Bilastine

Second-generation antihistamine

ATC code: R06AX29

Updated 26 May 2026 · Methodology

Indications

Allergic rhinitis

First line

First-line for seasonal and perennial allergic rhinitis per ARIA 2020 and 2022, on par with other second-generation antihistamines (desloratadine, levocetirizine, fexofenadine, rupatadine). Dose 20 mg once daily on empty stomach. Bilastine has the lowest sedative potential in the class (Wang 2016 psychomotor studies showed no cognitive impairment); EASA permits its use by commercial airline pilots.

Sources

ICD-10: J30.9 · ICD-11: CA08.0

Chronic urticaria

First line

First-line for chronic spontaneous urticaria under /GA²LEN/EDF/ 2022 at standard 20 mg. With insufficient response, up-titration to 80 mg/day is acceptable (off-label, EAACI consensus). When symptoms persist at quadruple-dose, add omalizumab.

Sources

ICD-10: L50.1 · ICD-11: EB00.1

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

Immune support and respiratory infection care

Not recommended

Bilastine is a second-generation antihistamine. It is prescribed for seasonal and perennial allergic rhinitis and urticaria ( 2024, AEMPS Ficha Técnica). Bilastine is taken for colds and for immunity with the expectation that the antihistamine effect will relieve runny nose and congestion in respiratory infections. The Cochrane review by De Sutter 2015 (16 RCTs) in people with common colds did not confirm benefit of antihistamines as monotherapy. Second-generation antihistamines (bilastine, cetirizine, loratadine, and others) cause virtually no drowsiness – a marketing advantage – but also no cold-relieving effect. If bilastine was prescribed for a cold without confirmed allergic rhinitis, consider seeking a second opinion.

Sources

How to read tiers A–F

AStrong evidence – first or second line in international guidelines
BRecommended in selected cases
CStudy data contradict each other
DBenefit not proven, no documented harm
FDocumented harm, or risk without benefit

Mechanism of action

A second-generation selective peripheral H1-antagonist. Minimal blood-brain barrier penetration and negligible central H1 binding result in almost no sedation. Not metabolized hepatically; 95% is excreted unchanged via the kidneys and gut, so it lacks meaningful CYP-mediated interactions. Developed by Spain's Faes Farma; brand Bilaxten in Spain.

Safety

Contraindications

Bilastine hypersensitivity
Age under 6

Serious adverse effects

Rare hypersensitivity reactions

Common adverse effects

Headache
Drowsiness (~3%, placebo-level)
Dry mouth

Pregnancy: can you take Bilastine?

Pregnancy data are limited. Per EMA: use only when clearly necessary. For pregnancy, antihistamines with more data are preferred – loratadine or cetirizine.

Breastfeeding: can you take Bilastine?

Hale L3 · Probably compatible, limited data

Compatible. Hale L3 (limited data). RID 0.4%. Does not cross BBB, minimal sedation. Per ARIA 2023, recommended for allergic rhinitis in adults, including nursing mothers.

RID, infant dose via milk: 0.4%
Maternal half-life: 14.0 h
Maternal peak time: 1 h
Peak milk concentration: 0.02 mg/L

Calculate RID Safe feeding window Full profile on NIH LactMed ↗

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Practical notes

Timing and administration

Take strictly on empty stomach: 1 hour before or 2 hours after meals and grapefruit juice. Food reduces bioavailability by about 30%. Avoid concurrent aluminum/magnesium antacids. No dose reduction is required in renal impairment or in older adults.

Drug–nutrient interactions

Grapefruit juice

Grapefruit juice cuts bilastine bioavailability by 30%, according to the Bilaxten SmPC, and other fruit juices may do the same. The problem here is loss of effect: allergy symptoms may be less well controlled. The SmPC says to take the tablet one hour before or two hours after food or fruit juice.

Source: AEMPS: Ficha técnica de Bilaxten 20 mg comprimidos (bilastina) (2026)

Label mentions9 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

ModerateCiclosporin
«En pacientes con insuficiencia renal moderada o severa la administración concomitante de bilastina con inhibidores de la P-glicoproteína, tales como p.ej., ketoconazol, eritromicina, ciclosporina…»
AEMPS, section 4.4 · Open on CIMA
ModerateDiltiazem
«En pacientes con insuficiencia renal moderada o severa la administración concomitante de bilastina con inhibidores de la P-glicoproteína, tales como p.ej., ketoconazol, eritromicina, ciclosporina…»
AEMPS, section 4.4 · Open on CIMA
ModerateErythromycin
«En pacientes con insuficiencia renal moderada o severa la administración concomitante de bilastina con inhibidores de la P-glicoproteína, tales como p.ej., ketoconazol, eritromicina, ciclosporina…»
AEMPS, section 4.4 · Open on CIMA
ModerateKetoconazole
«En pacientes con insuficiencia renal moderada o severa la administración concomitante de bilastina con inhibidores de la P-glicoproteína, tales como p.ej., ketoconazol, eritromicina, ciclosporina…»
AEMPS, section 4.4 · Open on CIMA
ModerateRitonavir
«En pacientes con insuficiencia renal moderada o severa la administración concomitante de bilastina con inhibidores de la P-glicoproteína, tales como p.ej., ketoconazol, eritromicina, ciclosporina…»
AEMPS, section 4.4 · Open on CIMA
depresores del SNCclass named in the label
«Interacción con lorazepam : La administración concomitante de bilastina 20 mg y lorazepam 3 mg durante 8 días no potenció los efectos depresores del SNC causados por lorazepam.»
AEMPS, section 4.5 · Open on CIMA
Lorazepam
«Interacción con lorazepam : La administración concomitante de bilastina 20 mg y lorazepam 3 mg durante 8 días no potenció los efectos depresores del SNC causados por lorazepam.»
AEMPS, section 4.5 · Open on CIMA
Rifampicin
«Interacción con zumo de pomelo: La administración concomitante de bilastina 20 mg y zumo de pomelo disminuyó la biodisponibilidad de bilastina en un 30%. Este efecto puede ocurrir también con otros…»
AEMPS, section 4.5 · Open on CIMA

From other drugs’ labels

Itraconazole
«Antihistamínicos para uso sist émico: Bilastina, Rupatidina»
AEMPS, section 4.5 · Open on CIMA

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Frequently asked

What is Bilastine used for?

Bilastine is evaluated for the following indications with varying evidence strength: Allergic rhinitis (evidence tier A), Chronic urticaria (evidence tier A), Immune support and respiratory infection care (evidence tier F). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Bilastine?

Common side effects of Bilastine (≥ 1 in 100): Headache, Drowsiness (~3%, placebo-level), Dry mouth. See the Safety section for uncommon and serious reactions.

Is Bilastine safe during pregnancy?

Pregnancy data are limited. Per EMA: use only when clearly necessary. For pregnancy, antihistamines with more data are preferred – loratadine or cetirizine.

Is Bilastine compatible with breastfeeding?

Compatible. Hale L3 (limited data). RID 0.4%. Does not cross BBB, minimal sedation. Per ARIA 2023, recommended for allergic rhinitis in adults, including nursing mothers.

Who should not take Bilastine?

Bilastine is contraindicated in: Bilastine hypersensitivity; Age under 6. Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

AEMPS / CIMALabel dated 11/14/2025

Other drugs in this group

Cetirizine, Chloropyramine, Chlorpheniramine, Desloratadine, Dimenhydrinate, Ebastine, Levocetirizine, Dexchlorpheniramine