Bilastine Polpharma: Uses, Dosage & Side Effects
Second-generation antihistamine for allergic rhinitis and urticaria
Quick Facts About Bilastine Polpharma
Key Takeaways About Bilastine Polpharma
- Non-sedating antihistamine: Bilastine does not significantly cross the blood-brain barrier, resulting in minimal drowsiness compared to older antihistamines
- Must be taken on an empty stomach: Food and fruit juice (especially grapefruit) significantly reduce absorption by up to 30-40%, decreasing effectiveness
- Once-daily dosing: A single 20 mg tablet provides 24-hour symptom relief for allergic rhinitis and urticaria
- Rapid onset of action: Symptom relief typically begins within 1 hour of taking the tablet, with peak effect at approximately 1.3 hours
- Minimal liver metabolism: Bilastine is excreted largely unchanged, resulting in fewer drug interactions compared to many other antihistamines
What Is Bilastine Polpharma and What Is It Used For?
Bilastine Polpharma contains the active substance bilastine, a second-generation antihistamine that selectively blocks histamine H1 receptors. It is prescribed for the symptomatic treatment of allergic rhinoconjunctivitis (hay fever) and urticaria (hives) in adults and adolescents aged 12 years and older.
Bilastine belongs to the pharmacological class of second-generation (non-sedating) antihistamines. When the body encounters an allergen such as pollen, dust mites, pet dander, or mold spores, the immune system releases histamine from mast cells and basophils. This histamine binds to H1 receptors in various tissues, triggering the characteristic symptoms of an allergic reaction: sneezing, nasal congestion, runny nose, itchy and watery eyes, and skin reactions such as hives and itching.
Bilastine works by competitively binding to peripheral H1 receptors, preventing histamine from activating these receptors. Unlike first-generation antihistamines such as diphenhydramine or chlorphenamine, bilastine is designed to have minimal ability to cross the blood-brain barrier at therapeutic doses. This means it provides effective symptom relief without the significant sedation, cognitive impairment, and anticholinergic side effects commonly associated with older antihistamines.
The European Medicines Agency (EMA) approved bilastine in 2010, and it has since been authorized in numerous countries worldwide. It is marketed under various brand names, with Bilastine Polpharma being one of the generic formulations manufactured by Polpharma, a major European pharmaceutical company headquartered in Poland.
Approved Indications
Bilastine Polpharma 20 mg tablets are indicated for the following conditions:
- Allergic rhinoconjunctivitis (seasonal and perennial): Relief of nasal symptoms (sneezing, rhinorrhea, nasal itching, and congestion) and ocular symptoms (itching, tearing, redness) associated with allergies triggered by pollen, dust mites, mold, or animal dander
- Urticaria (hives): Relief of pruritus (itching) and wheals associated with chronic spontaneous urticaria or other forms of urticaria in adults and adolescents
Clinical studies have demonstrated that bilastine 20 mg is effective in reducing the Total Symptom Score (TSS) in patients with seasonal allergic rhinitis, with efficacy comparable to cetirizine 10 mg and desloratadine 5 mg. In chronic spontaneous urticaria, bilastine has been shown to significantly reduce urticaria activity scores and improve quality of life.
Bilastine has a bioavailability of approximately 61% when taken on an empty stomach. It reaches peak plasma concentrations (Cmax) approximately 1.3 hours after oral administration. The elimination half-life is approximately 14.5 hours, supporting once-daily dosing. Bilastine is not significantly metabolized by cytochrome P450 enzymes and is excreted primarily unchanged in feces (approximately 67%) and urine (approximately 33%).
What Should You Know Before Taking Bilastine Polpharma?
Before starting bilastine, inform your doctor about all other medications you take, any kidney problems, pregnancy or breastfeeding status, and any known allergies. The most important practical consideration is that bilastine must be taken on an empty stomach for proper absorption.
