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Azelaic Acid

Class: Skin and Mucous Membrane Agents, Miscellaneous
ATC Class: D10AX03
VA Class: DE752
Chemical Name: Nonanedioic acid
Molecular Formula: C9H16O4
CAS Number: 123-99-9
Brands: Azelex, Finacea

Introduction

Antibacterial and antiproliferative agent; naturally occurring aliphatic dicarboxylic acid.1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 19 20 22 26

Uses for Azelaic Acid

Acne

Treatment of mild to moderate inflammatory acne vulgaris.1 2 4 5 6 7 8 10 11 12 13 14 15 19 20 26

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Not for the treatment of noninflammatory acne vulgaris.21

Rosacea

Treatment of inflammatory lesions (papules and pustules) associated with mild to moderate rosacea.22

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

Azelaic Acid Dosage and Administration

Administration

Topical Administration

Apply 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

For dermatologic use only; avoid contact with eyes, mouth, or other mucous membranes.1 22 26 If contact with the eye(s) occurs, wash with large amounts of water; consult clinician if ocular irritation persists.1 22 26

Wash skin and pat dry before applying cream or gel to affected areas.1 22 26 Use only very mild soaps or soapless cleansing lotions before applying gel for treatment of rosacea.22 b

Apply in a thin layer of cream or gel and rub gently into affected areas.1 22 26 Wash hands after application.1 22 26

If irritation is excessive or persists in patients with acne, decrease frequency of application to once daily or discontinue until manifestations subside.1 22 26 a

If irritation is excessive or persists in patients with rosacea, discontinue therapy.1 22 26 b

Do not use occlusive dressings or wrappings.1 22 26

Allow gel to dry before applying cosmetics to skin.22 26

Dosage

Pediatric Patients

Acne
Topical

Adolescents ≥12 years of age: Apply 20% cream in a thin film to affected areas twice daily (morning and evening).1 26

Improvement usually is detectable within 1–2 months of initiating therapy;1 2 11 14 15 16 19 however, maximum benefit generally requires more prolonged treatment.2 13

Usual duration of therapy is ≤6 months;2 19 however, therapy for ≥1 year has been required for control of individual lesions2 19 and repeat courses have been used for recurrences.19

Adults

Acne
Topical

Apply 20% cream in a thin film to affected areas twice daily (morning and evening).1 26

Improvement usually is detectable within 1–2 months of initiating therapy;1 2 11 14 15 16 19 however, maximum benefit generally requires more prolonged treatment.2 13

Usual duration of therapy is ≤6 months;2 19 however, therapy for ≥1 year has been required for control of individual lesions2 19 and repeat courses have been used for recurrences.19

Rosacea
Topical

Apply 15% gel in a thin film to affected area twice daily (morning and evening).22

Safety and efficacy of therapy with gel for >12 weeks not established.22

Prescribing Limits

Pediatric Patients

Acne
Topical

Adolescents ≥12 years of age: Some clinicians suggest maximum 6 months of therapy;2 19 however, ≥1 year of therapy has been used in for control of individual lesions.19

Adults

Acne
Topical

Some clinicians suggest maximum 6 months of therapy;2 19 however, ≥1 year of therapy has been used in for control of individual lesions.19

Rosacea
Topical

Safety and efficacy of therapy with gel for >12 weeks not established.22

Special Populations

No special population dosage recommendations at this time.1

Cautions for Azelaic Acid

Contraindications

  • Known hypersensitivity to azelaic acid or any of its components.a b

  • Known hypersensitivity to propylene glycol (for gel formulation).b

Warnings/Precautions

Warnings

Hypopigmentation

Hypopigmentation reported rarely;a b monitor patients with dark complexions for early signs of hypopigmentation during therapy.1 22 26

General Precautions

Dermatologic Effects

Possible skin irritation (e.g., pruritus, burning, stinging) during initial weeks of therapy.1 22 26 If sensitivity or severe irritation develops, discontinue therapy, contact clinician, and institute appropriate therapy.1 22 26 a

Specific Populations

Pregnancy

Category B.a b

Lactation

Minimally distributed into milk following topical application.a b Caution if used in nursing women.a b

