Drug intelligence / Profile preview

oxymetazoline

Development stage
Approved
Lead developer
Merck
Modality
Small Molecules
Administration
Intranasal, Topical, Ophthalmic
01

Overview

Oxymetazoline is a direct-acting sympathomimetic and imidazole derivative that acts as a potent agonist at alpha-1A adrenergic receptor and alpha-2 adrenergic receptor. It is primarily used as a topical decongestant for the temporary relief of nasal congestion caused by colds or allergies and for the treatment of facial erythema associated with rosacea. Oxymetazoline is also used in ophthalmic preparations to relieve eye redness and in topical formulations to treat acquired blepharoptosis (drooping eyelid). Its mechanism involves vasoconstriction of dilated arterioles through stimulation of adrenergic receptors in vascular smooth muscle. This reduces blood flow and swelling in mucosal tissues. The drug provides rapid relief from congestion with effects lasting up to 12 hours after intranasal administration.

Brand names
AfrinDristan 12-hour Nasal SprayDristan12-hour Nasal SprayDristan-12-hour Nasal SprayKovanazeNostrillaRhofadeSinex Long-actingUpneeq4-Way Long LastingDuramist PlusDurationGenasalMucinex Full ForceMucinex Moisture SmartNasaconNasinNeo-Synephrine 12 HourNeo-Synephrine12 HourNeo-Synephrine-12 HourNRS-Nasal ReliefSinarest Nasal SprayVicks Sinex 12 HourZicam Sinus ReliefAfrin NoDrip Severe CongestionZicam Extreme Congestion ReliefAfrin OriginalOcuClear
Other names
oxymetazoline nasal sprayoxymetazoline
02

Targets

ADRA2B (α2B)ADRA2A (α2A)HTR1B (5-Hydroxytryptamine Receptor 1B)HTR1D (5-hydroxytryptamine receptor 1D)ADRA1A (α1A)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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