Introduction ⬇
AHFS Class:
Generic Name(s):
Azelaic acid is a naturally occurring aliphatic dicarboxylic acid that exhibits various dermatologic effects including antibacterial and antiproliferative activity.1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,19,20,22,26
Uses ⬆ ⬇
Acne Vulgaris 
Azelaic acid 20% cream is used topically in the treatment of mild to moderate inflammatory acne vulgaris.1,2,4,5,6,7,8,10,11,12,13,14,15,19,20,26 The drug is not indicated in the treatment of noninflammatory acne vulgaris.21 Therapy of acne vulgaris must be individualized and frequently modified depending on the types of acne lesions that predominate and the response to therapy.18 Results of several studies indicate that topical azelaic acid 20% cream is more effective than vehicle placebo in the treatment of mild to moderate inflammatory acne2,12,14,19,20 and as effective as topical tretinoin2,3,4,6,8,12 or benzoyl peroxide. 2,3,4,6,8,15,19,20 Limited data indicate that topical azelaic acid also may be as effective as oral tetracycline hydrochloride in the management of acne vulgaris.2,3,11,13,19 A decrease in the number of inflammatory lesions occurs in most patients within 1-2 months of topical azelaic acid therapy,1,2,11,12,14,15,16,19 although maximum benefit generally requires more prolonged treatment.2,13
Rosacea
Azelaic acid 15% gel is used topically for the treatment of inflammatory lesions (papules and pustules) associated with mild to moderate rosacea in adults.22 In 2 clinical studies in adults with mild to moderate papulopustular rosacea, therapy with azelaic acid 15% gel (applied twice daily for 12 weeks) resulted in a 50-58% reduction in the number of papules and pustules compared with a 38-40% reduction in patients receiving vehicle alone.22 Patients were instructed to avoid spicy foods, thermally hot foods and drinks, and alcoholic beverages during the treatment period, as well as to use only very mild soaps or soapless cleansing lotion for facial cleaning.22 Azelaic acid 20% cream also has been used with some success in the treatment of papulopustular rosacea†.23,24,25
Dosage and Administration ⬆ ⬇
Administration
Azelaic acid is applied topically to the skin as a 20% cream or 15% gel.1,2,3,5,7,8,10,11,12,13,14,15,17,22,26 Prior to application of the cream or gel, the affected areas should be cleansed and dried.1,22,26 The cream or gel is then applied and massaged gently into the affected areas.1,22,26 Occlusive dressings or wrappings should not be used, and hands should be washed after applying the cream or gel.1,22,26 Cosmetics may be applied to the skin after the gel has dried.22,26 The cream or gel should not be applied to the eye.1,22,26 In addition, contact with the mouth, eyes, and other mucous membranes should be avoided.1,22,26 If contact with the eye(s) occurs, the eye(s) should be washed with large amounts of water;1,22,26 patients should consult a clinician if ocular irritation persists.1,22,26
The manufacturer states that patients receiving azelaic acid gel for the treatment of rosacea should be instructed to avoid spicy foods, thermally hot foods and drinks, and alcoholic beverages and to use only very mild soaps or soapless cleansing lotions for facial cleaning during therapy with the drug.22
Skin irritation (e.g., pruritus, burning, stinging) may occur during the initial weeks of therapy with azelaic acid cream or gel; if irritation is excessive or persists, the drug should be discontinued and the clinician should be contacted.1,22,26 Patients with dark complexions should be monitored for early signs of hypopigmentation during azelaic acid therapy.1,22,26
Dosage
The manufacturer states that safety and efficacy of azelaic acid cream in children younger than 12 years of age have not been established.1 The manufacturer states that safety and efficacy of azelaic acid gel in pediatric patients have not been established.22
Acne Vulgaris
For the topical treatment of acne vulgaris, a thin film of azelaic acid 20% cream should be applied to the cleansed affected area twice daily (morning and evening).1,26 Improvement usually is detectable within 1-2 months of topical therapy with the drug.1,2,11,14,15,16,19 Optimum duration of therapy depends on the severity of the acne.1,2,15,16,26 Although most reported experiences to date have been for treatment periods that did not exceed 6 months,2,19 topical azelaic acid therapy has been used for up to a year or longer in appropriately selected cases for control of individual lesions,19 and repeat courses have been employed for recurrences.19 however, some clinicians suggest that treatment with azelaic acid should not exceed 6 months.2,9
Rosacea
For the treatment of rosacea, a thin layer of azelaic acid 15% gel should be applied to the affected area twice daily (morning and evening).22 The manufacturer states that safety and efficacy of therapy with azelaic acid gel have not been established beyond 12 weeks.22
Other Information ⬆ ⬇
Description
Azelaic acid is a naturally occurring aliphatic dicarboxylic acid that exhibits various dermatologic effects including antibacterial and antiproliferative activity.1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,19,20
The exact mechanism of action of topically applied azelaic acid in the treatment of acne vulgaris has not been fully elucidated; however, the effect appears to result partly from the antibacterial activity of the drug.1,2,3,4,5,6,7,9,10,11,12,13,14,15,17,19,20 Azelaic acid inhibits the growth of susceptible organisms (principally Propionibacterium acnes )1,2,4,5,7,10,11,13,14,16,17,19,20 on the surface of the skin by inhibiting protein synthesis.1,2,7,10,11,19,20 In addition, the drug also may inhibit follicular keratinization,20 which may prevent development or maintenance of comedones.1,2,12,14,19 Azelaic acid usually is bacteriostatic in action, but may be bactericidal in high concentrations against P. acnes and Staphylococcus epidermidis .2,5,7,19 Azelaic acid also exhibits antiproliferative effects against hyperactive and abnormal melanocytes but does not exhibit an appreciable depigmenting effect on normally pigmented skin.9
The precise mechanism(s) of action of topically applied azelaic acid in the treatment of rosacea is unknown.22
Additional Information
The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.