Contraindications
Bilastine Polpharma should not be taken by individuals who have a known hypersensitivity (allergy) to bilastine or to any of the excipients listed in the tablet formulation. If you have experienced an allergic reaction to bilastine in the past, you should not take this medication again. Signs of a hypersensitivity reaction include skin rash, swelling of the face, lips, tongue, or throat, and difficulty breathing.
While bilastine itself does not have absolute contraindications beyond hypersensitivity, certain clinical situations require careful consideration. Patients with severe renal impairment (significantly reduced kidney function) should use bilastine with caution, as the drug is partially eliminated by the kidneys. In these patients, co-administration with P-glycoprotein inhibitors (such as ketoconazole or erythromycin) could lead to increased plasma levels of bilastine.
Warnings and Precautions
Several important precautions should be observed when taking bilastine:
- Empty stomach requirement: Bilastine must be taken at least 1 hour before or 2 hours after food or fruit juice. Food reduces the oral bioavailability of bilastine by approximately 30%, and grapefruit juice reduces it by approximately 30% as well, likely through inhibition of intestinal OATP1A2 transporter. This is a critical instruction that differs from many other antihistamines and must be followed for the drug to work properly.
- Renal impairment: Patients with moderate to severe kidney disease should discuss their condition with their physician, as bilastine elimination may be altered. Dose adjustments may be necessary in combination with P-glycoprotein inhibitors.
- Driving and operating machinery: While bilastine is classified as a non-sedating antihistamine, some patients may experience somnolence or dizziness. Until you know how bilastine affects you individually, exercise caution when driving or operating machinery, particularly during the first few days of treatment.
- Alcohol: Although bilastine at the recommended dose of 20 mg has not been shown to potentiate the effects of alcohol in controlled studies, combining alcohol with any antihistamine should be approached with caution.
- Elderly patients: No dose adjustment is generally required for elderly patients. However, clinical experience in patients over 65 years of age is limited compared to younger adults.
Pregnancy and Breastfeeding
The safety of bilastine during pregnancy has not been established in large-scale human studies. Animal studies have not shown direct harmful effects on embryonic or fetal development at therapeutic doses, but higher doses in animal studies were associated with reduced fetal body weight. As a precaution, bilastine is generally not recommended during pregnancy unless the potential benefit to the mother outweighs the potential risk to the fetus. If you are pregnant, planning to become pregnant, or suspect you may be pregnant, consult your healthcare provider before taking bilastine.
It is not known whether bilastine is excreted in human breast milk. In animal studies, bilastine was detected in breast milk. Therefore, a decision must be made whether to discontinue breastfeeding or discontinue bilastine treatment, taking into account the benefit of breastfeeding for the child and the benefit of therapy for the mother. Consult your physician for personalized guidance.
Do not exceed the recommended dose of 20 mg once daily. Higher doses do not provide additional therapeutic benefit but may increase the risk of side effects. If your symptoms are not adequately controlled, consult your physician rather than increasing the dose on your own.
How Does Bilastine Polpharma Interact with Other Drugs?
Bilastine interacts primarily through the P-glycoprotein (P-gp) and OATP1A2 transporter systems rather than cytochrome P450 enzymes. Key interactions include ketoconazole, erythromycin, diltiazem, ciclosporin, and grapefruit juice, all of which can increase bilastine plasma levels.
One of the pharmacological advantages of bilastine is its relatively limited potential for drug interactions compared to many other antihistamines. Bilastine is not significantly metabolized by the cytochrome P450 (CYP) enzyme system, which is responsible for the metabolism of a large proportion of drugs. Instead, bilastine is a substrate for the efflux transporter P-glycoprotein (P-gp) and the uptake transporter OATP1A2. This means that interactions primarily occur with drugs that inhibit these transporters.
When P-glycoprotein is inhibited, less bilastine is pumped out of intestinal cells back into the gut lumen, resulting in increased absorption and higher plasma levels. Similarly, inhibition of OATP1A2 in the gut (e.g., by grapefruit juice) can paradoxically reduce bilastine absorption because OATP1A2 facilitates the uptake of bilastine from the gut lumen into enterocytes.
