Drug intelligence / Profile preview

antazoline

Development stage
Phase 4
Lead developer
Novartis
Modality
Small Molecules
Administration
Ophthalmic, Intranasal, Intravenous
01

Overview

Antazoline is a first-generation antihistamine with anticholinergic properties, primarily used for the symptomatic treatment of nasal congestion and allergic conjunctivitis. It acts as a histamine H1 receptor antagonist, selectively binding to but not activating the receptor, thereby blocking the actions of endogenous histamine and providing temporary relief from symptoms such as itching, redness, and swelling associated with allergies. Antazoline is commonly formulated in eye drops—often in combination with naphazoline or tetryzoline—to treat allergic conjunctivitis. In addition to its antihistaminic effects, intravenous antazoline has demonstrated antiarrhythmic properties through multichannel action involving sodium and potassium channels; it prolongs atrial and ventricular refractory periods similar to class I antiarrhythmic agents like quinidine[1][2][6][7].

Brand names
Vasocon-ARefresh Eye Allergy Relief
Other names
antazoline hydrochloride
02

Targets

HRH1 (Histamine H1 Receptor)HRH2 (Histamine H2 Receptor)HRH3 (Histamine Receptor H3)

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