azelaic acid

Azelaic acid is an acid naturally present in whole grains such as wheat, barley, and rice, and is also produced by Malassezia furfur, a species of yeast that normally lives on human skin. 

Azelaic acid is commercially produced to treat skin conditions such as acne vulgaris, which causes pimples, bumps, pustules, cysts, and whiteheads or blackheads (comedones), and rosacea, a disorder that causes flushing and red bumps on the skin.

The exact mechanism of azelaic acid in the treatment of rosacea is not clear. Azelaic acid’s anti-inflammatory and antioxidant properties likely help clear the rosacea lesions. Azelaic acid appears to work in several ways in the treatment of acne vulgaris:

• Inhibits protein synthesis and growth of bacteria that cause acne, especially Staphylococcus epidermidis and Propionibacterium acnes.
• Reduces the secretion of sebum, the oily substance produced by sebaceous glands in the skin, and keeps the pores of the skin clear.
• Reduces the formation of keratin, a fibrous protein in the skin that is a contributing factor to acne.
• Reduces inflammation in the follicular area and also scavenges free radicals (reactive oxygen species), unstable molecules in cells that damage tissue.

• Do not use azelaic acid in patients with known hypersensitivity to any of the components in the formulation.
• Azelaic acid is intended for external use only, not for oral, ophthalmic, or intravaginal use.
• Azelaic acid may cause hypersensitivity reactions such as facial swelling, breathing difficulties, hives, or other skin reactions. Monitor patients and discontinue use in patients who develop such reactions.
• Skin irritation may occur in the first weeks of treatment. If irritation persists or becomes severe, discontinue azelaic acid.
• Azelaic acid may cause loss of skin pigmentation. Monitor for early signs of hypopigmentation, particularly in patients with dark complexions.
• Reassess the use of azelaic acid gel if no improvement is seen after 12 weeks of therapy.
• Azelaic acid may exacerbate asthma. Use with caution in patients with asthma.
• Some formulations may contain polysorbate 80. Avoid the use of these formulations in patients with hypersensitivity to polysorbate 80.
• Some formulations may contain propylene glycol which can be toxic in large amounts.

Common side effects of azelaic acid include:

• Application site reactions, including:
  • Burning
  • Tingling
  • Stinging
  • Pain
  • Itching (pruritus)
  • Dryness
  • Redness
  • Tightness
  • Scaling
  • Peeling
  • Irritation
• Skin rash
• Contact dermatitis
• Acne vulgaris

Less common side effects of azelaic acid include:

• Exacerbation of asthma or wheezing
• Hypersensitivity reactions, including:
  • Eye swelling
  • Facial swelling
  • Swelling under the skin and mucous membranes (angioedema)
  • Hives (urticaria)
• Facial burning and irritation
• Follicular rash (keratosis pilaris)
• Excessive hair growth (hypertrichosis)
• Reduced pigmentation (hypopigmentation)
• Loss of pigmentation in patches (vitiligo)
• Small depigmented spots
• Exacerbation or recurrence of herpes labialis
• Irritation in the eye and inflammation of the iris and ciliary muscle in the eye (iridocyclitis) with drug exposure to the eye

Call your doctor immediately if you experience any of the following symptoms or serious side effects while using this drug:

• Serious heart symptoms include fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness;
• Severe headache, confusion, slurred speech, severe weakness, vomiting, loss of coordination, feeling unsteady;
• Severe nervous system reaction with very stiff muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, and feeling like you might pass out; or
• Serious eye symptoms include blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.

Cream

• 20% (Azelex)

Gel

• 15% (Finacea)

Foam

• 15% (Finacea)

Adult:

Rosacea

• Treatment of inflammatory papules and pustules of mild to moderate rosacea
• Finacea: Massage a thin layer into the affected areas on the face every 12 hours

Adult and Pediatric

Acne Vulgaris

Children below 12 years

• Safety and efficacy not established

Adults and children above 12 years

• Azelex: Massage a thin layer into the affected areas on the face every 12 hours

Administration

• Cleanse the affected area with mild soap or soapless cleansing lotion and pat dry before applying
• Reassess if no improvement after 12 weeks of therapy

Overdose

• Excessive topical use of azelaic acid may cause skin irritation.
• Oral ingestion of azelaic acid may be toxic. Overdose treatment involves discontinuation of the drug and symptomatic and supportive care.

Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.

• Azelaic Acid has no known severe, serious, moderate, or mild interactions with other drugs.

The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.

It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.

• Animal reproductive studies did not show evidence of fetal harm with the use of azelaic acid, however, there are no adequate and well-controlled studies in pregnant women. Topical use of azelaic acid is unlikely to result in significant systemic absorption and may be used during pregnancy if potential maternal benefits justify potential fetal risks.
• Azelaic acid is naturally present in breastmilk. Systemic absorption from appropriate topical use of azelaic acid is minimal and unlikely to increase the baseline azelaic acid levels in breastmilk. Nevertheless, azelaic acid should be used with caution in nursing mothers and the decision to breastfeed during therapy should be made after considering the importance of therapy to the mother and the risk for exposure to the breastfed infant.

• Use azelaic acid exactly as prescribed. Wash your hands thoroughly after applying the medication.
• Do not use occlusive bandages or dressings over the treated area.
• Avoid contact with eyes and mucous membranes. In case of accidental contact with the eyes, flush out the eyes with clean water and check with your physician if the irritation persists.
• Avoid foods and beverages that cause flushing, blushing, or redness, such as alcohol, spicy or hot food, and drinks.
• Do not wax the treated area or apply other topical products that can further irritate the skin.
• Discontinue use and report to your physician if you:
  • Experience hypersensitivity reactions such as facial swelling, breathing difficulties, hives, or other skin reactions
  • Develop skin irritation that persists after the initial weeks of therapy
  • Notice changes in skin color
  • Find your asthma symptoms are worse
• Azelaic acid foam contains flammable propellants. Keep away from fire and flame.
• Store azelaic acid safely out of reach of children.
• In case of ingestion or overdose, seek medical help or contact Poison Control.