Major Interactions
| Drug | Type | Effect | Clinical Advice |
|---|---|---|---|
| Ketoconazole | P-gp inhibitor | Increases bilastine AUC by approximately 2-fold and Cmax by approximately 2-fold | Use with caution; monitor for increased sedation or side effects |
| Erythromycin | P-gp inhibitor | Increases bilastine AUC by approximately 2-fold | Use with caution; consider alternative antibiotic if possible |
| Ciclosporin | P-gp inhibitor | May significantly increase bilastine plasma levels | Avoid combination or use under close medical supervision |
| Ritonavir | P-gp inhibitor | May significantly increase bilastine plasma levels | Avoid combination if possible; consult prescriber |
Minor Interactions
| Substance | Type | Effect | Clinical Advice |
|---|---|---|---|
| Diltiazem | P-gp inhibitor | Increases bilastine Cmax by approximately 50% | Generally manageable; monitor for side effects |
| Grapefruit juice | OATP1A2 inhibitor | Decreases bilastine bioavailability by approximately 30% | Avoid grapefruit juice; take with water only |
| Food | Absorption modifier | Reduces bilastine AUC by approximately 30% | Take 1 hour before or 2 hours after meals |
| Alcohol | CNS depressant | No significant pharmacokinetic interaction at 20 mg dose | Exercise general caution with alcohol; no specific prohibition |
It is important to note that bilastine does not inhibit or induce CYP enzymes (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4) at therapeutic concentrations. This means it is unlikely to affect the metabolism of other drugs that are processed by these enzymes, which is a significant advantage for patients taking multiple medications.
Always inform your healthcare provider about all prescription and over-the-counter medications, herbal supplements, and vitamins you are taking. While bilastine has relatively few drug interactions compared to other antihistamines, individual circumstances may require careful evaluation, particularly if you are taking multiple medications that affect P-glycoprotein.
What Is the Correct Dosage of Bilastine Polpharma?
The standard dose for adults and adolescents (12 years and older) is one 20 mg tablet once daily, taken on an empty stomach. The tablet should be swallowed whole with water, at least 1 hour before or 2 hours after food or fruit juice.
Adults
Standard Adult Dose
20 mg once daily (one tablet), taken orally on an empty stomach with a glass of water. The dose remains the same for both allergic rhinoconjunctivitis and urticaria. Treatment duration depends on the underlying condition: seasonal allergic rhinitis treatment may be limited to the pollen season, while chronic urticaria may require longer-term therapy as directed by a physician.
The recommended dose of 20 mg once daily has been established through dose-ranging studies that evaluated doses of 2.5 mg, 10 mg, 20 mg, 40 mg, and 80 mg. The 20 mg dose was identified as the optimal balance between efficacy and tolerability. Higher doses did not provide clinically meaningful additional benefit in controlled studies. Consistent daily use is recommended for chronic conditions, although bilastine can also be used as needed for intermittent symptoms.
Adolescents (12 Years and Older)
Adolescent Dose (12+ years)
20 mg once daily (same as adult dose). No dose adjustment is required for adolescents aged 12 years and older. The same empty-stomach instructions apply. Bilastine Polpharma 20 mg tablets are the appropriate formulation for this age group.
Children (6 to 11 Years)
Pediatric Dose (6-11 years)
10 mg once daily is the recommended dose for children aged 6 to 11 years with a body weight of at least 20 kg. However, the Bilastine Polpharma 20 mg tablet is not the appropriate formulation for this age group. An age-appropriate formulation, such as a 10 mg orodispersible tablet or oral solution, should be used. Consult a healthcare provider for guidance on the correct formulation. Bilastine is not recommended for children under 6 years due to insufficient safety and efficacy data.
