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药品详细

Ardeparin(阿地肝素钠)

化学结构式图
中文名
阿地肝素钠
英文名
Ardeparin
分子式
C26H42N2O37S5
化学名
3-[(5-{[6-carboxy-4,5-dihydroxy-3-(sulfooxy)oxan-2-yl]oxy}-6-(hydroxymethyl)-3-(sulfoamino)-4-(sulfooxy)oxan-2-yl)oxy]-6-({5-acetamido-4,6-dihydroxy-2-[(sulfooxy)methyl]oxan-3-yl}oxy)-4-hydroxy-5-(sulfooxy)oxane-2-carboxylic acid
分子量
Average: 1134.928
Monoisotopic: 1134.006993818
CAS号
<span class="not-available">Not Available</span>
ATC分类
B01A 抗血栓药;B01A 抗血栓药
药物类型
small molecule
阶段
approved, withdrawn
商品名
同义名
基本介绍

Ardeparin, marketed under the US trade name Normiflo, is a low molecular weight heparin (LMWH) anticoagulant used for the prevention of postoperative venous thrombosis. Ardeparin is derived via peroxide degradation of heparin extracted from porcine intestinal mucosa. Its molecular weight ranges from 2000 to 15,000 with an average molecular weight of 5500 to 6500. Normiflo was withdrawn from the US market in March 2000.

生产厂家
  • Wyeth ayerst laboratories
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
  • Carbohydrates
Substructures
  • Carbohydrates
  • Aminoglycosides
  • Glycerol and Derivatives
  • Hydroxy Compounds
  • Pyrans
  • Acetates
  • Acetals and Derivatives
  • Glucuronides
  • Amino Ketones
  • Sulfuric Acids and Derivatives
  • Sulfonyls
  • Ethers
  • Sulfate Esters
  • Carboxylic Acids and Derivatives
  • Alcohols and Polyols
  • Heterocyclic compounds
  • Carboxamides and Derivatives
适应症
药理
Indication For prevention of deep vein thrombosis, which may result in pulmonary embolism, following knee surgery.
Pharmacodynamics Ardeparin, an anticoagulant, is a fractionated heparin. It acts at multiple sites in the normal coagulation system to inhibit reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo.
Mechanism of action Ardeparin binds to antithrombin III, accelerating its activity in inactivating factor Xa and thrombin, thereby inhibiting thrombosis. Ardeparin also binds to heparin cofactor II, inhibiting thrombin. Ardeparin does not effect prothrombin time (PT) assays and may prolong activated partial thromboplastin time (APTT). Ardeparin has double the anti-factor Xa activity versus anti-factor IIa activity, compared to unfractionated heparin which has approximately equal anti-factor Xa activity and anti-factor IIa activity.
Absorption Well absorbed following subcutaneous administration, with a mean bioavailability of 92% (based on anti-factor Xa activity).
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Liver and the reticulo-endothelial system are the sites of biotransformation.
Route of elimination Not Available
Half life Elimination half-life for anti-factor Xa activity averages 3.3 hours following a single intravenous dose, while elimination half-life for anti-factor IIa activity averages 1.2 hours following a single intravenous dose.
Clearance Not Available
Toxicity Symptoms of overdose may include excessive bleeding and bruising.
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00275 Ardeparin Pathway SMP00275
理化性质
Properties
State solid
Experimental Properties
Property Value Source
water solubility Soluble Not Available
Predicted Properties
Property Value Source
water solubility 1.08e+01 g/l ALOGPS
logP -1.7 ALOGPS
logP -8.3 ChemAxon
logS -2 ALOGPS
pKa (strongest acidic) -2.8 ChemAxon
physiological charge -7 ChemAxon
hydrogen acceptor count 33 ChemAxon
hydrogen donor count 15 ChemAxon
polar surface area 610.49 ChemAxon
rotatable bond count 20 ChemAxon
refractivity 195.91 ChemAxon
polarizability 93.37 ChemAxon
药物相互作用
食物相互作用
Not Available

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