Azelaic Acid

Uses

Azelaic acid is used for acne vulgaris, rosacea.

Azelaic Acid is also used to associated treatment for these conditions: Acne Vulgaris, Inflammatory lesions caused by rosacea, Susceptible Bacterial Infections, Nutritional supplementation

How Azelaic Acid works

The exact mechanism of action of azelaic acid is not known. It is thought that azelaic acid manifests its antibacterial effects by inhibiting the synthesis of cellular protein in anaerobic and aerobic bacteria, especially Staphylococcus epidermidis and Propionibacterium acnes. In aerobic bacteria, azelaic acid reversibly inhibits several oxidoreductive enzymes including tyrosinase, mitochondrial enzymes of the respiratory chain, thioredoxin reductase, 5-alpha-reductase, and DNA polymerases. In anaerobic bacteria, azelaic acid impedes glycolysis. Along with these actions, azelaic acid also improves acne vulgaris by normalizing the keratin process and decreasing microcomedo formation. Azelaic acid may be effective against both inflamed and noninflamed lesions. Specifically, azelaic acid reduces the thickness of the stratum corneum, shrinks keratohyalin granules by reducing the amount and distribution of filaggrin (a component of keratohyalin) in epidermal layers, and lowers the number of keratohyalin granules.

Dosage

Azelaic Acid dosage

Acne vulgaris:

• Adult: As 20% cream or 15% gel: Apply thinly into the affected areas bid (morning and evening) after cleansing. Improvement may be detectable w/n 4 wk. Duration of treatment: Up to 6 mth.
• Child: ≥12 yr Same as adult dose.

Rosacea:

• Adult: As 15% gel: Apply thinly into the affected areas bid (morning and evening). Improvement occurs in 4-8 wk.
• Child: ≥12 yr Same as adult dose.

Side Effects

Burning, erythema, stinging, pruritus, dryness and scaling, peeling, irritation, dermatitis, hypopigmentation, rash, and photosensitivity. Rarely, exacerbation of asthma.

Toxicity

Oral LD50 in rat: >5 g/kg

Precaution

Patient with sensitive skin. Not intended for application to broken, sunburnt or eczematous skin. Avoid use of occlusive dressing or wrappings. Pregnancy and lactation.

Interaction

Avoid spicy foods, alcoholic beverages and hot drinks that might provoke erythema, flushing and blushing during treatment of rosacea.

Food Interaction

• Avoid alcohol. Alcohol may cause flushing; therefore, it may worsen rosacea.
• Take with or without food. Food and drink, which have a high temperature or are spicy, may exacerbate flushing and rosacea, avoid if possible.

Elimination Route

Approximately 4% of the topically applied azelaic acid is systemically absorbed.

Half Life

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.

Elimination Route

Azelaic acid is mainly excreted unchanged in the urine, but undergoes some ß-oxidation to shorter chain dicarboxylic acids.

Pregnancy & Breastfeeding use

Pregnancy Category B. Either animal-reproduction studies have not demonstrated a fetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Contraindication

azelaic acid cream is contraindicated in individuals who have shown hypersensitivity to any of its components.

Storage Condition

Store between 15-30° C.

Innovators Monograph

You find simplified version here Azelaic Acid