Preparations ⬆ ⬇
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Azelaic Acid
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|
Topical | Cream | 20% | Azelex® | Allergan |
| Gel | 15% | Finacea® | Intendis |
Copyright ⬆ ⬇
AHFS® Drug Information. © Copyright, 1959-2024, Selected Revisions May 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
References ⬆
1. Allergan, Inc. Azelex® (azelaic acid cream 20%) prescribing information. Irvine, CA; 1999 Mar.
2. Anon. Azelaic acid—a new topical treatment for acne. Drug Ther Bull . 1993; 31:50-2. [PubMed 8344141]
3. Millikan LE, Shrum JP. An update on common skin diseases: acne, psoriasis, contact dermatitis, and warts. Postgrad Med . 1992; 91:96,98,101-104,107-110,115. [PubMed 1533716]
4. Murphy GM, Greaves MW. Acne and psoriasis. BMJ . 1988; 296:546-8. [PubMed 2964889][PubMedCentral]
5. Leeming JP, Holland KT, Bojar RA. The in vitro antimicrobial effect of azelaic acid. Br J Dermatol . 1986; 115:551-6. [PubMed 2947607]
6. Anon. Acne vulgaris. Int Pharm J . 1995; 9:11-3.
7. Bojar RA, Cutcliffe AG, Graupe K et al. Follicular concentrations of azelaic acid after a single topical application. Br J Dermatol . 1993; 129:399-402. [PubMed 8217752]
8. Hung CW. A review of the drug treatment in acne vulgaris. Hong Kong Pharm J . 1994; 3:24-5,29.
9. Healy E, Simpson N. Acne vulgaris. BMJ . 1994; 308:831-3. [PubMed 8167492][PubMedCentral]
10. Gassmueller H, Graupe K, Orfanos CE. Azelaic acid and sebum excretion rate. Br J Dermatol . 1985; 113:800-2. [PubMed 2937439]
11. Bladon PT, Burke BM, Cunliffe WJ et al. Topical azelaic acid and the treatment of acne: a clinical and laboratory comparison with oral tetracycline. Br J Dermatol . 1986; 114:493-9. [PubMed 2938615]
12. Katsambas A, Graupe K, Stratigos J. Clinical studies of 20% azelaic acid cream in the treatment of acne vulgaris: comparison with vehicle and topical tretinoin. Acta Derm Venereol (Stockh) . 1989; 143(Suppl):35-9.
13. Hjorth N, Graupe K. Azelaic acid for the treatment of acne: a clinical comparison with oral tetracycline. Acta Derm Venereol (Stockh) . 1989; 143(Suppl):45-8.
14. Cunliffe WJ, Holland KT. Clinical and laboratory studies on treatment with 20% azelaic acid cream for acne. Acta Derm Venereol (Stockh) . 1989; 143(Suppl):31-4.
15. Cavicchini S, Caputo R. Long-term treatment of acne with 20% azelaic acid cream. Acta Derm Venereol (Stockh) . 1989; 143(Suppl):40-4.
16. Nazzaro-Porro M, Passi S, Picardo M et al. Beneficial effect of 15% azelaic acid cream on acne vulgaris. Br J Dermatol . 1983; 109:45-8. [PubMed 6222755]
17. Breathnach AS, Nazzaro-Porro M, Passi S. Azelaic acid. Br J Dermatol . 1984; 111:115-20. [PubMed 6234914]
18. Hurwitz S. Acne vulgaris. Current concepts of pathogenesis and treatment. Am J Dis Child . 1979; 133:536-44. [PubMed 155397]
19. Fitton A, Goa KL. Azelaic acid: a review of its pharmacological properties and therapeutic efficacy in acne and hyperpigmentary skin disorders. Drugs . 1991; 41:780-98. [PubMed 1712709]
20. Anon. Azelaic acid—a new topical drug for acne. Med Lett Drugs Ther . 1996; 38:52-3. [PubMed 8637482]
21. Pharmacia & Upjohn, Kalamazoo, MI. Personal communication.
22. Berlex Laboratories. Finacea® (azelaic acid) gel 15% prescribing information. Montville, NJ; 2003 Jan.
23. Rebora A. The management of rosacea. Am J Clin Dermatol . 2002; 3:489-96. [PubMed 12180896]
24. Maddin S. A comparison of topical azelaic acid 20% cream and topical metronidazole 0.75% cream in the treatment of patients with papulopustular rosacea. J Am Acad Dermatol . 1999; 40:961-5. [PubMed 10365928]
25. Bjerke R, Fyrand O, Graupe K. Double-blind comparison of azelaic acid 20% cream and its vehicle in treatment of papulo-pustular rosacea. Acta Derm Venereol . 1999; 79:456-9. [PubMed 10598760]
26. Berlex Laboratories. Finevin® (azelaic acid) cream 20% prescribing information. Wayne, NJ; 2002 Mar.