Generic name and strength

Azelex Cream, 20% w/w (equivalent to 20 mg/g) is a white to off-white cream.

Inactive ingredients

  • carbomer 940
  • ceteareth-20
  • cetearyl alcohol
  • citric acid anhydrous
  • cyclomethicone 5 and dimethicone 350
  • glycerin
  • glyceryl stearate SE
  • methylparaben 0.3%
  • polyethylene glycol 400 monostearate
  • propylene glycol
  • Purified Water USP
  • sodium hydroxide solution

Azelex is a topical cream used to treat acne. It works by reducing the production of sebum, the oily substance that can clog pores and lead to breakouts. Azelex is available by prescription only and should be used as directed by your doctor.

Azelex is most effective when used in combination with other acne treatments, such as Benzaclin or Retin-A. When used alone, Azelex may take up to eight weeks to see results.

Azelex is a safe and effective acne treatment for most people. However, as with any medication, there is always the potential for side effects. Be sure to talk to your doctor about any concerns you may have before starting treatment with Azelex.

Pharmacokinetics

Azelex is rapidly absorbed following topical application with mean peak plasma concentrations of nordazepam and its active metabolite desmethyldiazepam occurring within 3 hours. Nordazepam and desmethyldiazepam are both highly bound to plasma proteins (>99%), whereas their respective glucuronides are only moderately bound (60-70%).

The elimination half-lives of nordazepam and desmethyldiazepam are about 50 hours and 100 hours, respectively. Both nordazepam and desmethyldiazepam are extensively metabolized, with less than 1% of the dose excreted unchanged in the urine. The primary route of metabolism for both compounds is through conjugation with glucuronic acid.

The pharmacokinetics of Azelex are similar in men and women.

Indications

Azelex is indicated for the treatment of acne vulgaris.

Contraindications

Azelex is contraindicated in patients with a known hypersensitivity to any of the ingredients in the formulation.

Warnings and Precautions

Avoid contact with the eyes, lips, and mucous membranes. If contact occurs, flush thoroughly with water.

If excessive skin irritation develops, discontinue use and consult a healthcare professional.

Pregnancy: Teratogenic Effects. Pregnancy Category C. Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Azelex is administered to a nursing woman.

Pediatric Use: Safety and efficacy have not been established in children below the age of 12.

Geriatric Use: Clinical studies of Azelex did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Adverse reactions

The most common adverse reaction (incidence ≥ 1%) reported with Azelex Cream is dry skin.

The following additional local adverse reactions have been reported with topical retinoids: erythema, scaling, pruritus, burning/stinging, and contact dermatitis. These reactions do not necessarily occur in every patient treated with Azelex Cream but have been reported in clinical trials and/or postmarketing reports. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to estimate reliably their frequency or establish a causal relationship to drug exposure:

  • Body as a Whole – Generalized allergic reaction, application site reaction (including application site edema)
  • Cardiovascular System – Hypertension
  • Digestive System – Gastroenteritis, nausea, vomiting
  • Hemic and Lymphatic System – Ecchymosis
  • Metabolic and Nutritional Disorders – Peripheral edema
  • Nervous System/Psychiatric – Dizziness, headache, insomnia
  • Respiratory System – Pharyngitis, rhinitis
  • Skin and Appendages – Alopecia, contact dermatitis, erythema, exfoliation, peeling skin, photosensitivity reaction, pruritus, skin reaction (including erythema multiforme), urticaria.

Side Effects

Side effects of Azelex include dry skin, redness, itching, and burning. These side effects are typically mild and will go away on their own with time. However, if you experience any severe side effects, stop using the cream and contact your doctor immediately.

Dosage and Administration

Azelex Cream should be applied to the skin once daily after washing, as part of the morning or evening skincare regimen. A pea-sized amount of cream should be applied evenly to the entire face, avoiding the eyes and lips.

Use of other potentially irritating topical products with Azelex Cream should be avoided or minimized during use because of potential for additive local irritation. If bothersome dryness or peeling occurs, reduce application to once every other day or every third day.

If going outside, use a sunscreen lotion with SPF 15 or higher and wear protective clothing over treated areas when exposure cannot be avoided. Daily use of sunscreen lotions and protective clothing over treated areas is recommended when using Azelex Cream and for at least one week following discontinuation.

Overdose

Topical overdosage with Azelex Cream is unlikely to produce clinically significant effects. If large amounts are ingested or if it is suspected that topical doses in excess of those recommended have been used, the patient should be counseled and referred to a physician.

Storage

Azelex (azelaic acid) Cream, 20% is available in 40 g tubes NDC 56258-438-40. Store at 20° – 25°C (68° – 77°F). Protect from freezing and excessive heat above 40°C (104°F). Retain this carton for future reference. Keep out of reach of children.