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Azelaic acid
Synonym(s)
DefinitionThis section has been translated automatically.
Azelaic acid (AZA) is a white, crystalline dicarboxylic acid that occurs naturally in wheat, rye and barley. The dicarboxylic acid is also produced by Malassezia furfur, a yeast that causes pityriasis (tinea) versicolor. Malassezia furfur interferes with melanogenesis by inhibiting tyrosinase in the skin, resulting in hypopigmentation. The salts and esters of AZA are called azelates.
Pharmacodynamics (Effect)This section has been translated automatically.
AZA also has antimicrobial and anticomedonal properties as well as a number of anti-inflammatory properties; it inhibits the production of reactive oxygen species and reduces proinflammatory cytokines such as IL1, IL6 and TNF-alpha (King S et al. 2023). AZA significantly reduces UV-B light-induced nuclear translocation of the p65 subunit of the NF-kB protein (see below NF-kappaB protein; NF-kappaB1 protein) and phosphorylation of p38 mitogen- and stress-activated protein kinase A. AZA also induces the activity of the peroxisome proliferator-activated receptor γ (PPARγ - seePPAR gene below), which plays a crucial role in the control of inflammation (Mastrofrancesco A et al. 2010).
Spectrum of actionThis section has been translated automatically.
In a meta-analysis based on 43 RCTs, the positive effects on rosacea were very clearly demonstrated. Improvements in the severity of erythema and a reduction in the number of inflammatory lesions were documented. Overall, there was a clear overall improvement in the inflammatory skin condition, which was clearly relevant after just 12 weeks of treatment (King S et al. 2023). AZA was more effective than metronidazole 0.75% in improving the severity of erythema, overall improvement and the number of inflammatory lesions. AZA applications also showed clear improvement over vehicle. A 20% AZA reduced significantly more lesions than an erythromycin gel.
IndicationThis section has been translated automatically.
AZA is currently approved and recommended worldwide for the treatment of rosacea and acne vulgaris (see below acne comedonica and acne papulopustulosa, adult female acne). AZA has also been used for melasma and post-inflammatory hyperpigmentation (see belowHyperpigmentation, melasma, lentigines).
Standard concentrationThis section has been translated automatically.
Apply 15-20% in creams, ointments or gels 2 times/day thinly to the affected areas.
Undesirable effectsThis section has been translated automatically.
ContraindicationThis section has been translated automatically.
PreparationsThis section has been translated automatically.
Skinoren Cream®; Finacea Gel®
LiteratureThis section has been translated automatically.
- Gamble R et al. (2012) Topical antimicrobial treatment of acne vulgaris: an evidence-based review. Am J Clin Dermatol 13:141-152.
King S et al. (2023) A systematic review to evaluate the efficacy of azelaic acid in the management of acne, rosacea, melasma and skin aging. J Cosmet Dermatol 22:2650-2662.
Leccia MT et al.(2015) Topical acne treatments in Europe and the issue of antimicrobial resistance. J Eur Acad Dermatol Venereol 29:1485-1492.
- Mastrofrancesco A et al. (2010) Azelaic acid modulates the inflammatory response in normal human keratinocytes through PPARgamma activation. Exp Dermatol 19: 813-820.
- Rademaker M (2016)Very low-dose isotretinoin in mild to moderate papulopustular rosacea; a retrospective review of 52 patients. Australas J Dermatol doi: 10.1111/ajd.12522.
- Schulte BC et al.(2015) Azelaic Acid: Evidence-based Update on Mechanism of Action and Clinical Application. J Drugs Dermatol 14:964-968.
- Sieber MA et al. (2014) Azelaic acid: Properties and mode of action. Skin Pharmacol Physiol 27 Suppl 1:9-17.
Singh SK et al. (2021) Cosmeceutical Aptitudes of Azelaic Acid. Curr Drug Res Rev 13:222-229.
Yin NC et al. (2014) Acne in patients with skin of color: practical management. Am J Clin Dermatol 15:7-16.