Elderly Patients
Elderly Dose (65+ years)
20 mg once daily (no dose adjustment required). Pharmacokinetic studies have not shown clinically significant differences in bilastine exposure between elderly and younger adult patients. However, clinical experience in patients over 65 years is more limited, and individual monitoring is advisable, particularly in patients with multiple comorbidities or reduced renal function.
Patients with Renal Impairment
Renal Impairment
No dose adjustment is typically required for patients with mild to moderate renal impairment. For patients with severe renal impairment, caution is advised, especially when co-administered with P-glycoprotein inhibitors, as this may result in elevated bilastine plasma concentrations. Consult a nephrologist or clinical pharmacologist for individualized dosing advice.
Patients with Hepatic Impairment
Hepatic Impairment
Since bilastine is not significantly metabolized by the liver, no dose adjustment is expected to be necessary for patients with hepatic impairment. However, specific studies in patients with severe liver disease have not been conducted. Use with caution in severe hepatic impairment and consult your physician.
Missed Dose
If you forget to take a dose of bilastine, take it as soon as you remember, provided it is still within a reasonable timeframe (e.g., within 12 hours of the usual dose time). If it is close to the time for your next scheduled dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a forgotten dose. Setting a daily reminder can help ensure consistent adherence to the dosing schedule.
Overdose
In clinical studies, single doses of up to 220 mg (11 times the recommended dose) and repeated doses of up to 200 mg daily for 7 days were administered without serious adverse effects. The most commonly reported symptoms at supratherapeutic doses were similar to those at the recommended dose, including headache, somnolence, and dizziness, though at slightly higher frequency.
If accidental overdose occurs, symptomatic and supportive treatment is recommended. There is no specific antidote for bilastine. Due to its pharmacokinetic properties (high protein binding, large volume of distribution), hemodialysis is unlikely to be effective for drug removal. If you suspect an overdose, contact your local poison control center or seek immediate medical attention.
Contact your local poison control center or emergency department immediately. Bring the medicine package with you so that medical staff can identify the exact medication and dose taken.
What Are the Side Effects of Bilastine Polpharma?
Bilastine is generally very well tolerated. The most commonly reported side effects are headache and somnolence (drowsiness), each occurring in approximately 1-3% of patients. In clinical trials, the overall side effect profile of bilastine 20 mg was similar to placebo.
Like all medicines, bilastine can cause side effects, although not everybody experiences them. Clinical trials involving over 4,800 patients treated with bilastine demonstrated an excellent safety profile. The incidence of adverse events at the recommended 20 mg dose was comparable to placebo, making bilastine one of the best-tolerated antihistamines available.
The side effects listed below are categorized by frequency according to internationally standardized conventions: very common (affects more than 1 in 10 patients), common (affects 1 in 10 to 1 in 100 patients), uncommon (affects 1 in 100 to 1 in 1,000 patients), and rare (affects fewer than 1 in 1,000 patients).
Common (1/100 to 1/10)
- Headache
- Somnolence (drowsiness)
Uncommon (1/1,000 to 1/100)
- Dizziness
- Fatigue
- Dry mouth
- Abdominal pain (upper)
- Nausea
- Nasal dryness
- Pharyngitis (sore throat)
- Insomnia
- Anxiety
Rare (<1/1,000)
- Tachycardia (rapid heartbeat)
- Vertigo
- ECG changes (QTc prolongation at supratherapeutic doses)
- Increased appetite
- Weight gain
- Skin rash
- Pruritus (itching, unrelated to underlying condition)
Importantly, clinical studies specifically designed to assess the sedation potential of bilastine have consistently shown that bilastine 20 mg does not significantly differ from placebo in objective measures of psychomotor performance, including the Wechsler Digit Symbol Substitution Test (DSST), the Vienna Test System driving simulation, and positron emission tomography (PET) studies measuring brain H1 receptor occupancy. At the 20 mg dose, brain H1 receptor occupancy was approximately 0%, indicating truly non-sedating properties.
