物质信息

ID:95

名称和标识
IUPAC传统名
differin
IUPAC标准名
6-[3-(adamantan-1-yl)-4-methoxyphenyl]naphthalene-2-carboxylic acid
商标名
AdaferinDifferin
别名
Adapaleno [INN-Spanish]Adapalenum [INN-Latin]Adapalene
数据登录号
PubChem CID
PubChem SID
化合物性质
理化性质
溶解度
Practically Insoluble
疏水性(logP)
8.6
描述信息
Drug Groups
approved
Description
Adapalene is a topical retinoid primarily used in the treatment of acne and is also used (off-label) to treat keratosis pilaris as well as other skin conditions. It is currently marketed by Galderma under the trade names Differin in some countries, and Adaferin in India. [Wikipedia]
Indication
For the topical treatment of comedo, papular and pustular acne (acne vulgaris) of the face, chest or back.
Pharmacology
Adapalene is a chemically stable retinoid-like compound. Biochemical and pharmacological profile studies have demonstrated that adapalene is a modulator of cellular differentiation, keratinization, and inflammatory processes all of which represent important features in the pathology of acne vulgaris.
Toxicity
The acute oral toxicity of adapalene in mice and rats is greater than 10 mL/kg. Chronic ingestion of the drug may lead to the same side effects as those associated with excessive oral intake of Vitamin A.
Affected Organisms
Humans and other mammals
Biotransformation
Metabolized mainly by O-demethylation, hydroxylation and conjugation, and excretion is primarily by the biliary route.
Absorption
Absorption of adapalene through human skin is low. Only trace amounts (<0.25 ng/mL) of parent substance have been found in the plasma of acne patients following chronic topical application of adapalene in controlled clinical trials
Elimination
Excretion appears to be primarily by the biliary route.
References
• Rolewski SL: Clinical review: topical retinoids. Dermatol Nurs. 2003 Oct;15(5):447-50, 459-65. [Pubmed]
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参考文献
• Rolewski SL: Clinical review: topical retinoids. Dermatol Nurs. 2003 Oct;15(5):447-50, 459-65. Pubmed