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药品详细

Amcinonide(安西奈德)

化学结构式图
中文名
安西奈德
英文名
Amcinonide
分子式
C28H35FO7
化学名
2-[(1'S,2'S,4'R,8'S,9'S,11'S,12'R,13'S)-12'-fluoro-11'-hydroxy-9',13'-dimethyl-16'-oxo-5',7'-dioxaspiro[cyclopentane-1,6'-pentacyclo[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icosane]-14',17'-dien-8'-yl]-2-oxoethyl acetate
分子量
Average: 502.5717
Monoisotopic: 502.236681679
CAS号
51022-69-6
ATC分类
D07A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Amcinonide is a corticosteroid. [Wikipedia]

生产厂家
  • Altana inc
  • Astellas pharma us inc
  • Taro pharmaceutical industries ltd
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Steroids and Steroid Derivatives
Substructures
  • Steroids and Steroid Derivatives
  • Carboxylic Acids and Derivatives
  • Hydroxy Compounds
  • Alkanes and Alkenes
  • Acetates
  • Acetals and Derivatives
  • Alkyl Halides
  • Ethers
  • Dioxoles
  • Heterocyclic compounds
  • Alcohols and Polyols
  • Ketones
适应症
药理
Indication For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.
Pharmacodynamics Amcinonide is a topical corticosteroid. The topical corticosteroids constitute a class of primarily synthetic steroids used as anti-inflammatory and antipruritic agents. Amcinonide reduces or inhibits the actions of chemicals in the body that cause inflammation, redness, and swelling. The mechanism of anti-inflammatory activity of the topical corticosteroids is unclear. Various laboratory methods, including vasoconstrictor assays, are used to compare and predict potencies and/or clinical efficacies of the topical corticosteroids. There is some evidence to suggest that a recognizable correlation exists between vasoconstrictor potency and therapeutic efficacy in man. When in an ointment form, amcinonide also helps the skin maintain moisture.
Mechanism of action The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Amcinonide has affinity for the glucocorticoid receptor. It has weak affinity for the progesterone receptor, and virtually no affinity for the mineralocorticoid, estrogen, or androgen receptors.
Absorption Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys.
Route of elimination Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.
Half life Not Available
Clearance Not Available
Toxicity Results from acute toxicity studies do not indicate that any risk of acute intoxication is to be expected following a single dermal application of an overdose (application over a large area under conditions favorable to absorption) or inadvertent oral ingestion.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP 2.3 Not Available
Predicted Properties
Property Value Source
water solubility 7.74e-03 g/l ALOGPS
logP 3.16 ALOGPS
logP 3.2 ChemAxon
logS -4.8 ALOGPS
pKa (strongest acidic) 13.63 ChemAxon
pKa (strongest basic) -3.4 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 6 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 99.13 ChemAxon
rotatable bond count 4 ChemAxon
refractivity 127.88 ChemAxon
polarizability 52.23 ChemAxon
药物相互作用
食物相互作用
Not Available

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