Azelaic first burst into the market 20 years ago, and it has steadily been gaining ground as a safe and effective treatment for rosacea. Want to know if it’s the right choice for you? Here are some of the most common questions people have about using azelaic acid on rosacea.
What is azelaic acid?
Azelaic acid (AzA) is a dicarboxylic acid that is naturally found in plants such as wheat, rye, and barley. It can also be produced by Malassezia furfur, a yeast that is part of our normal skin biome.
How does azelaic acid work against rosacea?
AzA has potent anti-inflammatory, anti-bacterial, anti- properties (Graupe et al., 1996; Zeichner, 2013). This multimodal approach makes it effective at minimizing rosacea flare-ups.
The skin of rosacea patients is sensitive to a wide variety of stimuli. When exposed to these, the skin mounts an immune response so overblown that it is even more harmful to the skin than the stimuli itself. AzA addresses this issue by curbing the deranged overproduction of pro-inflammatory molecules called cathelicidins, tempering the overzealous activity of pro-inflammatory enzymes like kallikrein-5, and reducing the expression of pro-inflammatory signaling receptors like TLR-2 (Yamasaki and Gallo, 2010; Two and Del Rosso 2014; Coda et al,. 2015).
A byproduct of the inflammation is the production of reactive oxygen species by immune cells. When these molecules are allowed to accumulate, they start to damage the cells of the body itself. In in-vitro studies, immune cells exposed to azelaic acid produced lower amounts of reactive oxygen species (Akamatsu et al., 1991; Jones, 2009), decreasing the collateral damage of the immune response.
AzA’s bactericidal activity helps prevent rosacea episodes triggered by bacterial overgrowth. It is effective against both Gram positive and Gram negative bacteria implicated in skin conditions, including Propionionibacterium acnes and Staphylococcus epidermidis (Sieber and Hegel, 2014).
For those with papulopustular rosacea or who suffer from concurrent acne, AzA’s comedolytic ability comes as an additional bonus (Schulte, Wu and Rosen, 2015). It regulates follicular keratinization, helping to tame those bumps and smoothen out skin.
Finally, it helps with the hyperpigmentation that often comes as a sequelae to inflammation. It inhibits the enzyme responsible for producing the skin pigment melanin, and downregulates the proliferation of abnormal melanocytes (Nguyen and Bui, 1995). This has been used effectively and safely in dark-skinned patients (Sarkar, Bhalla and Kanwar, 2002).
Is azelaic acid effective?
It’s a resounding yes. Many dermatologists recommend azelaic acid to rosacea patients because of the long history of evidence supporting its use.
In a study by Onder and Adisen (2008), patients with mild to moderate papulopustular rosacea found that facial redness was significantly decreased after four weeks of twice daily application of AzA.
A randomized, double-blind study found that AzA 15% gel resulted in a greater decrease in lesions and redness, and improved scores on both expert assessment and patient assessment over metronidazole in patients with moderate papulopustular rosacea after 15 weeks of twice daily application (Elewksi et al., 2003).
A double-blind controlled split-face study by Carmicheal et al. (1993) showed that 20% AzA cream administration over a period of 9 weeks led to a greater reduction in papules, pustules and redness compared to the vehicle cream.
A randomized, double-blind study by Draelos et al. (2013) found that the treatment success rate was 43.4% in the AzA foam group and 32.5% in the vehicle only group after 12 weeks of application. During a follow-up scheduled 4 weeks after the end of treatment, the 35.4% of the AzA foam group retained improvement.
A review of literature on the use of AzA in various dermatological disorders showed that the strongest evidence of its use is for rosacea (Tamara et al., 2022).
These studies show that AzA can effectively reduce the symptoms of mild to moderate papulopustular rosacea, with improvement first being seen as a decreased level of redness, with continued use resulting in a decrease in inflammatory lesions. It must be noted that there is no evidence showing that AzA can reduce telangiectasia (Liu et al., 2006). Other treatment options should be considered for this particular symptom.
Is azelaic acid safe?
Azelaic acid is generally well-tolerated among a wide variety of skin types and colors. In studies, up to 30-40% of patients experience mild itchiness, stinging, burning and stinging that eventually goes away with continued use (Gupta and Gover 2006; Onder and Adisen, 2008).
AzA is non-toxic, not known to cause any systemic side effects, and is safe even for pregnant women (Mingrone et al., 1986; Gaupe et al., 1996). It does not sensitize the skin to sunlight (though sunscreen is still a must for everyone, whether diagnosed with rosacea or not!). Unlike many topical agents, it does not stain or bleach clothes.
How do you use azelaic acid for rosacea?
Azelaic acid comes in several formulations, the most common being 15% gel, 20% cream, and 15% foam. With its good safety profile, it can be used once or twice a day, even as maintenance therapy.
But as in any skin disorder, it is best to consult your dermatologist on what works best for you and your situation. With expert advice and consistent practice, managing a condition as difficult as rosacea becomes possible.
This content is for general information only and is not a substitute for medical advice.
