Bilastine Tiefenbacher: Uses, Dosage & Side Effects
Bilastine 10 mg orodispersible tablet – second-generation antihistamine for allergic rhinitis and urticaria
Bilastine Tiefenbacher is a prescription second-generation antihistamine containing bilastine 10 mg in an orodispersible tablet formulation. It is primarily used to relieve symptoms of allergic rhinoconjunctivitis (hay fever) and urticaria (hives) in children aged 6 to 11 years weighing at least 20 kg. Bilastine works by selectively blocking histamine H1 receptors without causing significant sedation, making it suitable for daytime use. The orodispersible tablet dissolves on the tongue and can be taken without water.
Quick Facts
Key Takeaways
- Bilastine Tiefenbacher is a non-sedating antihistamine designed for children aged 6–11 years for relief of allergic rhinitis and urticaria symptoms.
- Must be taken on an empty stomach (at least 1 hour before or 2 hours after food or fruit juice) for optimal absorption.
- The orodispersible tablet dissolves on the tongue without water, making it convenient for paediatric use.
- Bilastine has minimal central nervous system effects and does not typically cause drowsiness at the recommended dose.
- Avoid co-administration with P-glycoprotein inhibitors such as ketoconazole, erythromycin, ciclosporin, ritonavir, and diltiazem, as they can increase bilastine plasma levels.
What Is Bilastine Tiefenbacher and What Is It Used For?
Bilastine Tiefenbacher belongs to the pharmacological class of second-generation (non-sedating) antihistamines. The active substance, bilastine, selectively antagonises peripheral histamine H1 receptors. Histamine is a chemical mediator released by mast cells and basophils during allergic reactions, causing symptoms such as sneezing, nasal congestion, itching, and hives. By blocking the action of histamine at its H1 receptor site, bilastine effectively reduces these allergic symptoms.
The medication is specifically formulated as an orodispersible tablet (ODT), meaning it is designed to dissolve rapidly on the tongue without the need for water. This formulation is particularly advantageous for paediatric patients who may have difficulty swallowing conventional tablets. The 10 mg strength is the approved dose for children aged 6 to 11 years with a body weight of at least 20 kg.
Bilastine Tiefenbacher is indicated for the symptomatic treatment of two main conditions. The first is allergic rhinoconjunctivitis, commonly known as hay fever, which encompasses symptoms such as sneezing, itchy and runny nose, nasal congestion, and itchy, red, watery eyes. These symptoms are triggered by allergens such as pollen (seasonal allergic rhinitis) or dust mites, pet dander, and mould (perennial allergic rhinitis).
The second indication is urticaria, also known as hives. Urticaria is characterised by the sudden appearance of raised, itchy wheals (welts) on the skin, often accompanied by redness and swelling. Bilastine helps reduce the itching and the number and size of wheals. Chronic spontaneous urticaria, where symptoms persist for more than six weeks without an identifiable external trigger, is a common form in which antihistamines serve as first-line therapy.
Bilastine was first authorised in the European Union in 2010 for adults and adolescents, and the paediatric orodispersible formulation has subsequently been approved following clinical trials demonstrating its safety and efficacy in the 6–11 year age group. The European Medicines Agency (EMA) has assessed and approved bilastine-containing products through both centralised and decentralised procedures across EU member states.
What Should You Know Before Taking Bilastine Tiefenbacher?
Contraindications
Bilastine Tiefenbacher must not be used in patients who have a known hypersensitivity (allergy) to bilastine or to any of the other ingredients contained in the tablet. While true allergy to bilastine is rare, patients who have experienced allergic reactions to similar antihistamine medications should exercise particular caution and discuss this with their healthcare provider before starting treatment.
The 10 mg orodispersible formulation is not indicated for children under 6 years of age or those weighing less than 20 kg, as safety and efficacy data in this population are insufficient. Adults and adolescents aged 12 years and older should use the 20 mg adult formulation instead of the 10 mg paediatric dose.
Warnings and Precautions
Patients with moderate to severe renal impairment should use Bilastine Tiefenbacher with caution. Bilastine is primarily eliminated from the body via renal and biliary excretion in its unchanged form. In patients with impaired kidney function, plasma levels of bilastine may be significantly elevated, potentially increasing the risk of side effects. Clinical studies have shown that concomitant use of P-glycoprotein inhibitors (such as ketoconazole, erythromycin, ciclosporin, ritonavir, or diltiazem) in patients with renal impairment could further increase bilastine plasma concentrations to clinically relevant levels.