Pediatric Use

Safety and efficacy of 20% cream not established in children <12 years of age.a

Safety and efficacy of 15% gel not established.b

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.a b

Common Adverse Effects

20% cream: Pruritus, burning, stinging, tingling.a

15% gel: Pruritus, burning, stinging, tingling, scaling, dryness.b

Interactions for Azelaic Acid

No formal interaction studies to date.b

Azelaic Acid Pharmacokinetics

Absorption

Minimally absorbed following topical administration.a b

Elimination

Metabolism

Minimally metabolized following topical application; undergoes some β-oxidation to shorter chain dicarboxylic acids.a b

Elimination Route

Excreted principally in urine as unchanged drug.a b

Half-life

12 hours following topical application.a

Stability

Storage

Topical

Cream

15–30°C; do not freeze.a Keep container on its side.a

Gel

25°C (may be exposed to 15–30°C).b

Actions

  • Exact mechanism of action for treatment of acne vulgaris not fully elucidated; however, effect appears to result partially from antibacterial activity.1 2 3 4 5 6 7 9 10 11 12 13 14 15 17 19 20

  • Inhibits growth of susceptible organisms (principally Propionibacterium acnes)1 2 4 5 7 10 11 13 14 16 17 19 20 on skin by inhibiting protein synthesis.1 2 7 10 11 19 20

  • Usually bacteriostatic; may be bactericidal in high concentrations against P. acnes and Staphylococcus epidermidis2 5 7 19

  • May inhibit follicular keratinization,20 which may prevent development or maintenance of comedones.1 2 12 14 19

  • Exhibits antiproliferative effects against hyperactive and abnormal melanocytes but does not exhibit an appreciable depigmenting effect on normally pigmented skin.9

  • Exact mechanism of action for treatment of rosacea is unknown.22

Advice to Patients

  • Importance of using for full prescribed treatment period.a

  • Importance of avoiding contact with eyes, mouth, or other mucous membranes.1 22 26 a If contact with eyes occurs, wash eyes with large amounts of water and contact clinician if eye irritation persists.1 22 26 a

  • Importance of discontinuing therapy and consulting clinician if severe local irritation, severe itching, and/or rash occurs.1 22 26 a

  • Importance of washing hands following application.1 22 26 a

  • Importance of avoiding occlusive dressings.1 22 26 a

  • Importance of reporting abnormal changes in skin color to a clinician.a b

  • Importance of patients being treated for rosacea avoiding foods or beverages that may cause flushing or blushing, such as spicy foods, alcoholic beverages, and thermally hot drinks.22 b

  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.a b

  • Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs.a b

  • Importance of informing patients of other important precautionary information.a b (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Azelaic Acid

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Cream

20%

Azelex (with propylene glycol)

Allergan

Gel

15%

Finacea (with propylene glycol)

Berlex

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Azelex 20% Cream (ALLERGAN DERMATOLOGICS): 30/$196.00 or 90/$557.95

Azelex 20% Cream (ALLERGAN DERMATOLOGICS): 50/$292.98 or 150/$833.94

Finacea 15% Gel (INTENDIS): 50/$178.49 or 150/$499.96

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions May 1, 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

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. [IDIS 297300] [PubMed 1533716]

4. Murphy GM, Greaves MW. Acne and psoriasis. BMJ. 1988; 296:546-8. [IDIS 238904] [PubMed 2964889]

5. Leeming JP, Holland KT, Bojar RA. The in vitro antimicrobial effect of azelaic acid. Br J Dermatol. 1986; 115:551-6. [IDIS 227852] [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. [IDIS 320947] [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. [IDIS 327706] [PubMed 8167492]

10. Gassmueller H, Graupe K, Orfanos CE. Azelaic acid and sebum excretion rate. Br J Dermatol. 1985; 113:800-2. [IDIS 210213] [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. [IDIS 215156] [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. [IDIS 173449] [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. [IDIS 429924] [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.

a. Allergan, Inc. Azelex (azelaic acid cream 20%) prescribing information. Irvine, CA; 2003 Jun.

b. Berlex Laboratories. Finacea (azelaic acid) gel 15% prescribing information. Montville, NJ; 2005 Apr.

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