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Azelex

Azelex - General Information

Azelaic acid is a saturated dicarboxylic acid found naturally in wheat, rye, and barley. It is a natural substance that is produced by Malassezia furfur (also known as Pityrosporum ovale), a yeast that lives on normal skin. It is effective against a number of skin conditions, such as mild to moderate acne, when applied topically in a cream formulation of 20%. It works in part by stopping the growth of skin bacteria that cause acne, and by keeping skin pores clear. Azelaic acid's antimicrobial action may be attributable to inhibition of microbial cellular protein synthesis.

 

Pharmacology of Azelex

Azelaic acid is a saturated dicarboxylic acid found naturally in wheat, rye, and barley. It is a natural substance that is produced by Malassezia furfur (also known as Pityrosporum ovale), a yeast that lives on normal skin. It is effective against a number of skin conditions, such as mild to moderate acne, when applied topically in a cream formulation of 20%. It works in part by stopping the growth of skin bacteria that cause acne, and by keeping skin pores clear. Azelaic acid's antimicrobial action may be attributable to inhibition of microbial cellular protein synthesis.

 

Azelex for patients

Patients should be told:

  1. To use AZELEX for the full prescribed treatment period.
  2. To avoid the use of occlusive dressings or wrappings.
  3. To keep AZELEX away from the mouth, eyes and other mucous membranes. If it does come in contact with the eyes, they should wash their eyes with large amounts of water and consult a physician if eye irritation persists.
  4. If they have dark complexions, to report abnormal changes in skin color to their physician.
  5. Due in part to the low pH of azelaic acid, temporary skin irritation (pruritus, burning, or stinging) may occur when AZELEX is applied to broken or inflamed skin, usually at the start of treatment. However, this irritation commonly subsides if treatment is continued. If it continues, AZELEX should be applied only once-a-day, or the treatment should be stopped until these effects have subsided. If troublesome irritation persists, use should be discontinued, and patients should consult their physician.

 

Azelex Interactions

No information provided

 

Azelex Contraindications

AZELEX® is contraindicated in individuals who have shown hypersensitivity to any of its components.

 

Additional information about Azelex

Azelex Indication: For the topical treatment of mild-to-moderate inflammatory acne vulgaris.
Mechanism Of Action: 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Azelaic Acid
Synonyms: n-Nonanedioic acid; Nonanedioic acid; Lepargylic acid; Heptanedicarboxylic acid; Azalaic Acid; Anchoic acid; Azelainic acid
Drug Category: Antineoplastic Agents; Dermatologic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Azelaic Acid: Azelex; Emerox 1110; Emerox 1144; Emery's L-110; Finacea; Finevin; Skinoren;
Absorption: Approximately 4% of the topically applied azelaic acid is systemically absorbed.
Toxicity (Overdose): Oral LD50 in rat: >5 g/kg
Protein Binding: Not Available
Biotransformation: Mainly excreted unchanged in the urine but undergoes some b-oxidation to shorter chain dicarboxylic acids.
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.
Dosage Forms of Azelex: Cream Topical
Chemical IUPAC Name: nonanedioic acid
Chemical Formula: C9H16O4
Azelaic Acid on Wikipedia: Not Available
Organisms Affected: Various aerobic and anaerobic microorganisms