Although bilastine is classified as non-sedating, some patients may experience drowsiness, particularly at the start of treatment. If somnolence occurs, patients should avoid driving, cycling, or operating machinery until the effects have resolved. Healthcare providers should assess each patient individually, especially if there is a history of sensitivity to sedating effects from other medications.
Bilastine must be taken on an empty stomach – at least 1 hour before or 2 hours after eating food or drinking fruit juice. Food and fruit juice (particularly grapefruit juice) significantly reduce the oral bioavailability of bilastine by up to 30%, which can decrease its therapeutic effectiveness.
Patients with phenylketonuria (PKU) should be informed if the formulation contains aspartame as a sweetener, as aspartame is a source of phenylalanine. Always check the specific product information for a complete list of excipients.
Pregnancy and Breastfeeding
While the 10 mg orodispersible tablet is a paediatric formulation, it is important to note that bilastine should not be used during pregnancy unless clearly necessary, as determined by a healthcare provider. Animal studies have not shown direct or indirect harmful effects on fertility, pregnancy, embryonic or foetal development, or postnatal development. However, no controlled clinical trials have been conducted in pregnant women, and as with all medications, a careful risk-benefit analysis should be performed.
It is not known whether bilastine is excreted in human breast milk. Animal studies have shown excretion in breast milk. Therefore, a decision must be made whether to discontinue breastfeeding or to discontinue bilastine therapy, taking into account the benefit of breastfeeding for the child and the benefit of therapy for the mother. Mothers who are breastfeeding should consult their doctor before taking this medication.
Bilastine has not been shown to affect fertility in preclinical studies. No human fertility data are available, but the pharmacological profile suggests negligible risk to reproductive function at therapeutic doses.
How Does Bilastine Tiefenbacher Interact with Other Drugs?
Bilastine has a unique pharmacokinetic profile among antihistamines because it undergoes minimal hepatic metabolism. It is not significantly metabolised by cytochrome P450 (CYP) enzymes, which are responsible for the metabolism of many other drugs. This means that bilastine has a lower potential for interactions mediated by these enzymes compared to some other antihistamines. However, bilastine is a substrate for the P-glycoprotein (P-gp) and organic anion transporting polypeptide (OATP) transport proteins, and interactions with inhibitors of these transporters are clinically relevant.
The absorption of bilastine in the gastrointestinal tract is mediated in part by P-glycoprotein efflux transporters. Drugs that inhibit P-gp can increase the amount of bilastine absorbed, leading to higher plasma concentrations. This is particularly important in patients with renal impairment, where the combination could result in clinically significant elevations in drug levels.
Major Interactions
| Interacting Drug | Mechanism | Effect | Clinical Advice |
|---|---|---|---|
| Ketoconazole | P-gp and CYP3A4 inhibitor | Increases bilastine AUC by approximately 2-fold | Avoid concomitant use; use alternative antifungal |
| Erythromycin | P-gp inhibitor | Increases bilastine Cmax by approximately 2-fold | Avoid concomitant use; consider azithromycin |
| Ciclosporin | P-gp inhibitor | Significantly increases bilastine exposure | Use with extreme caution; monitor for side effects |
| Ritonavir | Potent P-gp and CYP3A4 inhibitor | May substantially increase bilastine levels | Avoid concomitant use |
Minor Interactions
| Interacting Substance | Mechanism | Effect | Clinical Advice |
|---|---|---|---|
| Diltiazem | Moderate P-gp inhibitor | May modestly increase bilastine levels | Use with caution; monitor for somnolence |
| Grapefruit juice | OATP1A2 inhibitor in GI tract | Decreases bilastine bioavailability by ~30% | Avoid for 2 hours before and after dosing |
| Rifampicin | P-gp inducer | May decrease bilastine plasma levels | May reduce efficacy; consider dose adjustment |
| Alcohol (ethanol) | CNS depressant | No significant pharmacokinetic interaction, but potential additive sedation | Exercise caution with alcohol use |
Clinical interaction studies have confirmed that bilastine 20 mg (the adult dose) does not potentiate the CNS-depressant effects of alcohol or lorazepam as measured by psychomotor performance tests. However, individual variation exists, and patients should be counselled about the possibility of enhanced sedation when combining bilastine with other CNS depressants, particularly at higher doses or in sensitive individuals.
Because bilastine does not undergo significant CYP450 metabolism, it does not interact meaningfully with CYP substrates, inhibitors, or inducers. This is a notable advantage over older antihistamines and some second-generation antihistamines (such as cetirizine and fexofenadine) that may have more complex metabolic profiles. Patients taking multiple medications can generally use bilastine with lower risk of hepatic drug-drug interactions.
