Azelaic Acid

What is it?

Saturated dicarboxylic acid

Origin

Naturally occuring

Use

  • Acne - treatment of mild to moderate inflammatory acne vulgaris

    • Not for the treatment of non-inflammatory acne vulgaris

  • Rosacea - treatment of inflammatory lesions associated with mild to moderate rosacea

    • Treatment of erythema in rosacea without papules and pustules has not been evaluated

Existing monograph?

YES

Effective concentrations

  • 20%

    • Therapeutic cream for the treatment of comedonal acne, inflammatory acne, and various hyperpigmentation issues

Mechanism of Action

  • Unclear, but may be related to inhibiting mitochondrial oxidoreductase activity and DNA synthesis

  • Appears to have bacteriostatic and bactericidal properties against aerobic and anaerobic microorganisms found on skin with acne

Site of Action

  • Epidermis - Stratum Basale - melanocytes

Elimination

  • Metabolism

    • Minimally metabolized following topical application

    • Can undergo beta-oxidation to shorter chain dicarboxylic acids

  • Elimination

    • Excreted primarily through urine; molecule does not change

  • Half-life

    • 12 hours following topical application

References

  1. Fitton, A., & Goa, K. L. (1991). Azelaic Acid. Drugs, 41(5), 780–798. doi: 10.2165/00003495-199141050-00007