Exploring the Benefits of Topical Oxymetazoline

Introduction

Rosacea, facial redness, and flushing can be both uncomfortable and embarrassing for those who suffer from these conditions. In this article, we discuss topical oxymetazoline, a treatment option for these conditions that is available in some countries, but not commercially available in Australia. We will explore the benefits of oxymetazoline and compare it to brimonidine, another commonly used treatment. We will also discuss how we compound oxymetazoline regularly for dermatologists and their patients throughout Australia.

Background information

Rosacea is a common skin condition characterized by redness, flushing, and sometimes acne-like bumps on the face (1). It affects millions of people worldwide, with varying degrees of severity. Although there is no cure for rosacea, several treatments can help manage the symptoms. Topical medications such as oxymetazoline and brimonidine can help by reducing redness and flushing in patients with and without rosacea.

What is oxymetazoline cream and how is it used in rosacea, facial redness and flushing?

Oxymetazoline is a medication initially developed as a nasal decongestant (2). It is an alpha-adrenergic agonist, which means it works by constricting blood vessels (3). When applied topically to the skin, oxymetazoline can reduce redness and flushing associated with rosacea by narrowing the blood vessels in the affected areas (4). In some countries, such as the United States, oxymetazoline cream is available under the brand name Rhofade.

How was oxymetazoline cream discovered to help with rosacea, facial redness and flushing?

The discovery of oxymetazoline's potential for treating rosacea, facial redness, and flushing came about through the observation that patients using oxymetazoline nasal spray for allergies experienced improvement in their facial redness (5). This observation led to further research and the eventual development of a topical formulation specifically designed for rosacea treatment.

The Science Behind Oxymetazoline

What is the working principle of oxymetazoline?

As an alpha-adrenergic agonist, oxymetazoline works by stimulating the alpha receptors in blood vessels, causing them to constrict (3). This constriction reduces blood flow to the skin, thereby decreasing redness and flushing associated with rosacea and other facial redness conditions (4).

What does oxymetazoline cream do?

When applied to the skin, oxymetazoline cream constricts blood vessels, reducing the appearance of redness and flushing in the treated area (4).

How effective can oxymetazoline cream be?

Studies have shown that oxymetazoline cream can be effective in reducing facial redness and flushing associated with rosacea (6). In one study, more than 70% of patients reported a significant improvement in their rosacea symptoms after 29 days of treatment with oxymetazoline cream (6).

How long do the effects of a single application of topical oxymetazoline last?

The duration of the effects of a single application of topical oxymetazoline can vary among individuals, but generally, the relief from facial redness and flushing can last up to 12 hours (6). This extended duration of action allows patients to experience an improvement in their skin appearance throughout the day with just one daily application. However, it is important to note that the long-term efficacy and the lasting effects of oxymetazoline cream may differ among patients, and consistent daily use is typically necessary to maintain optimal results. Consult your healthcare provider for personalized advice on the usage and expected duration of the effects of oxymetazoline cream in your specific case.

Practical use of oxymetazoline cream

Why do patients use oxymetazoline cream?

Patients use oxymetazoline cream to manage their rosacea symptoms, including facial redness and flushing, and improve their overall skin appearance.

Suggested instructions for application of oxymetazoline cream (ask your prescriber or pharmacist for individualized advice)

It is essential to follow your prescriber's or pharmacist's advice when using oxymetazoline cream. Generally, the cream is applied once daily to the affected areas, avoiding the eyes and mouth (6). A thin layer should be spread evenly over the skin, and the hands should be washed immediately after application.

When are results seen?

Results can vary depending on the individual, but many patients report seeing an improvement in facial redness and flushing within a few hours of applying the cream (6).

When should oxymetazoline cream not be used?

Oxymetazoline cream should not be used if you are allergic to any of its ingredients or if you have a known hypersensitivity to alpha-adrenergic agonists (7). Pregnant and breastfeeding individuals should not use oxymetazoline as its safety during pregnancy and lactation used as a cream has not been established.

What should not be done with oxymetazoline cream?

Do not apply oxymetazoline cream to open wounds or broken skin, and avoid contact with the eyes and mouth. Do not use more than the recommended dose or apply the cream more frequently than directed by your healthcare provider.