What Is the Correct Dosage of Bilastine Tiefenbacher?
The dosage of Bilastine Tiefenbacher should be determined by a qualified healthcare professional based on the patient's age, body weight, and the condition being treated. The orodispersible tablet should be removed from the blister pack with dry hands and immediately placed on the tongue, where it dissolves within seconds. It can then be swallowed with or without water. It is essential that the tablet is taken on an empty stomach, at least 1 hour before or 2 hours after food or fruit juice, to ensure optimal absorption.
Children (6–11 Years)
Recommended Paediatric Dose
Children aged 6 to 11 years weighing at least 20 kg: 10 mg (one orodispersible tablet) once daily.
The duration of treatment depends on the type, duration, and course of the symptoms. For seasonal allergic rhinitis, treatment should continue for the duration of allergen exposure. For perennial allergic rhinitis and chronic urticaria, treatment may be required long-term under medical supervision.
Adults and Adolescents (≥12 Years)
Note on Adult Dosing
Adults and adolescents aged 12 years and older should use the 20 mg bilastine tablet (standard tablet formulation), not the 10 mg orodispersible tablet. The 10 mg orodispersible tablet is specifically designed for paediatric use and provides an insufficient dose for older patients.
Elderly Patients
Elderly Dosing Considerations
While the 10 mg ODT is a paediatric formulation, elderly patients using the adult 20 mg bilastine formulation generally do not require dose adjustment. However, bilastine should be used with caution in elderly patients with moderate to severe renal impairment, as reduced kidney function may lead to increased drug exposure. Renal function should be assessed before initiating therapy in this population.
Renal and Hepatic Impairment
Special Populations
Renal impairment: Bilastine is primarily excreted unchanged via the kidneys and bile. Patients with moderate to severe renal impairment should use bilastine with caution, as plasma levels may be elevated. Concomitant use of P-gp inhibitors in renally impaired patients may further increase bilastine exposure.
Hepatic impairment: Since bilastine is not significantly metabolised by the liver, no dose adjustment is expected to be necessary in patients with hepatic impairment. However, clinical data in this population are limited.
Missed Dose
If a dose is missed, the patient should take it as soon as they remember, provided it is still the same day. If it is almost time for the next scheduled dose, the missed dose should be skipped entirely. Patients should never take a double dose to make up for a forgotten one. Maintaining a consistent daily routine (for example, taking the tablet at the same time each morning on an empty stomach) can help reduce the likelihood of missed doses.
Overdose
In the event of suspected overdose, seek medical attention immediately. Contact your local poison control centre or emergency services. There is no specific antidote for bilastine.
Clinical studies in adults have evaluated bilastine at doses up to 220 mg (11 times the standard adult dose of 20 mg) without observing clinically significant adverse effects beyond those seen at therapeutic doses. In clinical trials at supratherapeutic doses, the most commonly reported effects were dizziness, headache, and somnolence. The QTc interval was not meaningfully prolonged even at very high doses, suggesting a wide therapeutic margin for cardiac safety.
In the event of overdose, standard supportive care measures should be employed, including monitoring of vital signs and symptomatic treatment as appropriate. Gastric lavage or activated charcoal may be considered if the overdose was recent. Due to its high protein binding and large volume of distribution, haemodialysis is unlikely to be effective for removing bilastine from the bloodstream.
What Are the Side Effects of Bilastine Tiefenbacher?
Like all medicines, Bilastine Tiefenbacher can cause side effects, although not everybody gets them. The overall safety profile of bilastine at the 10 mg paediatric dose has been evaluated in clinical trials involving children aged 2 to 11 years with allergic rhinoconjunctivitis or chronic urticaria. In these studies, bilastine demonstrated a favourable safety profile comparable to placebo, with a low incidence of adverse events leading to treatment discontinuation.
The side effects listed below are categorised according to their frequency of occurrence based on clinical trial data and post-marketing surveillance. The frequency categories follow the convention established by the Council for International Organizations of Medical Sciences (CIOMS): very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), and very rare (<1/10,000).
