药品详细
Azelaic Acid(壬二酸)
化学结构式图
中文名
壬二酸
英文名
Azelaic Acid
分子式
C9H16O4
化学名
nonanedioic acid
分子量
Average: 188.2209
Monoisotopic: 188.104859
Monoisotopic: 188.104859
CAS号
123-99-9
ATC分类
D10A Anti-Acne Preparations for Topical Use
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
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.
生产厂家
- Allergan inc
- Intendis inc
封装厂家
- Allergan Inc.
- Bayer Healthcare
- Intendis Inc.
- Physicians Total Care Inc.
- Professional Co.
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | For the topical treatment of mild-to-moderate inflammatory acne vulgaris. |
| Pharmacodynamics | 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. |
| 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. |
| Absorption | Approximately 4% of the topically applied azelaic acid is systemically absorbed. |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism |
Mainly excreted unchanged in the urine but undergoes some b-oxidation to shorter chain dicarboxylic acids.
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| Route of elimination | Azelaic acid is mainly excreted unchanged in the urine, but undergoes some ß-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. |
| Clearance | Not Available |
| Toxicity | Oral LD50 in rat: >5 g/kg |
| Affected organisms |
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| Pathways | Not Available |
理化性质
| Properties | ||||||||||||||||||||||||||||||||||||||||
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| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
食物相互作用
Not Available
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