azelaic acid (Rx)

>10%

Burning/ stinging/ tingling (4-16%)

1-10%

Pruritus (1-6%)

Scaling/ dry skin/ xerosis (1-5%)

Erythema/ irritation (1-2%)

<1%

Contact dermatitis

Edema

Acne

Postmarketing Reports

Facial burning

Irritation

Iridocyclitis after accidental exposure

Hypersensitivity reactions including angioedema, eye swelling, facial swelling, urticaria (revised)

Worsening of asthma, dyspnea, wheezing

Contraindications

Hypersensitivity to azelaic acid, propylene glycol or any of its components

Cautions

In case of known hypersensitivity to any component of the gel, avoid the use of gel dosage form; if hypersensitivity develops during treatment, discontinue and institute appropriate therapy

For dermatologic use only

Therapy has been reported to cause irritation of eyes; avoid contact with eyes and mucous membranes

Isolated cases of hypopigmentation reported after azelaic acid use; monitor patients with dark complexion for early signs of hypopigmentation

Skin irritation (i.e. pruritus, burning or stinging) may occur, usually during first few weeks of treatment; if sensitivity or severe irritation develops and persists, discontinue treatment and institute appropriate therapy

Do not wax treated area or apply topical products that may further irritate skin (eg, astringents, abrasive soaps and cleansers, exfoliants)

Avoid any foods and beverages that provoke erythema, flushing, and blushing (eg, alcoholic beverages, spicy food, hot drinks such as hot coffee and tea)

Report any abnormal changes in skin color to physician

Avoid use of occlusive dressings or wrappings

Wash hands after applying the cream

Worsening of asthma reported; consult a physician if asthma is exacerbated with therapy

Pregnancy

Azelaic acid is minimally absorbed systemically following topical route of administration; maternal use not expected to result in fetal exposure to drug

Animal data

• In animal reproduction studies, embryofetal toxicity was noted when azelaic acid was administered orally during period of organogenesis at doses 162, 19, and 65 times maximum recommended human dose (MRHD) in rats, rabbits, and monkeys, respectively; maternal toxicity was noted at these doses but no malformations were observed in these embryofetal developmental studies

Lactation

Azelaic acid is naturally present in human milk; when used as prescribed, azelaic acid is unlikely to be absorbed through skin in clinically relevant amounts to cause a change in azelaic acid concentration in milk or milk production; therefore, breastfeeding is not expected to result in exposure of infant to drug

The developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for drug and any potential adverse effects on breastfed child from drug or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Azelaic acid is an antibacterial agent that inhibits the growth of susceptible organisms (principally Propionibacterium acnes) on the surface of the skin by inhibiting protein synthesis; may also inhibit follicular keratinization, which prevents development or maintenance of comedones

Mechanism by which it interferes with pathogenic events in rosacea is unknown

Pharmacokinetics

Half-Life: 12 hours

Absorption: systemic (4%)

Metabolism: Negligible cutaneous metabolism

Excretion: Unchanged in urine