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Oxymetazoline

Generic Name
Oxymetazoline
Brand Names
Afrin, Dristan 12-hour Nasal Spray, Kovanaze, Nostrilla, Rhofade, Sinex Long-acting, Upneeq, Zicam Sinus Relief
Drug Type
Small Molecule
Chemical Formula
C16H24N2O
CAS Number
1491-59-4
Unique Ingredient Identifier
8VLN5B44ZY
Background

Oxymetazoline is an imidazole derivative and a potent, direct-acting alpha (α)-adrenergic agonist with affinity to both α- and α-adrenoceptors. Oxymetazoline is available in various formulations with a wide variety of clinical implications. The topical formulation of the drug is used to treat persistent facial redness in adults. As an effective decongestant, oxymetazoline is available in over-the-counter intranasal sprays used to relieve nasal and sinus congestion caused by a wide variety of conditions, such as common cold, hay fever, and upper respiratory allergies. In dentistry, oxymetazoline and tetracaine combination intranasal spray (Kovanaze) is used for regional anesthesia during dental procedures in children and adults. In July 2020, the FDA approved the use of an ophthalmic formulation of oxymetazoline (Upneeq) in adults with acquired blepharoptosis, or ptosis, making it the first FDA-approved medical treatment for this medical condition.

Indication

Oxymetazoline is indicated for the topical treatment of persistent facial erythema associated with rosacea in adults.

Ophthalmic oxymetazoline is indicated for the treatment of acquired blepharoptosis in adults.

When used in combination with tetracaine intranasally, oxymetazoline is indicated for regional anesthesia when performing a restorative procedure on Teeth 4-13 and A-J in adults and children who weigh 40 kg or more.

Oxymetazoline can be found in over-the-counter nasal products as a nasal decongestant.

For off-label uses, oxymetazoline has been used during nasal intubation and during ear, nose, and throat surgery to improve visualization of the airway and to minimize post-operative bleeding.

Associated Conditions
Acquired Blepharoptosis, Allergic Rhinitis (AR), Nasal Congestion, Postoperative Hemorrhages, Rhinorrhoea, Sinus Congestion, Acute Rhinitis, Persistent facial erythema
Associated Therapies
Airway visualization

Effectiveness of Oxymetazoline Added on Nasal Steroid in Rhinitis With Persistent Nasal Obstruction

Phase 4
Completed
Conditions
Nasal Obstruction Present Finding
Interventions
Drug: Placebo nasal spray
Drug: oxymetazoline
First Posted Date
2013-05-06
Last Posted Date
2015-01-05
Lead Sponsor
Mahidol University
Target Recruit Count
50
Registration Number
NCT01847131
Locations
🇹🇭

Faculty of Medicine Siriraj Hospital, Mahidol University, Bangkok, Thailand

Preventing Tolerance to Oxymetazoline in Allergic Rhinitis

Phase 4
Withdrawn
Conditions
Tachyphylaxis
Rhinitis Medicamentosa
Allergic Rhinitis
Interventions
Drug: oxymetazoline-fluticasone propionate
Drug: Oxymetazoline
First Posted Date
2009-02-18
Last Posted Date
2016-10-25
Lead Sponsor
Brian J Lipworth
Registration Number
NCT00846326
Locations
🇬🇧

Perth Royal Infirmary (Tayside NHS Trust), Perth, United Kingdom

🇬🇧

Ninewells Hospital and Medical School (Tayside NHS Trust, University of Dundee), Dundee, United Kingdom

Intranasal Steroids and Oxymetazoline in Allergic Rhinitis

Phase 4
Completed
Conditions
Allergic Rhinitis
Interventions
First Posted Date
2008-01-02
Last Posted Date
2013-12-17
Lead Sponsor
University of Chicago
Target Recruit Count
64
Registration Number
NCT00584987
Locations
🇺🇸

University of Chicago, Chicago, Illinois, United States

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