodispersible tablets with dry hands. Remove the tablet from the blister pack only immediately before placing it on the tongue.
- Children: Keep the medication in a safe place out of the sight and reach of children. A locked medicine cabinet is recommended.
- Expiry date: Do not use Bilacina after the expiry date stated on the carton and blister after "EXP." The expiry date refers to the last day of that month.
- Disposal: Do not dispose of medicines via wastewater or household waste. Ask your pharmacist about proper disposal methods to help protect the environment.
If a tablet appears discolored, crumbled, or otherwise damaged when removed from the blister, do not use it. Discard the damaged tablet and take a new one from an intact blister. If you notice any changes in the appearance or smell of the tablets, consult your pharmacist before continuing to use the medication.
What Does Bilacina Contain?
Understanding the composition of your medication is important, particularly if you have known allergies or sensitivities to specific pharmaceutical ingredients. The Bilacina 10 mg orodispersible tablet has been formulated using ingredients specifically chosen to enable rapid disintegration on the tongue while maintaining tablet stability during storage.
Active Ingredient
Each orodispersible tablet contains 10 mg of bilastine (also known by its chemical name 2-[4-(2-(4-(1-(2-ethoxyethyl)-1H-benzimidazol-2-yl)piperidin-1-yl)ethyl)phenyl]-2-methylpropionic acid). Bilastine is a white to off-white crystalline powder that is practically insoluble in water. The molecular formula is C28H37N3O3, and its molecular weight is 463.6 g/mol.
Excipients (Inactive Ingredients)
The orodispersible tablet formulation contains excipients that serve various pharmaceutical functions:
- Microcrystalline cellulose: Used as a filler and binder to give the tablet its structural form.
- Croscarmellose sodium: A superdisintegrant that promotes the rapid break-up of the tablet when it comes into contact with moisture on the tongue.
- Colloidal anhydrous silica: A flow agent that ensures uniform distribution of the active ingredient during tablet manufacturing.
- Magnesium stearate: A lubricant used during the tableting process to prevent the tablet from sticking to manufacturing equipment.
- Mannitol: A sugar alcohol used as a sweetener and filler, providing a pleasant taste to the orodispersible formulation.
- Aspartame (E951): An artificial sweetener that provides taste masking. Note: contains a source of phenylalanine, which may be harmful for patients with phenylketonuria (PKU).
- Tutti-frutti flavoring: Provides a pleasant flavor to the orodispersible tablet, improving palatability particularly for pediatric patients.
Bilacina orodispersible tablets contain aspartame, which is a source of phenylalanine. If you or your child has phenylketonuria (PKU), discuss this with your doctor before taking Bilacina, as phenylalanine intake must be carefully managed in individuals with this condition.
Frequently Asked Questions About Bilacina
Bilacina (bilastine) is a second-generation antihistamine that distinguishes itself from other antihistamines in several important ways. Unlike first-generation antihistamines such as diphenhydramine and chlorpheniramine, bilastine does not significantly cross the blood-brain barrier, resulting in minimal sedation. Compared to other second-generation antihistamines like cetirizine, bilastine has shown a lower incidence of somnolence in clinical trials. Unlike fexofenadine, bilastine is not metabolized by CYP3A4, reducing the risk of certain drug interactions. The orodispersible tablet formulation also offers a practical advantage for patients who have difficulty swallowing conventional tablets.
Clinical studies have demonstrated that bilastine at the recommended dose of 20 mg does not significantly impair driving ability. In a standardized on-the-road driving test (the gold standard for assessing the effects of medications on driving performance), bilastine at 20 mg did not show a significant difference from placebo. However, as individual responses to medications can vary, it is advisable to be aware of how Bilacina affects you before driving or operating heavy machinery, especially when first starting the medication.
Bilacina must be taken on an empty stomach because food and fruit juice significantly reduce its absorption. Pharmacokinetic studies have shown that taking bilastine with food reduces its bioavailability (the amount of drug that reaches the bloodstream) by approximately 30%. Grapefruit juice has a similar reducing effect by inhibiting the OATP1A2 transporter responsible for bilastine absorption in the gut. Taking the medication on an empty stomach ensures consistent and optimal drug levels, providing reliable symptom relief throughout the day.