What are the Side effects of using oxymetazoline cream?

Side effects of oxymetazoline cream are uncommon. They may include skin irritation, dryness, or itching at the application site (6). Some patients may also experience worsening of facial redness or flushing, known as rebound erythema, after discontinuing the cream (8). Both brimonidine and oxymetazoline, being alpha-adrenergic agonists, have the potential to cause rebound erythema due to their vasoconstrictive effects on blood vessels. However, Brimonidine has been reported to cause rebound erythema more frequently, with some studies suggesting that up to 16-18% of patients may experience this side effect (9). In contrast, oxymetazoline appears to have a lower potential for causing rebound erythema (8). A study by Dover et al. (2007) reported no cases of rebound erythema in the subjects treated with oxymetazoline (5). Additionally, the REVEAL trials demonstrated that oxymetazoline had a favourable safety profile with a lower incidence of side effects, including rebound erythema (6).

General information

Storage

Oxymetazoline cream should be stored at room temperature, away from heat, moisture, and direct sunlight. Keep it out of reach of children and pets.

Appearance

When compounded, oxymetazoline cream is typically a white to off-white, smooth, and uniform cream that is packaged in a tube or pump dispenser.

Conclusion

In conclusion, topical oxymetazoline is a promising treatment for rosacea, facial redness, and flushing. Its benefits over brimonidine include a faster onset of action and potentially fewer side effects (9). While it is not commercially available in Australia, specialised compounding pharmacies such as Skin Plus Compounding Pharmacy can prepare oxymetazoline cream from-scratch and on-demand for dermatologists and their patients throughout the country.

Purpose of this information

The information presented on this website and in this article is for general information and example purposes only, does not contain health advice specific for users and must not be relied on for that purpose. Please see your GP, dermatologist or other health care professional for specific advice.

References

1. Two AM, Wu W, Gallo RL, Hata TR. Rosacea: part I. Introduction, categorization, histology, pathogenesis, and risk factors. J Am Acad Dermatol. 2015 May;72(5):749-58; quiz 759-60.

2. Kligman AM, Sadiq I. The uses of topical decongestants in dermatology. J Am Acad Dermatol. 1993 Dec;29(6):1004-6.

3. Scherer T, Pleiner J, Schmetterer L. Oxymetazoline: a pharmacological overview. Expert Opin Pharmacother. 2000 Jan;1(1):125-35.

4. Fowler J Jr, Jackson M, Moore A, Jarratt M, Jones T, Meadows K, et al. Efficacy and Safety of Once-Daily Topical Brimonidine Tartrate Gel 0.5% for the Treatment of Moderate to Severe Facial Erythema of Rosacea: Results of Two Randomized, Double-blind, and Vehicle-Controlled Pivotal Studies. J Drugs Dermatol. 2013 Jun;12(6):650-6.

5. Dover JS, Batton H, Pham H, Arndt KA. Oxymetazoline: a new topical vasoconstrictor for the treatment of rosacea. J Am Acad Dermatol. 2007 Aug;57(2 Suppl):S47-8.

6. Fowler J Jr, Weiss J, Zug KA, Rodney I, Sherertz EF, Sato S, et al. Efficacy and safety of once-daily topical oxymetazoline cream 1.0% for the treatment of persistent facial erythema associated with rosacea: Findings from the two phase 3, 29-day, randomized, controlled REVEAL trials. J Am Acad Dermatol. 2018 Jan;78(1):115-123.

7. Rhofade [package insert]. Irvine, CA: Allergan, Inc.; 2017.

8. Kircik LH. Rebound Erythema and Flushing of Rosacea: Disease Pathogenesis and Topical Treatment Options for Sustainable Success. J Drugs Dermatol. 2019 Jul 1;18(7):630-634.

9. Moore A, Kempers S, Murakawa G, Weiss R, Tauscher A, Swinyer L, et al. Long-term safety and efficacy of once-daily topical brimonidine tartrate gel 0.5% for the treatment of moderate to severe facial erythema of rosacea: results of a 1-year open-label study. J Drugs Dermatol. 2014 Jan;13(1):56-61.