References:
Akamatsu, H., Komura, J., Asada, Y. et al. Inhibitory effect of azelaic acid on neutrophil functions: a possible cause for its efficacy in treating pathogenetically unrelated diseases. Arch. Dermatol. Res. 238, 162–166 (1991).
Aj Carmichael, R Marks, Ka Graupe & Rp Zaumseil (1993) Topical azelaic acid in the treatment of rosacea, Journal of Dermatological Treatment, 4:sup1, S19-S22, DOI: 10.3109/09546639309082150
Coda, A. B., Hata, T., Miller, J., Audish, D., Kotol, P., Two, A., Shafiq, F., Yamasaki, K., Harper, J. C., Del Rosso, J. Q., & Gallo, R. L. (2013). Cathelicidin, kallikrein 5, and serine protease activity is inhibited during treatment of rosacea with azelaic acid 15% gel. Journal of the American Academy of Dermatology, 69(4), 570–577. https://doi.org/10.1016/j.jaad.2013.05.019
Draelos, Zoe & Elewski, Boni & Staedtler, Gerald & Havlickova, Blanka. (2013). Azelaic acid foam 15% in the treatment of papulopustular rosacea: A randomized, double-blind, vehicle-Controlled study. Cutis. 92. 306-17.
Elewski BE, Fleischer AB, Pariser DM. A Comparison of 15% Azelaic Acid Gel and 0.75% Metronidazole Gel in the Topical Treatment of Papulopustular Rosacea: Results of a Randomized Trial. Arch Dermatol. 2003;139(11):1444–1450. doi:10.1001/archderm.139.11.1444
Graupe, K., Cunliffe, W. J., Gollnick, H. P., & Zaumseil, R. P. (1996). Efficacy and safety of topical azelaic acid (20 percent cream): an overview of results from European clinical trials and experimental reports. Cutis, 57(1 Suppl), 20–35.
Gupta, A. K., & Gover, M. D. (2007). Azelaic acid (15% gel) in the treatment of acne rosacea. International journal of dermatology, 46(5), 533–538. https://doi.org/10.1111/j.1365-4632.2005.02769.x
Mingrone G. GrecoAV, Nazzaro-Porro M, et al, Toxicity of azelaic acid. Drugs Exp Clin Res. 1983;9:447–55.
Liu RH, Smith MK, Basta SA, Farmer ER. Azelaic Acid in the Treatment of Papulopustular Rosacea: A Systematic Review of Randomized Controlled Trials. Arch Dermatol. 2006;142(8):1047–1052. doi:10.1001/archderm.142.8.1047
Nguyen, Q. H., & Bui, T. P. (1995). Azelaic acid: pharmacokinetic and pharmacodynamic properties and its therapeutic role in hyperpigmentary disorders and acne. International journal of dermatology, 34(2), 75–84. https://doi.org/10.1111/j.1365-4362.1995.tb03583.x
Jones D. A. (2009). Rosacea, reactive oxygen species, and azelaic Acid. The Journal of clinical and aesthetic dermatology, 2(1), 26–30.
Onder M, Adisen E (2008). Photographic evaluation of 15% azelaic acid gel in acne rosacea. Journal of the Turkish Academy of Dermatology, 2(3). http://www.jtad.org/2008/3/jtad82301a.pdf
Sarkar, R., Bhalla, M., & Kanwar, A. J. (2002). A comparative study of 20% azelaic acid cream monotherapy versus a sequential therapy in the treatment of melasma in dark-skinned patients. Dermatology (Basel, Switzerland), 205(3), 249–254. https://doi.org/10.1159/000065851
Schulte, B. C., Wu, W., & Rosen, T. (2015). Azelaic Acid: Evidence-based Update on Mechanism of Action and Clinical Application. Journal of drugs in dermatology : JDD, 14(9), 964–968.
Sieber, M. A., & Hegel, J. K. (2014). Azelaic acid: Properties and mode of action. Skin pharmacology and physiology, 27 Suppl 1, 9–17. https://doi.org/10.1159/000354888
Tamara Searle, Faisal R. Ali & Firas Al-Niaimi (2022) The versatility of azelaic acid in dermatology, Journal of Dermatological Treatment, 33:2, 722-732, DOI: 10.1080/09546634.2020.1800579
Thiboutot, D. M., Fleischer, A. B., Jr, Del Rosso, J. Q., & Graupe, K. (2008). Azelaic acid 15% gel once daily versus twice daily in papulopustular rosacea. Journal of drugs in dermatology : JDD, 7(6), 541–546.
Two, A. M., & Del Rosso, J. Q. (2014). Kallikrein 5-mediated inflammation in rosacea: clinically relevant correlations with acute and chronic manifestations in rosacea and how individual treatments may provide therapeutic benefit. The Journal of clinical and aesthetic dermatology, 7(1), 20–25.
Yamasaki Y, Gallo RL: Azelaic acid gel alters kallikrein 5 and cathelicidin expression in epidermal keratinocytes, critical elements in the pathogenesis of rosacea. J Am Acad Dermatol 2010;62:AB1