An orodispersible tablet (ODT) is specially designed to disintegrate rapidly when placed on the tongue, typically within seconds. Once the tablet breaks apart, the active ingredient mixes with saliva and is swallowed. The bilastine is then absorbed in the gastrointestinal tract, just as with a conventional swallowed tablet. The ODT formulation does not provide faster absorption compared to a conventional tablet; rather, its advantage lies in convenience and ease of administration, particularly for children and patients who have difficulty swallowing pills. No water is required, making it practical for use anytime and anywhere.
Clinical studies have evaluated bilastine for treatment periods of up to 12 months and have shown a consistent safety profile with no evidence of tolerance (reduced effectiveness over time) or increased adverse effects with prolonged use. For chronic conditions such as chronic spontaneous urticaria, long-term treatment may be necessary. Your doctor will periodically reassess the need for continued treatment and may recommend periodic breaks to evaluate whether symptoms recur. If you have been using Bilacina for an extended period, do not stop the medication abruptly without consulting your physician.
Bilacina may be used in combination with certain other allergy medications, but this should only be done under medical supervision. For example, nasal corticosteroid sprays (such as fluticasone or mometasone) are commonly used alongside oral antihistamines for moderate to severe allergic rhinitis, and this combination is supported by clinical guidelines. However, combining Bilacina with another oral antihistamine is generally not recommended, as it does not provide additional benefit and may increase the risk of side effects. Always inform your doctor about all medications you are taking, including over-the-counter products and supplements.
References
This article is based on the following peer-reviewed sources and authoritative medical references:
- European Medicines Agency (EMA). Bilastine - Summary of Product Characteristics. Available at: www.ema.europa.eu.
- Bachert C, et al. Bilastine in allergic rhinoconjunctivitis and urticaria. Clinical and Translational Allergy. 2012;2:1. doi:10.1186/2045-7022-2-1.
- Church MK, et al. Bilastine: a lifetime companion for the treatment of allergies. Current Medical Research and Opinion. 2020;36(3):445-454. doi:10.1080/03007995.2019.1681134.
- Jauregui I, et al. Bilastine in the treatment of allergic rhinitis and urticaria: a comprehensive review. Expert Opinion on Pharmacotherapy. 2022;23(8):941-955.
- Kawauchi H, et al. Antihistamines for allergic rhinitis treatment from the viewpoint of nonsedative properties. International Journal of Molecular Sciences. 2019;20(1):213. doi:10.3390/ijms20010213.
- Garcia-Gea C, et al. Bilastine, a new antihistamine: no evidence of impairment with single and repeated doses of 20 mg in a standard driving test. Journal of Clinical Psychopharmacology. 2014;34(4):475-481.
- Zuberbier T, et al. The international EAACI/GA2LEN/EuroGuiDerm/APAAACI guideline for the definition, classification, diagnosis, and management of urticaria. Allergy. 2022;77(3):734-766. doi:10.1111/all.15090.
- Bousquet J, et al. Allergic Rhinitis and its Impact on Asthma (ARIA) 2023 revision. Journal of Allergy and Clinical Immunology. 2023;152(5):1141-1163.
- British National Formulary (BNF). Bilastine. National Institute for Health and Care Excellence (NICE). Available at: bnf.nice.org.uk.
- World Health Organization (WHO). WHO Model List of Essential Medicines, 23rd List. 2023. Available at: www.who.int.
Editorial Team
This article has been written and reviewed by the iMedic Medical Editorial Team, comprising licensed specialist physicians with expertise in clinical pharmacology, allergy medicine, and pediatrics.
Written by iMedic's medical editorial team following evidence-based medicine principles. All clinical claims are supported by peer-reviewed literature and current international guidelines.
Independently reviewed by the iMedic Medical Review Board. All dosage information, drug interactions, and contraindications have been verified against current EMA and BNF references.
Content follows the GRADE evidence framework. No pharmaceutical company funding or influence. All information is independent and unbiased. Read our editorial standards.
Published: September 4, 2025. Last medical review: February 3, 2026. This article is updated whenever new evidence or guideline changes warrant revision.