Chemistry:Antazoline

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Short description: Chemical compound
Antazoline
Antazoline.svg
Clinical data
Trade namesVasocon-a
AHFS/Drugs.comMicromedex Detailed Consumer Information
Routes of
administration
Topical (nasal, eye drops)
ATC code
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC17H19N3
Molar mass265.360 g·mol−1
3D model (JSmol)
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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. "Effects of topically applied occular decongestant and antihistamine". American Journal of Ophthalmology 90 (2): 254–257. August 1980. doi:10.1016/s0002-9394(14)74864-0. PMID 7425039. 
  2. "Topical antihistamines and mast cell stabilisers for treating seasonal and perennial allergic conjunctivitis". The Cochrane Database of Systematic Reviews 2015 (6): CD009566. June 2015. doi:10.1002/14651858.CD009566.pub2. PMID 26028608. 
  3. "The suppression of olfactory bulbectomy-induced muricide by antidepressants and antihistamines via histamine H1 receptor blocking". Physiology & Behavior 51 (6): 1123–1127. June 1992. doi:10.1016/0031-9384(92)90297-f. PMID 1353628. 
  4. "Cumulative use of strong anticholinergics and incident dementia: a prospective cohort study". JAMA Internal Medicine 175 (3): 401–407. March 2015. doi:10.1001/jamainternmed.2014.7663. PMID 25621434.