Azelec

Approved Indications:

• Acne Vulgaris:
  Mild to moderate inflammatory and non-inflammatory acne. Azelaic acid is used topically to reduce acne lesions and comedones.
• Rosacea (Papulopustular subtype):
  Treatment of inflammatory papules and pustules associated with rosacea.
• Hyperpigmentation Disorders:
  Including melasma, post-inflammatory hyperpigmentation (PIH), and solar lentigines. Used as a skin-lightening agent.

Clinically Accepted Off-label Uses:

• Keratosis pilaris
• Seborrheic dermatitis
• Perioral dermatitis (adjunct therapy)
• Prevention and treatment of post-inflammatory hyperpigmentation in darker skin types.

Formulations:
Available as topical gels, creams, foam, and sometimes as a foam spray.

Typical Dosing:

• Acne & Rosacea:
• Apply 15% to 20% azelaic acid gel or cream twice daily to affected areas.
• Duration: Minimum of 6 weeks; often continued for 12 weeks or longer based on clinical response.
• Hyperpigmentation:
• Usually 15–20% azelaic acid cream applied twice daily.
• Treatment may continue for several months (up to 6 months) for visible improvement.

Special Populations:

• Pediatrics:
• Generally safe for use in children aged 12 years and above for acne.
• Elderly:
• No specific dose adjustment required; tolerability generally good.
• Application Instructions:
• Cleanse and dry skin before application.
• Apply a thin layer to the entire affected area, not just individual lesions.
• Avoid contact with eyes, mouth, and mucous membranes.

Azelaic acid is a naturally occurring dicarboxylic acid with antimicrobial, anti-inflammatory, and keratolytic properties. It selectively inhibits mitochondrial oxidoreductase enzymes in Propionibacterium acnes (now Cutibacterium acnes), reducing bacterial proliferation. It normalizes keratinization by inhibiting abnormal follicular epithelial differentiation and keratinocyte hyperproliferation, which reduces comedone formation. Azelaic acid also exerts tyrosinase inhibition, which decreases melanin production, thereby reducing hyperpigmentation. Its anti-inflammatory effects help reduce erythema in rosacea and acne.

• Absorption:
  Minimal systemic absorption (<4%) after topical application.
• Distribution:
  Primarily remains localized within the epidermis and upper dermis.
• Metabolism:
  Metabolized by the skin and possibly systemic esterases after minimal absorption.
• Elimination:
  Negligible systemic exposure; thus, elimination kinetics are not clinically relevant.
• Onset of Action:
  Clinical improvements in acne and rosacea typically observed within 4 to 8 weeks of therapy.

• Pregnancy:
  Classified as Category B by the FDA. Animal studies have shown no evidence of teratogenicity or fetal harm. However, well-controlled human studies are lacking. Use during pregnancy is generally considered safe when clinically necessary.
• Lactation:
  Due to minimal systemic absorption, azelaic acid is considered compatible with breastfeeding. No adverse effects reported in nursing infants.
• Caution:
  Always use under medical supervision during pregnancy and lactation.

• Primary Therapeutic Class: Topical Anti-acne Agent
• Subclass: Dicarboxylic Acid Derivative with Antimicrobial and Keratolytic properties.

• Known hypersensitivity to azelaic acid or any formulation excipients.
• Open or severely damaged skin at the application site.
• Concurrent use with other topical products that cause severe irritation (unless under physician supervision).

• May cause skin irritation, burning, stinging, or itching, especially during initial weeks of treatment.
• Avoid contact with eyes, mouth, and mucous membranes.
• Use cautiously in patients with eczema, atopic dermatitis, or very sensitive skin.
• Discontinue if severe irritation or allergic reaction occurs.
• Protect skin from excessive sun exposure; use sunscreen as azelaic acid can increase photosensitivity.
• Not for oral or ophthalmic use.

Common Side Effects:

• Mild burning sensation
• Pruritus (itching)
• Dryness
• Erythema (redness)
• Scaling or peeling

Less Common / Rare Side Effects:

• Contact dermatitis
• Hypersensitivity reactions (rash, swelling)
• Hyperpigmentation or hypopigmentation (rare)

Severity & Timing:
Side effects are usually mild to moderate, occurring early during treatment, and often improve with continued use.

• No significant systemic drug interactions due to minimal absorption.
• Concurrent use with other topical products causing irritation (e.g., retinoids, benzoyl peroxide, salicylic acid) may increase local irritation.
• Avoid combining with skin irritants unless advised by a physician.

• Updated acne management guidelines increasingly recommend azelaic acid as a first-line or adjunctive topical therapy due to favorable safety and tolerability profiles.
• Newer foam formulations approved, offering improved skin penetration and patient compliance.
• Recognized for effective use in skin of color to minimize post-inflammatory hyperpigmentation.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from excessive moisture and heat.
• Keep container tightly closed when not in use.
• Avoid freezing or exposure to direct sunlight.
• Use within the expiration date printed on the package.