| Item |
Information |
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Drug Groups
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approved |
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Description
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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. |
| Indication |
For the topical treatment of mild-to-moderate inflammatory acne vulgaris. |
| Pharmacology |
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. |
| Toxicity |
Oral LD50 in rat: >5 g/kg |
| Affected Organisms |
| • |
Various aerobic and anaerobic microorganisms |
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| Biotransformation |
Mainly excreted unchanged in the urine but undergoes some b-oxidation to shorter chain dicarboxylic acids. |
| Absorption |
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 |
Azelaic acid is mainly excreted unchanged in the urine, but undergoes some ?-oxidation to shorter chain dicarboxylic acids. |
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