Tìm theo
Adapalene
Các tên gọi khác (5 ) :
  • 6-(3-(1-Adamantyl)-4-methoxyphenyl)-2-naphthoic acid
  • Adaferin
  • Adapaleno
  • Adapalenum
  • Differine
Thuốc điều trị bệnh da liễu
Thuốc Gốc
Small Molecule
CAS: 106685-40-9
ATC: D10AD03
ĐG : Ameri-Pac Inc. , http://www.ameri-pac.com
CTHH: C28H28O3
PTK: 412.5201
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]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C28H28O3
Phân tử khối
412.5201
Monoisotopic mass
412.203844762
InChI
InChI=1S/C28H28O3/c1-31-26-7-6-23(21-2-3-22-12-24(27(29)30)5-4-20(22)11-21)13-25(26)28-14-17-8-18(15-28)10-19(9-17)16-28/h2-7,11-13,17-19H,8-10,14-16H2,1H3,(H,29,30)
InChI Key
InChIKey=LZCDAPDGXCYOEH-UHFFFAOYSA-N
IUPAC Name
6-[3-(adamantan-1-yl)-4-methoxyphenyl]naphthalene-2-carboxylic acid
Traditional IUPAC Name
adapalene
SMILES
COC1=C(C=C(C=C1)C1=CC2=C(C=C1)C=C(C=C2)C(O)=O)C12CC3CC(CC(C3)C1)C2
Độ hòa tan
Practically Insoluble
logP
8.6
logS
-8
pKa (strongest acidic)
3.99
pKa (Strongest Basic)
-4.8
PSA
46.53 Å2
Refractivity
122.07 m3·mol-1
Polarizability
47.65 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
6
Bioavailability
1
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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] Mechanistically, adapalene binds to specific retinoic acid nuclear receptors (gamma and beta) and retinoid X receptors but does not bind to the cytosolic receptor protein. Although the exact mode of action of adapalene is unknown, it is suggested that topical adapalene may normalize the differentiation of follicular epithelial cells resulting in decreased microcomedone formation.
Dược Động Học :
▧ 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
▧ Metabolism :
Metabolized mainly by O-demethylation, hydroxylation and conjugation, and excretion is primarily by the biliary route.
▧ Route of Elimination :
Excretion appears to be primarily by the biliary route.
Độc Tính : 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.
Chỉ Định : For the topical treatment of comedo, papular and pustular acne (acne vulgaris) of the face, chest or back.
Liều Lượng & Cách Dùng : Cream - Topical
Gel - Topical
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Adaferin
  • Công ty :
    Sản phẩm biệt dược : Differin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00210
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60164
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505019
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01112
ChemSpider
http://www.chemspider.com/Chemical-Structure.54244.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0299-5910-45
PharmGKB
http://www.pharmgkb.org/drug/PA448047
Wikipedia
http://en.wikipedia.org/wiki/Adapalene
RxList
http://www.rxlist.com/cgi/generic3/adapalene.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/dif1134.shtml
Drugs.com
http://www.drugs.com/cdi/adapalene-cream.html
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