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);
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 ;
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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

^ 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.
^ 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.
^ 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.
^ 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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[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.

[Castillo-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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v t e Antihistamines (R06)
Benzimidazoles (*)	Astemizole Azelastine Bilastine Emedastine Mizolastine Talastine
Diarylmethanes	Diarylmethoxyalkylamines: Bromazine (bromodiphenhydramine) Carbinoxamine Chlorphenoxamine Clemastine Diphenhydramine (+naproxen) Diphenylpyraline Doxylamine Ebastine Orphenadrine Diphenylmethanolpiperidines: Fexofenadine Terfenadine Diphenylmethylpiperazines: Buclizine Cetirizine Levocetirizine Chlorcyclizine Cinnarizine Cyclizine Etodroxizine Hydroxyzine Meclizine Oxatomide Phenylpyridinylpropanamines: Brompheniramine Chlorphenamine Dexbrompheniramine (+pseudoephedrine) Dexchlorpheniramine (+betamethasone) Pheniramine Others: Acrivastine Bamipine Dimetindene Phenyltoloxamine Pyrrobutamine Quifenadine Triprolidine
Ethylenediamines	Antazoline Chloropyramine Histapyrrodine Mepyramine (pyrilamine) Methapyrilene Phenbenzamine Thenalidine Tripelennamine (pyribenzamine)
Tricyclics	Dibenzocycloheptenes: Antidepressants (e.g., amitriptyline) Azatadine Cyproheptadine Deptropine Desloratadine Ketotifen Loratadine Rupatadine Phenothiazines: Alimemazine Fenethazine Hydroxyethylpromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine Others: Antidepressants (e.g., doxepin, mirtazapine, trimipramine) Epinastine Latrepirdine Mebhydrolin Olopatadine Perlapine Phenindamine Pimethixene
Others	Phenylpiperazines: Antidepressants (e.g., trazodone) Phenbenzamine
For topical use	Bamipine Chloropyramine Chlorphenoxamine Clemastine Dimetindene Diphenhydramine Doxepin Isothipendyl Mepyramine (pyrilamine) Promethazine