Bilastine

Bilastine is an antihistamine medication used to treat hives (urticaria), allergic rhinitis and itchy inflamed eyes (allergic conjunctivitis) caused by an allergy. It is a second-generation antihistamine and takes effect by selectively inhibiting the histamine H1 receptor, preventing these allergic reactions. Bilastine has an effectiveness similar to cetirizine, fexofenadine, and desloratadine.

Bilastine
Clinical data
Trade namesBlexten, others
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth
Drug classAntihistamine
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability61%
Protein binding84-90% binding to plasma proteins
MetabolismNot significantly metabolised
Onset of action1 hour (Allertine)
Elimination half-life14.5 hours
Duration of action24 hours (Allertine)
Excretion95% in urine and faeces
Identifiers
  • 2-[4-(2-{4-[1-(2-Ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl}ethyl)phenyl]-2-methylpropanoic acid
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.260.016
Chemical and physical data
FormulaC28H37N3O3
Molar mass463.622 g·mol−1
3D model (JSmol)
  • O=C(O)C(c1ccc(cc1)CCN4CCC(c2nc3ccccc3n2CCOCC)CC4)(C)C
  • InChI=1S/C28H37N3O3/c1-4-34-20-19-31-25-8-6-5-7-24(25)29-26(31)22-14-17-30(18-15-22)16-13-21-9-11-23(12-10-21)28(2,3)27(32)33/h5-12,22H,4,13-20H2,1-3H3,(H,32,33) Y
  • Key:ACCMWZWAEFYUGZ-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)

Bilastine is approved in the European Union for the symptomatic treatment of allergic conjunctivitis and urticaria. It is not approved for any use in the United States.

Evidence has shown that bilastine is effective in treating skin and eye symptoms of allergic reactions, improving patient's quality of life. Bilastine meets the treatment criteria for allergic rhinitis, as published by the European Academy of Allergy and Clinical Immunology (EAACI) and the Allergic Rhinitis and its Impact of Asthma (ARIA) initiative.

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