In contrast to some other second-generation antihistamines, bilastine at the recommended dose has not been associated with clinically significant QTc prolongation. Thorough QT/QTc studies at supratherapeutic doses (up to 200 mg, i.e., 10 times the recommended dose) showed a mild, dose-dependent increase in QTc interval, but no cases of torsades de pointes or other serious cardiac arrhythmias have been reported.
Although very rare, allergic reactions to bilastine can occur. Seek immediate medical help if you experience signs of a severe allergic reaction (anaphylaxis), including swelling of the face, lips, tongue, or throat; difficulty breathing or swallowing; severe dizziness; or a widespread skin rash with itching. These reactions require emergency treatment.
If you experience any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in the patient information leaflet. You can also report side effects directly to your national medicines regulatory authority. By reporting side effects, you help provide more information on the safety of this medicine.
How Should You Store Bilastine Polpharma?
Store Bilastine Polpharma at room temperature below 25°C (77°F) in the original packaging to protect from moisture. Keep out of the sight and reach of children. Do not use after the expiry date printed on the packaging.
Proper storage of medications is essential to ensure their effectiveness and safety throughout the shelf life. Bilastine Polpharma tablets should be stored under the following conditions:
- Temperature: Store below 25°C (77°F). Do not freeze. Avoid exposure to excessive heat.
- Moisture protection: Keep tablets in the original blister packaging or container until you are ready to take them. Do not transfer tablets to pill organizers for extended periods if the environment is humid.
- Light protection: Store in the original packaging to protect from light.
- Child safety: Keep out of the sight and reach of children. Use child-resistant packaging where available.
- Expiry date: Do not use Bilastine Polpharma after the expiry date (EXP) printed on the carton and blister. The expiry date refers to the last day of that month.
Do not dispose of medications via wastewater or household waste. Ask your pharmacist how to dispose of medicines you no longer use. Proper disposal helps to protect the environment and prevent accidental ingestion by children or pets.
If the tablets appear discolored, crumbled, or have an unusual smell, do not take them. Return them to your pharmacy for proper disposal and obtain a fresh supply.
What Does Bilastine Polpharma Contain?
Each Bilastine Polpharma tablet contains 20 mg of the active substance bilastine. The tablets also contain standard pharmaceutical excipients required for manufacturing and stability.
Active Ingredient
Each film-coated tablet contains 20 mg bilastine as the active substance. Bilastine (chemical name: 2-[4-(2-(4-(1-(2-ethoxyethyl)-1H-benzimidazol-2-yl)piperidin-1-yl)ethyl)phenyl]-2-methylpropionic acid) is a piperidine derivative with a molecular weight of 463.6 g/mol. It is a white to off-white crystalline powder that is practically insoluble in water at neutral pH.
Excipients (Inactive Ingredients)
The inactive ingredients in Bilastine Polpharma 20 mg tablets typically include:
- Microcrystalline cellulose: Used as a filler and binder to give the tablet its structure
- Sodium starch glycolate: A disintegrant that helps the tablet break apart in the gastrointestinal tract for proper absorption
- Colloidal anhydrous silica: A glidant that improves powder flow during manufacturing
- Magnesium stearate: A lubricant that prevents the tablet from sticking to the manufacturing equipment
- Hypromellose: Used in the film coating of the tablet
- Titanium dioxide (E171): Used as a whitening agent in the film coating
- Macrogol/polyethylene glycol: Used as a plasticizer in the film coating
If you have a known allergy or intolerance to any excipient, review the full list on the product packaging or patient information leaflet before taking the medication. Patients with rare hereditary galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption should consult their prescriber regarding the suitability of this formulation, as some versions may contain lactose.
Appearance
Bilastine Polpharma 20 mg tablets are typically white to off-white, round or oval-shaped, film-coated tablets. They may be plain or have a score line for identification purposes (the score line is not intended for dividing the tablet). The tablets are supplied in blister packs, typically containing 10, 20, 30, or 50 tablets per box.