Common
Affects 1 to 10 in every 100 patients
- Headache
- Abdominal pain (stomach ache)
Uncommon
Affects 1 to 10 in every 1,000 patients
- Somnolence (drowsiness)
- Dizziness
- Nausea
- Upper respiratory tract infection
- Fatigue
- Increased appetite
- Irregular heartbeat (palpitations)
- Weight increase
Rare
Affects 1 to 10 in every 10,000 patients
- Tachycardia (fast heart rate)
- Vertigo
- Dyspnoea (difficulty breathing)
- Dry mouth
- Dyspepsia (indigestion)
- Pruritus (itching – paradoxical)
- Herpes labialis (cold sores)
- Anxiety or insomnia
Very Rare / Post-marketing
Affects fewer than 1 in 10,000 patients
- Hypersensitivity reactions (skin rash, urticaria, anaphylaxis)
- QT prolongation (at supratherapeutic doses only)
A key distinguishing feature of bilastine compared with first-generation antihistamines is its minimal effect on the central nervous system. In clinical studies using objective psychomotor testing and electroencephalography, bilastine at the recommended dose did not differ significantly from placebo in terms of sedation or cognitive impairment. This is because bilastine has poor penetration across the blood-brain barrier and shows negligible affinity for muscarinic, serotonergic, and adrenergic receptors.
Post-marketing pharmacovigilance data have confirmed the favourable safety profile observed in clinical trials. No significant new safety signals have been identified since market authorisation. The most frequently reported adverse drug reactions in post-marketing experience remain consistent with those identified during clinical development: headache, somnolence, and dizziness.
Seek urgent medical attention if you experience signs of a severe allergic reaction such as swelling of the face, lips, tongue or throat, difficulty breathing, severe skin rash, or if the child collapses. These are signs of anaphylaxis and require immediate emergency treatment.
Patients and caregivers should report any suspected adverse reactions to their healthcare provider or to the national pharmacovigilance reporting system (such as the Yellow Card scheme in the UK or the EudraVigilance system in the EU). Reporting side effects helps to continuously monitor the safety of medicines after they reach the market.
How Should You Store Bilastine Tiefenbacher?
Proper storage of medication is essential to maintain its efficacy and safety throughout its shelf life. Bilastine Tiefenbacher orodispersible tablets should be stored at a temperature not exceeding 30°C (86°F). There is no requirement for refrigeration. The tablets should be kept in the original blister packaging to protect them from moisture, as orodispersible tablets are particularly sensitive to humidity due to their rapid-dissolving formulation.
The blister should only be opened immediately before taking the tablet. Patients and caregivers should use dry hands when handling the tablet and place it directly on the tongue. If the tablet breaks or crumbles during removal from the blister, a new tablet should be used.
As with all medications, Bilastine Tiefenbacher should be kept out of the reach and sight of children to prevent accidental ingestion. The medicine should not be used after the expiry date printed on the carton and blister pack. The expiry date refers to the last day of that month.
Unused or expired medication should not be disposed of via household waste or flushed down the toilet. Patients should return unused medicines to a pharmacy or use an appropriate medicine take-back programme. Proper disposal of medicines helps to protect the environment and prevents the contamination of water supplies with pharmaceutical compounds.
What Does Bilastine Tiefenbacher Contain?
The active substance in Bilastine Tiefenbacher orodispersible tablets is bilastine. Each tablet contains exactly 10 mg of bilastine. Bilastine has the chemical name 2-[4-(2-(4-(1-(2-ethoxyethyl)-1H-benzimidazol-2-yl)piperidin-1-yl)ethyl)phenyl]-2-methylpropionic acid, and its molecular formula is C28H37N3O3 with a molecular weight of 463.6 g/mol.
In addition to the active ingredient, the tablet contains several excipients (inactive ingredients) that serve specific pharmaceutical functions:
- Mannitol: A sugar alcohol used as a bulk sweetener and filler in orodispersible tablets, providing pleasant taste and enabling rapid disintegration on the tongue.
- Microcrystalline cellulose: A widely used pharmaceutical excipient that serves as a binder and diluent, helping to form the tablet structure.
- Crospovidone: A super-disintegrant that enables the tablet to break apart rapidly upon contact with saliva, facilitating the orodispersible mechanism.
- Magnesium stearate: A lubricant used in the tablet manufacturing process to prevent the tablet material from sticking to machinery.
- Colloidal anhydrous silica: A glidant that improves the flow properties of the powder blend during manufacturing.
- Flavouring agent: Added to improve the taste of the tablet, making it more acceptable for paediatric patients.
Patients or caregivers with known allergies to any excipient should carefully review the full list of ingredients provided in the package leaflet before use. Importantly, bilastine orodispersible tablets do not contain lactose or gluten, making them suitable for patients with lactose intolerance or coeliac disease. If the formulation contains aspartame, patients with phenylketonuria should be informed, as aspartame is metabolised to phenylalanine.
