Azelaic Acid

Azelaic acid is a prescription medication used to treat acne and rosacea.

Azelaic acid belongs to a group of drugs called carboxylic acids. These work by killing the bacteria that infect pores and by decreasing the production of keratin. Too much keratin can cause rosacea.

This medication comes in cream and gel forms and is usually applied to the skin two times a day. The cream is indicated for the treatment of mild-to-moderate acne and the gel is indicated for mild-to-moderate rosacea.

Common side effects of azelaic acid include itching, burning, stinging, and tingling of the skin.

Azelaic Acid is part of the drug class:

• Other anti acne preparations for topical use

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X - are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Azelaic acid falls into category B. There are no well-done studies that have been done in humans with azelaic acid. In animal studies, pregnant animals were given this medication, and the babies did not show any medical issues related to this medication.

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if azelaic acid crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using azelaic acid.

Use azelaic acid exactly as prescribed.

Azelaic acid comes in gel and cream forms and is usually applied to the skin two times every day, in the morning and in the evening.

Before applying azelaic acid, wash the affected skin with water and mild soap or cleanser and pat dry with a soft towel. Apply a thin layer of cream or gel to the affected skin. Gently massage it into the skin. Do not get azelaic acid in your eyes or mouth. If you get azelaic acid in your eyes, wash thoroughly with water and call your doctor if your eyes are irritated.

Do not cover the affected skin with bandages, dressings, or wraps. You may apply non-irritating cosmetics after the cream or gel is dry.

Wash your hands after handling azelaic acid.

If you miss a dose, apply the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and apply your next dose at the regular time. Do not apply two doses of azelaic acid at the same time.

Serious side effects have been reported with the use of azelaic acid including the following:

• Skin irritation. Though this is likely to occur early on, if skin irritation is excessive or persistent, it is necessary to contact you provider right away if you have some or all of the following symptoms of skin irritation
  • rash
  • itching
  • burning
  • stinging
• Hypopigmentation. Skin discoloration may occur with the use of azelaic acid.

Do not use azelaic acid if you are allergic to azelaic acid or to any of its ingredients.

Before using azelaic acid, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to azelaic acid or to any of its ingredients
• are pregnant or plan to become pregnant
• are breastfeeding

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

If you use too much azelaic acid, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

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

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

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

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

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

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

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

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

Special Populations

No special population dosage recommendations at this time.1

• 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.)

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Cream, External:

Azelex: 20% (30 g, 50 g)

Foam, External:

Finacea: 15% (50 g) [contains benzoic acid, cetostearyl alcohol, polysorbate 80, propylene glycol]

Gel, External:

Finacea: 15% (50 g) [contains benzoic acid, disodium edta, polysorbate 80, propylene glycol]

Azelaic acid is a dietary constituent normally found in whole grain cereals; can be formed endogenously. Exact mechanism is not known. In vitro, azelaic acid possesses antimicrobial activity against Cutibacterium acnes and Staphylococcus epidermidis. May decrease microcomedo formation.

Absorption

Cream: ~3% to 5% penetrates stratum corneum; up to 10% found in epidermis and dermis; 4% systemic

Metabolism

Negligible after topical application; some beta-oxidation to shorter chain dicarboxylic acids

Excretion

Urine (primarily as unchanged drug)

If the patient experiences skin irritations that persist beyond 2-4 weeks, a once a day application may be tried.

No adjustment recommended