Bilastine is a 2nd generation antihistamine used for symptomatic treatment of allergic rhinoconjuctivitis (allergic disease of the nasal mucosa and eyes) and urticaria (hives). Unlike other antihistamines, it has a hardly sedating, fast and long-lasting effect.



During an allergic reaction, histamine and other substances are released from the cells of the body's defense system. Bilastine binds to the H1 receptor instead of histamine and thus inhibits their activation. This reduces allergic symptoms. Since it has no effect on the central nervous system, it does not have a sedative effect.
Die Effekte des Wirkstoffes halten bis zu 24 Stunden an.


Bilastine is 61% absorbed and is 84-90% protein-bound in plasma. It is a substrate of the P-glycoprotein and an inhibitor of the organo-anion transporter and, unlike other antihistamines, does not interact with the CYP450 enzyme. In keeping with its long duration of action, it has a half-life of 14.5 hours. The active ingredient is excreted largely unchanged in the feces and urine.


Food, especially grapefruit juice, reduces oral bioavailability, so the drug should be taken fasting. A high-fat meal also significantly inhibits absorption.
Die gleichzeitige Anwendung des Antihistaminikums mit Ketokonazol, Ritonavir, Erythromycin, Diltiazem und Ciclosporin sollte vermieden werden.


Side effects

Possible adverse reactions include headache, dizziness, and drowsiness or fatigue.

Toxicological Data

NOAEL (rat): 1200 mg/kg/day.
NOAEL (Hund): 125 mg/kg/Tag

Chemical & physical properties

ATC Code R06AX29
Formula C18H37N3O3
Molar Mass (g·mol−1) 463,622
CAS Number 202189-78-4
PUB Number 185460
Drugbank ID DB11591

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All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

The content of this page is an automated and high-quality translation from DeepL. You can find the original content in German here.


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