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User:Mr. Ibrahem/Azelastine

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Mr. Ibrahem/Azelastine
Clinical data
Trade namesAstelin, Optivar, Allergodil, others.[1]
AHFS/Drugs.comMonograph
MedlinePlusa603009
License data
Routes of
administration		Eye drops, nasal spray, by mouth
Drug class2nd-generation antihistamine[2][3]
Legal status
Legal status
  • AU: S2 (Pharmacy medicine)
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetic data
Bioavailability40% (intranasal)
Elimination half-life22 hours
Identifiers
  • (RS)-4-[(4-Chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-phthalazin-1-one
Chemical and physical data
FormulaC22H24ClN3O
Molar mass381.90 g·mol−1
3D model (JSmol)
  • Clc1ccc(cc1)CC\3=N\N(C(=O)c2ccccc2/3)C4CCCN(C)CC4
  • 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 checkY
  • Key:MBUVEWMHONZEQD-UHFFFAOYSA-N checkY
  (verify)

Azelastine, sold under the brand name Optivar among others, is a medication primarily used as a nasal spray to treat allergic rhinitis (hay fever) and as eye drops for allergic conjunctivitis.[4][3] Other uses may include asthma and skin rashes for which it is taken by mouth.[2] Onset of effects is within minutes when used in the eyes and within an hour when used in the nose.[3] Effects last for up to 12 hours.[3]

Common side effects include headache, sleepiness, change in taste, and sore throat.[3] It is unclear if use is safe during pregnancy or breastfeeding.[7] It is a second-generation antihistamine and works by blocking the release of a number of inflammatory mediators including histamine.[2][3]

Azelastine was patented in 1971 and came into medical use in 1986.[8] It is available as a generic medication. A 22 millilitre bottle in the United Kingdom costs the NHS about £10.50 as of 2019.[4] In the United States the wholesale cost of this amount is about US$8.40.[9] In 2017, it was the 297th most commonly prescribed medication in the United States, with more than one million prescriptions.[10][11]

References[edit]

  1. ^ Drugs.com Drugs.com international listings for azelastine Archived 2016-06-05 at the Wayback Machine Page accessed June 28, 2015
  2. ^ a b c Aronson, Jeffrey K. (2015). Meyler's Side Effects of Drugs: The International Encyclopedia of Adverse Drug Reactions and Interactions. Elsevier. p. 782. ISBN 9780444537164. Archived from the original on 2019-03-27. Retrieved 2019-03-26.
  3. ^ a b c d e f g h "Azelastine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 2019-03-26. Retrieved 2019-03-26.
  4. ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 1169. ISBN 9780857113382.
  5. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 30 January 2021. Retrieved 9 September 2020.
  6. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 20 September 2020. Retrieved 9 September 2020.
  7. ^ "Azelastine ophthalmic (Optivar) Use During Pregnancy". Drugs.com. Archived from the original on 26 March 2019. Retrieved 26 March 2019.
  8. ^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 548. ISBN 9783527607495. Archived from the original on 2020-03-06. Retrieved 2019-03-03.
  9. ^ "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Archived from the original on 2019-03-06. Retrieved 3 March 2019.
  10. ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
  11. ^ "Azelastine Hydrochloride - Drug Usage Statistics". ClinCalc. Archived from the original on 13 April 2020. Retrieved 11 April 2020.
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