Azelaic Acid Cream

Name: Azelaic Acid Cream

Description

AZELEX (azelaic acid cream) 20% contains azelaic acid, a naturally occurring saturated dicarboxylic acid.

Structural Formula: HOOC-(CH2)7-COOH.
Chemical Name: 1,7-heptanedicarboxylic acid
Empirical Formula: C9H16O4
Molecular Weight: 188.22

Active Ingredient: Each gram of AZELEX contains azelaic acid..........0.2 gm (20% w/w).

Inactive Ingredients: cetearyl octanoate; glycerin; glyceryl stearate and cetearyl alcohol and cetyl palmitate and cocoglycerides; PEG-5 glyceryl stearate; propylene glycol; and purified water. Benzoic acid is present as a preservative.

How supplied

AZELEX (azelaic acid cream) Cream is supplied in a closed orifice tube with a white, spiked screwcap in the following sizes:

30 g - NDC 0023-8694-30
50 g - NDC 0023-8694-50

Note: Protect from freezing. Store product on its side.

Store between 15° - 30° C (59° - 86° F).

Distributed by: Allergan, Inc., Irvine, California 92612, U.S.A. Made in Italy. FDA Rev date: 6/10/2003

Clinical pharmacology

The exact mechanism of action of azelaic acid is not known. The following in vitro data are available, but their clinical significance is unknown. Azelaic acid has been shown to possess antimicrobial activity against Propionibacterium acnes and Staphylococcus epidermidis. The antimicrobial action may be attributable to inhibition of microbial cellular protein synthesis.

A normalization of keratinization leading to an anticomedonal effect of azelaic acid may also contribute to its clinical activity. Electron microscopic and immunohistochemical evaluation of skin biopsies from human subjects treated with AZELEX (azelaic acid cream) Cream demonstrated a reduction in the thickness of the stratum corneum, a reduction in number and size of keratohyalin granules, and a reduction in the amount and distribution of filaggrin (a protein component of keratohyalin) in epidermal layers. This is suggestive of the ability to decrease microcomedo formation.

Pharmacokinetics

Following a single application of AZELEX (azelaic acid cream) Cream to human skin in vitro, azelaic acid penetrates into the stratum corneum (approximately 3 to 5% of the applied dose) and other viable skin layers (up to 10% of the dose is found in the epidermis and dermis). Negligible cutaneous metabolism occurs after topical application. Approximately 4% of the topically applied azelaic acid is systemically absorbed. Azelaic acid is mainly excreted unchanged in the urine but undergoes some β-oxidation to shorter chain dicarboxylic acids. The observed half-lives in healthy subjects are approximately 45 minutes after oral dosing and 12 hours after topical dosing, indicating percutaneous absorption rate-limited kinetics.

Azelaic acid is a dietary constituent (whole grain cereals and animal products), and can be formed endogenously from longer-chain dicarboxylic acids, metabolism of oleic acid, and ψ-oxidation of monocarboxylic acids. Endogenous plasma concentration (20 to 80 ng/mL) and daily urinary excretion (4 to 28 mg) of azelaic acid are highly dependent on dietary intake. After topical treatment with AZELEX (azelaic acid cream) Cream in humans, plasma concentration and urinary excretion of azelaic acid are not significantly different from baseline levels.

Uses of Azelaic Acid Cream

  • It is used to treat pimples (acne).

What are some things I need to know or do while I take Azelaic Acid Cream?

  • Tell all of your health care providers that you take azelaic acid cream. This includes your doctors, nurses, pharmacists, and dentists.
  • It may take several weeks to see the full effects.
  • If you use this medicine too often, your skin problem may become worse.
  • Use of other skin products while using azelaic acid cream may cause more irritation.
  • Talk with your doctor before you use other drugs or products on your skin.
  • It is common to have skin irritation with this medicine. Skin irritation may include burning, itching, or stinging. Most of the time, skin irritation happened during the first few weeks after starting azelaic acid cream. Call your doctor if you have skin irritation that is very bad, bothers you, or does not go away.
  • If you have asthma, use this medicine with care. Worsening of asthma has happened in people using azelaic acid cream. Call your doctor right away if your asthma gets worse while you use this medicine.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using azelaic acid cream while you are pregnant.
  • Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

How do I store and/or throw out Azelaic Acid Cream?

  • Store at room temperature. Do not freeze.
  • Store in a dry place. Do not store in a bathroom.
  • Store this product on its side.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Check with your pharmacist about how to throw out unused drugs.

What is the most important information i should know about azelaic acid topical (azelex, finacea, finacea plus, finevin)?

You should not use this medication if you are allergic to azelaic acid or propylene glycol.

Avoid getting this medication in your eyes, nose, mouth, rectum, or vagina. Do not use on sunburned, windburned, dry, chapped, irritated, or broken skin. Wait until these conditions have healed before using this medication.

Do not cover the area after applying azelaic acid. Doing so could cause too much medicine to be absorbed by your body and could be harmful.

It may take up 4 weeks or longer before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve after 12 weeks of treatment.

If you have excessive burning, dryness, or irritation, ask your doctor about using azelaic acid once daily.

Side effects

During U.S. clinical trials with AZELEX (azelaic acid cream) Cream, adverse reactions were generally mild and transient in nature. The most common adverse reactions occurring in approximately 1-5% of patients were pruritus, burning, stinging and tingling. Other adverse reactions such as erythema, dryness, rash, peeling, irritation, dermatitis, and contact dermatitis were reported in less than 1% of subjects. There is the potential for experiencing allergic reactions with use of AZELEX Cream. In patients using azelaic acid formulations, the following additional adverse experiences have been reported rarely: worsening of asthma, vitiligo depigmentation, small depigmented spots, hypertrichosis, reddening (signs of keratosis pilaris), and exacerbation of recurrent herpes labialis.

Read the entire FDA prescribing information for Azelex (Azelaic Acid Cream)

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