The tablets are typically round, white to off-white, flat-faced with bevelled edges, and may have a characteristic smell from the flavouring agent. Each tablet is individually sealed in an aluminium blister pack to protect against moisture and light degradation.
Frequently Asked Questions About Bilastine Tiefenbacher
Bilastine Tiefenbacher 10 mg orodispersible tablets are used to treat allergic rhinoconjunctivitis (hay fever with sneezing, itchy and runny nose, itchy and watery eyes) and urticaria (hives with itching and wheals) in children aged 6–11 years weighing at least 20 kg. It contains bilastine, a second-generation antihistamine that blocks histamine H1 receptors to relieve allergy symptoms.
The tablet should be placed on the tongue where it dissolves rapidly and can be swallowed without water. It must be taken on an empty stomach, at least 1 hour before or 2 hours after eating food or drinking fruit juice. The recommended dose is one 10 mg tablet once daily. Use dry hands when removing the tablet from the blister pack.
Bilastine is classified as a non-sedating antihistamine. Clinical studies have shown that at the recommended dose, bilastine does not cause significant sedation compared to placebo. However, drowsiness is listed as an uncommon side effect, affecting 1–10 in every 1,000 patients. If drowsiness occurs, avoid activities that require full alertness until the effect resolves.
No. Bilastine should be taken on an empty stomach because food and fruit juice (especially grapefruit juice) significantly reduce its absorption by up to 30%. This can decrease the medication's effectiveness. Always take it at least 1 hour before or 2 hours after food or fruit juice for optimal results.
Bilastine is a second-generation antihistamine that is highly selective for H1 receptors. Unlike first-generation antihistamines (diphenhydramine, chlorphenamine), it does not significantly cross the blood-brain barrier, causing minimal sedation. Compared to other second-generation antihistamines like cetirizine, bilastine shows less sedation potential. Additionally, bilastine is not metabolised by the liver's CYP450 enzymes, which reduces the risk of drug-drug interactions.
The 10 mg orodispersible tablet is specifically formulated for children aged 6–11 years. Adults and adolescents aged 12 years and older should use the 20 mg bilastine tablet (standard formulation). Taking only 10 mg would provide an insufficient dose for older patients and may not adequately control allergy symptoms.
References
This article is based on the following peer-reviewed sources and official medical guidelines:
- European Medicines Agency (EMA). Bilastine – Summary of Product Characteristics (SmPC). European public assessment reports. Available at: www.ema.europa.eu.
- Bachert C, et al. “Bilastine in allergic rhinoconjunctivitis and urticaria.” Clinical and Experimental Allergy. 2014;44(7):977–985. doi:10.1111/cea.12341.
- Church MK, Maurer M. “H1-antihistamines and urticaria: how can we predict the best drug for our patient?” Clinical and Experimental Allergy. 2012;42(10):1423–1429.
- Jauregizar N, et al. “Pharmacokinetic profile of bilastine: a second-generation antihistamine.” Expert Opinion on Drug Metabolism & Toxicology. 2013;9(5):619–627.
- 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.
- World Health Organization. WHO Model List of Essential Medicines – 23rd List (2023). Geneva: WHO; 2023.
- British National Formulary (BNF). Bilastine monograph. National Institute for Health and Care Excellence (NICE). Available at: bnf.nice.org.uk.
- Sadaba B, et al. “Bilastine: a new antihistamine with an optimal benefit-to-risk ratio for safety during driving.” Expert Opinion on Drug Safety. 2013;12(1):89–98.
- Horak F, et al. “The effects of bilastine compared with cetirizine, fexofenadine, and placebo on allergen-induced nasal and ocular symptoms in patients exposed to aeroallergen in the Vienna Challenge Chamber.” Inflammation Research. 2010;59(5):391–398.
- Scaglione F. “Safety profile of bilastine: 2nd generation H1-antihistamines.” European Review for Medical and Pharmacological Sciences. 2012;16(14):1999–2005.
Editorial Team
This article has been written and reviewed by the iMedic Medical Editorial Team, comprising licensed physicians and clinical pharmacologists with expertise in allergy, immunology, and pharmacotherapy.
iMedic Clinical Pharmacology Team – Specialists in drug information, pharmacokinetics, and evidence-based therapeutics.
iMedic Medical Review Board – Independent panel of board-certified physicians who review all content according to EMA, FDA, and WHO guidelines.
All drug information on iMedic is based on approved Summaries of Product Characteristics (SmPC), peer-reviewed clinical trials, and international clinical guidelines. We follow the GRADE evidence framework and maintain complete editorial independence with no pharmaceutical industry funding. Learn more about our editorial standards.