Overview
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.
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
Research Report
Oxymetazoline: A Comprehensive Pharmacological and Clinical Review
1. Introduction to Oxymetazoline
Overview, Historical Context, and Therapeutic Class
Oxymetazoline is an imidazole derivative that functions as a potent, direct-acting sympathomimetic agent. Its primary pharmacological activity is as an alpha (α)-adrenergic agonist.[1] Developed in 1961 by Wolfgang Fruhstorfer and Helmut Müller-Calgan at E. Merck Darmstadt, oxymetazoline was derived from xylometazoline.[2] Therapeutically, it is classified as a vasoconstrictor and topical decongestant, initially recognized for its utility in alleviating nasal congestion.[2]
The clinical applications of oxymetazoline have expanded considerably since its introduction. It is widely available in over-the-counter (OTC) intranasal sprays for the management of nasal congestion. Furthermore, its therapeutic scope now includes prescription formulations such as topical creams for persistent facial erythema associated with rosacea and ophthalmic solutions for acquired blepharoptosis (drooping eyelids) and nonspecific ocular redness.[1] Oxymetazoline is also a constituent of a combination product, Kovanaze, used to achieve regional anesthesia in certain dental procedures.[1]
The brand Afrin, a well-known oxymetazoline nasal spray, was first marketed as a prescription medication in 1966. Its success led to its transition to an over-the-counter product in 1975.[2] This long history of use, coupled with recent FDA approvals for novel indications—Rhofade for rosacea in 2017 and Upneeq for blepharoptosis in 2020—underscores the sustained therapeutic relevance and versatility of oxymetazoline.[1]
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/02/17 | Phase 2 | Recruiting | |||
2024/07/23 | Phase 3 | Recruiting | |||
2023/07/14 | Phase 3 | ENROLLING_BY_INVITATION | |||
2021/12/08 | Phase 1 | Completed | |||
2021/04/05 | Phase 4 | Completed | |||
2019/11/06 | Phase 4 | Completed | |||
2019/09/26 | Phase 2 | Withdrawn | |||
2019/09/26 | Phase 2 | Withdrawn | |||
2019/05/24 | Phase 2 | Terminated | |||
2019/05/17 | Phase 3 | Completed |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Aclaris Therapeutics, Inc. | 71180-003 | TOPICAL | 1 g in 100 g | 11/30/2018 | |
| St. Renatus | 69803-100 | NASAL | 0.5 mg in 1 mL | 11/16/2018 | |
| Taro Pharmaceuticals U.S.A., Inc. | 51672-1405 | TOPICAL | 10 mg in 1 g | 10/8/2021 | |
| EPI Health, LLC | 71403-003 | TOPICAL | 1 g in 100 g | 11/30/2019 | |
| H E B | 59640-388 | NASAL | 0.05 g in 100 mL | 4/22/2025 | |
| RVL Pharmaceuticals, Inc. | 73687-062 | OPHTHALMIC | 1 mg in 1 mL | 5/9/2023 | |
| Walmart Inc | 79903-346 | NASAL | 0.05 g in 100 mL | 3/3/2025 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| OXY-NASE NASAL DROPS 0.05% | SIN09606P | SOLUTION | 0.05% w/v | 1/9/1998 | |
| ILIADIN SOLUTION 0.025% | SIN03162P | SOLUTION | 0.25mg | 6/2/1989 | |
| OXY-NASE NASAL DROPS 0.025% | SIN09618P | SOLUTION | 0.025% w/v | 2/4/1998 | |
| OXY-NASE PAEDIATRIC NASAL SPRAY 0.025% w/v | SIN12295P | SPRAY | 0.025% w/v | 5/14/2003 | |
| ILIADIN SOLUTION 0.05% | SIN03163P | SOLUTION | 0.5 mg | 6/2/1989 | |
| ILIADIN SPRAY 0.05% | SIN02674P | SPRAY | 0.5 mg | 4/28/1989 | |
| ILIADIN SOLUTION FOR NOSE 0.01% | SIN06533P | SOLUTION | 0.1 mg/ml | 8/29/1991 | |
| CLARICLEAR NASAL SPRAY 0.05% | SIN02656P | SPRAY | 0.500 mg/ml | 4/27/1989 | |
| OXY-NASE NASAL SPRAY 0.05% w/v | SIN12296P | SPRAY | 0.05% w/v | 5/14/2003 | |
| NAZOLIN NASAL SPRAY 0.05% | SIN10520P | SPRAY | 0.05% | 12/8/1998 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Oxymetazoline Hydrochloride Spray | 国药准字H20058017 | 化学药品 | 喷雾剂 | 8/21/2020 | |
| Oxymetazoline Hydrochloride Spray | 国药准字H10980317 | 化学药品 | 喷雾剂 | 7/2/2020 | |
| Oxymetazoline Hydrochloride Spray | 国药准字H20163026 | 化学药品 | 喷雾剂 | 1/5/2021 | |
| Oxymetazoline Hydrochloride Spray | 国药准字H20000457 | 化学药品 | 喷雾剂 | 7/2/2020 | |
| Oxymetazoline Hydrochloride Spray | 国药准字H20066792 | 化学药品 | 喷雾剂 | 2/1/2021 | |
| Oxymetazoline Hydrochloride Spray | 国药准字H20031192 | 化学药品 | 喷雾剂 | 7/27/2020 | |
| Oxymetazoline Hydrochloride Spray | 国药准字H20057401 | 化学药品 | 喷雾剂 | 7/14/2020 | |
| Oxymetazoline Hydrochloride Spray | 国药准字H20093704 | 化学药品 | 喷雾剂 | 12/18/2023 | |
| Oxymetazoline Hydrochloride Eye Drops | 国药准字H20030231 | 化学药品 | 眼用制剂 | 6/14/2024 | |
| Oxymetazoline Hydrochloride Eye Drops | 国药准字H20073742 | 化学药品 | 滴眼剂 | 5/9/2022 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| XTRA NASAL RELIEF SPRAY 0.05% | N/A | N/A | N/A | 4/28/2007 | |
| LOGICIN RAPID RELIEF NASAL SPRAY 0.05% | N/A | aspen pharmacare asia limited o/b aspen pharmacare asia limited | N/A | N/A | 10/3/1998 |