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Antazoline

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
Antazoline
Clinical data
Trade namesVasocon-a
AHFS/Drugs.comMicromedex Detailed Consumer Information
Routes of
administration
Topical (nasal,eye drops)
ATC code
Legal status
Legal status
Identifiers
  • N-(4,5-Dihydro-1H-imidazol-2-ylmethyl)-N-(phenylmethyl)aniline
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.001.904Edit 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)
  • Key:REYFJDPCWQRWAA-UHFFFAOYSA-N

Antazoline is a 1st generationantihistamine withanticholinergic properties used to relievenasal congestion and ineye drops, usually in combination withnaphazoline, to relieve the symptoms ofallergicconjunctivitis.[2] To treat allergic conjunctivitis, antazoline can be combined in a solution withtetryzoline.[3] The drug is aHistamine H1 receptor antagonist:[4] selectively binding to but not activating the receptor, thereby blocking the actions of endogenoushistamine and subsequently leading to the temporary relief of the negative symptoms brought on by histamine.

Research

[edit]

A 2015 study on people aged 65 years of age or older linked the development ofAlzheimer's disease and other forms of dementia to the "higher cumulative" use of first-generation antihistamines, due to theiranticholinergic properties.[5]

References

[edit]
  1. ^"Therapeutic Goods (Poisons Standard— June 2025) Instrument 2025"(pdf).Therapeutic Goods Administration (TGA). May 2025. Retrieved31 August 2025.
  2. ^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.
  3. ^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.
  4. ^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.
  5. ^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.
Decongestants and other nasal preparations (R01)
Topical
Sympathomimetics, plain
Antiallergic agents,
excluding corticosteroids
Corticosteroids
Other nasal preparations
Combination products
Systemic use:
Sympathomimetics
Benzimidazoles(*)
Diarylmethanes
Ethylenediamines
Tricyclics
Others
Fortopical use
mAChRsTooltip Muscarinic acetylcholine receptors
Agonists
Antagonists
Precursors
(andprodrugs)
nAChRsTooltip Nicotinic acetylcholine receptors
Agonists
(andPAMsTooltip positive allosteric modulators)
Antagonists
(andNAMsTooltip negative allosteric modulators)
Precursors
(andprodrugs)
H1
Agonists
Antagonists
H2
Agonists
Antagonists
H3
Agonists
Antagonists
H4
Agonists
Antagonists
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