Azelastine

Azelastine
Clinical data
Trade namesAstelin, others
AHFS/Drugs.comMonograph
MedlinePlusa603009
License data
Pregnancy
category
  • AU: B3
Routes of
administration		Eye drops, nasal spray, by mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability40% (intranasal)
Metabolitesdesmethylazelastine (active)
Onset of actionWithin 1 hour
Elimination half-life22 hours
Duration of action12 hours
Identifiers
IUPAC name
  • (RS)-4-[(4-Chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-phthalazin-1-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.133.278
Chemical and physical data
FormulaC22H24ClN3O
Molar mass381.90 g·mol−1
3D model (JSmol)
SMILES
  • Clc1ccc(cc1)CC\3=N\N(C(=O)c2ccccc2/3)C4CCCN(C)CC4
InChI
  • InChI=1S/C22H24ClN3O/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16/h2-3,6-11,18H,4-5,12-15H2,1H3 Y
  • Key:MBUVEWMHONZEQD-UHFFFAOYSA-N Y
  (verify)

Azelastine, sold under the brand name Astelin among others, is a H1 receptor-blocking medication primarily used as a nasal spray to treat allergic rhinitis (hay fever) and as eye drops for allergic conjunctivitis.[4][5] Other uses may include asthma and skin rashes for which it is taken by mouth.[6] Onset of effects is within minutes when used in the eyes and within an hour when used in the nose.[7] Effects last for up to 12 hours.[7]

Common side effects include headache, sleepiness, change in taste, and sore throat.[7] It is unclear if use is safe during pregnancy or breastfeeding.[8] It is a second-generation antihistamine and works by blocking the release of a number of inflammatory mediators including histamine.[6][7]

Azelastine was patented in 1971 and came into medical use in 1986.[9] It is available as a generic medication.[3][10] In 2022, it was the 124th most commonly prescribed medication in the United States, with more than 5 million prescriptions.[11][12]

  1. ^ Cite error: The named reference Astelin FDA label was invoked but never defined (see the help page).
  2. ^ Cite error: The named reference Optivar FDA label was invoked but never defined (see the help page).
  3. ^ a b "FDA Approves a Nasal Antihistamine for Nonprescription Use". U.S. Food and Drug Administration (FDA) (Press release). 17 June 2021. Archived from the original on 17 June 2021. Retrieved 21 June 2021.
  4. ^ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 1169. ISBN 9780857113382.
  5. ^ Al-Ahmad M, Hassab M, Al Ansari A (21 December 2020). "Allergic and Non-allergic Rhinitis". Textbook of Clinical Otolaryngology. Cham: Springer International Publishing. pp. 241–252. doi:10.1007/978-3-030-54088-3_22. ISBN 978-3-030-54087-6. S2CID 234142758.
  6. ^ a b Aronson JK (2015). Meyler's Side Effects of Drugs: The International Encyclopedia of Adverse Drug Reactions and Interactions. Elsevier. p. 782. ISBN 9780444537164.
  7. ^ a b c d "Azelastine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists.
  8. ^ "Azelastine ophthalmic (Optivar) Use During Pregnancy". Drugs.com. Retrieved 26 March 2019.
  9. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 548. ISBN 9783527607495.
  10. ^ "First Generic Drug Approvals". U.S. Food and Drug Administration (FDA). 8 July 2024. Retrieved 9 July 2024.
  11. ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
  12. ^ "Azelastine Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.
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