Antazoline

Antazoline

Clinical data
Trade names	Vasocon-a
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Routes of administration	Topical (nasal, eye drops)
ATC code	R01AC04 ( WHO ) R06AX05 ( WHO )
Legal status
Legal status	AU: S4 (Prescription only)/ Schedule 2 [1]
Identifiers
IUPAC name N-(4,5-Dihydro-1H-imidazol-2-ylmethyl)-N-(phenylmethyl)aniline
CAS Number	91-75-8
PubChem CID	2200
IUPHAR/BPS	7116
DrugBank	DB08799
ChemSpider	2115
UNII	DHA8014SS1
KEGG	D07458
ChEBI	CHEBI:84115
ChEMBL	ChEMBL1305
CompTox Dashboard (EPA)	DTXSID3022613
ECHA InfoCard	100.001.904
Chemical and physical data
Formula	C17H19N3
Molar mass	265.360 g·mol−1
3D model (JSmol)	Interactive image
SMILES N\1=C(\NCC/1)CN(c2ccccc2)Cc3ccccc3
InChI 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 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. ^[2] To treat allergic conjunctivitis, antazoline can be combined in a solution with tetryzoline. ^[3] The drug is a Histamine H1 receptor antagonist: ^[4] 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.

Research

A 2015 study on people aged 65 years of age 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. ^[5]

References

1. "Therapeutic Goods (Poisons Standard— June 2025) Instrument 2025" (pdf). Therapeutic Goods Administration (TGA). May 2025. Retrieved 31 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.