Drug intelligence / Profile preview

antazoline + xylometazoline

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

Antazoline + xylometazoline is a fixed-dose combination ophthalmic solution used for the symptomatic relief of allergic conjunctivitis. It contains antazoline, a small molecule H1 receptor antagonist, and xylometazoline, a small molecule sympathomimetic vasoconstrictor. Antazoline works by competitively blocking the binding of histamine to H1 receptors, thereby inhibiting histamine-mediated allergic responses such as itching, redness, and swelling. Xylometazoline acts as an agonist at alpha-adrenergic receptors, leading to vasoconstriction of the conjunctival blood vessels, which effectively reduces ocular congestion and edema. The product is marketed under brand names such as Otrivine-Antistin and is available both as a prescription medication and over-the-counter in various regions.

Brand names
Otrivine-AntistinSpersallerg
Other names
antazoline hydrochloride + xylometazoline hydrochloride
02

Targets

ADRA1B (α1B)ADRA1D (α1D)ADRA2B (α2B)ADRA2C (α2C)HRH1 (Histamine H1 Receptor)ADRA1A (α1A)ADRA2A (α2A)

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