Frequently Asked Questions About Bilastine Polpharma
Bilastine Polpharma 20 mg tablets are used to relieve symptoms of allergic rhinoconjunctivitis (hay fever), including sneezing, runny nose, nasal itching, congestion, and itchy or watery eyes. It is also used to treat urticaria (hives), relieving itchy skin rashes and wheals. Bilastine is a second-generation antihistamine that works by blocking histamine H1 receptors, preventing the allergic cascade that causes these symptoms.
Bilastine is classified as a non-sedating antihistamine. At the recommended 20 mg dose, PET studies have shown approximately 0% brain H1 receptor occupancy, meaning it does not significantly enter the brain. Clinical studies confirm that bilastine does not impair psychomotor performance more than placebo. However, somnolence has been reported in approximately 1-3% of patients, so you should assess your individual response before driving.
No, bilastine must be taken on an empty stomach. Take it at least 1 hour before or 2 hours after eating food or drinking fruit juice. Food reduces bilastine absorption by approximately 30%, and grapefruit juice has a similar effect through OATP1A2 transporter inhibition. Swallow the tablet with a glass of plain water for optimal absorption.
Bilastine Polpharma 20 mg tablets are approved for adults and adolescents aged 12 years and older. For children aged 6 to 11 years, a lower dose of 10 mg is used, requiring an age-appropriate formulation such as orodispersible tablets or oral solution. Bilastine is not recommended for children under 6 years of age due to insufficient data. Always consult a pediatrician before giving this medication to children.
All three are second-generation antihistamines, but they differ in key ways. Bilastine has the lowest brain penetration (approximately 0% H1 receptor occupancy at therapeutic dose), making it the least sedating. Cetirizine shows approximately 12-20% brain H1 occupancy and is known to cause more drowsiness. Loratadine is less sedating than cetirizine but undergoes significant hepatic metabolism (CYP3A4/CYP2D6), creating more potential for drug interactions. Bilastine's minimal liver metabolism gives it an advantage for patients on multiple medications. Efficacy for allergic rhinitis symptoms is broadly comparable among the three.
The most common side effects are headache and drowsiness (somnolence), each affecting approximately 1-3% of patients. Less common side effects include dizziness, dry mouth, fatigue, and abdominal pain. In clinical trials, bilastine 20 mg showed an overall adverse event profile very similar to placebo. Serious side effects are extremely rare. If you experience any persistent or concerning symptoms, consult your healthcare provider.
References
This article is based on the following peer-reviewed sources and international guidelines:
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- Jauregizar N, de la Fuente L, Lucero ML, et al. Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine. Clinical Pharmacokinetics. 2009;48(8):543-554. doi:10.2165/11317180-000000000-00000
- Kawauchi H, Yanai K, Wang DY, 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
- Bousquet J, Khaltaev N, Cruz AA, et al. Allergic Rhinitis and its Impact on Asthma (ARIA) 2008 update. Allergy. 2008;63 Suppl 86:8-160. doi:10.1111/j.1398-9995.2007.01620.x
- Zuberbier T, Abdul Latiff AH, Abuzakouk M, 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. National Institute for Health and Care Excellence (NICE), 2024.
About Our Medical 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 medicine, dermatology, and drug information. Our team follows the GRADE evidence framework and adheres to international guidelines from the EMA, WHO, and professional allergy organizations.
iMedic Medical Editorial Team, specialists in clinical pharmacology and evidence-based medicine. All content is based on peer-reviewed research and approved product information.
iMedic Medical Review Board, an independent panel of medical experts who verify clinical accuracy and adherence to international guidelines (EMA SmPC, ARIA, EAACI/GA2LEN).
Evidence Level: This article is based on Level 1A evidence from systematic reviews, randomized controlled trials, and internationally recognized clinical guidelines. All medical claims are supported by referenced, peer-reviewed sources.
Conflict of Interest: iMedic has no commercial relationships with pharmaceutical companies. All content is independently produced without industry funding or sponsorship.