Antazoline
Clinical data
Trade namesVasocon-a
AHFS/Drugs.comMicromedex Detailed Consumer Information
Routes of
administration		Topical (nasal, eye drops)
ATC code
Identifiers
  • N-(4,5-Dihydro-1H-imidazol-2-ylmethyl)-N-(phenylmethyl)aniline
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.001.904 Edit this at Wikidata
Chemical and physical data
FormulaC17H19N3
Molar mass265.360 g·mol−1
3D model (JSmol)
  • N\1=C(\NCC/1)CN(c2ccccc2)Cc3ccccc3
  • InChI=1S/C17H19N3/c1-3-7-15(8-4-1)13-20(14-17-18-11-12-19-17)16-9-5-2-6-10-16/h1-10H,11-14H2,(H,18,19) checkY
  • Key:REYFJDPCWQRWAA-UHFFFAOYSA-N checkY
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Antazoline is a 1st generation antihistamine with anticholinergic properties used to relieve nasal congestion and in eye drops, usually in combination with naphazoline, to relieve the symptoms of allergic conjunctivitis.[1] To treat allergic conjunctivitis, antazoline can be combined in a solution with tetryzoline.[2] The drug is a Histamine H1 receptor antagonist:[3] selectively binding to but not activating the receptor, thereby blocking the actions of endogenous histamine and subsequently leading to the temporary relief of the negative symptoms brought on by histamine.

A large study on people 65 years old or older linked the development of Alzheimer's disease and other forms of dementia to the "higher cumulative" use of first-generation antihistamines, due to their anticholinergic properties.[4]

References

  1. ^ Abelson MB, Allansmith MR, Friedlaender MH (August 1980). "Effects of topically applied occular decongestant and antihistamine". American Journal of Ophthalmology. 90 (2): 254–257. doi:10.1016/s0002-9394(14)74864-0. PMID 7425039.
  2. ^ Castillo M, Scott NW, Mustafa MZ, Mustafa MS, Azuara-Blanco A (June 2015). "Topical antihistamines and mast cell stabilisers for treating seasonal and perennial allergic conjunctivitis". The Cochrane Database of Systematic Reviews. 2015 (6): CD009566. doi:10.1002/14651858.CD009566.pub2. hdl:2164/6048. PMC 10616535. PMID 26028608.
  3. ^ Noguchi S, Inukai T, Kuno T, Tanaka C (June 1992). "The suppression of olfactory bulbectomy-induced muricide by antidepressants and antihistamines via histamine H1 receptor blocking". Physiology & Behavior. 51 (6): 1123–1127. doi:10.1016/0031-9384(92)90297-f. PMID 1353628. S2CID 29562845.
  4. ^ Gray SL, Anderson ML, Dublin S, Hanlon JT, Hubbard R, Walker R, et al. (March 2015). "Cumulative use of strong anticholinergics and incident dementia: a prospective cohort study". JAMA Internal Medicine. 175 (3): 401–407. doi:10.1001/jamainternmed.2014.7663. PMC 4358759. PMID 25621434.
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